{"id":98125,"date":"2019-02-26T00:00:50","date_gmt":"2019-05-17T08:13:11","guid":{"rendered":"http:\/\/www.05921.net\/index.php\/98125\/"},"modified":"2019-05-17T16:13:13","modified_gmt":"2019-05-17T08:13:13","slug":"1160d7811c","status":"publish","type":"post","link":"https:\/\/www.05921.net\/index.php\/98125\/","title":{"rendered":"\u901a\u8fc7\u589e\u52a0\u6eb6\u89e3\u5ea6\u63d0\u9ad8BCS \u2161\u7c7b\u836f\u7269\u53e3\u670d\u5438\u6536:\u5e38\u5e38\u88ab\u5ffd\u7565\u7684\u836f\u7269\u6e17\u900f\u6027"},"content":{"rendered":"
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\u901a\u8fc7\u589e\u52a0\u6eb6\u89e3\u5ea6\u63d0\u9ad8BCS \u2161\u7c7b\u836f\u7269\u53e3\u670d\u5438\u6536:\u5e38\u5e38\u88ab\u5ffd\u7565\u7684\u836f\u7269\u6e17\u900f\u6027<\/span><\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n

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Improving oral absorption of BCS \u2161 drugs by increasing solubility: frequently overlooked permeability<\/span><\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u836f\u5b66\u5b66\u62a5 Acta Pharmaceutica Sinica 2019, 54(1): 1 \u22127<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u91c7\u7528\u5236\u5242\u624b<\/span>\u6bb5\u589e\u52a0BCS \u2161\u7c7b\u836f\u7269\u6eb6\u89e3\u5ea6\u7684\u540c\u65f6\u5018\u82e5\u4e0d\u8003\u8651\u5176\u5bf9\u836f\u7269\u6e17\u900f\u6027\u7684\u5f71\u54cd, \u5c06\u96be\u4ee5\u5b9e\u73b0\u836f\u7269\u6700\u4f73\u53e3\u670d\u5438\u6536\u7684\u6700\u5927\u5316\u3002<\/span><\/p>\n

\u672c\u6587\u7efc\u8ff0\u4e86\u5e38\u7528\u5236\u5242\u7b56\u7565, \u5982\u73af\u7cca\u7cbe\u5305\u5408\u7269\u3001\u8868\u9762\u6d3b\u6027\u5242\u3001\u6df7\u5408\u6f5c\u6eb6\u5242\u548c\u56fa\u4f53\u5206\u6563\u4f53\u7b49\u589e\u52a0\u836f\u7269\u6eb6\u89e3\u5ea6\u7684\u540c\u65f6\u5bf9\u836f\u7269\u6e17\u900f\u6027\u7684\u5f71\u54cd, \u5e76\u8bc4\u8ff0\u4e86\u4ee5\u4e0a\u7b56\u7565\u4e2d\u65b0\u6280\u672f\u7684\u8fd0\u7528\u53ca\u8f6c\u8fd0\u86cb\u767d\u7684\u5f71\u54cd, \u4ee5\u671f\u4e3a\u4ee5\u63d0\u9ad8\u53e3\u670d\u5438\u6536\u4e3a\u76ee\u7684\u7684\u5236\u5242\u8bbe<\/span>\u8ba1\u3001\u8f85\u6599\u7b5b\u9009\u548c\u7814\u7a76\u65b9\u6cd5\u63d0\u4f9b\u4f9d\u636e\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u6b63 \u6587<\/strong><\/p>\n<\/section>\n

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1995 \u5e74\u7f8e\u56fd\u5bc6\u897f\u6839\u5927\u5b66\u7684Amidon \u7b49[1]\u6307\u51fa\u836f\u7269\u7684\u53e3\u670d\u5438\u6536\u4e3b\u8981\u53d7\u836f\u7269\u5728\u80c3\u80a0\u9053\u6eb6\u89e3\u5ea6\u6216\u6eb6\u51fa\u901f\u5ea6\u4e0e<\/span>\u8de8\u819c\u6e17\u900f\u80fd\u529b\u7684\u5f71\u54cd, \u5e76\u9996\u6b21\u63d0\u51fa\u4e86\u751f\u7269\u836f\u5242\u5b66\u5206\u7c7b<\/span>\u7cfb\u7edf(biopharmaceutics classification system, BCS) \u7684<\/span>\u6982\u5ff5, \u5c06\u836f\u7269\u6309\u7167\u4f53\u5916\u6eb6\u89e3\u6027(solubility) \u548c\u80a0\u9053\u6e17\u900f<\/span>\u6027(permeability) \u5206\u4e3a4 \u7c7b, \u7528\u4e8e\u533a\u5206\u4e0d\u540c\u6027\u8d28\u836f\u7269\u53e3<\/span>\u670d\u5438\u6536\u7684\u7279\u70b9\u3002<\/span><\/p>\n

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\u5176\u4e2dBCS \u2161\u7c7b\u836f\u7269\u8868\u73b0\u4e3a\u4f4e\u6eb6\u89e3\u6027\/\u9ad8\u6e17\u900f\u6027, \u901a\u8fc7\u7ec4\u5408\u5316\u5b66\u53ca\u9ad8\u901a\u91cf\u7b5b\u9009\u7b49\u65b9\u6cd5\u5f97\u5230\u5927\u91cf\u5019\u9009\u836f\u7269\u4e2d, \u6709<\/span>\u8d85\u8fc740%\u7684\u5316\u5408\u7269\u4e3a\u4f4e\u6eb6\u89e3\u6027, \u589e\u52a0\u8fd9\u4e9b\u836f\u7269\u7684\u6eb6\u89e3<\/span>\u5ea6\u662f\u63d0\u9ad8\u5176\u6210\u836f\u6027\u7684\u91cd\u8981\u624b\u6bb5[2,3]\u3002<\/span><\/p>\n

\u7531\u4e8e\u5b9e\u9645\u6d4b\u5b9a\u4e2d<\/span>\u8981\u5b8c\u5168\u6392\u9664\u836f\u7269\u89e3\u79bb\u548c\u6eb6\u5242\u7684\u5f71\u54cd\u4e0d\u6613\u505a\u5230, \u901a\u5e38\u5bf9<\/span>\u4e8e\u836f\u7269\u6eb6\u89e3\u5ea6\u7684\u6d4b\u5b9a\u6570\u503c\u591a\u662f\u5e73\u8861\u6eb6\u89e3\u5ea6(equilibrium <\/span>solubility) \u6216\u8868\u89c2\u6eb6\u89e3\u5ea6(apparent solubility)\u3002<\/span><\/p>\n

\u5e38\u7528\u7684<\/span>\u589e\u52a0\u836f\u7269\u8868\u89c2\u6eb6\u89e3\u5ea6\u7684\u65b9\u6cd5\u6709: \u751f\u6210\u53ef\u6eb6\u6027\u76d0\u7c7b; \u6539<\/span>\u53d8\u6676\u578b\/\u5f62\u6210\u6eb6\u5242\u5316\u7269\u3001\u5171\u6676; \u8868\u9762\u6d3b\u6027\u5242\u589e\u6eb6; \u51cf\u5c0f\u7c92<\/span>\u5f84; \u91c7\u7528\u6f5c\u6eb6\u5242\/\u52a9\u6eb6\u5242; \u5236\u5907\u56fa\u4f53\u5206\u6563\u4f53; \u5f62\u6210\u5305\u5408<\/span>\u7269; \u8bbe\u8ba1\u6210\u7eb3\u7c73\u7ed9\u836f\u7cfb\u7edf\u7b49[4]\u3002<\/span><\/p>\n

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\u73af\u7cca\u7cbe\u662f\u4e00\u7c7b\u5177\u6709\u4eb2\u6c34\u6027\u8868\u9762\u548c\u758f\u6c34\u6027\u7a7a\u8154\u7684\u73af\u72b6\u5be1\u7cd6, \u5177\u6709\u9ad8\u5ea6\u7684\u6c34\u6eb6\u6027, \u7a7a\u8154\u53ef\u4e0e\u758f\u6c34\u6027\u6eb6\u8d28\u76f8\u7ed3<\/span>\u5408\u5f62\u6210\u5305\u5408\u7269\u800c\u589e\u5927\u6eb6\u8d28\u7684\u8868\u89c2\u6eb6\u89e3\u5ea6\u3002<\/span><\/p>\n

\u901a\u5e38, \u836f\u7269<\/span>\u5728\u80c3\u80a0\u9053\u6eb6\u89e3\u662f\u53e3\u670d\u5438\u6536\u7684\u5148\u51b3\u6761\u4ef6, \u67d0\u4e9b\u73af\u7cca\u7cbe\u53ef<\/span>\u4e0e\u4eb2\u8102\u6027\u836f\u7269\u5f62\u6210\u6c34\u6eb6\u6027\u5305\u5408\u7269, \u4ece\u800c\u63d0\u9ad8\u836f\u7269\u7684\u8868<\/span>\u89c2\u6eb6\u89e3\u5ea6\u3002<\/span><\/p>\n

\u7136\u800c\u7814\u7a76\u8868\u660e, \u73af\u7cca\u7cbe\u5728\u63d0\u9ad8\u836f\u7269\u6eb6\u89e3\u5ea6<\/span>\u7684\u540c\u65f6, \u5e38\u4f34\u968f\u7740\u836f\u7269\u6e17\u900f\u6027\u7684\u964d\u4f4e[6]\u3002<\/span><\/p>\n

Beig \u7b49[7] \u53d1\u73b0\u78fa\u4e01\u57fa- \u03b2 – \u73af\u7cca\u7cbe(SEB7 – \u03b2 -CD, <\/span>captisol) \u5bf9\u63d0\u9ad8\u96be\u6eb6\u6027\u6297\u5fc3\u5f8b\u5931\u5e38\u836f\u7269\u80fa\u78fa\u916e\u7684\u8868\u89c2\u6eb6\u89e3\u5ea6\u662f2-\u7f9f\u4e19\u57fa-\u03b2-\u73af\u7cca\u7cbe(HP-\u03b2-CD) \u768410 \u500d\u3002<\/span><\/p>\n

\u539f<\/span>\u56e0\u662f\u9664\u4e86\u758f\u6c34\u4f5c\u7528, captisol \u5bf9\u80fa\u7898\u916e\u7684\u589e\u6eb6\u8fd8\u5b58\u5728\u9759<\/span>\u7535\u4f5c\u7528, captisol \u5728\u751f\u7406\u6761\u4ef6\u4e0b\u5e26\u8d1f\u7535, \u800c\u80fa\u78fa\u916e\u5728\u6574<\/span>\u4e2a\u6d88\u5316\u9053pH\u5747\u5e26\u6b63\u7535\u3002<\/span><\/p>\n

