{"id":98145,"date":"2019-02-27T00:00:50","date_gmt":"2019-05-17T08:13:16","guid":{"rendered":"http:\/\/www.05921.net\/index.php\/98145\/"},"modified":"2019-05-17T16:13:21","modified_gmt":"2019-05-17T08:13:21","slug":"62824db5ea","status":"publish","type":"post","link":"https:\/\/www.05921.net\/index.php\/98145\/","title":{"rendered":"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76"},"content":{"rendered":"
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In vitro-in vivo correlation of goserelin acetate microspheres<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n
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\u6765\u6e90<\/strong><\/p>\n<\/section>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/section>\n

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\u836f\u5b66\u5b66\u62a5 Acta Pharmaceutica Sinica, 2019, 54(1): 159 \u2212165<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n
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\u4f5c\u8005<\/strong><\/p>\n<\/section>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/section>\n

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\u738b\u68a6\u8fea, \u859b\u82f1, \u51b7\u5e7f\u610f, \u8bb8\u4e3d\u6653, \u95eb\u9759\u9759, \u4f59\u98de, \u6768\u5316\u65b0, \u5218\u4e07\u5349<\/p>\n

\u70df\u53f0\u5927\u5b66\u836f\u5b66\u9662\u65b0\u578b\u5236\u5242\u4e0e\u751f\u7269\u6280\u672f\u836f\u7269\u7814\u7a76\u5c71\u4e1c\u7701\u9ad8\u6821\u534f\u540c\u521b\u65b0\u4e2d\u5fc3<\/p>\n

\u5c71\u4e1c\u7eff\u53f6\u5236\u836f\u6709\u9650\u516c\u53f8\u957f\u6548\u548c\u9776\u5411\u5236\u5242\u56fd\u5bb6\u91cd\u70b9\u5b9e\u9a8c\u5ba4<\/span><\/p>\n

\u4e2d\u56fd<\/span>\u98df\u54c1\u836f\u54c1\u68c0\u5b9a\u7814\u7a76\u9662<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n
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\u6458\u8981<\/strong><\/p>\n<\/section>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/section>\n

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\u76ee\u7684\uff1a<\/strong>\u672c\u7814\u7a76\u662f\u5bf9\u6ce8\u5c04\u7528\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u5efa\u7acb\u4f53\u5185\u5916\u76f8\u5173\u6027(in vitro-in vivo correlation, IVIVC)\u3002<\/p>\n

\u65b9\u6cd5\uff1a<\/span><\/strong>\u5236<\/span>\u5907\u4e863 \u79cd\u91ca\u653e\u901f\u7387\u4e0d\u540c\u7684\u6ce8\u5c04\u7528\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403, \u5e76\u5bf9\u5176\u7269\u7406\u5316\u5b66\u6027\u8d28\u8fdb\u884c\u4e86\u8868\u5f81; \u91c7\u7528\u6052\u6e29\u6c34\u6d74\u632f\u8361\u6cd5\u6d4b\u5b9a\u4e86<\/span>3 \u79cd\u5fae\u7403\u7684\u4f53\u5916\u91ca\u653e\u5ea6\u66f2\u7ebf\u5e76\u7814\u7a76\u4e86\u5728\u8be5\u6761\u4ef6\u4e0b\u7684\u91ca\u653e\u673a\u5236; \u4ee5SD\u5927\u9f20\u4e3a\u52a8\u7269\u6a21\u578b, \u7814\u7a763 \u79cd\u5fae\u7403\u5728\u4f53\u5185\u7684\u836f\u4ee3\u52a8<\/span>\u529b\u5b66\u7279\u6027, \u836f\u4ee3\u52a8\u529b\u5b66\u5b9e\u9a8c\u65b9\u6848\u7ecf\u5c71\u4e1c\u7eff\u53f6\u5236\u836f\u6709\u9650\u516c\u53f8\u52a8\u7269\u4f26\u7406\u59d4\u5458\u4f1a\u6279\u51c6\u5b9e\u65bd; \u8840\u836f\u6d53\u5ea6-\u65f6\u95f4\u66f2\u7ebf\u7ecf% AUC<\/span>\u6cd5\u5904\u7406\u540e\u5f97\u5230\u4f53\u5185\u7d2f\u79ef\u91ca\u653e\u66f2\u7ebf, \u5e76\u4e0e\u4f53\u5916\u7d2f\u79ef\u91ca\u653e\u66f2\u7ebf\u8fdb\u884c\u76f8\u5173\u6027\u5206\u6790\u3002<\/span><\/p>\n

\u7ed3\u679c\u8868\u660e<\/span><\/strong>, \u672c\u6587\u5f00\u53d1\u7684\u4f53\u5916\u91ca\u653e\u5ea6\u6d4b\u5b9a<\/span>\u65b9\u6cd5\u5bf9\u4e0d\u540c\u7684\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u5177\u6709\u826f\u597d\u7684\u533a\u5206\u80fd\u529b, \u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u826f\u597d(r > 0.98), \u5e76\u5728SD<\/span>\u5927\u9f20\u4f53\u5185\u5177\u6709\u826f\u597d\u7684\u9884\u6d4b\u80fd\u529b\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/section>\n

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\u53ef\u751f\u7269\u964d\u89e3\u7684\u805a\u5408\u7269\u5fae\u7403\u4f5c\u4e3a\u4e00\u79cd\u50a8\u5e93\u578b\u91ca\u836f\u7cfb\u7edf, \u7531\u4e8e\u5176\u9aa8\u67b6\u6750\u6599\u5177\u6709\u826f\u597d\u7684\u751f\u7269\u76f8\u5bb9\u6027\u548c\u751f\u7269\u53ef<\/span>\u964d\u89e3\u6027, \u80fd\u589e\u5f3a\u86cb\u767d\u7c7b\u836f\u7269\u7684\u7a33\u5b9a\u6027, \u964d\u4f4e\u6bd2\u526f\u4f5c\u7528,<\/span>\u5ef6\u957f\u836f\u7269\u91ca\u653e\u65f6\u95f4, \u51cf\u5c11\u7ed9\u836f\u9891\u6b21, \u6539\u5584\u60a3\u8005\u4f9d\u4ece\u6027,<\/span>\u5728\u8fc7\u53bb\u51e0\u5341\u5e74\u5f15\u8d77\u4e86\u5e7f\u6cdb\u7684\u5173\u6ce8[1-5], \u5e76\u6709\u591a\u4e2a\u4ea7\u54c1\u4e0a<\/span>\u5e02\u3002<\/span><\/p>\n

\u7136\u800c, \u5236\u5907\u5de5\u827a\u5fae\u5c0f\u7684\u53d8\u5316\u90fd\u53ef\u80fd\u6539\u53d8\u805a\u5408\u7269\u5fae<\/span>\u7403\u7684\u5173\u952e\u8d28\u91cf\u53c2\u6570, \u8fd9\u6709\u53ef\u80fd\u6539\u53d8\u836f\u7269\u5728\u4f53\u5185\u7684\u91ca\u653e<\/span>\u7279\u6027[6], \u4ece\u800c\u4ea7\u751f\u4e25\u91cd\u7684\u4e0d\u826f\u53cd\u5e94\u548c\u6bd2\u6027\u3002<\/span><\/p>\n

\u91ca\u836f\u884c\u4e3a<\/span>\u662f\u65b0\u578b\u91ca\u836f\u7cfb\u7edf(\u5982\u53e3\u670d\u7f13\u63a7\u91ca\u5236\u5242\u3001\u5fae\u7403\u3001\u7eb3\u7c73\u7c92<\/span>\u7b49) \u7684\u91cd\u8981\u8d28\u91cf\u5c5e\u6027, \u826f\u597d\u7684\u4f53\u5916\u91ca\u653e\u5ea6\u65b9\u6cd5\u65e2\u53ef\u7528<\/span>\u4e8e\u4ea7\u54c1\u7684\u8d28\u91cf\u63a7\u5236\u53c8\u53ef\u53cd\u6620\u836f\u7269\u5728\u4f53\u5185\u91ca\u653e\u6027\u80fd\u4ee5\u786e<\/span>\u4fdd\u4ea7\u54c1\u7684\u6709\u6548\u6027\u548c\u5b89\u5168\u6027[7,8], \u8f83\u4f53\u5185\u91ca\u653e\u5ea6\u6d4b\u5b9a\u66f4\u9002<\/span>\u4e8e\u5236\u5242\u91ca\u836f\u884c\u4e3a\u7684\u8bc4\u4ef7\u3002<\/span><\/p>\n

\u4f53\u5916\u91ca\u653e\u5ea6\u65b9\u6cd5\u80fd\u4ee3\u66ff\u4f53\u5185<\/span>\u65b9\u6cd5\u8fdb\u884c\u5236\u5242\u8bc4\u4ef7\u7684\u524d\u63d0\u662f\u4f53\u5916\u91ca\u653e\u5ea6\u65b9\u6cd5\u80fd\u8f83\u597d\u5730<\/span>\u53cd\u6620\u5236\u5242\u5728\u4f53\u5185\u7684\u91ca\u836f\u884c\u4e3a, \u5373\u5177\u6709\u4f53\u5185\u5916\u76f8\u5173\u6027 <\/span>(in vitro-in vivo correlation, IVIVC)\u3002<\/p>\n

