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1\u3001Zhang L. The use of low molecular weight protamine to enhance oral absorption of exenatide. Int J Pharm. 2018 Aug 25;547(1-2):265-273.<\/span><\/p>\n

\u70df\u53f0\u5927\u5b66\u7684Zhang L\u7b49\u4eba\u5236\u5907\u4e86\u950c\u79bb\u5b50\u4e0e\u827e\u585e\u90a3\u80bd\u590d\u5408\u7269\u529f\u80fd\u5316\u7eb3\u7c73\u7c92\uff0c\u4ee5\u5b9e\u73b0\u827e\u585e\u90a3\u80bd\u7684\u53e3\u670d\u7ed9\u836f\u3002\u5177\u4f53\u7684\uff0c\u91c7\u7528PEG-PLGA\u4f5c\u4e3a\u8f7d\u4f53\u4ee5\u907f\u514d\u80c3\u80a0\u9053\u5185\u7684\u9176\u89e3\u4f5c\u7528\uff0c\u5e76\u91c7\u7528\u4f4e\u5206\u5b50\u91cf\u7cbe\u86cb\u767d\uff08LMWP\uff09\u4f5c\u4e3a\u5b98\u80fd\u56e2\uff0c\u4ee5\u589e\u52a0\u7eb3\u7c73\u7c92\u5bf9\u5c0f\u80a0\u4e0a\u76ae\u7684\u7a7f\u900f\u529b\u3002\u8be5\u7eb3\u7c73\u7c92\u5177\u6709\u826f\u597d\u7684\u7406\u5316\u7279\u5f81\uff0c\u7ec6\u80de\u6444\u53d6\u4e0e\u8de8\u819c\u8f6c\u8fd0\u8bd5\u9a8c\u4e5f\u8bc1\u5b9e\u4e86\u8be5\u7eb3\u7c73\u5bf9\u5c0f\u80a0\u4e0a\u76ae\u7684\u826f\u597d\u7684\u7a7f\u900f\u529b\u3002\u52a8\u7269\u8bd5\u9a8c\u663e\u793a\uff0c\u8be5\u7eb3\u7c73\u7c92\u5177\u6709\u663e\u8457\u7684\u964d\u8840\u7cd6\u6548\u679c\uff0c\u800c\u5176\u53e3\u670d\u540e\u827e\u585e\u90a3\u80bd\u7684\u76f8\u5bf9\u751f\u7269\u5229\u7528\u5ea6\u4e3a7.44%\uff0c\u662f\u827e\u585e\u90a3\u80bd-\u950c\u79bb\u5b50\u6eb6\u6db2\u768429\u500d\u3002<\/span><\/p>\n

2\u3001Zhang L et al. Tf ligand-receptor-mediated exenatide-Zn2+ complex oral-delivery system for penetration enhancement of exenatide. J Drug Target. 2018 Apr 16:1-10. doi: 10.1080\/1061186X.2018.1455839. [Epub ahead of print]<\/span><\/p>\n

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3\u3001Menzel C et al. In vivo evaluation of an oral self-emulsifying drug delivery system (SEDDS) for exenatide. J Control Release. 2018 May 10;277:165-172. doi: 10.1016\/j.jconrel.2018.03.018. Epub 2018 Mar 21.<\/span><\/p>\n

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4\u3001<\/span>Shi Y et al. Fc-modified exenatide-loaded nanoparticles for oral delivery to improve hypoglycemic effects in mice. Sci Rep. 2018 Jan 15;8(1):726. doi: 10.1038\/s41598-018-19170-y.<\/span><\/p>\n

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5\u3001Soudry-Kochavi L et al. Improved oral absorption of exenatide using an original nanoencapsulation and microencapsulation approach. J Control Release. 2015 Nov 10;217:202-10.<\/span><\/p>\n

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6\u3001<\/span>Li X et al. The glucose-lowering potential of exenatide delivered orally via goblet cell-targeting nanoparticles. Pharm Res. 2015 Mar;32(3):1017-27.<\/span><\/p>\n