\u7136\u800c\u4eba\u5de5PAMPA\u819c\u6e17\u900f\u6027\u5b9e<\/span>\u9a8c\u548c\u5927\u9f20\u80a0\u9053\u704c\u6d41\u5b9e\u9a8c\u8868\u660e, \u80fa\u7898\u916e\u7684\u8868\u89c2\u6e17\u900f\u6027\u5747<\/span>\u968f\u4e24\u79cd\u73af\u7cca\u7cbe\u6d53\u5ea6\u53ca\u836f\u7269\u8868\u89c2\u6eb6\u89e3\u5ea6\u7684\u5347\u9ad8\u800c\u964d\u4f4e,<\/span>\u5e76\u4e14captisol \u964d\u4f4e\u80fa\u7898\u916e\u6e17\u900f\u6027\u7684\u4f5c\u7528\u8f83HP-\u03b2-CD\u663e<\/span>\u8457\u3002<\/span><\/p>\n

\u6b64\u5916, Fine-Shamir \u7b49[8]\u63d0\u51fa\u8bbe\u8ba1\u73af\u7cca\u7cbe\u5305\u5408\u7269\u5904<\/span>\u65b9\u65f6, \u73af\u7cca\u7cbe\u6d53\u5ea6\u5e94\u4e0d\u8d85\u8fc7\u80fd\u589e\u52a0\u836f\u7269\u6eb6\u89e3\u5ea6\u7684\u6700\u5927<\/span>\u91cf, \u5426\u5219\u8fc7\u91cf\u7684\u73af\u7cca\u7cbe\u53cd\u800c\u4f1a\u5bfc\u81f4BCS \u2161\u7c7b\u836f\u7269\u8fbe\u90a3<\/span>\u5511\u6e17\u900f\u6027\u4e0b\u964d, \u4ece\u800c\u5f71\u54cd\u836f\u7269\u7684\u53e3\u670d\u5438\u6536\u3002<\/span><\/p>\n

\u73af\u7cca\u7cbe\u4e0e<\/span>\u836f\u7269\u76f8\u4e92\u4f5c\u7528\u5f62\u6210\u7ed3\u5408\u6001\u7684\u5305\u5408\u7269\u5b58\u5728\u8131\u5305\u5408\u4e0e\u88ab\u5305<\/span>\u5408\u7684\u5fae\u89c2\u52a8\u6001\u5e73\u8861, Carrier \u7b49[9]\u8ba4\u4e3a\u7531\u4e8e\u73af\u7cca\u7cbe\u5f62\u6210<\/span>\u7684\u5305\u5408\u7269\u4e0d\u80fd\u6e17\u900f\u901a\u8fc7\u80a0\u58c1, \u53ea\u80fd\u901a\u8fc7\u6e38\u79bb\u72b6\u6001\u6eb6\u89e3<\/span>\u7684\u836f\u7269\u53d1\u6325\u53e3\u670d\u836f\u6548, \u73af\u7cca\u7cbe\u6d53\u5ea6\u589e\u52a0\u5230\u4e00\u5b9a\u7a0b\u5ea6\u548c<\/span>\u5f62\u6210\u5305\u5408\u7269\u7684\u7ed3\u5408\u5e38\u6570\u8f83\u9ad8\u65f6, \u8131\u5305\u5408\u4e0e\u88ab\u5305\u5408\u7684\u52a8<\/span>\u6001\u5e73\u8861\u5411\u5f62\u6210\u5305\u5408\u7269\u7684\u7ed3\u5408\u6001\u65b9\u5411\u8fdb\u884c, \u5bfc\u81f4\u52a8\u6001\u5e73<\/span>\u8861\u4e2d\u8131\u5305\u5408\u51fa\u6765\u7684\u975e\u7ed3\u5408\u6001\u6e38\u79bb\u6eb6\u89e3\u7684\u836f\u7269\u6d53\u5ea6\u964d<\/span>\u4f4e, \u4ece\u800c\u95f4\u63a5\u5730\u964d\u4f4e\u4e86\u836f\u7269\u5728\u80c3\u80a0\u9053\u7684\u6e17\u900f\u5438\u6536\u3002<\/span><\/p>\n

\u53ef<\/span>\u89c1, \u836f\u7269\u6eb6\u89e3\u6027\u4e0e\u6e17\u900f\u6027\u76f8\u4e92\u8054\u7cfb, \u5171\u540c\u5f71\u54cd\u73af\u7cca\u7cbe\u4e2d<\/span>\u836f\u7269\u53e3\u670d\u5438\u6536\u3002<\/span><\/p>\n

Miller \u7b49[10]\u5bf9\u73af\u7cca\u7cbe\u5305\u5408\u7269\u4e2d\u836f\u7269\u6eb6\u89e3\u6027-\u6e17\u900f<\/span>\u6027\u7684\u76f8\u5173\u6027\u5efa\u7acb\u4e86\u6570\u5b66\u6a21\u578b, \u8bd5\u56fe\u9610\u660e\u73af\u7cca\u7cbe\u5bf9\u836f\u7269<\/span>\u901a\u8fc7\u80a0\u9053\u9759\u6d41\u5c42(unstirred water layer, UWL) \u7684\u6e17\u900f<\/span>\u7cfb\u6570(<\/span>Paq<\/span><\/sub>) \u548c\u80a0\u819c\u6e17\u900f\u7cfb\u6570(Pm) \u7684\u5f71\u54cd, \u5e76\u7528\u4e8e\u9884<\/span>\u6d4b\u6709\u6548\u6e17\u900f\u7cfb\u6570(Peff<\/sub><\/span>) \u548c\u73af\u7cca\u7cbe\u6d53\u5ea6(cyclodextrin <\/span>concentration, CCD) \u7684\u76f8\u5173\u6027\u3002\u8be5\u6a21\u578b\u63d0\u51fa, \u4eb2\u8102\u6027\u836f<\/span>\u7269\u901a\u8fc7\u80a0\u9053\u5438\u6536\u8fdb\u5165\u8840\u6db2\u5faa\u73af\u9700\u8981\u4f9d\u6b21\u6e17\u900f\u901a\u8fc7<\/span>UWL \u548c\u80a0\u9053\u4e0a\u76ae\u7ec6\u80de\u819c, \u5176\u4e2dUWL \u7684\u539a\u5ea6\u968f\u7740CCD<\/span>\u7684\u589e\u52a0\u8fc5\u901f\u964d\u4f4e, \u800cPaq\u663e\u8457\u589e\u52a0\u3002<\/span><\/p>\n

Miller \u7b49[10]\u63a8\u5bfc\u7684\u516c\u5f0f:<\/p>\n

\"\u901a\u8fc7\u589e\u52a0\u6eb6\u89e3\u5ea6\u63d0\u9ad8BCS<\/p>\n

\u7531\u516c\u5f0f\u53ef\u77e5, P<\/span>aq<\/span><\/sub>\u589e\u5927\u4f1a\u4f7f\u5176\u5bf9P<\/span>eff<\/sub> \u5f71\u54cd\u51cf\u5c0f, \u6545CCD\u9ad8\u4e8e\u4e00\u5b9a\u6d53\u5ea6\u540e, UWL \u88ab\u73af\u7cca\u7cbe\u6709\u6548\u6d88\u9664\u3002<\/span><\/p>\n

\u4eb2\u8102\u6027\u836f\u7269\u4e2dP<\/span>aq<\/span><\/sub>\u662f\u5438\u6536\u9650\u901f\u6b65\u9aa4, \u5f53\u73af\u7cca\u7cbe\u7684\u6d53\u5ea6\u8fbe\u5230\u4e00\u5b9a\u7a0b\u5ea6\u80fd\u6d88\u9664UWL\u7684\u5f71\u54cd, \u4f7fP<\/span>aq<\/span><\/sub>\u53d8\u6210\u65e0\u5173\u53c2\u6570, \u7531\u4e8e\u53ea\u6709\u8131\u5305\u5408\u4e2d\u6e38\u79bb\u72b6\u6001\u6eb6\u89e3\u7684\u836f\u7269\u624d\u88ab\u7eb3\u5165\u6e17\u900f\u6027\u5224\u65ad, \u6b64\u65f6\u6e38\u79bb\u6001\u836f\u7269\u7684<\/span>Peff<\/sub><\/span>\u2248<\/span>Pm<\/sub>, <\/span>Peff<\/sub><\/span><\/span>\u53d8\u5316\u53d6\u51b3\u4e8e\u836f\u7269\u8de8\u80a0\u9053\u4e0a\u76ae\u7ec6\u80de\u819c\u7684\u6548\u7387\u3002\u5982\u4e0a\u6240\u8ff0, \u8f83\u9ad8\u6d53\u5ea6\u7684\u73af\u7cca\u7cbe\u5305\u5408\u4f1a\u5bfc\u81f4\u6e38\u79bb\u6001\u6eb6\u89e3\u836f\u7269\u7684\u6d53\u5ea6\u4e0b\u964d, \u8fdb\u800c\u4f7fPm\u51cf\u5c0f, \u5e76\u6700\u7ec8\u5bfc\u81f4\u836f\u7269P<\/span>eff<\/sub>\u4e0b\u964d[6,11]\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
\n
\n
\n
\n
\n

2<\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
\n

\u8868\u9762\u6d3b\u6027\u5242\u589e\u6eb6\u5bf9\u836f\u7269\u6e17\u900f\u6027<\/strong>\u5f71\u54cd<\/p>\n<\/section>\n<\/section>\n

<\/section>\n<\/section>\n<\/section>\n<\/section>\n
\n
\n
\n

\u5177\u6709\u4eb2\u6c34\u4eb2\u6cb9\u4e24\u4eb2\u6027\u7684\u8868\u9762\u6d3b\u6027\u5242, \u5f53\u5176\u6d53\u5ea6\u8d85\u8fc7\u4e34\u754c\u80f6\u675f\u6d53\u5ea6\u65f6, \u96be\u6eb6\u6027\u836f\u7269\u88ab\u5305\u88f9\u5728\u8868\u9762\u6d3b\u6027\u5242<\/span>\u80f6\u675f\u7684\u4eb2\u8102\u6027\u6805\u680f\u4e2d, \u53ef\u63d0\u9ad8\u836f\u7269\u7684\u8868\u89c2\u6eb6\u89e3\u5ea6, \u5e7f\u6cdb<\/span>\u5e94\u7528\u4e8e\u4eb2\u8102\u6027\u836f\u7269\u53e3\u670d\u9012\u9001\u7cfb\u7edf\u3002<\/span><\/p>\n