FDA \u836f\u54c1\u8bc4\u4ef7\u548c\u7814\u7a76\u4e2d\u5fc3(CDER) \u5c06IVIVC \u5b9a\u4e49\u4e3a: \u63cf\u8ff0\u67d0\u4e00\u836f\u7269\u7f13<\/span>\u63a7\u91ca\u5236\u5242\u7684\u4f53\u5916\u7279\u5f81(\u901a\u5e38\u662f\u836f\u7269\u7684\u4f53\u5916\u91ca\u653e\u901f\u7387\u6216<\/span>\u91ca\u653e\u7a0b\u5ea6) \u4e0e\u4f53\u5185\u53cd\u5e94(\u5982\u8840\u6d46\u836f\u7269\u6d53\u5ea6\u6216\u5438\u6536\u7684\u836f<\/span>\u7269\u91cf) \u4e4b\u95f4\u76f8\u5173\u5173\u7cfb\u7684\u4e00\u79cd\u9884\u6d4b\u6027\u7684\u6570\u5b66\u6a21\u578b[9]\u3002<\/span><\/p>\n

IVIVC \u5206\u4e3a4 \u4e2a\u7b49\u7ea7:<\/span><\/p>\n

 A\u7ea7\u76f8\u5173\u7a0b\u5ea6\u6700\u9ad8, \u662f\u4f53\u5185\u91ca\u653e<\/span>\u8fc7\u7a0b\u4e0e\u4f53\u5185\u54cd\u5e94\u8fc7\u7a0b\u4e4b\u95f4\u7684\u70b9\u70b9\u5bf9\u5e94\u5173\u7cfb; <\/span><\/p>\n

B \u7ea7\u662f\u5c06<\/span>\u4f53\u5916\u91ca\u653e\u65f6\u95f4\u5e73\u5747\u503c\u4e0e\u6ede\u7559\u65f6\u95f4\u5e73\u5747\u503c\u6216\u4f53\u5185\u91ca\u653e\u65f6<\/span>\u95f4\u5e73\u5747\u503c\u8fdb\u884c\u6bd4\u8f83, \u6b64\u7c7b\u76f8\u5173\u6027\u4e0d\u5c5e\u4e8e\u70b9\u5bf9\u70b9\u76f8\u5173; <\/span><\/p>\n

C\u7ea7\u4e3a\u4f53\u5916\u91ca\u653e\u5ea6\u53c2\u6570(\u5982t50%, t90%) \u4e0e\u836f\u52a8\u5b66\u53c2\u6570[\u8840\u836f\u6d53\u5ea6\u65f6\u95f4\u66f2\u7ebf\u4e0b\u9762\u79ef(AUC)\u3001<\/span>t<\/span>max<\/span><\/span>\u3001<\/span>Cmax<\/sub><\/span>] \u4e4b\u95f4\u7684\u5355\u70b9\u5bf9\u5e94\u5173\u7cfb; <\/span><\/p>\n

\u591a\u91cdC \u7ea7\u4e3a\u5c061 \u4e2a\u6216\u591a\u4e2a\u836f\u4ee3\u52a8\u529b\u5b66\u53c2\u6570<\/span>\u4e0e\u91ca\u653e\u5ea6\u66f2\u7ebf\u4e2d\u51e0\u4e2a\u65f6\u95f4\u70b9\u7684\u836f\u7269\u91ca\u653e\u91cf\u76f8\u8054\u7cfb\u7684\u4e00<\/span>\u79cd\u5bf9\u5e94\u5173\u7cfb[6]\u3002<\/span><\/p>\n

IVIVC \u7684\u5efa\u7acb, \u53ef\u4ee5\u5728\u836f\u7269\u5f00\u53d1\u7684\u5404<\/span>\u4e2a\u9636\u6bb5\u6307\u5bfc\u5904\u65b9\u7b5b\u9009\u4ee5\u53ca\u5de5\u827a\u53d8\u66f4, \u6709\u52a9\u4e8e\u5236\u5b9a\u91ca\u653e<\/span>\u5ea6\u9650\u5ea6\u4ee5\u786e\u4fdd\u4ea7\u54c1\u7684\u8d28\u91cf, \u82e5\u6210\u529f\u5efa\u7acbA\u7ea7IVIVC, \u5c31<\/span>\u53ef\u8c41\u514d\u751f\u7269\u7b49\u6548\u6027\u7814\u7a76, \u51cf\u5c11\u4eba\u4f53\u548c\u52a8\u7269\u5b9e\u9a8c\u6570\u91cf, \u540c<\/span>\u65f6\u51cf\u8f7b\u76d1\u7ba1\u7684\u538b\u529b[10-12]\u3002<\/p>\n

\u4e0d\u540c\u4e8e\u4f20\u7edf\u7684\u53e3\u670d\u56fa\u4f53\u5236\u5242, \u5bf9\u6ce8\u5c04\u7528\u7f13\u91ca\u5236\u5242\u5efa\u7acbIVIVC\u5b58\u5728\u8bf8\u591a\u56f0\u96be, \u4f8b\u5982, \u91ca\u653e\u673a\u5236\u590d\u6742, \u901a\u5e38<\/span>\u5b58\u5728\u4e24\u4e2a\u62163 \u4e2a\u91ca\u653e\u9636\u6bb5, \u4f53\u5185\u836f\u4ee3\u52a8\u529b\u5b66\u66f2\u7ebf\u7684\u53bb<\/span>\u5377\u79ef\u5206\u8ba1\u7b97\u53ca\u6a21\u578b\u7684\u5efa\u7acb\u5b58\u5728\u56f0\u96be[3]; \u7ed9\u836f\u65b9\u5f0f\u901a\u5e38<\/span>\u4e3a\u76ae\u4e0b\u6216\u808c\u8089\u6ce8\u5c04, \u9176\u50ac\u5316\u6216\u708e\u75c7\u53cd\u5e94\u7684\u53d1\u751f\u4f7f\u5f97\u836f<\/span>\u7269\u5728\u4f53\u5185\u5916\u7684\u91ca\u653e\u673a\u5236\u6709\u6240\u4e0d\u540c[4,13]; \u6ca1\u6709\u6807\u51c6\u7684\u4f53\u5916<\/span>\u91ca\u653e\u5ea6\u6d4b\u5b9a\u65b9\u6cd5, \u4e0d\u80fd\u5f88\u597d\u5730\u6a21\u62df\u836f\u7269\u5728\u4f53\u5185\u7684\u91ca\u653e<\/span>\u884c\u4e3a\u7b49[5]\u3002<\/span><\/p>\n

\u56e0\u6b64, \u6587\u732e[3,6]\u4e2d\u4ec5\u62a5\u9053\u4e86\u5bf9\u5229\u57f9\u916e\u548c\u7eb3\u66f2<\/span>\u916e(\u5c0f\u5206\u5b50\u836f\u7269) \u805a\u5408\u7269\u5fae\u7403\u5efa\u7acb\u4e86A\u7ea7IVIVC\u3002<\/span><\/p>\n

\u4e3a\u4e86\u7814\u7a76\u662f\u5426\u80fd\u5bf9\u6ce8\u5c04\u7528\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u5efa\u7acb<\/span>IVIVC, \u672c\u6587\u5236\u5907\u4e863 \u79cd\u91ca\u653e\u901f\u7387\u4e0d\u540c\u7684\u918b\u9178\u6208\u820d\u745e\u6797<\/span>\u5fae\u7403, \u4ee5SD\u5927\u9f20\u4e3a\u52a8\u7269\u6a21\u578b, \u8fdb\u884c\u4e86\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814<\/span>\u7a76, \u6700\u7ec8\u5efa\u7acb\u4e86\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684A\u7ea7IVIVC\u6a21\u578b\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u6750\u6599\u4e0e\u65b9\u6cd5<\/strong><\/p>\n<\/section>\n<\/section>\n