\u5409\u6797\u5927\u5b66\u7684Li X\u7b49\u4eba\u91c7\u7528\u676f\u72b6\u7ec6\u80de\u9776\u5411\u7684CSKSSDYQC (CSK)\u80bd\u5bf9\u58f3\u805a\u7cd6\u8fdb\u884c\u4fee\u9970\uff0c\u5e76\u4ee5\u4fee\u9970\u4ea7\u7269\u4e3a\u8f7d\u4f53\uff0c\u5236\u5907\u5f97\u5230\u4e86\u827e\u585e\u90a3\u80bd\u7eb3\u7c73\u7c92\u3002\u8be5\u7eb3\u7c73\u7c92\u53ef\u663e\u8457\u964d\u4f4e\u58f3\u805a\u7cd6\u7684\u6bd2\u6027\uff0c\u5e76\u53ef\u589e\u5f3a\u836f\u7269\u5bf9Caco-2\/HT-29\u5171\u57f9\u80b2\u7ec6\u80de\u5355\u5c42\u7684\u6e17\u900f\u529b\u3002\u52a8\u7269\u8bd5\u9a8c\u7ed3\u679c\u663e\u793a\uff0cCSK\u4fee\u9970\u7684\u58f3\u805a\u7cd6-\u827e\u585e\u90a3\u80bd\u7eb3\u7c73\u7c92\u53e3\u670d\u7ed9\u836f\u540e\uff0c\u7eb3\u7c73\u7c92\u5148\u4ece\u98df\u9053\u6563\u5e03\uff0c\u800c\u540e\u8fdb\u5165\u80c3\u4e0e\u5c0f\u80a0\uff0c\u968f\u540e\u5438\u6536\u8fdb\u5165\u809d\u810f\uff0c\u6700\u540e\u7531\u8180\u80f1\u6392\u6cc4\uff0c\u800c\u4e14\u4fee\u9970\u540e\u7eb3\u7c73\u7c92\u4e2d\u827e\u585e\u90a3\u80bd\u7684\u53e3\u670d\u751f\u7269\u5ea6\u6bd4\u672a\u4fee\u9970\u7684\u7eb3\u7c73\u7c92\u4e2d\u827e\u585e\u90a3\u80bd\u751f\u7269\u5229\u7528\u5ea6\u9ad81.7\u500d\uff0c\u6b64\u5916\u524d\u8005\u7684\u964d\u8840\u7cd6\u4f5c\u7528\u4ea6\u6709\u6240\u63d0\u9ad8\u3002<\/span><\/p>\n

7\u3001Zhang B et al. Oral delivery of exenatide via microspheres prepared by cross-linking of alginate and hyaluronate. PLoS One. 2014 Jan 21;9(1):e86064.<\/span><\/p>\n

\u4e2d\u56fd\u836f\u79d1\u5927\u5b66\u7684Zhang B\u7b49\u4eba\u4ee5pH\u654f\u611f\u6027\u7684\u85fb\u9178\u76d0\u4e0e\u73bb\u7483\u9178\u76d0\u7684\u4ea4\u8054\u4ea7\u7269\u4e3a\u8f7d\u4f53\uff0c\u5236\u4e86\u88c5\u8f7d\u6709\u827e\u585e\u90a3\u80bd\u7684\u5fae\u7403\u3002\u8be5\u5fae\u7403\u5177\u6709\u7403\u72b6\u7ed3\u6784\uff0c\u8f7d\u836f\u6027\u80fd\u826f\u597d\uff08\u8f7d\u836f\u7387\u9ad8\u8fbe72.9%\uff09\uff0c\u4e14\u5728\u6a21\u62df\u7684\u6d88\u5316\u9053\u73af\u5883\u4e2d\u663e\u793a\u51fa\u4f18\u826f\u7684\u91ca\u653e\u6027\u80fd\u3002\u7cd6\u5c3f\u75c5\u5c0f\u9f20\u5355\u6b21\u53e3\u670d\u7ed9\u836f\u8bd5\u9a8c\u7ed3\u679c\u663e\u793a\uff0c\u827e\u585e\u90a3\u80bd\u7684\u8840\u836f\u6d53\u5ea6\u5728\u7eb3\u7c73\u7c92\u53e3\u670d\u7ed9\u836f\u540e4\u5c0f\u65f6\u8fbe\u5176\u5cf0\u503c\uff0c\u800c\u5c0f\u9f20\u8840\u7cd6\u6c34\u5e73\u5728\u7ed9\u836f\u540e2\u5c0f\u65f6\u5185\u964d\u4f4e\u81f3\u6b63\u5e38\u503c\uff0c\u4e14\u53ef\u7ef4\u63014\u5c0f\u65f6\u3002\u6b64\u5916\uff0c\u8be5\u7eb3\u7c73\u53e3\u670d\u7ed9\u836f\u540e\u4e0e\u76ae\u4e0b\u6ce8\u5c04\u7ed9\u836f\u76f8\u6bd4\u7684\u76f8\u5bf9\u751f\u7269\u5229\u7528\u5ea6\u4e3a10.2%\u3002<\/span><\/p>\n