\u8fd1\u671f\u6709\u7814\u7a76\u53d1\u73b0,<\/span>\u8868\u9762\u6d3b\u6027\u5242\u5728\u589e\u52a0\u96be\u6eb6\u6027\u836f\u7269\u8868\u89c2\u6eb6\u89e3\u5ea6\u7684\u540c\u65f6,<\/span><\/p>\n

BCS \u2161\u7c7b\u836f\u7269\u7684\u6e17\u900f\u6027\u4e0e\u73af\u7cca\u7cbe\u76f8\u4f3c, \u4e5f\u5448\u73b0\u4e0b\u964d\u8d8b\u52bf\u3002Miller \u7b49[12]\u901a\u8fc7\u6539\u53d8\u8868\u9762\u6d3b\u6027\u5242\u5341\u4e8c\u70f7\u57fa\u78fa\u9178\u94a0<\/span>(SLS) \u548c\u725b\u78fa\u80c6\u9178\u94a0(STC) \u7684\u6d53\u5ea6, \u7814\u7a76\u80f6\u675f\u589e\u6eb6\u5bf9<\/span>\u9ec4\u4f53\u916eP<\/span>m<\/sub>\u548cPaq\u7684\u5f71\u54cd, \u4ee5\u9884\u6d4b\u6574\u4f53P<\/span>eff<\/sub>\u503c\u3002<\/span><\/p>\n

\u7ecf\u5927\u9f20\u7a7a<\/span>\u80a0\u704c\u6ce8\u5b9e\u9a8c, \u6e38\u79bb\u9ec4\u4f53\u916e\u8868\u73b0\u51fa\u9ad8\u6e17\u900f\u6027, \u800c\u5728SLS \u548c<\/span>STC \u9ad8\u4e8e\u4e34\u754c\u80f6\u675f\u6d53\u5ea6\u9ec4\u4f53\u916e\u88ab\u589e\u6eb6\u540e, \u968f\u7740\u8868\u9762\u6d3b<\/span>\u6027\u5242\u6d53\u5ea6\u5347\u9ad8, \u9ec4\u4f53\u916eP<\/span>eff<\/sub>\u663e\u8457\u964d\u4f4e\u3002<\/span><\/p>\n

\u63d0\u793a\u8868\u9762\u6d3b\u6027\u5242<\/span>\u8fbe\u5230\u4e34\u754c\u80f6\u675f\u6d53\u5ea6\u540e, \u63d0\u9ad8\u836f\u7269\u8868\u89c2\u6eb6\u89e3\u5ea6\u4ee5\u964d\u4f4e\u6e17<\/span>\u900f\u6027\u4e3a\u4ee3\u4ef7\u3002<\/span><\/p>\n

\u4e0e\u73af\u7cca\u7cbe\u589e\u52a0\u6eb6\u89e3\u5ea6\u7c7b\u4f3c, \u8868\u9762\u6d3b\u6027\u5242\u5f62\u6210\u80f6\u675f\u540e\u5c06\u4eb2\u8102\u6027\u836f\u7269\u589e\u6eb6\u5728\u80f6\u675f\u5185\u90e8\u5b58\u5728\u7ed3\u5408\u6001\u4e0e\u975e\u7ed3\u5408<\/span>\u6001\u7684\u5fae\u89c2\u8f7d\u836f\u52a8\u529b\u5b66\u5e73\u8861, \u5f53\u8868\u9762\u6d3b\u6027\u5242\u6d53\u5ea6\u589e\u52a0\u5bfc<\/span>\u81f4\u4f53\u7cfb\u4e2d\u6e38\u79bb\u72b6\u6001\u6eb6\u89e3\u7684\u836f\u7269\u6d53\u5ea6\u76f8\u5bf9\u4e0b\u964d, \u800c\u80f6\u675f<\/span>\u96be\u6e17\u900f\u901a\u8fc7\u80c3\u80a0\u9053, \u6b64\u65f6\u80c3\u80a0\u901a\u900f\u6027\u4e3b\u8981\u7531\u6e38\u79bb\u6001\u6eb6<\/span>\u89e3\u7684\u836f\u7269\u6d53\u5ea6\u51b3\u5b9a, \u4ece\u800c\u5bfc\u81f4\u836f\u7269\u6e17\u900f\u6027\u4e0b\u964d\u3002<\/span><\/p>\n

\u56e0\u6b64,<\/span>\u4e0d\u96be\u7406\u89e3\u4e3a\u4f55\u8868\u9762\u6d3b\u6027\u5242\u5bf9BCS \u2161\u7c7b\u836f\u7269\u7684\u6eb6\u89e3\u6027<\/span>\u548c\u6e17\u900f\u6027\u5f71\u54cd\u663e\u8457[12,13]\u3002\u8868\u9762\u6d3b\u6027\u5242\u63d0\u9ad8\u5176\u4ed6\u7c7b\u578b\u836f<\/span>\u7269(\u5982BCS \u2162\u3001BCS \u2163\u7c7b\u836f\u7269) \u53e3\u670d\u5438\u6536, \u5219\u53ef\u80fd\u4e0e<\/span>\u5176\u7834\u574f\u751f\u7269\u819c\u7684\u5b8c\u6574\u6027\u3001\u589e\u52a0\u7ec6\u80de\u65c1\u8def\u8f6c\u8fd0\u7b49\u56e0\u7d20<\/span>\u6709\u5173[14]\u3002<\/span><\/p>\n

\u8fd1\u671fBeig \u7b49[15]\u53d1\u73b0, \u7ef4\u751f\u7d20E \u805a\u4e59\u4e8c\u9187\u7425<\/span>\u73c0\u9178\u916f(vitamin E-TPGS, TPGS) \u589e\u6eb6\u4f9d\u6258\u6cca\u82f7\u4e2d,<\/span>\u968f\u7740TPGS \u6d53\u5ea6\u63d0\u9ad8, \u4f9d\u6258\u6cca\u82f7\u5728\u5e73\u884c\u4eba\u5de5\u6e17\u900f\u819c<\/span>(PAMPA) \u7684\u6e17\u900f\u7387\u663e\u8457\u4e0b\u964d, \u800c\u5728\u5927\u9f20\u80a0\u704c\u6d41\u7684\u6e17\u900f<\/span>\u7387\u5374\u589e\u52a0, \u8fd9\u53ef\u80fd\u662f\u7531\u4e8eTPGS \u80fd\u6291\u5236\u4f53\u5185p-\u7cd6\u86cb\u767d<\/span>(P-gp) \u8868\u8fbe, \u51cf\u5c11\u836f\u7269\u5916\u6392\u4ece\u800c\u603b\u4f53\u4e0a\u63d0\u9ad8\u4e86\u836f\u7269\u7684<\/span>\u6e17\u900f\u6027\u3002<\/span><\/p>\n

\u56e0\u6b64, \u4e3a\u4e86\u5b9e\u73b0\u53e3\u670d\u5438\u6536\u7684\u6700\u5927\u5316, \u9664\u4e86\u540c\u65f6<\/span>\u8003\u8651\u8868\u9762\u6d3b\u6027\u5242\u80f6\u675f\u5bf9\u836f\u7269\u7684\u6eb6\u89e3\u6027\u548c\u6e17\u900f\u6027\u7684\u5f71<\/span>\u54cd, \u8fd8\u8981\u5173\u6ce8\u5176\u4ed6\u4f53\u5185\u590d\u6742\u56e0\u7d20\u7684\u5f71\u54cd, \u5e76\u4ee5\u4f53\u5185\u5b9e\u9a8c<\/span>\u7ed3\u679c\u4e3a\u51c6\u3002<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\n
\n

3<\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
\n

\u6f5c\u6eb6\u5242\u5bf9\u6eb6\u89e3\u5ea6\u4e0e\u6e17\u900f\u6027\u7684\u5f71\u54cd<\/strong><\/p>\n<\/section>\n<\/section>\n

<\/section>\n<\/section>\n<\/section>\n<\/section>\n
\n
\n
\n

\u6e38\u79bb\u72b6\u6001\u6eb6\u89e3\u7684\u836f\u7269\u5728\u80a0\u819c\u4e24\u4fa7\u7684\u6d53\u5ea6\u68af\u5ea6\u662f\u836f\u7269\u8de8\u819c\u6e17\u900f\u7684\u9a71\u52a8\u529b, \u4e0a\u6587\u6240\u8ff0\u7684\u4e24\u79cd\u589e\u52a0\u836f\u7269\u6eb6\u89e3<\/span>\u5ea6\u65b9\u6cd5\u2014\u2014\u73af\u7cca\u7cbe\u548c\u8868\u9762\u6d3b\u6027\u5242, \u589e\u52a0\u836f\u7269\u8868\u89c2\u6eb6\u89e3<\/span>\u5ea6\u4f1a\u5bfc\u81f4\u4f53\u7cfb\u4e2d\u975e\u7ed3\u5408\u6001\u6eb6\u89e3\u836f\u7269\u7684\u6d53\u5ea6\u964d\u4f4e, \u4ece\u800c<\/span>\u964d\u4f4e\u836f\u7269\u6e17\u900f\u6027, \u8be5\u73b0\u8c61\u4f3c\u4e4e\u5728BCS \u2161\u7c7b\u836f\u7269\u4e2d\u5e7f\u6cdb<\/span>\u5b58\u5728\u3002<\/span><\/p>\n

\u5f53\u5176\u4ed6\u589e\u52a0\u836f\u7269\u6eb6\u89e3\u5ea6\u7684\u624b\u6bb5\u4e2d\u4e0d\u5b58\u5728\u8f7d\u4f53\u4e0e\u836f\u7269\u76f8\u4e92\u4f5c\u7528\u5f62\u6210\u7ed3\u5408\u6001\u7684\u5173\u7cfb, \u6eb6\u89e3\u7684\u836f\u7269\u4ec5\u4ee5\u5355<\/span>\u5206\u5b50(\u79bb\u5b50) \u72b6\u6001\u5206\u6563\u4e8e\u6eb6\u5242\u4e2d, BCS \u2161\u7c7b\u836f\u7269\u662f\u5426\u8fd8<\/span>\u51fa\u73b0\u589e\u52a0\u6eb6\u89e3\u5ea6\u800c\u964d\u4f4e\u836f\u7269\u6e17\u900f\u6027\u7684\u73b0\u8c61\uff1f\u6f5c\u6eb6\u5242<\/span>(cosolvent) \u5219\u80fd\u89e3\u51b3\u8fd9\u4e00\u95ee\u9898\u7528\u4e8e\u8be5\u73b0\u8c61\u7684\u7814\u7a76\u3002<\/span><\/p>\n