<\/section>\n<\/section>\n<\/section>\n<\/section>\n
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1.\u4e3b\u8981\u4eea\u5668<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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Aglient1260 \u7cfb\u5217\u9ad8\u6548\u6db2\u76f8\u8272\u8c31\u7cfb\u7edf(\u7f8e\u56fd\u5b89\u6377\u4f26\u79d1\u6280\u6709\u9650\u516c\u53f8); EM-30 Plus \u578b\u626b\u63cf\u7535\u955c<\/span>(\u97e9\u56fd\u5e93\u8428\u59c6\u516c\u53f8); DSC822E\u578b\u5dee\u793a\u626b\u63cf\u91cf\u70ed\u4eea(\u745e\u58eb<\/span>Mettler Toledo \u516c\u53f8); Masterizer 2000 \u6fc0\u5149\u7c92\u5ea6\u4eea(\u82f1<\/span>\u56fd\u9a6c\u5c14\u6587\u516c\u53f8); QTRAP5500 \u8d28\u8c31\u4eea(\u7f8e\u56fdABSciex\u516c\u53f8)\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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2 \u836f\u54c1\u4e0e\u8bd5\u5242<\/strong>
<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u918b\u9178\u6208\u820d\u745e\u6797(\u745e\u58ebBachem\u516c\u53f8,\u6279\u53f7: 1068468); \u6208\u820d\u745e\u6797-D10 (\u5370\u5ea6Clearsynth \u516c\u53f8,<\/span>\u6279\u53f7: CS-GR-102); PLGA 5050 (\u5c71\u4e1c\u7eff\u53f6\u5236\u836f\u6709\u9650\u516c<\/span>\u53f8, \u6279\u53f7: LY1180045); \u7532\u9187(\u8272\u8c31\u7eaf, \u6279\u53f7: SJ6SF66957)\u3001<\/span>\u4e59\u8148(\u8272\u8c31\u7eaf, \u6279\u53f7: DI6DF66786)\u3001\u56db\u6c22\u544b\u5583(\u8272\u8c31\u7eaf,<\/span>\u6279\u53f7: I0891701720)\u5747\u8d2d\u4e8e\u5fb7\u56fdMerck \u516c\u53f8; Tween 20<\/span>(\u5316\u5b66\u7eaf, \u6279\u53f7: 20170323)\u3001\u4e8c\u6c2f\u7532\u70f7(\u8272\u8c31\u7eaf, \u6279\u53f720170402)\u3001\u805a\u4e59\u70ef\u9187(PVA, \u6279\u53f7: 20160203) \u5747\u8d2d\u4e8e\u56fd<\/span>\u836f\u96c6\u56e2\u5316\u5b66\u8bd5\u5242\u6709\u9650\u516c\u53f8; \u4e59\u9178(\u8272\u8c31\u7eaf, \u7f8e\u56fdTEDIA<\/span>\u516c\u53f8, \u6279\u53f7: 17060467); \u7532\u9178(\u8272\u8c31\u7eaf, \u7f8e\u56fdAnaqua <\/span>Chemicals Supply \u516c\u53f8, \u6279\u53f7: 73C1606TD)\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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3 \u52a8\u7269<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u96c4\u6027SD \u5927\u9f20(\u6d4e\u5357\u670b\u60a6\u5b9e\u9a8c\u52a8\u7269\u6709\u9650\u516c\u53f8, \u751f\u4ea7\u8bb8\u53ef\u8bc1\u53f7: SCXK (\u9c81) 2014-0007), \u4f53\u91cd: 220\uff5e<\/span>250 g\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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4 \u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u5236\u5907<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u91c7\u7528\u590d\u4e73\u6cd5(S\/O\/W\u6cd5) \u5236\u5907\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u3002\u5177\u4f53\u5236\u5907\u6b65\u9aa4\u5982\u4e0b: \u53d6<\/span>PLGA 2 g \u6eb6\u4e8e8 mL \u4e8c\u6c2f\u7532\u70f7\u4e2d, \u78c1\u529b\u6405\u62cc\u4f7f\u4e4b\u5b8c\u5168<\/span>\u6eb6\u89e3\u4f5c\u4e3a\u6cb9\u76f8\u3002\u5c06\u918b\u9178\u6208\u820d\u745e\u6797\u539f\u6599\u836f\u52a0\u5165\u5230\u6cb9\u76f8<\/span>\u4e2d, \u572811 000 r \u00b7min-1<\/sup><\/span>\u6761\u4ef6\u4e0b\u9ad8\u901f\u5206\u6563\u5236\u6210S\/O\u578b\u521d\u4e73\u3002<\/span><\/p>\n

\u5c06PVA(1%, v\/v) \u6eb6\u6db21 L \u9884\u51b7\u81f38 \u2103\u540e\u7f6e\u4e8e\u5747\u8d28\u673a\u4e0a,\u57282 000 r \u00b7<\/span><\/span>min<\/span>-1<\/sup><\/span><\/span>\u6761\u4ef6\u4e0b, \u6ce8\u5165\u521d\u4e73\u5e76\u4e73\u53164 min, \u5236\u6210S\/O\/W\u578b\u590d\u4e73\u3002\u5c06\u5236\u5907\u7684\u590d\u4e73\u4f4e\u901f\u6405\u62cc4 h, \u6325\u53d1\u6709\u673a\u6eb6\u5242, \u5c06\u5fae\u7403\u8fc7150 \u76ee\u7b5b\u540e\u7528\u84b8\u998f\u6c34\u51b2\u6d174 \u6b21, \u4e8e\u771f\u7a7a\u51b7\u51bb\u5e72\u71e5\u673a\u4e2d\u51bb\u5e72\u5373\u5f97\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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5 \u5fae\u7403\u7684\u8868\u5f81<\/span><\/strong>
<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u8f7d\u836f\u91cf \uff1a<\/strong>\u53d6\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u740320.0 mg\u7f6e\u4e8e10 mL<\/span>\u91cf\u74f6\u4e2d, \u52a02 mL\u4e59\u8148\u8d85\u58f0\u4f7f\u4e4b\u6eb6\u89e3, \u75280.1% (v\/v) \u918b\u9178<\/span>\u7a00\u91ca\u81f3\u523b\u5ea6, \u6447\u5300\u3002\u53d6\u8be5\u6eb6\u6db2\u7ea61 mL\u4e8e1.5 mL\u79bb\u5fc3\u7ba1<\/span>\u4e2d, \u4ee513 000 r \u00b7min-1<\/sup><\/span>\u79bb\u5fc310 min, \u53d6\u4e0a\u6e05\u6db2\u4f5c\u4e3a\u4f9b\u8bd5\u54c1<\/span>\u6eb6\u6db2, \u7528HPLC \u6d4b\u5b9a\u6208\u820d\u745e\u6797\u6d53\u5ea6\u3002<\/span>\u8272\u8c31\u6761\u4ef6\u4e3a\u8272\u8c31<\/span>\u67f1: Ultimate XB-C18, 250 mm \u00d7 4.6 mm, 5 \u03bcm, \u6d41\u52a8<\/span>\u76f8: 0.5%\u78f7\u9178\u6c34-0.5%\u78f7\u9178\u4e59\u8148(75\u223625, v\/v); \u6d41\u901f: 1<\/span>mL\u00b7min<\/span>-1<\/sup><\/span>; \u67f1\u6e29: 40 \u2103; \u68c0\u6d4b\u6ce2\u957f: 220 nm\u3002\u6309\u7167\u4e0b\u5f0f<\/span>\u8ba1\u7b97\u5fae\u7403\u8f7d\u836f\u91cf:<\/span><\/p>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\", <\/span><\/p>\n

\u5176\u4e2dDL \u4e3a\u5fae\u7403<\/span>\u8f7d\u836f\u91cf, WD\u4e3a\u5fae\u7403\u4e2d\u603b\u836f\u91cf, WM\u4e3a\u5fae\u7403\u603b\u91cf\u3002<\/span><\/p>\n

\u7c92\u5ea6\uff1a<\/strong>\u5c06\u5fae\u7403\u5206\u6563\u57280.1% Tween 20 \u4e2d, \u7528\u9a6c\u5c14\u6587<\/span>2000 \u7c92\u5ea6\u4eea\u8fdb\u884c\u7c92\u5ea6\u6d4b\u5b9a\u3002<\/span><\/p>\n

\u73bb\u7483\u5316\u8f6c\u53d8\u6e29\u5ea6(Tg)\uff1a <\/strong>\u4f7f\u7528\u793a\u5dee\u626b\u63cf\u91cf\u70ed\u6cd5(DSC) \u6d4b\u5b9a\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403Tg\u3002\u53d6\u9002\u91cf\u5fae\u7403\u4e8e\u94dd\u5769<\/span>\u57da\u4e2d, \u538b\u76d6\u5bc6\u5c01, \u57280\uff5e100 \u2103\u5185, \u5347\u6e29\u901f\u738710 \u2103\u00b7min<\/span>-1<\/sup><\/span><\/span>\u7684\u6761\u4ef6\u4e0b\u6d4b\u5b9a, \u6bcf\u4e2a\u6837\u54c1\u6d4b\u4e24\u6b21, \u53d6\u7b2c2 \u6b21\u7ed3\u679c\u8fdb\u884c<\/span>\u5206\u6790\u3002<\/span><\/p>\n