8\u3001<\/span>Ara\u00fajo F et al. The impact of nanoparticles on the mucosal translocation and transport of GLP-1 across the intestinal epithelium. Biomaterials. 2014, 35(33):9199\u20139207<\/span><\/p>\n

\u8d6b\u5c14\u8f9b\u57fa\u5927\u5b66Ara\u00fajo F\u7b49\u4eba\u5206\u522b\u91c7\u7528PLGA\u3001Witepsol E85 \u8102\u8d28\u4f53\u4e0e\u591a\u4e5f\u4e8c\u6c27\u5316\u7845\u4f5c\u4e3a\u8f7d\u4f53\u5236\u5907\u4e86\u88c5\u8f7d\u6709GLP-1\u7684\u7eb3\u7c73\u7c92\uff0c\u5e76\u8bc4\u4ef7\u4e86\u5404\u81ea\u7684\u4f53\u5916\u6e17\u900f\u529b\u3002\u6240\u8ff0\u7eb3\u7c73\u7c92\u7684\u7c92\u5f84\u5747\u7ea6\u4e3a200nm\uff0c\u800c\u4e14\u82e5\u4ee5\u58f3\u805a\u7cd6\u4f5c\u4e3a\u5305\u8863\uff0c\u5219\u53ef\u63d0\u9ad8\u6240\u6709\u7eb3\u7c73\u7c92\u4e0e\u9ecf\u6db2\u7684\u76f8\u4e92\u4f5c\u7528\u3002\u5404\u79cd\u7eb3\u7c73\u7cfb\u7edf\u5747\u89c2\u5bdf\u5230\u4e86\u8f83\u9ad8\u7684\u5305\u5c01\u7387\uff0c\u4f46\u5176\u4e2d\uff0c\u591a\u5b54\u4e8c\u6c27\u5316\u7845\u7eb3\u7c73\u7cfb\u7edf\u7684\u5305\u5c01\u7387\u6700\u9ad8\u3002\u6b64\u5916\uff0c\u53ea\u6709PLGA\u4e0e\u591a\u5b54\u4e8c\u6c27\u5316\u7845\u7eb3\u7c73\u7cfb\u7edf\u5728\u7528\u58f3\u805a\u7cd6\u5305\u8863\u540e\u80fd\u4f7fGLP-1\u7684\u751f\u7269\u6d41\u4f53\u73af\u5883\u4e2d\u5b9e\u73b0\u7f13\u91ca\u7684\u6548\u679c\uff0c\u800c\u4e14\u5f53\u4e0a\u8ff0\u7eb3\u7c73\u7cfb\u7edf\u4e0e\u80a0Caco-2\u7ec6\u80de\u53caHT29-MTX\u7ec6\u80de\u63a5\u89e6\u65f6\uff0c\u89c2\u5bdf\u5230\u4e86\u76f8\u4f3c\u7684\u7ed3\u679c\u3002<\/span><\/p>\n

9\u3001Chuang EY et al. Combination therapy via oral co-administration of insulin- and exendin-4-loaded nanoparticles to treat type 2 diabetic rats undergoing OGTT. Biomaterials. 2013 Oct;34(32):7994-8001.<\/span><\/p>\n