\u4e3a\u4e86\u63d0\u9ad8\u96be\u6eb6\u6027\u836f\u7269\u7684\u6eb6\u89e3\u5ea6, \u5e38\u4f7f\u7528\u4e24\u79cd\u6216\u591a\u79cd\u6df7\u5408\u6eb6\u5242, \u5f53\u6df7\u5408\u6eb6\u5242\u4e2d\u5404\u6eb6\u5242\u8fbe\u5230\u4e00\u5b9a\u6bd4\u4f8b\u65f6, \u836f<\/span>\u7269\u7684\u6eb6\u89e3\u5ea6\u51fa\u73b0\u6700\u5927\u503c, \u8fd9\u79cd\u6eb6\u5242\u88ab\u79f0\u4e3a\u6f5c\u6eb6\u5242\u3002<\/span><\/p>\n

\u6f5c<\/span>\u6eb6\u5242\u5177\u6709\u6c22\u952e\u4f9b\u4f53\u548c\/\u6216\u53d7\u4f53\u4ee5\u53ca\u5c0f\u7684\u70c3\u533a, \u5176\u4e2d\u4eb2\u6c34<\/span>\u6c22\u952e\u57fa\u56e2\u4fdd\u8bc1\u4e86\u4e0e\u6c34\u7684\u76f8\u5bb9\u6027, \u758f\u6c34\u70c3\u533a\u5219\u53ef\u4ee5\u5e72\u6270<\/span>\u6c34\u7684\u6c22\u952e\u7f51\u7edc, \u901a\u8fc7\u7834\u574f\u6c34\u7684\u81ea\u7f14\u5408, \u6f5c\u6eb6\u5242\u964d\u4f4e\u6c34\u6392<\/span>\u65a5\u758f\u6c34\u5316\u5408\u7269\u7684\u80fd\u529b, \u4ece\u800c\u589e\u52a0\u4eb2\u8102\u836f\u7269\u7684\u6eb6\u89e3\u6027, \u4e0d<\/span>\u5b58\u5728\u8f7d\u4f53\u4e0e\u836f\u7269\u76f8\u4e92\u4f5c\u7528\u5f62\u6210\u7ed3\u5408\u6001\u4e0e\u975e\u7ed3\u5408\u6001\u7684\u5173<\/span>\u7cfb, \u6eb6\u89e3\u7684\u836f\u7269\u5747\u4ee5\u5355\u5206\u5b50(\u79bb\u5b50) \u72b6\u6001\u5206\u6563\u4e8e\u6eb6\u5242<\/span>\u4e2d[16,17]\u3002\u7136\u800c\u7814\u7a76\u8868\u660e\u6f5c\u6eb6\u5242\u5728\u589e\u52a0\u836f\u7269\u6eb6\u89e3\u5ea6\u7684\u540c<\/span>\u65f6\u836f\u7269\u6e17\u900f\u6027\u4e5f\u5b58\u5728\u4e0b\u964d\u8d8b\u52bf\u3002<\/span><\/p>\n

Riad \u548cBeig \u7b49[18,19] \u4f7f\u7528\u52a8\u7269\u80a0\u704c\u6ce8\u5b9e\u9a8c\u5206\u6790PEG 400 \u5bf9\u5361\u9a6c\u897f\u5e73\u80a0\u6e17\u900f\u6027\u7684\u5f71\u54cd, \u53d1\u73b0\u968f\u7740PEG<\/span>400 \u6bd4\u4f8b\u589e\u52a0, \u836f\u7269\u6e17\u900f\u6027\u5448\u73b0\u964d\u4f4e\u8d8b\u52bf\u3002<\/span><\/p>\n

\u7c7b\u4f3c\u5730,<\/span>Beig \u7b49[20]\u6bd4\u8f83\u4e8620%\u300160% \u548c100% PEG 400 \u5bf9\u5361\u9a6c<\/span>\u897f\u5e73\u6eb6\u89e3\u6027\u548c\u6e17\u900f\u6027\u7684\u5f71\u54cd\u3002\u53d1\u73b0100% PEG 400 \u589e\u52a0\u6eb6\u89e3\u5ea6\u80fd\u529b\u6700\u5f3a, 20% PEG \u6700\u5f31, \u800c\u836f\u7269\u6e17\u900f\u6027<\/span>\u4f5c\u7528\u5219\u76f8\u53cd\u3002\u53e3\u670d\u751f\u7269\u5229\u7528\u5ea6\u4ece\u9ad8\u5411\u4f4e\u6392\u5217\u4e3a60%<\/span>PEG 400 > 100% PEG 400 > 20% PEG 400\u3002<\/span><\/p>\n

\u63d0\u793aPEG<\/span>400 \u63d0\u9ad8\u53e3\u670d\u751f\u7269\u5229\u7528\u5ea6\u662f\u836f\u7269\u6eb6\u89e3\u6027\u548c\u6e17\u900f\u6027\u7684\u7efc<\/span>\u5408\u6548\u5e94\u3002<\/p>\n

Miller \u7b49[14]\u7814\u7a76\u4e0d\u540c\u6d53\u5ea6PEG 400 \u548c\u4e19\u4e8c\u9187\u5bf9\u9ec4\u4f53\u916e\u7684\u6eb6\u89e3\u6027\u548c\u5927\u9f20\u80a0\u9053\u6e17\u900f\u6027\u7684\u5f71\u54cd, \u5e76\u4f7f\u6240<\/span>\u6709\u6f5c\u6eb6\u5242\u4fdd\u6301\u5728\u7b49\u6548\u7684\u70ed\u529b\u5b66\u6d3b\u6027\u6c34\u5e73, \u4ecd\u51fa\u73b0\u4e86\u7c7b<\/span>\u4f3c\u836f\u7269\u8868\u89c2\u6eb6\u89e3\u5ea6\u589e\u52a0\u800c\u6e17\u900f\u6027\u4e0b\u964d\u7684\u89c4\u5f8b; \u540c\u65f6\u901a<\/span>\u8fc7\u5efa\u7acb\u6570\u5b66\u6a21\u578b\u8bd5\u56fe\u9610\u8ff0\u6f5c\u6eb6\u5242\u4e2dBCS \u2161\u7c7b\u836f\u7269\u6eb6<\/span>\u89e3\u5ea6\u589e\u52a0\u800c\u6e17\u900f\u6027\u4e0b\u964d\u7684\u73b0\u8c61, \u53d1\u73b0\u4e0d\u540c\u4e8e\u73af\u7cca\u7cbe\u548c<\/span>\u8868\u9762\u6d3b\u6027\u5242\u8f7d\u4f53\u6d53\u5ea6\u589e\u52a0\u800c\u964d\u4f4e\u6e38\u79bb\u72b6\u6001\u6240\u6eb6\u89e3\u7684\u836f<\/span>\u7269\u542b\u91cf, \u6f5c\u6eb6\u5242\u6d53\u5ea6\u589e\u52a0\u5bfc\u81f4\u4eb2\u8102\u6027\u836f\u7269\u7684\u8868\u89c2\u6eb6\u89e3<\/span>\u5ea6\u589e\u52a0, \u800c\u964d\u4f4e\u836f\u7269\u7684\u8868\u89c2\u819c\/\u6c34\u5206\u914d\u7cfb\u6570, \u7531\u836f\u7269\u8de8<\/span>\u819c\u6e17\u900f\u7cfb\u6570\u516c\u5f0f\u5206\u6790, \u836f\u7269\u8de8\u819c\u6e17\u900f\u7684\u70ed\u529b\u5b66\u9a71\u52a8\u529b<\/span>\u4e0b\u964d, \u4ece\u800c\u964d\u4f4e\u836f\u7269\u7684\u6e17\u900f\u6027\u3002<\/span><\/p>\n

\u56e0\u6b64, \u901a\u8fc7\u5206\u6790\u73af\u7cca<\/span>\u7cbe\u3001\u8868\u9762\u6d3b\u6027\u5242\u548c\u6f5c\u6eb6\u5242\u4e2dBCS \u2161\u7c7b\u836f\u7269\u7684\u6eb6\u89e3\u6027\u4e0e<\/span>\u6e17\u900f\u6027, \u8ba4\u4e3a\u80fd\u591f\u5f71\u54cd\u6eb6\u89e3\u836f\u7269\u7684\u6e38\u79bb\u6001\u542b\u91cf\u6216\u6539\u53d8<\/span>\u836f\u7269\u8868\u89c2\u819c\/\u6c34\u5206\u914d\u7cfb\u6570\u7684\u5236\u5242\u624b\u6bb5, \u5fc5\u7136\u4f1a\u6539\u53d8BCS<\/span>\u2161\u7c7b\u836f\u7269\u7684\u6e17\u900f\u6027, \u5f53\u8be5\u7406\u8bba\u5e94\u7528\u4e8e\u4f53\u5185\u65f6\u5fc5\u987b\u7ed3\u5408<\/span>\u4f53\u5185\u590d\u6742\u73af\u5883\u8fdb\u884c\u7efc\u5408\u5224\u65ad[21-23]\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
\n
\n
\n
\n
\n

4<\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
\n

\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u5bf9\u836f\u7269\u6eb6\u89e3\u6027-\u6e17\u900f\u6027\u7684\u5f71\u54cd<\/strong><\/p>\n<\/section>\n<\/section>\n

<\/section>\n<\/section>\n<\/section>\n<\/section>\n
\n
\n
\n

\u4e0e\u524d\u8ff0\u6eb6\u89e3\u6027-\u6e17\u900f\u6027\u5185\u5728\u5173\u8054\u7684\u89c4\u5f8b\u4e0d\u540c, \u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u901a\u8fc7\u7ef4\u6301\u836f\u7269\u7684\u8fc7\u9971\u548c\u72b6\u6001\u6765\u589e\u52a0\u5176<\/span>\u6eb6\u89e3\u5ea6, \u5219\u8f83\u5c11\u51fa\u73b0\u836f\u7269\u6e17\u900f\u6027\u964d\u4f4e\u7684\u60c5\u51b5\u3002<\/span><\/p>\n

\u65e0\u5b9a\u5f62<\/span>\u56fa\u4f53\u5206\u6563\u4f53\u4e2d\u836f\u7269\u6eb6\u89e3\u6027\u4e0e\u6e17\u900f\u6027\u7684\u8fd9\u79cd\u76f8\u5173\u6027\u53ef\u4ee5<\/span>\u7528\u524d\u8ff0\u7684\u836f\u7269\u8de8\u819c\u6e17\u900f\u65b9\u7a0b\u89e3\u91ca[24-26]\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
\n
\n

4.1 \u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u4e2d\u836f\u7269\u6eb6\u89e3\u6027-\u6e17\u900f\u6027\u7684\u76f8\u5173<\/strong>\u6027<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
\n
\n