\u5f62\u8c8c\u5206\u6790\uff1a<\/strong>\u4f7f\u7528\u626b\u63cf\u7535\u955c(SEM) \u5bf9\u5236\u5907\u7684\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u5f62\u8c8c\u8fdb\u884c\u8868\u5f81\u3002\u5c06\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403<\/span>\u6d82\u5e03\u5728\u7c98\u6709\u5bfc\u7535\u80f6\u7684\u6837\u54c1\u5ea7\u4e0a, \u5bf9\u6837\u54c1\u8fdb\u884c\u55b7\u91d1\u5904\u7406\u3002<\/span>\u5c06\u5904\u7406\u597d\u7684\u6837\u54c1\u7528SEM\u8fdb\u884c\u5206\u6790\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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6 \u4f53\u5916\u91ca\u653e\u5ea6\u7814\u7a76<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u91c7\u7528\u6052\u6e29\u6c34\u6d74\u632f\u8361\u6cd5\u6d4b\u5b9a\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5916\u91ca\u653e\u5ea6\u3002\u79f0\u53d6\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403<\/span>\u7ea620 mg, \u7f6e\u4e8e25 mL \u5851\u6599\u79bb\u5fc3\u7ba1\u4e2d, \u52a0\u5165\u91ca\u653e\u4ecb\u8d28<\/span>5% (v\/v) \u7532\u9187\u6c345 mL, \u653e\u5165\u6e29\u5ea6\u4e3a(45 \u00b1 0.5) \u2103\u3001\u8f6c\u901f<\/span>\u4e3a50 r \u00b7min-1\u7684\u6052\u6e29\u6c34\u6d74\u632f\u8361\u5668\u4e2d, \u5728\u9884\u5b9a\u7684\u65f6\u95f4\u95f4\u9694<\/span>\u7cbe\u5bc6\u91cf\u53d6\u6bcf\u4efd\u6eb6\u6db24 mL, \u540c\u65f6\u8865\u52a0\u7b49\u4f53\u79ef\u7684\u91ca\u653e\u4ecb<\/span>\u8d28, \u53d6\u51fa\u6eb6\u6db2\u4ee513 000 r \u00b7min<\/span>-1<\/sup><\/span>\u8f6c\u901f\u79bb\u5fc310 min\u3002<\/span><\/p>\n

\u79bb\u5fc3<\/span>\u7ed3\u675f\u540e, \u53d6\u4e0a\u6e05\u6db2\u4f5c\u4e3a\u4f9b\u8bd5\u54c1\u6eb6\u6db2, \u7528HPLC \u8fdb\u884c\u6d4b<\/span>\u5b9a, \u65b9\u6cd5\u540c\u8f7d\u836f\u91cf\u6d4b\u5b9a\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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7 \u5fae\u7403\u91ca\u653e\u673a\u5236\u7814\u7a76<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u5728\u4f53\u5916\u91ca\u653e\u5ea6\u6d4b\u5b9a\u6761\u4ef6\u4e0b,\u5206\u522b\u5728\u4e0d\u540c\u7684\u65f6\u95f4\u70b9\u53d6\u51fa\u91ca\u653e\u6837\u54c1, \u5c3d\u91cf\u79fb\u9664\u91ca\u653e\u4ecb<\/span>\u8d28\u540e25 \u2103\u771f\u7a7a\u5e72\u71e512 h, \u4f7f\u7528SEM\u89c2\u5bdf\u5fae\u7403\u5f62\u8c8c\u3002\u4f7f<\/span>\u7528\u51dd\u80f6\u6e17\u900f\u8272\u8c31\u6cd5(GPC) \u6d4b\u5b9aPLGA\u5206\u5b50\u91cf, \u5177\u4f53\u64cd\u4f5c\u4e3a: \u53d6\u4e00\u5957\u805a\u82ef\u4e59\u70ef\u5206\u5b50\u91cf\u6807\u51c6\u54c1, \u52a0\u5165\u56db\u6c22\u544b\u5583<\/span>1.5 mL, \u4f5c\u4e3a\u5bf9\u7167\u54c1\u6eb6\u6db2; \u53d6\u91ca\u653e\u8fc7\u7a0b\u4e2d\u5fae\u7403\u7ea66 mg,<\/span>\u52a0\u5165\u56db\u6c22\u544b\u55831.5 mL, \u632f\u6447\u6eb6\u89e3, \u4f5c\u4e3a\u4f9b\u8bd5\u54c1\u6eb6\u6db2\u3002<\/span><\/p>\n

\u8272\u8c31<\/span>\u6761\u4ef6\u4e3a: \u8272\u8c31\u67f1Styragel\u00ae HT3 (300 mm\u00d77.8 mm, 10 \u03bcm, <\/span>Mw: 500\uff5e30 000) \u4e0e\u8272\u8c31\u67f1Styragel\u00ae6E (300 mm\u00d77.8mm, 10 \u03bcm, Mw: 5 000\uff5e60 000) \u4e32\u8054\u4f7f\u7528; \u67f1\u6e29\u4e3a<\/span>30 \u2103; \u6d41\u901f\u4e3a: 1.0 mL\u00b7min<\/span>-1<\/sup><\/span>; \u8fdb\u6837\u4f53\u79ef\u4e3a20 \u03bcL; \u68c0\u6d4b<\/span>\u5668\u4e3a\u793a\u5dee\u6298\u5149\u68c0\u6d4b\u5668, \u68c0\u6d4b\u5668\u6e29\u5ea6\u4e3a35 \u2103, \u7528\u51dd\u80f6\u6e17<\/span>\u900f\u8272\u8c31\u8f6f\u4ef6\u8ba1\u7b97PLGA\u7684Mw\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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8 \u4f53\u5185\u836f\u4ee3\u52a8\u529b\u5b66\u7814\u7a76<\/span><\/strong>
<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\u6ce8\u5c04\u7528\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u5728SD\u5927\u9f20\u4f53\u5185\u7684\u836f\u4ee3\u52a8\u529b\u5b66\u5b9e\u9a8c\u65b9\u6848\u7ecf\u5c71\u4e1c\u7eff\u53f6<\/span>\u5236\u836f\u6709\u9650\u516c\u53f8\u52a8\u7269\u4f26\u7406\u59d4\u5458\u4f1a\u6279\u51c6\u5b9e\u65bd\u3002<\/span><\/p>\n

\u53d6\u918b\u9178\u6208\u820d<\/span>\u745e\u6797\u5fae\u7403\u9002\u91cf, \u52a0\u5165CMC-Na \u6eb6\u6db2\u914d\u6210\u6df7\u60ac\u5242\u540e\u6309<\/span>1.8 mg\u00b7kg-1\u5242\u91cf\u5bf9SD\u5927\u9f20\u7ecf\u808c\u5185\u6ce8\u5c04\u7ed9\u836f\u3002<\/span><\/p>\n

\u5206\u522b\u4e8e\u7ed9<\/span>\u836f\u524d\u53ca\u7ed9\u836f\u540e\u4e0d\u540c\u65f6\u95f4\u7ecf\u5927\u9f20\u773c\u7403\u540e\u9759\u8109\u4e1b\u53d6\u8840, \u6536<\/span>\u96c6\u5230\u7684\u8840\u6db2\u6837\u54c1\u7f6e\u4e8e\u809d\u7d20\u5316\u8bd5\u7ba1\u4e2d, 4 \u2103\u300113 000 r\u00b7min<\/span>-1<\/sup><\/span><\/span>\u79bb\u5fc310 min, \u5c06\u4e0a\u6e05\u6db2\u79fb\u81f3EP \u7ba1\u4e2d, \u5206\u6790\u524d\u5c06\u8840\u6d46\u6837<\/span>\u54c1\u7f6e\u4e8e-80 \u2103\u51b0\u7bb1\u4e2d\u4fdd\u5b58\u3002\u5efa\u7acb\u7684\u5206\u6790\u65b9\u6cd5\u6309\u7167CFDA<\/span>\u9881\u5e03\u7684\u300a\u751f\u7269\u6837\u54c1\u5b9a\u91cf\u5206\u6790\u65b9\u6cd5\u9a8c\u8bc1\u6307\u5bfc\u539f\u5219\u300b\u8fdb\u884c\u9a8c<\/span>\u8bc1\u3002<\/span><\/p>\n

\u91c7\u7528\u7ecf\u8fc7\u65b9\u6cd5\u5b66\u8003\u5bdf\u5408\u683c\u7684\u6db2\u76f8\u8272\u8c31-\u4e32\u8054\u8d28\u8c31<\/span>(LC-MS\/MS) \u6cd5[14]\u6d4b\u5b9a\u8840\u6d46\u4e2d\u6208\u820d\u745e\u6797\u7684\u6d53\u5ea6\u3002<\/span><\/p>\n

\u6837\u54c1\u524d\u5904\u7406\uff1a<\/strong><\/p>\n

\u53d6\u5927\u9f20\u8840\u6d46100 \u03bcL \u4e8e\u79bb\u5fc3\u7ba1\u4e2d, \u52a0\u5165100 \u03bcL\u5185\u6807\u6eb6\u6db2(\u6208\u820d\u745e\u6797-D10, 10 \u03bcg\u00b7L-1<\/sup><\/span>)\u3001100 \u03bcL<\/span>\u7532\u9187-\u6c34(60\u223640, v\/v)\u3001100 \u03bcL \u7532\u9187, \u6da1\u65cb\u6df7\u54081 min\u3002<\/span><\/p>\n

