4.6 Article

Efficacy of a new sustained-release microsphere formulation of exenatide, DA-3091, in Zucker diabetic fatty (ZDF) rats

期刊

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 40, 期 2, 页码 103-109

出版社

ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejps.2010.03.006

关键词

GLP-1 agonist; Exenatide; Sustained-release formulation; Poly(D,L-lactide-co-glycolide); Zucker diabetic fatty (ZDF) rats; Type 2 diabetes mellitus

资金

  1. Ministry for Health, Welfare and Family Affairs [A080017]
  2. Ministry of Science and Technology, Republic of Korea [ROA-2006-000-10290-0]

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Exenatide must be administered serially by twice-daily subcutaneous (SC) injection due to its short half-life. The purpose of the present study is to develop an improved sustained-release exenatide formulation with a therapeutic efficacy comparable to serial, twice-daily injections of exenatide. A novel SR formulation of exenatide, DA-3091, was prepared by single-emulsion solvent evaporation using PLGA. It was administered by SC injection to ZDF rats in single exenatide doses of 0.1, 0.25, 0.5, 1 or 2 mg/kg. On the 28th, 49th and 70th days, a 1 or 2 mg/kg dose of DA-3091 was further administered to rats in dose groups of 1 or 2 mg/kg. The efficacy of DA-3091 was then compared with that of serial, twice-daily SC injections of an exenatide solution for 13 weeks. NFBG and HbA1c concentrations were decreased both significantly and linearly as the exenatide dose in DA-3091 increased. In addition, food intake and body weight were suppressed both significantly and dose-dependently. In equivalent or half doses of exenatide, the efficacy of DA-3091 was comparable to that of twice-daily injections of exenatide solution for 13 weeks. In conclusion, DA-3091 has the potential to be clinically effective when administered every 3 weeks, or less frequently, which promises to significantly improve patient compliance. (C) 2010 Elsevier B.V. All rights reserved.

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