\u6709\u6587\u732e[27]\u53d1\u73b0, \u4e0e\u5bf9\u7167\u7ec4(\u7ed3\u6676\u836f\u7269) \u76f8\u6bd4, \u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u4e2d\u836f\u7269\u7684\u8fc7\u9971\u548c\u5ea6\u5e73\u5747\u80fd\u591f\u8fbe\u5230\u5176\u7279\u6027<\/span>\u6eb6\u89e3\u5ea6\u768428.2 \u500d, \u6e17\u900f\u6027\u5219\u5e73\u5747\u589e\u52a02.39 \u500d\u3002<\/span><\/p>\n

\u7528\u55b7\u96fe\u5e72\u71e5\u6cd5\u5236\u5907BCS \u2161\u7c7b\u836f\u7269\u785d\u82ef\u5730\u5e73\u7684\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53, \u5176\u836f\u7269\u8fc7\u9971\u548c\u5ea6\u53ef\u4ee5\u8fbe\u5230\u5e73\u8861\u6eb6\u89e3<\/span>\u5ea6\u768420 \u500d\u3002<\/span><\/p>\n

\u901a\u8fc7\u7814\u7a76\u4e0d\u540c\u7a0b\u5ea6\u8fc7\u9971\u548c\u6eb6\u6db2\u4e2d\u785d\u82ef\u5730<\/span>\u5e73\u5728PAMPA\u548c\u5927\u9f20\u5c0f\u80a0\u5355\u5411\u704c\u6d41\u4e2d\u7684\u6e17\u900f, \u53d1\u73b0\u6eb6\u89e3<\/span>\u5ea6\u7684\u589e\u52a0\u5e76\u6ca1\u6709\u964d\u4f4e\u836f\u7269\u6e17\u900f\u6027[25]\u3002\u5bf9\u9ec4\u4f53\u916e\u65e0\u5b9a\u5f62<\/span>\u56fa\u4f53\u5206\u6563\u4f53\u7684\u7814\u7a76\u4e5f\u5448\u73b0\u7c7b\u4f3c\u7ed3\u679c[26]\u3002<\/span><\/p>\n

Beig \u7b49[24]\u6bd4\u8f83<\/span>\u4e86HP-\u03b2-CD\u3001PEG 400-\u6c34\u6f5c\u6eb6\u5242\u4f53\u7cfb\u3001\u8868\u9762\u6d3b\u6027\u5242SDS<\/span>\u53caPVP \u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f534 \u79cd\u589e\u52a0\u6eb6\u89e3\u5ea6\u7684\u65b9\u6cd5\u5bf9\u6297<\/span>\u764c\u836f\u4f9d\u6258\u6cca\u82f7\u6eb6\u89e3\u5ea6\u548c\u6e17\u900f\u6027\u7684\u5f71\u54cd\u3002\u53d1\u73b0\u4f7f\u7528\u73af\u7cca<\/span>\u7cbe\u3001\u8868\u9762\u6d3b\u6027\u5242\u548c\u6f5c\u6eb6\u5242\u589e\u52a0\u836f\u7269\u8868\u89c2\u6eb6\u89e3\u5ea6\u65f6\u4f1a\u5bfc<\/span>\u81f4\u836f\u7269\u7684\u6e17\u900f\u6027\u964d\u4f4e, \u800c\u5c06\u836f\u7269\u5236\u5907\u6210\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206<\/span>\u6563\u4f53\u5219\u4e0d\u4f1a\u3002<\/span><\/p>\n

\u7531\u6b64\u53ef\u89c1\uff0c\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u5bf9\u836f\u7269\u6eb6\u89e3\u6027-\u6e17\u900f\u6027\u7684\u5f71\u54cd\u4e0e\u4ee5\u4e0a\u5176\u4ed6\u51e0\u79cd\u589e\u52a0\u6eb6\u89e3\u5ea6\u7684\u65b9\u6cd5\u4e0d\u540c,<\/span>\u5176\u673a\u5236\u53ef\u4ee5\u7528\u836f\u7269\u8de8\u819c\u6e17\u900f\u7cfb\u6570\u65b9\u7a0b\u89e3\u91ca\u3002<\/span><\/p>\n

\u7b80\u800c\u8a00<\/span>\u4e4b, \u836f\u7269\u7684\u6e17\u900f\u6027\u53d7\u5230\u836f\u7269\u819c\/\u6c34\u5206\u914d\u7cfb\u6570\u7684\u5f71\u54cd, \u800c<\/span>\u819c\/\u6c34\u5206\u914d\u7cfb\u6570\u53c8\u7531\u836f\u7269\u7684\u6eb6\u89e3\u6027\u51b3\u5b9a, \u65e0\u5b9a\u5f62\u56fa\u4f53\u5206<\/span>\u6563\u4f53\u662f\u901a\u8fc7\u975e\u5e73\u8861\u52a8\u529b\u5b66\u7684\u9014\u5f84\u589e\u52a0\u836f\u7269\u6eb6\u89e3\u6027, \u5bf9<\/span>\u836f\u7269\u7684\u819c\/\u6c34\u5206\u914d\u7cfb\u6570\u6ca1\u6709\u5f71\u54cd\u3002\u56e0\u6b64, \u836f\u7269\u7684\u6e17\u900f\u7387<\/span>\u4e0d\u53d8\u4e14\u4e0e\u836f\u7269\u7684\u8fc7\u9971\u548c\u7a0b\u5ea6\u65e0\u5173\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
\n
\n

4.2 \u6dfb\u52a0\u805a\u5408\u7269\u8f85\u6599\u5bf9\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u7684\u5f71\u54cd<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
\n
\n

\u56fa\u4f53\u5206\u6563\u4f53\u867d\u7136\u80fd\u663e\u8457\u589e\u52a0\u96be\u6eb6\u6027\u836f\u7269\u6eb6\u89e3\u6027, \u4f46\u5bb9\u6613\u8001\u5316, \u5373\u7269\u7406\u7a33\u5b9a\u6027\u5dee\u662f\u5176\u5e94\u7528\u7684\u7f3a\u70b9\u4e4b\u4e00\u3002<\/span><\/p>\n

\u8fd1\u5e74<\/span>\u6765, \u8bf8\u591a\u7814\u7a76\u5728\u56fa\u4f53\u5206\u6563\u4f53\u4e2d\u6dfb\u52a0\u9002\u5b9c\u7684\u805a\u5408\u7269, \u6709\u52a9<\/span>\u4e8e\u7ef4\u6301\u836f\u7269\u7684\u65e0\u5b9a\u5f62\u72b6\u6001\u3002\u805a\u5408\u7269\u7684\u52a0\u5165\u662f\u5426\u5f71\u54cd<\/span>\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u6eb6\u89e3\u6027-\u6e17\u900f\u6027\u539f\u6709\u7684\u7279\u6027\uff1fFan<\/span>\u7b49[28]\u5728\u7528Eudragit 100 \u5236\u5907\u7684\u59dc\u9ec4\u7d20\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563<\/span>\u4f53\u4e2d\u6dfb\u52a0\u7f9f\u4e19\u57fa\u7532\u57fa\u7ea4\u7ef4\u7d20E5 (HPMC E5), \u53d1\u73b0<\/span>HPMC E5 \u80fd\u591f\u6291\u5236\u836f\u7269\u7ed3\u6676\u7ef4\u6301\u65e0\u5b9a\u5f62\u72b6\u6001, \u540c\u65f6\u964d<\/span>\u4f4e\u78f7\u8102\u53cc\u5206\u5b50\u5c42\u7684\u6709\u5e8f\u5ea6, \u4ece\u800c\u6539\u5584\u836f\u7269\u6e17\u900f\u6027\u3002<\/span><\/p>\n

\u4f46\u4e5f<\/span>\u6709\u7814\u7a76\u8868\u660e, \u4f7f\u7528\u6811\u679d\u72b6\u751f\u7269\u805a\u5408\u7269(dendrimer-like <\/span>biopolymers, DLB) \u5236\u5907\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u65f6, \u7531\u4e8e\u805a<\/span>\u5408\u7269\u548c\u836f\u7269\u5206\u5b50\u53ef\u4ee5\u53d1\u751f\u5206\u5b50\u76f8\u4e92\u4f5c\u7528, \u5728\u6c34\u4e2d\u5f62\u6210<\/span>\u7a33\u5b9a\u7684\u836f\u7269-\u805a\u5408\u7269\u7cfb\u7edf\u901a\u8fc7\u5f71\u54cd\u836f\u7269\u91ca\u653e\u4ece\u800c\u964d\u4f4e<\/span>\u53e3\u670d\u5438\u6536[29,30]\u3002<\/span><\/p>\n

F\u00fcl\u00f6p \u7b49[31]\u901a\u8fc7\u5206\u522b\u6dfb\u52a0\u4e0d\u540c\u7c7b\u578b\u805a<\/span>\u5408\u7269PEG 6000\u3001\u6708\u6842\u9178\u916fD-1216\u3001\u68d5\u6988\u9178\u916fP-1670 \u548c<\/span>\u786c\u8102\u9178\u916fS-1670 \u6210\u529f\u589e\u52a0BCS \u2161\u7c7b\u836f\u7269\u7532\u82ac\u90a3\u9178\u7684<\/span>\u6eb6\u89e3\u5ea6, \u4f46Caco-2 \u7ec6\u80de\u6e17\u900f\u8f6c\u8fd0\u5b9e\u9a8c\u8868\u660e, \u8fd9\u4e9b\u805a\u5408<\/span><\/p>\n

\u7269\u7684\u6dfb\u52a0\u5e76\u6ca1\u6709\u663e\u8457\u6539\u53d8\u836f\u7269\u6e17\u900f\u6027\u3002\u7531\u6b64\u53ef\u89c1, \u805a\u5408\u7269\u8f85\u6599\u7684\u6dfb\u52a0\u4f7f\u5f97\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u4f53\u7cfb\u53d8\u5f97\u590d<\/span>\u6742, \u6b64\u65f6\u836f\u7269\u7684\u6eb6\u89e3\u6027\u548c\u6e17\u900f\u6027\u53d8\u5316\u9700\u8981\u4f9d\u636e\u836f\u7269\u7684<\/span>\u7406\u5316\u6027\u8d28\u548c\u6240\u6dfb\u52a0\u7684\u7269\u8d28\u7efc\u5408\u5224\u65ad\u3002\u53ea\u6709\u9009\u62e9\u9002\u5b9c\u7684<\/span>\u805a\u5408\u7269\u8f85\u6599\u624d\u80fd\u540c\u65f6\u589e\u52a0\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u4e2d\u836f\u7269\u6eb6<\/span>\u89e3\u6027\u548c\u6e17\u900f\u6027, \u66f4\u6709\u6548\u5730\u63d0\u9ad8\u53e3\u670d\u5438\u6536\u3002<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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5<\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
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\u5176\u4ed6\u8fc7\u9971\u548c\u836f\u7269\u9012\u9001\u7cfb(supersaturating drug delivery systems, SDDS)<\/span><\/strong><\/p>\n<\/section>\n<\/section>\n