\u4e0a\u5c42\u5bfc\u5165\u5df2\u6d3b\u5316\u7684HLB \u56fa\u76f8\u8403\u53d6\u67f1(1 cc, 30 mg), \u75281 mL\u7532\u9187-\u6c34(60\u223640, v\/v) \u6d17\u6742\u8d28, \u518d\u75281 mL 0.01% (v\/v)<\/span>\u7532\u9178\u7532\u9187\u6d17\u8131, \u6d17\u8131\u6db2\u7f6e\u4e8e50 \u2103\u6c34\u6d74, \u7528\u5e72\u71e5\u7684\u6c2e\u6c14<\/span>\u6d41\u5439\u5e72, \u518d\u7528100 \u03bcL\u7532\u9187-\u6c34(60\u223640, v\/v) \u590d\u6eb6, \u6da1\u65cb\u540e<\/span>\u53d610 \u03bcL\u8fdb\u6837\u81f3\u6db2\u8d28\u7cfb\u7edf\u3002<\/span><\/p>\n

\u8272\u8c31\u6761\u4ef6\uff1a<\/strong><\/p>\n

\u8272\u8c31\u67f1\u4e3aZORBAX Eclipse Plus C18\u67f1(50 mm \u00d7 2.1 mm, 1.8 \u03bcm); \u6d41\u52a8\u76f8\u4e3a\u7532\u9187(A) \u548c<\/span>0.02 % (v\/v) \u7532\u9178\u6c34(B); \u6d41\u901f\u4e3a0.3 mL \u00b7min<\/span>-1<\/sup><\/span>; \u67f1\u6e29<\/span>40 \u2103\u3002<\/span><\/p>\n

\u8d28\u8c31\u6761\u4ef6\uff1a<\/strong><\/p>\n

\u79bb\u5b50\u6e90: \u7535\u55b7\u96fe\u79bb\u5b50\u5316\u6e90(ESI); \u6781\u6027:\u6b63\u79bb\u5b50; CE \u7535\u538b: 30 eV; DP \u7535\u538b\u4e3a40 V; \u79bb\u5b50\u55b7\u5c04\u7535<\/span>\u538b: 5 500 V; \u6e29\u5ea6: 550 \u2103; \u6e90\u5185\u6c14\u4f531 (N2) \u538b\u529b: 50 psi;<\/span>\u6c14\u4f532 (N2) \u538b\u529b: 50 psi; \u6c14\u5e18\u6c14(N2) \u538b\u529b: 30 psi; \u78b0\u649e<\/span>\u6c14\u538b\u529b: 8 psi; \u7528\u4e8e\u5b9a\u91cf\u5206\u6790\u7684\u79bb\u5b50\u53cd\u5e94\u4e3a: \u6208\u820d\u745e\u6797<\/span>(635.4\/607.3), \u5185\u6807\u6208\u820d\u745e\u6797-D10 (640.4\/612.5)\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
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9 IVIVC\u7684\u5efa\u7acb<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
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\n

\u6839\u636e\u6587\u732e\u62a5\u9053[15,16], \u5c06\u8840\u836f\u6d53\u5ea6-\u65f6\u95f4\u66f2\u7ebf\u7ecf%AUC \u6cd5\u5904\u7406\u540e\u5f97\u5230\u4f53\u5185\u7d2f\u79ef\u5438\u6536\u66f2\u7ebf,<\/span>\u4f7f\u7528\u68af\u5f62\u9762\u79ef\u6cd5\u8ba1\u7b97AUC, \u516c\u5f0f\u5982\u4e0b:<\/span><\/p>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n

\u5176\u4e2d,Fa<\/sub>(t)\u4e3a\u5728\u65f6\u95f4t \u5185\u88ab\u5438\u6536\u7684\u836f\u7269\u7684\u767e\u5206\u6570,(AUC)t \u4e3a\u5728\u65f6\u95f4t \u5185\u8840\u836f\u6d53\u5ea6-\u65f6\u95f4\u66f2\u7ebf\u4e0b\u9762\u79ef, <\/span>(AUC)\u221e<\/span><\/sub>\u4e3a\u8840\u836f\u6d53\u5ea6-\u65f6\u95f4\u66f2\u7ebf\u4e0b\u603b\u9762\u79ef\u3002\u4ee5\u4f53\u5916\u7d2f\u79ef<\/span>\u91ca\u653e\u5ea6\u4e3a\u81ea\u53d8\u91cf, \u4ee5\u4f53\u5185\u7d2f\u79ef\u91ca\u653e\u5ea6\u4e3a\u56e0\u53d8\u91cf\u8fdb\u884c\u7ebf<\/span>\u6027\u56de\u5f52, \u5efa\u7acbIVIVC\u65b9\u7a0b, \u6839\u636e\u76f8\u5173\u7cfb\u6570(r) \u503c\u5224\u65ad\u4e8c<\/span>\u8005\u76f8\u5173\u6027[17]\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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10 \u7edf\u8ba1\u5b66\u65b9\u6cd5<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\n
\n

\u91c7\u7528SPSS 16.0 \u7a0b\u5e8f\u8fdb\u884c\u7edf\u8ba1\u5b66\u5206\u6790, \u5b9e\u9a8c\u7ed3\u679c\u4ee5x\u02c9 \u00b1 s \u8868\u793a\u3002\u591a\u6837\u672c\u5747\u6570\u95f4\u6bd4\u8f83\u91c7\u7528\u5355<\/span>\u56e0\u7d20\u65b9\u5dee\u5206\u6790, \u663e\u8457\u6027\u5dee\u5f02\u8868\u793a\u4e3aP<0.05\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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

\n
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\u7ed3\u679c\u4e0e\u8ba8\u8bba<\/strong><\/p>\n<\/section>\n<\/section>\n

<\/section>\n<\/section>\n<\/section>\n<\/section>\n
\n
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1  \u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u8868\u5f81<\/strong><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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3 \u79cd\u91ca\u653e\u901f\u7387\u4e0d\u540c\u7684\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u7269\u7406\u5316\u5b66\u6027\u8d28\u89c1\u88681\u3002\u7ed3\u679c\u663e\u793a, 3 \u79cd\u5fae\u7403\u7684\u8f7d\u836f\u91cf\u76f8\u4f3c, \u5747<\/span>\u4e3a3.5%\u5de6\u53f3\u3002\u5236\u5907\u76843 \u79cd\u5fae\u7403\u5236\u5242(F\u3001M\u548cS) \u7684\u7c92\u5f84<\/span>\u89c1\u56fe1A, 3 \u79cd\u5fae\u7403\u7684\u7c92\u5f84\u8f83\u76f8\u4f3c(P>0.05), \u5747\u572880\uff5e<\/span>87 \u03bcm\u3002<\/span><\/p>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n

\u5fae\u7403\u5236\u5907\u65f6\u6240\u4f7f\u7528\u7684\u9ad8\u5206\u5b50PLGA\u5206\u5b50\u91cf\u4e0d<\/span>\u540c, 3 \u79cd\u5fae\u7403\u7684\u73bb\u7483\u5316\u8f6c\u53d8\u6e29\u5ea6\u7565\u6709\u5dee\u5f02\u30023 \u79cd\u918b\u9178\u6208<\/span>\u820d\u745e\u6797\u5fae\u7403\u7684\u626b\u63cf\u7535\u955c\u7167\u7247\u89c1\u56fe1B\uff5eD, 3 \u79cd\u5fae\u7403\u5236<\/span>\u5242\u5747\u5448\u73b0\u826f\u597d\u7684\u7403\u5f62\u5f62\u6001, \u5176\u4e2d\u5236\u5242F \u4e0e\u5236\u5242M\u5706\u6574<\/span>\u5ea6\u8f83\u597d\u4e14\u8868\u9762\u8f83\u5149\u6ed1, \u800c\u5236\u5242S \u5706\u6574\u5ea6\u8f83\u5dee, \u8868\u9762\u8936\u76b1<\/span>\u8f83\u591a\u3002<\/span><\/p>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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2  \u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5916\u91ca\u653e\u66f2\u7ebf<\/span><\/strong>
<\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
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\n

\u918b\u9178\u6208\u820d\u745e\u6797\u5728\u6c34\u4e2d\u6eb6\u89e3\u5ea6\u597d, \u91ca\u653e\u4ecb\u8d28\u4f53\u79ef\u9009\u62e9\u4e3a5 mL\u4fbf\u53ef\u6ee1\u8db3\u6f0f\u69fd\u6761\u4ef6; \u918b\u9178\u6208\u820d\u745e\u6797\u5728\u8be5\u4ecb\u8d28<\/span>\u4e2d\u7a33\u5b9a\u6027\u8f83\u597d, \u4e145% (v \/ v) \u7532\u9187\u6c34\u6eb6\u6db2\u4e3aTrelstar\u00ae<\/span>Depot ( \u6ce8\u5c04\u7528\u53cc\u7f9f\u8418\u9178\u66f2\u666e\u745e\u6797) \u4f7f\u7528\u7684\u91ca\u653e\u4ecb<\/span>\u8d28[18], \u7531\u4e8e\u6208\u820d\u745e\u6797\u548c\u66f2\u666e\u745e\u6797\u90fd\u662f\u5341\u80bd\u7ec4\u6210\u7684\u4fc3\u6027<\/span>\u817a\u6fc0\u7d20\u91ca\u653e\u6fc0\u7d20(GnRH) \u7c7b\u4f3c\u7269, \u5176\u91ca\u653e\u884c\u4e3a\u53ef\u80fd\u5177<\/span>\u6709\u76f8\u4f3c\u6027\u3002\u56e0\u6b64, \u9009\u62e95% (v\/v) \u7532\u9187\u6c34\u4f5c\u4e3a\u91ca\u653e\u4ecb\u8d28\u3002<\/span><\/p>\n

