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Preparation, characterization and in vitro drug release properties of polytrimethylene carbonate/polyadipic anhydride blend microspheres

机译:聚碳酸三亚甲基酯/聚己二酸酐共混物微球的制备,表征及体外释药性能

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Polyadipic anhydride (PAA), an aliphatic polyanhydride, and polytrimethylene carbonate (PTMC), an aliphatic polycarbonate, were synthesized via ring opening polymerization of oxepan-2,7-dione and melt-condensation of trimethylene carbonate (1,3 dioxan-2-one), respectively. PTMC-PAA blend microspheres containing different ratios of buprenorphine HCl (2, 5, and 10%) were prepared by an oil-in-oil emulsion solvent removal method. Microspheres with different ratios of PTMC-PAA (85 /15, 70 / 30, and 55 / 45) containing 5% buprenorphine HCl were prepared. Microspheres were spherical with visible cracks and pores on the surface. The average particle size of microspheres was around 200 mu m for all microspheres. Drug loading efficiency of PTMC-PAA microspheres (85/15, 70/30, and 55/45) was 97.2, 95.2, and 70.2%, respectively. With the increase in the PTMC ratio, the melting point and the enthalpy of melting were both decreased. The mechanism for drug release from PTMC-PAA blend microspheres were generally a combination of drug diffusion through polymers and biodegradation of the polymers. In first three days, the release from microspheres followed zero order kinetics and was dependent on the PAA content. After three days the drug release from microspheres followed first order kinetics. In conclusion it was demonstrated that buprenorphine HCl release from microspheres could be successfully controlled by using different ratios of PTMC-PAA blends. (c) 2006 Wiley Periodicals, Inc.
机译:通过环氧丙烷-2,7-二酮的开环聚合和碳酸三亚甲基酯(1,3-二恶烷-2-)的熔融缩合反应合成了脂肪族聚酐聚己二酸酐(PAA)和脂肪族聚碳酸亚丙酯(PTMC)。一)。通过油包油型乳液溶剂去除法制备了含有不同比例的丁丙诺啡HCl(2%,5%和10%)的PTMC-PAA共混微球。制备了含有5%丁丙诺啡HCl的比例不同的PTMC-PAA(85 / 15、70 / 30和55/45)的微球。微球是球形的,在表面上可见裂纹和孔。对于所有微球,微球的平均粒径为约200μm。 PTMC-PAA微球(85 / 15、70 / 30和55/45)的载药效率分别为97.2%,95.2和70.2%。随着PTMC比的增加,熔点和熔融焓均降低。从PTMC-PAA共混微球释放药物的机制通常是药物通过聚合物扩散和聚合物的生物降解的组合。在开始的三天内,从微球的释放遵循零级动力学,并且取决于PAA含量。三天后,药物从微球释放遵循一级动力学。结论表明,通过使用不同比例的PTMC-PAA共混物,可以成功地控制盐酸丁丙诺啡从微球中的释放。 (c)2006年Wiley Periodicals,Inc.

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