<\/section>\n<\/section>\n<\/section>\n<\/section>\n
\n
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\n

\u4efb\u4f55\u8fc7\u9971\u548c\u836f\u7269\u9012\u9001\u7cfb\u7edf\u90fd\u53ef\u80fd\u5177\u6709\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u8fd9\u6837\u7684\u7279\u70b9, \u5373\u63d0\u9ad8\u6eb6\u89e3\u5ea6\u540c\u65f6\u4e0d\u964d\u4f4e\u836f\u7269\u6e17<\/span>\u900f\u6027[26]\u3002<\/span>\u56e0\u6b64SDDS \u5236\u5242\u5c06\u4f5c\u4e3a\u63d0\u9ad8\u53e3\u670d\u5438\u6536\u7684\u6709\u6548<\/span>\u624b\u6bb5\u3002<\/span><\/p>\n

SDDS \u4e2d\u7814\u7a76\u6700\u591a\u7684\u662f\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53<\/span>(44.9%), \u5176\u6b21\u662f\u8d85\u9971\u548c\u8102\u8d28\u914d\u65b9(22.2%)\u3001\u7eb3\u7c73\u836f\u7269\u7cfb<\/span>\u7edf(12.4%)\u3001\u4e8c\u6c27\u5316\u7845\u836f\u7269\u7cfb\u7edf(6.5%) \u548c\u5176\u4ed6<\/span>(11.3%)[26]\u3002<\/span><\/p>\n

\u901a\u8fc7\u5bf9\u524d4 \u79cdSDDS \u8fdb\u884cMeta \u5206\u6790, \u53d1\u73b0<\/span>\u4e0e\u836f\u7269\u7ed3\u6676\u76f8\u6bd4, \u5236\u5242\u7684\u6700\u5927\u8fc7\u9971\u548c\u5ea6\u901a\u5e38\u53ef\u4ee5\u8fbe\u5230<\/span>\u836f\u7269\u7279\u6027\u6eb6\u89e3\u5ea6\u768426.7 \u500d; \u4f53\u5916(\u5305\u62ec\u4eba\u5de5\u819c, \u900f\u6790<\/span>\u819c, Caco-2 \u7ec6\u80de\u548cMDCK\u7ec6\u80de\u6a21\u578b\u5b9e\u9a8c) \u548c\u4f53\u5185\u5b9e\u9a8c<\/span>\u6570\u636e(\u5927\u9f20\u80a0\u704c\u6d41\u5b9e\u9a8c) \u4e2dSDDS \u80fd\u4f7f\u836f\u7269\u7684\u603b\u6e17\u900f\u6027\u589e\u52a03.1 \u500d[26]\u3002<\/span><\/p>\n

\u5176\u4e2d, \u7eb3\u7c73\u7ed9\u836f\u7cfb\u7edf\u7684\u4f53\u5916\u8fc7\u9971\u548c\u5ea6\u548c<\/span>\u4f53\u5185\u751f\u7269\u5229\u7528\u5ea6(AUC \u548cCmax) \u63d0\u9ad8\u6700\u660e\u663e, Tmax\u964d\u4f4e<\/span>\u6700\u663e\u8457\u3002<\/span><\/p>\n

Li \u7b49[32]\u7814\u7a76\u53d1\u73b0, BCS \u2161\u7c7b\u836f\u7269\u918b\u9178\u7532\u5730\u5b55<\/span>\u916e\u7684\u7eb3\u7c73\u4e73\u4e0e\u5176\u5fae\u6676\u6df7\u60ac\u5242\u76f8\u6bd4, \u5728\u6bd4\u683c\u72ac\u4e2d\u7684\u53e3\u670d<\/span>\u751f\u7269\u5229\u7528\u5ea6\u63d0\u9ad85 \u500d\u3002\u7eb3\u7c73\u836f\u7269\u7cfb\u7edf\u7684\u6700\u5927\u4f18\u52bf\u662f\u7c92<\/span>\u5f84\u51cf\u5c0f, \u80fd\u591f\u4f7f\u836f\u7269\u7684\u6e17\u900f\u6027\u63d0\u9ad8\u81f3\u539f\u672c\u76843.09 \u500d, \u5176<\/span>\u4ea7\u751f\u8fc7\u9971\u548c\u7684\u80fd\u529b\u4e3b\u8981\u662f\u7531\u4e8e\u7eb3\u7c73\u6676\u4f53\u8868\u9762\u7684\u66f2\u7387\u589e<\/span>\u52a0\u3001\u6676\u4f53\u68f1\u8fb9\u7684\u6bd4\u4f8b\u589e\u52a0\u53ca\u8fb9\u754c\u6269\u6563\u5c42\u7684\u539a\u5ea6\u51cf\u5c0f, \u540c<\/span>\u65f6\u90e8\u5206\u836f\u7269\u975e\u6676\u5316[33,34]\u3002<\/span><\/p>\n

\u4ee5\u4e0a\u7ed3\u679c\u5747\u63d0\u793a, SDDS \u7684\u8fc7<\/span>\u9971\u548c\u7279\u5f81\u80fd\u591f\u540c\u65f6\u63d0\u9ad8\u836f\u7269\u6eb6\u89e3\u6027-\u6e17\u900f\u6027, \u5373\u5728\u589e<\/span>\u52a0\u836f\u7269\u6eb6\u89e3\u5ea6\u7684\u540c\u65f6, \u4e0d\u4f1a\u964d\u4f4e\u751a\u81f3\u63d0\u9ad8\u5176\u6e17\u900f\u6027\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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6<\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
\n

\u8f6c\u8fd0\u86cb\u767d\u5bf9\u836f\u7269\u6eb6\u89e3\u6027-\u6e17\u900f\u6027\u7684\u5f71\u54cd<\/strong><\/p>\n<\/section>\n<\/section>\n

<\/section>\n<\/section>\n<\/section>\n<\/section>\n
\n
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\n

BCS \u2161\u7c7b\u836f\u7269\u4e3b\u8981\u901a\u8fc7\u88ab\u52a8\u6269\u6563\u8fdb\u5165\u7ec6\u80de, \u7136\u800c\u5916\u6392\u8f6c\u8fd0\u86cb\u767d\u5982P-gp \u53c2\u4e0e\u4eb2\u8102\u6027\u836f\u7269\u7684\u80c3\u80a0\u9053\u6e17\u900f<\/span>\u8fc7\u7a0b\u5219\u4f1a\u6781\u5927\u5730\u5f71\u54cd\u836f\u7269\u7684\u6e17\u900f[35,36]\u3002<\/span><\/p>\n

\u5927\u91cf\u7814\u7a76\u8868<\/span>\u660e, \u4f7f\u836f\u7269\u5904\u4e8e\u8fc7\u9971\u72b6\u6001\u548c\/\u6216\u6291\u5236\u8f6c\u8fd0\u86cb\u767d\u53ef\u589e\u52a0<\/span>BCS \u2161\u7c7b\u836f\u7269\u5728\u80c3\u80a0\u9053\u4e2d\u7684\u6e17\u900f\u6027\u3002<\/p>\n

\u5229\u798f\u6614\u660e\u662f\u7531\u5229\u798f\u9709\u7d20\u6539\u826f\u7684\u6297\u751f\u7d20\u884d\u751f\u7269, \u4e3aBCS \u2163\u7c7b\u836f\u7269\u5177\u6709\u4f4e\u6eb6\u89e3\u5ea6\u548c\u4f4e\u6e17\u900f\u6027, \u5e7f\u6cdb\u7528\u4e8e\u6cbb<\/span>\u7597\u80c3\u80a0\u9053\u7ec6\u83cc\u611f\u67d3\u3002\u9664\u4e86\u53d7\u9650\u4e8e\u6eb6\u89e3\u5ea6, \u5229\u798f\u6614\u660e\u6e17<\/span>\u900f\u6027\u53d7\u5230P-gp \u4ecb\u5bfc\u7684\u5916\u6392\u8f6c\u8fd0\u5f71\u54cd\u3002Beig \u7b49[37]\u8bbe\u8ba1<\/span>\u4e86\u4e00\u79cd\u9ad8\u8fc7\u9971\u548c\u6c34\u5e73\u7684\u5229\u798f\u6614\u660e\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u3002<\/span><\/p>\n

\u5f53\u836f\u7269\u7684\u8fc7\u9971\u548c\u6c34\u5e73\u4e3a\u7279\u6027\u6eb6\u89e3\u5ea6\u7684100 \u500d\u65f6, \u5229\u798f\u6614\u660e\u5728\u5927\u9f20\u4f53\u5185\u7684\u80a0\u9053\u6e17\u900f\u6027\u4fdd\u6301\u4e0d\u53d8; \u5f53\u836f\u7269\u7684\u8fc7<\/span>\u9971\u548c\u6c34\u5e73\u4e3a\u7279\u6027\u6eb6\u89e3\u5ea6\u7684250 \u500d\u65f6, \u836f\u7269\u7684\u80a0\u9053\u6e17\u900f<\/span>\u6027\u663e\u8457\u589e\u52a0\u3002\u7136\u800c\u836f\u7269\u5728PAMPA\u4e0a\u7684\u6e17\u900f\u6027\u59cb\u7ec8\u4fdd<\/span>\u6301\u4e0d\u53d8\u3002\u8fd9\u63d0\u793a, \u5f53\u836f\u7269\u662fP-gp \u7684\u5e95\u7269\u65f6, \u65e0\u5b9a\u5f62\u56fa<\/span>\u4f53\u5206\u6563\u4f53\u53ef\u4ee5\u901a\u8fc7\u9971\u548c\u5916\u6392\u8f6c\u8fd0\u86cb\u767dP-gp \u589e\u52a0\u836f\u7269<\/span>\u6e17\u900f\u6027\u3002<\/span><\/p>\n

Beig \u7b49[15]\u53d1\u73b0\u7ef4\u751f\u7d20E \u805a\u4e59\u4e8c\u9187\u7425\u73c0\u9178\u916f<\/span>(TPGS) \u80fd\u6291\u5236\u4f53\u5185p-\u7cd6\u86cb\u767d(P-gp) \u8868\u8fbe, \u51cf\u5c11\u836f\u7269\u5916<\/span>\u6392, \u968f\u7740TPGS \u6d53\u5ea6\u63d0\u9ad8\u4f9d\u6258\u6cca\u82f7\u6eb6\u89e3\u5ea6\u589e\u52a0\u540c\u65f6\u5728<\/span>\u5927\u9f20\u80a0\u9053\u704c\u6d41\u7684\u6e17\u900f\u7387\u4e5f\u663e\u8457\u589e\u52a0\u3002<\/span><\/p>\n