\u6b64\u5916, \u7ecf\u8fc7\u5bf9\u91ca\u653e\u88c5\u7f6e\u548c\u91ca\u653e\u6e29\u5ea6\u7b49\u5f71\u54cd\u56e0\u7d20\u8fdb\u884c\u8003<\/span>\u5bdf\u540e, \u786e\u5b9a\u4f7f\u7528\u6052\u6e29\u6c34\u6d74\u9707\u8361\u6cd5, \u572845 \u2103\u6761\u4ef6\u4e0b\u8003\u5bdf3<\/span>\u79cd\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5916\u91ca\u653e\u66f2\u7ebf, \u7ed3\u679c\u5982\u56fe2 \u6240<\/span>\u793a\u3002<\/span><\/p>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n

\u7531\u56fe\u53ef\u89c1, 3 \u79cd\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u57285%\u7532\u9187\u6c34\u3001<\/span>45 \u2103\u6761\u4ef6\u4e0b\u7684\u91ca\u653e\u66f2\u7ebf\u663e\u793a, \u5728\u91ca\u653e\u4e2d\u540e\u671f, 3 \u79cd\u5fae\u7403<\/span>\u7684\u91ca\u653e\u901f\u5ea6\u4e3a\u5236\u5242F>\u5236\u5242M>\u5236\u5242S, \u8fd9\u662f\u56e0\u4e3a\u7528\u4e8e\u5236<\/span>\u5907\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684PLGA\u5206\u5b50\u91cf\u4f9d\u6b21\u589e\u52a0, \u968f\u7740<\/span>PLGA\u5206\u5b50\u91cf\u7684\u589e\u52a0, \u5fae\u7403\u964d\u89e3\u901f\u7387\u53d8\u6162, \u4f7f\u5f97\u918b\u9178\u6208<\/span>\u820d\u745e\u6797\u7684\u91ca\u653e\u901f\u7387\u51cf\u6162, \u8be5\u7ed3\u679c\u4e0e\u6587\u732e\u62a5\u9053[19]\u4e00\u81f4\u3002<\/span><\/p>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n

\u5728\u91ca\u653e\u524d\u671f, \u5236\u5242S \u7684\u91ca\u653e\u901f\u5ea6\u5feb\u4e8e\u5236\u5242M\u4e0e\u5236\u5242F,<\/span>\u4e0d\u7b26\u5408\u4e0a\u8ff0\u5fae\u7403\u7684\u91ca\u653e\u89c4\u5f8b\u3002<\/span><\/p>\n

\u56e0\u6b64, \u672c\u6587\u901a\u8fc7\u5bf9\u91ca\u653e<\/span>\u8fc7\u7a0b\u4e2d\u5fae\u7403\u7684\u5f62\u8c8c\u89c2\u5bdf\u53caPLGA\u5206\u5b50\u91cf\u6d4b\u5b9a, \u5e76\u7ed3\u5408<\/span>\u91ca\u653e\u66f2\u7ebf\u53ca\u6587\u732e\u62a5\u9053\u63a8\u6d4b\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u91ca\u653e<\/span>\u673a\u5236\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
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3 \u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u91ca\u653e\u673a\u5236\u7684\u7814\u7a76<\/span><\/strong>
<\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
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\u6839\u636e\u6587\u732e[20]\u62a5\u9053, \u5fae\u7403\u7684\u91ca\u653e\u8fc7\u7a0b\u4e3b\u8981\u5206\u4e3a3 \u4e2a\u9636\u6bb5\u2014\u2014\u7a81\u91ca\u9636\u6bb5\u3001\u6269\u6563\u9636\u6bb5\u548c\u6eb6\u8680\u9636\u6bb5\u3002<\/span><\/p>\n

\u7a81\u91ca\u9636\u6bb5:<\/span>\u5fae\u7403\u8868\u9762\u88ab\u6da6\u6e7f, \u9ecf\u9644\u5728\u5fae\u7403\u8868\u9762\u7684\u836f\u7269\u6eb6\u89e3\u5230\u4ecb\u8d28<\/span>\u4e2d; \u6269\u6563\u9636\u6bb5: \u5fae\u7403\u8868\u9762\u51fa\u73b0\u4e00\u4e9b\u6c34\u6027\u901a\u9053, \u836f\u7269\u901a\u8fc7<\/span>\u8fd9\u4e9b\u6c34\u6027\u901a\u9053\u4ece\u5fae\u7403\u5185\u90e8\u6269\u6563\u5230\u4ecb\u8d28\u4e2d; <\/span><\/p>\n

\u6eb6\u8680\u9636\u6bb5:<\/span>PLGA\u964d\u89e3\u901f\u5ea6\u589e\u52a0, \u5fae\u7403\u6eb6\u8680, \u836f\u7269\u5feb\u901f\u91ca\u653e\u3002<\/span><\/p>\n

\u5fae\u7403<\/span>\u91ca\u653e\u8fc7\u7a0b\u4e2d\u5206\u5b50\u91cf\u6d4b\u5b9a\u7ed3\u679c(\u56fe3) \u663e\u793a, PLGA\u5206\u5b50\u91cf<\/span>\u5448\u6301\u7eed\u4e0b\u964d\u8d8b\u52bf, \u4e14\u6574\u4e2a\u91ca\u653e\u8fc7\u7a0b\u4e2d, \u5206\u5b50\u91cf\u5927\u5c0f\u59cb\u7ec8<\/span>\u4e3a\u5236\u5242F<\u5236\u5242M<\u5236\u5242S, \u8bf4\u660ePLGA\u7684\u964d\u89e3, \u5fae\u7403\u6eb6<\/span>\u8680\u662f\u5fae\u7403\u4e2d\u836f\u7269\u91ca\u653e\u7684\u4e3b\u8981\u9014\u5f84\u3002\u56fe4 \u4e3a\u918b\u9178\u6208\u820d\u745e<\/span>\u6797\u5fae\u7403\u5236\u5242F\u3001\u5236\u5242M\u548c\u5236\u5242S \u5728\u91ca\u653e\u8fc7\u7a0b\u4e2d\u4e0d\u540c\u65f6<\/span>\u95f4\u70b9\u7684\u7535\u955c\u626b\u63cf\u7167\u7247\u3002<\/span><\/p>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n

Figure 4 SEMmicrographs of the goserelin acetatemicrosphere during release<\/span><\/span>
<\/p>\n

\u5728\u91ca\u653e\u521d\u671f(\u7b2c1 \u5929), \u5236\u5242S \u5fae<\/span>\u7403\u8868\u9762\u8936\u76b1\u8f83\u591a, \u4e0d\u5e73\u6574\u3002\u56e0\u6b64, \u4e0e\u91ca\u653e\u4ecb\u8d28\u63a5\u89e6\u9762\u79ef<\/span>\u8f83\u5927, \u4e14\u8868\u9762\u5f62\u6210\u4e86\u8f83\u591a\u7684\u5b54\u6d1e, \u8fd9\u4e0e\u5fae\u7403\u4f53\u5916\u91ca\u653e\u7ed3<\/span>\u679c(\u56fe2) \u4e2d\u91ca\u653e\u524d\u671f\u5236\u5242S \u91ca\u653e\u901f\u5ea6\u5feb\u4e8e\u5236\u5242F \u548c\u5236<\/span>\u5242M\u662f\u4e00\u81f4\u7684, \u8bf4\u660e\u5728\u6b64\u9636\u6bb5\u6269\u6563\u4f5c\u7528\u662f\u5fae\u7403\u91ca\u653e\u7684<\/span>\u4e3b\u8981\u56e0\u7d20\u3002<\/span><\/p>\n

\u7b2c2 \u5929\u7535\u955c\u7167\u7247\u663e\u793a, \u5fae\u7403\u4e4b\u95f4\u9ecf\u8fde\u4e25\u91cd,<\/span>\u5185\u90e8\u5b54\u5f84\u589e\u5927, \u4e0d\u518d\u5177\u6709\u6574\u7403\u5f62\u6001, \u4f53\u5916\u91ca\u653e\u66f2\u7ebf\u663e\u793a<\/span>\u91ca\u653e\u901f\u5ea6\u52a0\u5feb, \u8bf4\u660e\u6b64\u65f6\u5fae\u7403\u5904\u4e8e\u6eb6\u8680\u9636\u6bb5, PLGA\u7684<\/span>\u964d\u89e3\u662f\u836f\u7269\u91ca\u653e\u7684\u4e3b\u8981\u9014\u5f84\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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4 \u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u91ca\u653e\u7279\u6027<\/span><\/strong>
<\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
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4.1 \u65b9\u6cd5\u5b66\u9a8c\u8bc1<\/strong><\/span><\/p>\n