\u53f0\u6e7e\u56fd\u7acb\u6e05\u534e\u5927\u5b66\u7684Chuang EY\u7b49\u4eba\u91c7\u7528\u7531\u58f3\u805a\u7cd6\u4e0e\u805a\uff08\u03b3-\u8c37\u6c28\u9178\uff09\u6784\u6210\u7684\u8f7d\u4f53\u5236\u5907\u4e86\u540c\u65f6\u88c5\u8f7d\u6709\u827e\u585e\u90a3\u80bd\u4e0e\u80f0\u5c9b\u7d20\u7684\u7eb3\u7c73\u7c92\u3002\u4f53\u5916\u8bd5\u9a8c\u7ed3\u679c\u663e\u793a\uff0c\u8be5\u7eb3\u7c73\u7c92\u53ef\u589e\u5f3a\u80a0\u65c1\u7ec6\u80de\u6e17\u900f\u4f5c\u7528\uff0c\u8fdb\u800c\u80fd\u5c06\u53e3\u670d\u7684\u80f0\u5c9b\u7d20\u4e0e\u827e\u585e\u90a3\u80bd\u9001\u81f3\u809d\u810f\u4e0e\u80f0\u810f\uff0c\u5e76\u4f7f\u5176\u53d1\u6325\u5404\u81ea\u964d\u7cd6\u4f5c\u7528\u3002\u800c\u4e14\u540c\u65f6\u5305\u88f9\u6709\u80f0\u5c9b\u7d20\u4e0e\u827e\u585e\u90a3\u80bd\u7684\u7eb3\u7c73\u7c92\u7684\u964d\u7cd6\u6548\u679c\u663e\u8457\u4f18\u4e8e\u53ea\u5305\u88f9\u80f0\u5c9b\u7d20\u7684\u7eb3\u7c73\u3002<\/span><\/p>\n

10\u3001<\/span>Qu W et al. A silica-based pH-sensitive nanomatrix system improves the oral absorption and efficacy of incretin hormone glucagon-like peptide-1. Int J Nanomed. 2012, 7:4983\u20134994.<\/span><\/p>\n

\u5317\u4eac\u5927\u5b66\u7684Qu W\u7b49\u4eba\u5236\u5907\u4e86\u7531GLP-1\u3001\u4e8c\u6c27\u5316\u7845\u4e0epH-\u654f\u611f\u6027Eudragit\u6784\u6210\u7684\u7eb3\u7c73\u7c92\uff0c\u8be5\u7eb3\u7c73\u7c92\u5bf9\u80a0\u9ecf\u819c\u7684\u6e17\u900f\u529b\u662f\u5355\u72ecGLP-1\u76845\u500d\uff0c\u800c\u5176\u86cb\u767d\u6c34\u89e3\u7a33\u5b9a\u6027\u4ea6\u663e\u8457\u9ad8\u4e8e\u540e\u8005\u3002\u52a8\u7269\u8bd5\u9a8c\u663e\u793a\uff0c\u8be5\u7eb3\u7c73\u7c92\u53e3\u670d\u7ed9\u836f4\u5206\u949f\u540e\u7ea670%\u7684\u836f\u7269\u4ecd\u7136\u4fdd\u6301\u539f\u6837\uff0c\u800cGLP-1\u5355\u72ec\u53e3\u670d\u7ed9\u836f4\u5206\u949f\u540e\u4ec5\u4e0d\u8db320%\u7684\u836f\u7269\u4ecd\u7136\u4fdd\u6301\u539f\u6837\uff0c\u6b64\u5916\uff0c\u7eb3\u7c73\u7c92\u7684\u76f8\u5bf9\u53e3\u670d\u751f\u7269\u5229\u7528\u5ea6\u4e3a35.67%\uff08\u4e0e\u8179\u8154\u5185\u6ce8\u5c04\u76f8\u6bd4\uff09\u3002\u964d\u7cd6\u8bd5\u9a8c\u7ed3\u679c\u663e\u793a\uff0c\u7eb3\u7c73\u7c92\u53e3\u670d\u7ed9\u836f\u540e\u7684\u964d\u7cd6\u6548\u679c\u6bd4\u8179\u8154\u5185\u6ce8\u5c04\u7684GLP-1\u9ad877%\u3002\u8be5\u7eb3\u7c73\u7c92\u52a8\u7269\u8bd5\u9a8c\u4e0e\u6d88\u5316\u9053\u7ec4\u7ec7\u7684\u7ec4\u7ec7\u5316\u5b66\u5206\u6790\u4ea6\u672a\u89c1\u663e\u8457\u7684\u6bd2\u6027\u53cd\u5e94\u3002<\/span><\/p>\n