\u503c\u5f97\u6ce8\u610f\u7684\u662f, \u5bf9\u4e8e\u975eP-gp \u4f5c\u7528\u5e95\u7269\u7684\u836f\u7269, \u52a0\u5165\u5177\u6709\u5916\u6392\u8f6c\u8fd0\u4f53\u6291\u5236\u4f5c\u7528\u7684\u805a\u5408\u7269, \u4e5f\u80fd\u83b7\u5f97\u7c7b\u4f3c<\/span>\u7ed3\u679c\u3002<\/span><\/p>\n

\u5229\u4f10\u6c99\u6591\u662f\u4e00\u79cd\u53e3\u670d\u6d3b\u6027\u4e1d\u6c28\u9178\u86cb\u767d\u9176\u56e0\u5b50<\/span>Xa \u6291\u5236\u5242, \u7528\u4e8e\u6cbb\u7597\u9759\u8109\u8840\u6813\u6813\u585e\u75c7, \u88ab\u8ba4\u4e3a\u662fP-gp<\/span>\u7684\u4e0d\u9971\u548c\u5e95\u7269, \u6781\u5927\u9650\u5236\u5b83\u7684\u6e17\u900f\u6027\u3002<\/span><\/p>\n

Mohammadzadeh<\/span>\u7b49[38]\u7814\u7a76\u4f7f\u7528Eudragit S100\u3001Eudragit L100 \u548cSoluplus<\/span>\u5236\u5907\u5229\u4f10\u6c99\u6591\u7684\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53, \u7ed3\u679c\u663e\u793aSoluplus<\/span>\u5236\u5907\u7684\u5229\u4f10\u6c99\u6591\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u7684\u8868\u89c2\u6eb6\u89e3\u5ea6\u6bd4\u5229\u4f10\u6c99\u6591\u6676\u4f53\u589e\u52a0\u4e8610 \u500d\u3002<\/span><\/p>\n

Caco-2 \u8f6c\u8fd0\u5b9e\u9a8c\u8868\u660e,<\/span>Eudragit S100 \u6240\u5236\u5907\u7684\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u7684\u5916\u6392\u7387\u6bd4<\/span>\u5229\u4f10\u6c99\u6591\u6676\u4f53\u663e\u8457\u964d\u4f4e\u4e86\u7ea666.7%, \u800cEudragit L100<\/span>\u7ec4\u6ca1\u6709\u663e\u8457\u53d8\u5316\u3002<\/p>\n

\u56e0\u6b64\u63a8\u6d4bEudragit S100 \u5177\u6709\u964d\u4f4eP-gp \u8868\u8fbe\u7684\u80fd\u529b, \u5bf9P-gp \u5e95\u7269\u7684\u5916\u6392\u8fc7\u7a0b\u6709\u6291\u5236\u4f5c\u7528<\/span>\u800c\u589e\u5f3a\u836f\u7269\u6e17\u900f\u6027\u3002Soluplus \u5236\u5907\u7684\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563<\/span>\u4f53\u7684\u5916\u6392\u7387\u4e0b\u964d, \u4f46Soluplus \u4e0d\u5f71\u54cd\u5e95\u7269\u4e0eP-gp \u7684\u7ed3<\/span>\u5408, \u4e5f\u4e0d\u6539\u53d8\u7ec6\u80de\u819c\u4e0aP-gp \u7684\u8868\u8fbe, \u8bf4\u660eSoluplus \u662f\u901a\u8fc7\u4e0eP-gp \u53d1\u751f\u95f4\u63a5\u76f8\u4e92\u4f5c\u7528\u548c\u6539\u53d8\u7ec6\u80de\u819c\u7684\u6d41\u52a8\u6027<\/span>\u6765\u5b9e\u73b0\u5bf9P-gp \u7684\u6291\u5236\u4ece\u800c\u63d0\u9ad8\u836f\u7269\u5728\u80c3\u80a0\u9053\u7684\u6e17\u900f<\/span>\u6027[39]\u3002<\/span><\/p>\n

\u7efc\u4e0a, \u4f7f\u7528\u9002\u5b9c\u7684\u8f85\u6599\u5236\u5907\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53<\/span>\u53ef\u4ee5\u589e\u52a0\u836f\u7269\u6eb6\u89e3\u6027\u53c8\u6291\u5236P-gp \u6d3b\u6027, \u4ece\u800c\u63d0\u9ad8\u836f\u7269<\/span>\u53e3\u670d\u5438\u6536\u751f\u7269\u5229\u7528\u5ea6[40]\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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7<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u65b0\u578b\u836f\u7269\u6eb6\u89e3\u6027\u4e0e\u6e17\u900f\u6027\u8bc4\u4ef7\u65b9\u6cd5<\/strong><\/p>\n<\/section>\n<\/section>\n

<\/section>\n<\/section>\n<\/section>\n<\/section>\n
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\u968f\u7740\u5206\u6790\u548c\u5fae\u578b\u5316\u6280\u672f\u7684\u53d1\u5c55, \u836f\u7269\u5438\u6536\u7b5b\u9009\u6a21\u578b\u5728\u836f\u7269\u7814\u7a76\u4e2d\u7684\u5e94\u7528\u8fc5\u901f\u53d1\u5c55\u8d77\u6765, \u4ece\u751f\u7269\u819c\u8f6c\u8fd0<\/span>\u5668\u7ec6\u80de\u6a21\u578b\u5982Caco-2 \u7ec6\u80de\u3001\u5230\u4f53\u5916\u5438\u6536\u5b9e\u9a8c\u5982Ussing <\/span>chamber \u6269\u6563\u6c60\u53ca\u5728\u4f53\u52a8\u7269\u5b9e\u9a8c\u5982\u5c0f\u80a0\u5355\u5411\u704c\u6d41<\/span>\u7b49[41,42]\u3002<\/span><\/p>\n

\u76ee\u524d\u5df2\u5efa\u7acb\u8bb8\u591a\u65b0\u578b\u836f\u7269\u5438\u6536\u8bc4\u4ef7\u6a21\u578b, \u5177<\/span>\u6709\u540c\u6b65\u8bc4\u4ef7\u836f\u7269\u6eb6\u89e3\u6027\u548c\u6e17\u900f\u6027\u7684\u4f18\u52bf, \u4fbf\u4e8e\u7b5b\u9009\u836f<\/span>\u7269\u53e3\u670d\u5438\u6536\u6700\u4f73\u5904\u65b9\u3002<\/span><\/p>\n

Fong \u7b49[43]\u63d0\u51fa\u4e00\u79cd\u65b0\u578b\u7684\u5fae\u900f\u6790-\u6eb6\u51fa\/\u6e17\u900f\u7cfb\u7edf[microdialysis-dissolution\/permeation (M-D\/P) system],<\/span>\u5c06\u5fae\u900f\u6790\u5355\u5143\u56fa\u5b9a\u5728\u6eb6\u51fa\u6c60\u4e2d, \u4eff\u751f\u819cPermeapad\u00ae\u4f5c<\/span>\u4e3a\u80a0\u9053\u5438\u6536\u5c4f\u969c\u56fa\u5b9a\u4e8e\u63a5\u6536\u5ba4, \u80fd\u591f\u540c\u65f6\u8bc4\u4ef7\u836f\u7269\u7684<\/span>\u6eb6\u89e3\u4e0e\u6e17\u900f\u884c\u4e3a, \u5177\u6709\u5bf9\u6e17\u900f\u8fc7\u7a0b\u5e72\u6270\u5c0f\u3001\u8282\u7701\u65f6\u95f4<\/span>\u548c\u91c7\u6837\u65f6\u95f4\u51c6\u786e\u7684\u4f18\u52bf\u3002Ruponen \u7b49[44]\u5229\u7528PAMPA<\/span>\u56fa\u5b9a\u4e8e\u7279\u6b8a\u7684\u6269\u6563\u6c60\u4e2d, \u540c\u65f6\u6d4b\u5b9a\u683c\u5217\u672c\u8132\u4e0e\u4e1d\u6c28\u9178<\/span>\u6216\u7cbe\u6c28\u9178\u5171\u6676\u4f53\u7cfb\u4e2d\u836f\u7269\u7684\u6eb6\u89e3\u548c\u6e17\u900f\u6027, \u5efa\u7acb\u4e86<\/span>\u4e00\u4e2a\u7b80\u5355\u6613\u5f97\u7528\u4e8e\u7b5b\u9009\u65e0\u5b9a\u5f62\u5236\u5242\u7684\u5de5\u5177\u3002<\/span><\/p>\n

\u4e0d\u540c\u4e8e\u7ec6<\/span>\u80de\u6216\u7ec4\u7ec7\u4e0a\u7684\u6e17\u900f\u5b9e\u9a8c, Berben \u7b49[45]\u53d1\u660e\u4e86\u4e00\u79cd\u9ad8\u6548<\/span>\u53c8\u7ecf\u6d4e\u7684\u4eba\u5de5\u819c\u5d4c\u5165\u7cfb\u7edf(artificial membrane insert system, AMI-system), \u7ed3\u5408\u6eb6\u51fa\u5b9e\u9a8c\u7528\u4e8e\u521d\u6b65\u8bc4\u4ef7\u5236<\/span>\u5242\u53e3\u670d\u5438\u6536\u6548\u679c\u3002\u5b9e\u9a8c\u8868\u660e, AMI-system\u80fd\u5f88\u597d\u5730\u9884<\/span>\u6d4b3 \u79cd\u96be\u6eb6\u6027\u836f\u7269\u7684\u6eb6\u89e3\u6027\u548c\u6e17\u900f\u6027, \u5305\u62ecpH\u53d8\u5316\u5bf9<\/span>\u6df7\u60ac\u5242\u4e2d\u6cca\u6c99\u5eb7\u5511\u5438\u6536\u7684\u5f71\u54cd; \u80a0\u9053\u7a00\u91ca\u5bf9\u73af\u7cca\u7cbe\u5305<\/span>\u5408\u7269\u4e2d\u4f0a\u66f2\u5eb7\u5511\u5438\u6536\u7684\u5f71\u54cd; \u98df\u7269\u6444\u53d6\u5bf9\u975e\u8bfa\u8d1d\u7279\u5438\u6536\u7684\u5f71\u54cd\u3002<\/span><\/p>\n