4.1.1 \u4e13\u5c5e\u6027<\/strong><\/p>\n

\u7a7a\u767d\u8840\u6d46\u4e2d\u7684\u5185\u6e90\u6027\u7269\u8d28\u4e0d\u5e72\u6270\u6208\u820d\u745e\u6797\u548c\u6208\u820d\u745e\u6797D-10 \u7684\u6d4b\u5b9a\u3002<\/span><\/p>\n

4.1.2 \u6807\u51c6\u66f2\u7ebf<\/strong><\/p>\n

\u53d6\u7a7a\u767d\u5927\u9f20\u8840\u6d46\u5236\u5907\u6210\u7cfb\u5217\u6d53\u5ea6\u7684\u6208\u820d\u745e\u6797\u6807\u51c6\u6837\u672c, \u6309\u7167\u201c\u4f53\u5185\u836f\u4ee3\u52a8\u529b\u5b66\u7814\u7a76\u4e2d\u6837<\/span>\u672c\u524d\u5904\u7406\u201d\u9879\u64cd\u4f5c\u3002\u4ee5\u6208\u820d\u745e\u6797\u6d53\u5ea6\u4e3a\u6a2a\u5750\u6807, \u6208\u820d\u745e<\/span>\u6797\u4e0e\u6208\u820d\u745e\u6797-D10 \u7684\u5cf0\u9762\u79ef\u6bd4\u4e3a\u7eb5\u5750\u6807, \u7528\u52a0\u6743(w =<\/span>1\/x2) \u6700\u5c0f\u4e8c\u4e58\u6cd5\u8fdb\u884c\u56de\u5f52\u8fd0\u7b97, \u6c42\u5f97\u6208\u820d\u745e\u6797\u6807\u51c6\u66f2<\/span>\u7ebf\u65b9\u7a0b\u4e3ay = 0.232 x + 0.000 981, r = 0.999 0\u3002<\/span><\/p>\n

4.1.3 \u51c6\u786e\u5ea6\u548c\u7cbe\u5bc6\u5ea6<\/strong><\/p>\n

\u8003\u5bdf\u4e86\u4f4e\u3001\u4e2d\u3001\u9ad83 \u4e2a\u6d53\u5ea6\u7684\u8d28\u63a7\u6837\u672c\u7684\u7cbe\u5bc6\u5ea6\u548c\u51c6\u786e\u5ea6\u3002\u7ed3\u679c\u8868\u660e, \u6279\u5185\u3001\u6279\u95f4<\/span>\u7cbe\u5bc6\u5ea6RSD\u57281.25%\uff5e9.07%, \u51c6\u786e\u5ea6RE \u5728-2.08%\uff5e<\/span>7.96%, \u5747\u5728\u53ef\u63a5\u53d7\u8303\u56f4\u5185\u3002<\/span><\/p>\n

4.1.4 \u57fa\u8d28\u6548\u5e94<\/strong><\/p>\n

\u7a7a\u767d\u57fa\u8d28\u63d0\u53d6\u540e\u6dfb\u52a0\u76f8\u5e94\u6d53\u5ea6\u6807\u51c6\u6eb6\u6db2, \u4ee5\u57fa\u8d28\u5b58\u5728\u4e0b\u7684\u5cf0\u9762\u79ef\u4e0e\u4e0d\u542b\u57fa\u8d28\u7684\u76f8\u5e94\u5cf0\u9762<\/span>\u79ef\u76f8\u6bd4, \u8ba1\u7b97\u6208\u820d\u745e\u6797\u7684\u57fa\u8d28\u6548\u5e94\u3002\u4f4e\u3001\u9ad8\u6c34\u5e73\u7684\u57fa\u8d28<\/span>\u6548\u5e94\u5206\u522b\u4e3a100.7%\u548c98.9%\u3002<\/span><\/p>\n

4.1.5 \u7a33\u5b9a\u6027<\/strong><\/p>\n

\u89c2\u5bdf\u5927\u9f20\u8840\u6d46\u6837\u54c1\u7ecf\u8fc73 \u6b21\u51b7\u51bb-\u89e3\u51bb\u5faa\u73af, \u5ba4\u6e29\u653e\u7f6e3 h, \u5728-80 \u2103\u4e0b\u653e\u7f6e60 \u5929\u53ca\u6837\u54c1\u7ecf<\/span>\u5904\u7406\u540e\u5ba4\u6e29\u653e\u7f6e10 h \u7684\u7a33\u5b9a\u6027\u3002\u76f8\u5bf9\u6807\u51c6\u504f\u5dee\u7edd\u5bf9\u503c<\/span>\u5747\u5c0f\u4e8e10%, \u8868\u660e\u5927\u9f20\u8840\u6d46\u4e2d\u6208\u820d\u745e\u6797\u5728\u4ee5\u4e0a\u6240\u6709\u6761<\/span>\u4ef6\u4e0b\u5747\u7a33\u5b9a\u3002<\/span><\/p>\n

4.2 \u8840\u836f\u6d53\u5ea6-\u65f6\u95f4\u66f2\u7ebf<\/strong><\/span><\/p>\n

\u5927\u9f20\u808c\u5185\u6ce8\u5c04\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u540e, \u5176\u8840\u836f\u6d53\u5ea6-\u65f6\u95f4\u66f2\u7ebf\u89c1\u56fe5\u3002<\/span><\/p>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n

\u7ed9\u836f\u540e1 h \u5185, \u8840\u6d46\u4e2d\u6208\u820d\u745e\u6797<\/span>\u6d53\u5ea6\u8fbe\u5230\u7b2c1 \u6b21\u5cf0\u503c, \u8868\u73b0\u4e3a\u7a81\u91ca\u9636\u6bb5\u3002\u5728\u8be5\u9636\u6bb5\u540e,<\/span>\u5236\u5242S \u5448\u660e\u663e\u7684\u53cc\u5cf0, \u5728\u7b2c1\uff5e5 \u5929\u8840\u836f\u6d53\u5ea6\u9ad8\u4e8e\u5236\u5242<\/span>F \u548c\u5236\u5242M, \u8fd9\u4e0e\u4f53\u5916\u91ca\u653e\u66f2\u7ebf\u524d\u671f, \u5236\u5242S \u91ca\u653e\u901f\u5ea6<\/span>\u5feb\u4e8e\u5236\u5242F \u548c\u5236\u5242M\u7684\u60c5\u51b5\u76f8\u5bf9\u5e94\u3002\u4ece\u8fbe\u5cf0\u65f6\u95f4\u6765<\/span>\u770b, \u5236\u5242S \u7684\u8fbe\u5cf0\u65f6\u95f4\u6700\u957f, \u5236\u5242M\u7684\u8fbe\u5cf0\u65f6\u95f4\u4ecb\u4e8eS<\/span>\u5236\u5242\u4e0e\u5236\u5242F \u4e4b\u95f4, \u4f53\u5916\u91ca\u653e\u5ea6\u6d4b\u5b9a\u7684\u918b\u9178\u6208\u820d\u745e\u6797<\/span>\u5fae\u7403\u7684\u91ca\u653e\u8d8b\u52bf\u4e0e\u918b\u9178\u6208\u820d\u745e\u6797\u5728SD\u5927\u9f20\u4f53\u5185\u7684\u91ca<\/span>\u653e\u8d8b\u52bf\u4e00\u81f4, \u8bc1\u660e\u4f53\u5916\u91ca\u653e\u5ea6\u65b9\u6cd5\u80fd\u5f88\u597d\u5730\u53cd\u6620\u918b\u9178<\/span>\u6208\u820d\u745e\u6797\u5fae\u7403\u5728SD\u5927\u9f20\u4f53\u5185\u7684\u91ca\u653e\u60c5\u51b5\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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5 \u4f53\u5185\u5916\u76f8\u5173\u6027\u6a21\u578b\u7684\u6784\u5efa<\/span><\/strong><\/span>
<\/p>\n<\/section>\n<\/section>\n<\/section>\n

\n
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\n

\u5c063 \u79cd\u91ca\u653e\u901f\u7387\u4e0d\u540c\u7684\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u5728SD\u5927\u9f20\u4f53\u5185\u7684\u8840\u836f\u6d53\u5ea6-\u65f6\u95f4\u6570\u636e\u7ecf%AUC\u6cd5\u8fdb\u884c\u5904\u7406\u540e, \u5f97\u52303 \u79cd\u5fae\u7403\u5728SD\u5927\u9f20\u4f53\u5185\u7684\u7d2f\u79ef\u91ca\u653e\u66f2\u7ebf, \u7ed3\u679c\u89c1\u56fe6\u3002<\/span><\/p>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n