11\u3001Nguyen HN et al. The glucose-lowering potential of exendin-4 orally delivered via a pH-sensitive nanoparticle vehicle and effects on subsequent insulin secretion in vivo. Biomaterials. 2011 Apr;32(10):2673-82.<\/span><\/p>\n

\u53f0\u6e7e\u56fd\u7acb\u6e05\u534e\u5927\u5b66\u7684Nguyen HN\u7b49\u4eba\u4ee5\u58f3\u805a\u7cd6\u4e0e\u805a\uff08\u03b3-\u8c37\u6c28\u9178\uff09\u7684\u6df7\u5408\u7269\u4e3a\u8f7d\u4f53\uff0c\u5236\u5907\u5f97\u5230\u4e86\u5305\u88f9\u6709\u827e\u585e\u90a3\u80bd\u7684PH-\u654f\u611f\u6027\u7eb3\u7c73\u7c92\uff0c\u5e76\u8003\u5bdf\u4e86\u94dc\uff08\u2161\uff09\u3001\u950c\uff08\u2161\uff09\u4e0e\u94c1\uff08\u2161\u3001\u2162\uff09\u7b49\u91d1\u5c5e\u79bb\u5b50\u5bf9\u7eb3\u7c73\u7c92\u6027\u80fd\u7684\u5f71\u54cd\u3002\u7ed3\u679c\u53d1\u73b0\uff0c\u94c1\uff08\u2162\uff09\u79bb\u5b50\u80fd\u663e\u8457\u5347\u9ad8\u7eb3\u7c73\u7c92\u7684\u8f7d\u836f\u7387\uff0860.9\u00b12.0%\uff09\u3002\u52a8\u7269\u8bd5\u9a8c\u7ed3\u679c\u663e\u793a\uff0c\u8be5\u7eb3\u7c73\u7c92\u53e3\u670d\u7ed9\u836f\u540e\u53ef\u7ecf\u8fc7\u98df\u9053\u3001\u80c3\u4e0e\u5c0f\u80a0\uff0c\u800c\u540e\u5438\u6536\u5165\u8840\uff0c\u5e76\u5728\u4ee3\u8c22\u540e\u7ecf\u7531\u8180\u80f1\u6392\u6cc4\u3002\u827e\u585e\u90a3\u80bd\u7684\u8840\u836f\u6d53\u5ea6\u5728\u7eb3\u7c73\u7c92\u53e3\u670d\u7ed9\u836f\u540e5\u5c0f\u65f6\u8fbe\u5176\u5cf0\u503c\uff0c\u800c\u5176\u53e3\u670d\u7ed9\u836f\u540e\u4e0e\u76ae\u4e0b\u6ce8\u5c04\u7ed9\u836f\u76f8\u6bd4\u7684\u76f8\u5bf9\u751f\u7269\u5229\u7528\u5ea6\u4e3a14.0 \u00b1 1.8%\u3002<\/span><\/p>\n

12\u3001<\/span>Joseph J et al. Oral delivery of glucagon-like peptide-1 in a modified polymer preparation normalizes basal glycaemia in diabetic db\/db mice. Diabetologia. 2000, 43(10):1319\u20131328<\/span><\/p>\n