\u56e0\u6b64, \u5408\u7406\u9009\u62e9\u65b0\u578b\u836f\u7269\u5438\u6536\u8bc4\u4ef7\u624b\u6bb5, \u80fd<\/span>\u591f\u540c\u6b65\u8bc4\u4ef7\u836f\u7269\u6eb6\u89e3\u6027\u4e0e\u6e17\u900f\u6027, \u4fbf\u4e8e\u7814\u7a76\u8005\u7b5b\u9009\u53e3<\/span>\u670d\u5438\u6536\u7684\u6700\u4f73\u5904\u65b9\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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8<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u7ed3\u8bed<\/strong><\/p>\n<\/section>\n<\/section>\n

<\/section>\n<\/section>\n<\/section>\n<\/section>\n
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\u63d0\u9ad8BCS \u2161\u7c7b\u836f\u7269\u53e3\u670d\u5438\u6536, \u5bf9\u4e8e\u4e34\u5e8a\u5e94\u7528\u5177\u6709\u5341\u5206\u91cd\u8981\u7684\u610f\u4e49\u3002\u4f20\u7edf\u7684\u5236\u5242\u8bbe\u8ba1\u4e3b\u8981\u805a\u7126\u4e8e\u63d0\u9ad8\u836f<\/span>\u7269\u6eb6\u89e3\u6027, \u800c\u5ffd\u7565\u4e86\u5176\u5bf9\u80c3\u80a0\u9053\u6e17\u900f\u6027\u7684\u5f71\u54cd, \u4ece\u800c\u5f31<\/span>\u5316\u4e86\u5236\u5242\u7b56\u7565\u5bf9\u836f\u7269\u53e3\u670d\u5438\u6536\u7684\u603b\u6548\u5e94\u3002\u63d0\u9ad8\u836f\u7269\u8868<\/span>\u89c2\u6eb6\u89e3\u5ea6\u7684\u4e0d\u540c\u7b56\u7565\u5982\u73af\u7cca\u7cbe\u5305\u5408\u7269\u3001\u8868\u9762\u6d3b\u6027\u5242\u8f7d<\/span>\u4f53\u3001\u6f5c\u6eb6\u5242\u3001\u65e0\u5b9a\u5f62\u56fa\u4f53\u5206\u6563\u4f53\u548c\u5176\u4ed6\u8fc7\u9971\u548c\u836f\u7269\u9012\u9001<\/span>\u7cfb\u7edf\u5bf9\u6e17\u900f\u6027\u7684\u5f71\u54cd\u4e0d\u540c\u3002<\/span><\/p>\n

\u836f\u7269\u5f62\u6210\u73af\u7cca\u7cbe\u5305\u5408\u7269\u6216<\/span>\u88ab\u8868\u9762\u6d3b\u6027\u5242\u589e\u6eb6, \u7531\u4e8e\u4f53\u7cfb\u4e2d\u6e38\u79bb\u72b6\u6001\u6eb6\u89e3\u7684\u836f\u7269<\/span>\u6d53\u5ea6\u964d\u4f4e, \u4f7f\u5f97\u836f\u7269\u5728\u80c3\u80a0\u9053\u6e17\u900f\u6027\u4e0b\u964d; \u6f5c\u6eb6\u5242\u901a\u8fc7<\/span>\u964d\u4f4e\u6c34\u6392\u65a5\u758f\u6c34\u5316\u5408\u7269\u7684\u80fd\u529b\u589e\u52a0\u836f\u7269\u8868\u89c2\u6eb6\u89e3\u5ea6,\u800c\u964d\u4f4e\u836f\u7269\u819c\/\u6c34\u5206\u914d\u7cfb\u6570\u5bfc\u81f4\u6e17\u900f\u6027\u4e0b\u964d; \u65e0\u5b9a\u5f62\u56fa<\/span>\u4f53\u5206\u6563\u4f53\u548c\u5176\u4ed6\u8fc7\u9971\u548c\u836f\u7269\u9012\u9001\u7cfb\u7edf\u80fd\u5728\u6709\u6548\u63d0\u9ad8\u836f<\/span>\u7269\u6eb6\u89e3\u5ea6\u7684\u540c\u65f6, \u4e0d\u6539\u53d8\u751a\u81f3\u589e\u52a0\u5176\u836f\u7269\u6e17\u900f\u6027, \u4f46\u4ecd<\/span>\u9700\u9488\u5bf9\u5177\u4f53\u836f\u7269\u9009\u62e9\u9002\u5b9c\u7684\u8f85\u6599\u63a7\u5236\u8fc7\u9971\u548c\u7a0b\u5ea6\u3002<\/span><\/p>\n

\u6b64<\/span>\u5916, \u5916\u6392\u8f6c\u8fd0\u86cb\u767d(P-gp) \u5728\u4f53\u5185\u80c3\u80a0\u9053\u8f6c\u8fd0\u4e2d\u53d1\u6325\u91cd<\/span>\u8981\u4f5c\u7528, \u4f7f\u836f\u7269\u5904\u4e8e\u8fc7\u9971\u548c\u72b6\u6001\u548c\/\u6216\u6291\u5236\u8f6c\u8fd0\u86cb\u767d\u53ef<\/span>\u4ee5\u589e\u52a0BCS \u2161\u7c7b\u836f\u7269\u5728\u80c3\u80a0\u9053\u4e2d\u7684\u6e17\u900f\u6027, \u540c\u65f6\u5229\u7528<\/span>\u65b0\u578b\u6280\u672f\u624b\u6bb5\u80fd\u591f\u66f4\u597d\u6a21\u62df\u4f53\u5185\u836f\u7269\u6eb6\u89e3\u4e0e\u6e17\u900f\u884c<\/span>\u4e3a, \u7b5b\u9009\u6700\u4f73\u53e3\u670d\u5438\u6536\u5904\u65b9\u3002<\/span><\/p>\n

\u7efc\u4e0a, \u836f\u5b66\u5de5\u4f5c\u8005\u5728\u8fdb\u884c<\/span>\u5236\u5242\u8bbe\u8ba1\u65f6\u5e94\u5468\u5bc6\u8003\u8651\u4e0d\u540c\u5242\u578b\u4e2d\u836f\u7269\u6eb6\u89e3\u6027\u548c\u6e17\u900f<\/span>\u6027\u7684\u5f71\u54cd, \u6df1\u5165\u4e86\u89e3\u4e0d\u540c\u5236\u5242\u7b56\u7565\u4e2d\u836f\u7269\u7684\u6eb6\u89e3\u4e0e\u6e17<\/span>\u900f\u6027\u76f8\u5173\u6027, \u5e76\u7ed3\u5408\u4f53\u5185\u590d\u6742\u56e0\u7d20\u624d\u80fd\u66f4\u597d\u5730\u5236\u5b9a\u63d0<\/span>\u9ad8\u53e3\u670d\u5438\u6536\u6700\u4f73\u5904\u65b9, \u63d0\u9ad8\u5236\u5242\u8bbe\u8ba1\u7684\u5408\u7406\u6027\u4e0e\u89c4<\/span>\u8303\u6027\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\"\u901a\u8fc7\u589e\u52a0\u6eb6\u89e3\u5ea6\u63d0\u9ad8BCS<\/p>\n
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\u53c2\u8003\u6587\u732e<\/strong><\/p>\n<\/section>\n

\"\u901a\u8fc7\u589e\u52a0\u6eb6\u89e3\u5ea6\u63d0\u9ad8BCS<\/section>\n

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\u8be6\u89c1\u539f\u6587\uff0c\u836f\u5b66\u5b66\u62a5 Acta Pharmaceutica Sinica 2019, 54(1): 1 \u22127<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u514d\u8d23\u58f0\u660e<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n

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\u672c\u516c\u4f17\u53f7\u53d1\u5e03\u7684\u6587\u7ae0\u5747\u4e3a\u4fc3\u8fdb\u5236\u836f\u754c\u540c\u884c\u7684\u4ea4\u6d41\u4e0e\u5b66\u4e60\uff1b\u5185\u5bb9\u7531\u5c0f\u7f16\u67e5\u9605\u6587\u732e\u9009\u53d6\uff0c\u6392\u7248\u4e0e\u7f16\u8f91\u4e3a\u539f\u521b\u3002\u5982\u8f6c\u8f7d\uff0c\u8bf7\u6ce8\u660e\u6765\u6e90\u3002<\/p>\n

\u9009\u53d6\u7684\u6587\u7ae0\u5df2\u660e\u786e\u6ce8\u660e\u6765\u6e90\u548c\u4f5c\u8005\uff0c\u7248\u6743\u5f52\u539f\u4f5c\u8005\u6240\u6709\uff0c\u5982\u6d89\u53ca\u4f5c\u54c1\u5185\u5bb9\u3001\u7248\u6743\u6216\u5176\u4ed6\u95ee\u9898\uff0c\u8bf7\u8054\u7cfb\u6211\u4eec\u8fdb\u884c\u5220\u9664\u3002<\/strong><\/p>\n

\u6587\u7ae0\u5185\u5bb9\u4e3a\u4f5c\u8005\u89c2\u70b9\uff0c\u4e0d\u4ee3\u8868\u672c\u516c\u4f17\u53f7\u7acb\u573a\u3002<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u6587\u7ae0\u641c\u7d22<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n<\/section>\n

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\u672c\u516c\u4f17\u53f7\u5f00\u901a\u5f80\u671f\u6587\u7ae0\u4efb\u610f\u641c\u529f\u80fd\u5566
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\u5728\u516c\u4f17\u53f7\u83dc\u5355\u680f\u4e2d\u8f93\u5165\u201c\u641c\u7d22\u201d\uff0c\u5373\u53ef\u641c\u7d22\u5f80\u671f\u5fae\u4fe1\u5185\u5bb9<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\"\u901a\u8fc7\u589e\u52a0\u6eb6\u89e3\u5ea6\u63d0\u9ad8BCS<\/section>\n<\/section>\n<\/section>\n<\/section><\/div>\n","protected":false},"excerpt":{"rendered":"

\u901a\u8fc7\u589e\u52a0\u6eb6\u89e3\u5ea6\u63d0\u9ad8BCS \u2161\u7c7b\u836f\u7269\u53e3\u670d\u5438\u6536:\u5e38\u5e38\u88ab\u5ffd\u7565\u7684\u836f\u7269\u6e17\u900f\u6027 Improving oral absorp […]<\/p>\n","protected":false},"author":1,"featured_media":98126,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":[],"categories":[1],"tags":[],"_links":{"self":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts\/98125"}],"collection":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/comments?post=98125"}],"version-history":[{"count":1,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts\/98125\/revisions"}],"predecessor-version":[{"id":98140,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts\/98125\/revisions\/98140"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/media\/98126"}],"wp:attachment":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/media?parent=98125"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/categories?post=98125"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/tags?post=98125"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}