\u9009\u7528\u91ca\u653e\u901f\u7387\u4e0d\u540c\u76843 \u6279\u5fae\u7403\u5236\u5242\u4e24\u4e24\u7ec4\u5408\u5efa\u7acb\u4f53\u5185\u5916\u76f8\u5173\u6027\u6a21\u578b, \u5373\u4ee5\u4f53\u5916\u7d2f\u79ef\u91ca\u653e\u5ea6\u4e3a\u6a2a\u5750\u6807, \u4ee5\u4f53\u5185\u7d2f\u79ef\u91ca\u653e\u5ea6\u4f5c\u4e3a\u7eb5\u5750\u6807, \u7ed8\u5236\u76f8\u5173\u6027\u66f2\u7ebf, \u5e76\u7528\u6570\u5b66\u516c\u5f0f\u5bf9\u76f8\u5173\u6027\u66f2\u7ebf\u8fdb\u884c\u62df\u5408, \u7ed3\u679c\u89c1\u56fe7 (A\uff5eC), \u6240\u5f97\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u65b9\u7a0b\u89c1\u88682\u3002<\/span><\/p>\n

\u7ed3\u679c\u8868\u660e, \u4f53\u5916\u7d2f\u79ef\u91ca\u653e\u5ea6\u4e0e\u4f53\u5185\u7d2f\u79ef\u91ca\u653e\u5ea6\u4e4b\u95f4\u76f8\u5173\u6027\u826f\u597d(r>0.98)\u3002<\/span><\/p>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n

\u5c06\u672a\u53c2\u4e0e\u5efa\u6a21\u7684\u7b2c3 \u6279\u5fae\u7403\u5236\u5242\u4f5c\u4e3a\u5916\u90e8\u9884\u6d4b\u80fd\u529b\u9a8c\u8bc1\u6279\u6b21, \u5c06\u5176\u4f53\u5916\u7d2f\u79ef\u91ca\u653e\u66f2\u7ebf\u4ee3\u5165\u4f53\u5185\u5916\u76f8\u5173\u6027\u6a21\u578b\u8ba1\u7b97\u5f97\u5230\u4f53\u5185\u7d2f\u79ef\u91ca\u653e\u66f2\u7ebf, \u5e76\u4e0e\u5176\u5728\u5927\u9f20\u4f53\u5185\u7684\u5b9e\u9645\u7d2f\u79ef\u91ca\u653e\u66f2\u7ebf\u8fdb\u884c\u6bd4\u8f83, \u7ed3\u679c\u89c1\u56fe7 (D\uff5eF)\u3002<\/span><\/p>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n

Figure 7 In vitro-in vivo correlation (IVIVC) developed for goserelin acetate microspheres. A: IVIVC developed using Formulation S and <\/span>M; B: IVIVC developed using Formulation S and F; C: IVIVC developed using Formulation F and M; D: Observed and predicted in vivo <\/span>release profiles of formulation F; E: Observed and predicted in vivo release profiles of formulation M; F: Observed and predicted in vivo <\/span>release profiles of formulation S<\/span><\/p>\n

\u7531\u56fe\u663e\u793a, \u9884\u6d4b\u5f97\u5230\u7684\u4f53\u5185\u7d2f\u79ef\u91ca\u653e\u66f2\u7ebf\u4e0e\u5b9e\u6d4b\u5f97\u5230\u7684\u4f53\u5185\u7d2f\u79ef\u91ca\u653e\u66f2\u7ebf\u57fa\u672c\u91cd\u5408, \u8bc1\u660e\u672c\u7814\u7a76\u6240\u5efa\u7acb\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u6a21\u578b\u5728\u5927\u9f20\u4f53\u5185\u5177\u6709\u826f\u597d\u7684\u9884\u6d4b\u80fd\u529b\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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

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\u7ed3\u8bba<\/strong><\/p>\n<\/section>\n<\/section>\n

<\/section>\n<\/section>\n<\/section>\n<\/section>\n
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\u672c\u7814\u7a76\u91c7\u7528\u590d\u4e73\u6cd5(S\/O\/W\u6cd5) \u5236\u5907\u4e863 \u79cd\u91ca\u653e\u901f\u7387\u4e0d\u540c\u7684\u6ce8\u5c04\u7528\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u3002<\/span><\/p>\n

\u7ed3\u5408\u918b\u9178\u6208\u820d\u745e<\/span>\u6797\u5fae\u7403\u5728\u4f53\u5185\u5916\u7684\u91ca\u653e\u60c5\u51b5\u53ca\u91ca\u653e\u8fc7\u7a0b\u4e2dPLGA\u5206\u5b50<\/span>\u91cf\u548c\u5f62\u8c8c\u7684\u7814\u7a76, \u63a8\u6d4b\u5176\u5177\u67093 \u4e2a\u91ca\u653e\u9636\u6bb5, \u5373: \u7a81\u91ca<\/span>\u9636\u6bb5, \u5fae\u7403\u8868\u9762\u7684\u836f\u7269\u6eb6\u89e3\u91ca\u653e; \u6269\u6563\u9636\u6bb5, \u5fae\u7403\u5185\u90e8<\/span>\u836f\u7269\u6269\u6563\u81f3\u5fae\u7403\u8868\u9762\u540e\u91ca\u653e; \u6eb6\u8680\u9636\u6bb5(\u4e3b\u8981\u9636\u6bb5), \u968f<\/span>\u7740PLGA\u7684\u964d\u89e3, \u836f\u7269\u5728\u805a\u5408\u7269\u6eb6\u8680\u548c\u6269\u6563\u7684\u53cc\u91cd\u4f5c<\/span>\u7528\u4e0b\u5b8c\u5168\u91ca\u653e\u3002<\/span><\/p>\n

\u672c\u6587\u6240\u5f00\u53d1\u7684\u4f53\u5916\u91ca\u653e\u5ea6\u6d4b\u5b9a\u65b9\u6cd5\u5bf9<\/span>\u4e0d\u540c\u7684\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u5177\u6709\u826f\u597d\u7684\u533a\u5206\u80fd\u529b\u3002<\/span><\/p>\n

\u6587\u4e2d<\/span>\u9009\u62e9\u4e0d\u540c\u7684\u5efa\u6a21\u6279\u6b21\u5fae\u7403\u5efa\u7acbIVIVC, \u5747\u76f8\u5173\u6027\u826f\u597d<\/span>(r>0.98), \u5916\u90e8\u9884\u6d4b\u80fd\u529b\u9a8c\u8bc1\u7ed3\u679c\u8868\u660e, \u6240\u5efa\u7acb\u7684<\/span>IVIVC\u65b9\u7a0b\u5728\u5927\u9f20\u4f53\u5185\u5177\u6709\u826f\u597d\u7684\u9884\u6d4b\u80fd\u529b\u3002<\/span><\/p>\n

\u918b\u9178\u6208<\/span>\u820d\u745e\u6797\u5fae\u7403IVIVC \u7684\u5efa\u7acb, \u8bc1\u660e\u672c\u7814\u7a76\u6240\u5f00\u53d1\u4f53\u5916\u91ca<\/span>\u653e\u5ea6\u6d4b\u5b9a\u65b9\u6cd5\u53ef\u4ee5\u5f88\u597d\u5730\u9884\u6d4b\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u5728\u5927<\/span>\u9f20\u4f53\u5185\u7684\u91ca\u836f\u884c\u4e3a, \u5e76\u4e14\u53ef\u7528\u4e8e\u4f53\u5916\u91ca\u653e\u5ea6\u65b9\u6cd5\u9650\u5ea6<\/span>\u7684\u5236\u5b9a, \u540c\u65f6\u53ef\u6307\u5bfc\u5904\u65b9\u7b5b\u9009, \u52a0\u5feb\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403<\/span>\u5236\u5242\u7684\u5f00\u53d1\u8fdb\u7a0b\u3002<\/span><\/p>\n<\/section>\n<\/section>\n<\/section>\n

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\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/p>\n
\n

\u53c2\u8003\u6587\u732e<\/strong><\/p>\n<\/section>\n

\"\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76\"<\/section>\n

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<\/section>\n<\/section>\n<\/section>\n<\/section>\n
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\u836f\u5b66\u5b66\u62a5 Acta Pharmaceutica Sinica, 2019, 54(1): 159 \u2212165<\/p>\n<\/section>\n<\/section>\n<\/section>\n

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<\/p>\n<\/p><\/div>\n","protected":false},"excerpt":{"rendered":"

\u918b\u9178\u6208\u820d\u745e\u6797\u5fae\u7403\u7684\u4f53\u5185\u5916\u76f8\u5173\u6027\u7814\u7a76 In vitro-in vivo correlation of goser […]<\/p>\n","protected":false},"author":1,"featured_media":98146,"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\/98145"}],"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=98145"}],"version-history":[{"count":1,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts\/98145\/revisions"}],"predecessor-version":[{"id":98169,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts\/98145\/revisions\/98169"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/media\/98146"}],"wp:attachment":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/media?parent=98145"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/categories?post=98145"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/tags?post=98145"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}