\u591a\u4f26\u591a\u5927\u5b66\u7684Joseph J\u7b49\u4eba\u91c7\u7528PLGA\u4f5c\u4e3a\u8f7d\u4f53\uff0c\u5e76\u4ee5\u6a44\u6984\u6cb9\u4f5c\u4e3a\u586b\u5145\u5242\uff0c\u5236\u5907\u5f97\u5230\u4e86\u5305\u88f9\u6709D-\u03b12<\/sub>-GLP-1\u7684\u5fae\u7403\u3002\u6b63\u5e38\u7684CD1\u5c0f\u9f20\u4e0e\u7cd6\u5c3f\u75c5\u6027db\/db\u5c0f\u9f20\u91c7\u7528\u4e0a\u8ff0\u5fae\u7403\u53e3\u670d\u7ed9\u836f\u540e\uff0c4\u5c0f\u65f6\u53e3\u670d\u8461\u8404\u7cd6\u6311\u6218\u8bd5\u9a8c\u7ed3\u679c\u663e\u793a\u5176\u8840\u7cd6\u6c34\u5e73\u5206\u522b\u964d\u4f4e\u4e8641\u00b112%\u4e0e27\u00b15%\uff0c\u800c8\u5c0f\u65f6\u53e3\u670d\u8461\u8404\u7cd6\u6311\u6218\u8bd5\u9a8c\u7684\u8840\u7cd6\u6c34\u5e73\u5206\u522b\u964d\u4f4e\u4e8619\u00b111%\u4e0e28\u00b14%\u3002\u7cd6\u5c3f\u75c5\u6027\u5c0f\u9f20\u53e3\u670d\u5fae\u74034\u5c0f\u65f6\u540e\u7684\u57fa\u7840\u8840\u7cd6\u6c34\u5e73\u4ece13\u00b11 mmol\/l \u964d\u4f4e\u81f310\u00b11 mmol\/l\uff0c\u800c\u53e3\u670d\u5fae\u74038\u5c0f\u65f6\u540e\u7684\u57fa\u7840\u6c34\u5e73\u5219\u4ece12\u00b11 mmol\/l\u964d\u4f4e\u81f38\u00b11 mmol\/l\u3002\u76f8\u6bd4\u4e4b\u4e0b\uff0cD-\u03b12<\/sub>-GLP-1\u5355\u72ec\u53e3\u670d\u7ed9\u836f\u5219\u5bf9\u5c0f\u9f20\u7684\u8840\u7cd6\u6c34\u5e73\u65e0\u663e\u8457\u4f5c\u7528\u3002<\/span><\/p>\n

\u603b\u7ed3 <\/strong><\/span><\/p>\n

\u672c\u6587\u7684\u6587\u732e\u68c0\u7d22\u4e0e\u6574\u7406\u53d1\u73b0\uff0c\u76ee\u524d\u7eb3\u7c73\u6280\u672f\u5728\u53e3\u670dGLP-1\u5f00\u53d1\u4e2d\u7684\u5e94\u7528\u4e3b\u8981\u96c6\u4e2d\u4e8e\u539f\u751f\u6001\u7684GLP-1\u4e0e\u7b2c\u4e00\u4e2a\u4e0a\u5e02\u7684GLP-1\u53d7\u4f53\u6fc0\u52a8\u5242\u827e\u585e\u90a3\u80bd\uff0c\u8fd9\u4e0eMoonschi FH\u7b49\u4eba\u5728\u5176Advances in micro- and nanotechnologies for the GLP-1-based therapy and imaging of pancreatic beta-cells.<\/em>\u4e00\u6587\u4e2d\u6240\u62ab\u9732\u7684\u60c5\u51b5\u76f8\u4e00\u81f4\uff0c\u76f8\u6bd4\u4e4b\u4e0b\uff0c\u672c\u6587\u6536\u5f55\u7684\u53e3\u670dGLP-1\u76f8\u5173\u6587\u732e\u6570\u91cf\u6bd4Moonschi FH\u7b49\u4eba\u7684\u6587\u7ae0\u591a\u4e867\u7bc7\u3002<\/span><\/p>\n

\u5f53\u7136\uff0c\u7531\u4e8e\u7b14\u8005\u65f6\u95f4\u4e0e\u80fd\u529b\u7684\u9650\u5236\uff0c\u672c\u6587\u4ec5\u5728Pubmed\u4e2d\u5bf9\u76f8\u5173\u6587\u732e\u8fdb\u884c\u4e86\u68c0\u7d22\u4e0e\u6574\u7406\uff0c\u80af\u5b9a\u4f1a\u6709\u6240\u9057\u6f0f\u3002\u800c\u4e14\u4e13\u5229\u6587\u732e\u4e5f\u662f\u65b0\u6280\u672f\u7684\u91cd\u8981\u6765\u6e90\u4e4b\u4e00\uff0c\u7b14\u8005\u5c06\u4f1a\u5728\u4ee5\u540e\u7684\u6587\u7ae0\u4e2d\u5bf9\u4e13\u5229\u6587\u732e\u4e2d\u62ab\u9732\u7684\u53e3\u670dGLP-1\u6280\u672f\u8fdb\u884c\u6574\u7406\uff0c\u656c\u8bf7\u671f\u5f85\u3002<\/span><\/p>\n


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