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盐酸丁丙诺啡控释制剂的研制。

Development of an enhanced formulation for delivering sustained release of buprenorphine hydrochloride.

机构信息

Membrane Research Center, Chemical Engineering Department, Razi University, Kermanshah, Iran.

出版信息

Saudi Pharm J. 2011 Oct;19(4):255-62. doi: 10.1016/j.jsps.2011.05.001. Epub 2011 May 12.

Abstract

To control the minimum effective dose, and reduce the number and quantity of administered potent drugs are unique features of advanced drug delivery in situ forming gel formulation. The efficacy, consistency, and increasing the application of existing injection therapies can be enhanced through optimization of controlled released systems by using FDA approved biodegradable PLGA (poly-d,l-lactide-co-glycolide) polymer. The purpose of this study was to develop different in situ forming implant (ISFI) formulations of buprenorphine hydrochloride for post treatment of drug addicts, acute and chronic pains. The drug releases from different ISFIs membranes with and without Tween 80 were compared over a period of time. Kinetic equation followed the Korsmeyer-Peppas model, as the plots showed high linearity. The influence of this additive on polymer properties was investigated using differential scanning calorimetry (DSC), and the membranes structure was studied by X-ray diffractometry (XRD) and scanning electron microscope (SEM). Data revealed that Tween 80 modified the drug release pattern using diffusion mechanism and decreased the glass transition temperature (T g) significantly. The degree of crystallinity was decreased after phase inversion which helps the dissolution of drug from membrane. The porosity of modified membranes was in accordance with release profiles. These findings suggest four different in situ forming implant formulations which can release various dose of the buprenorphine hydrochloride in a prolonged time. Also this surfactant can be an attractive additive for modifying the release rate of drugs from PLGA-based membrane drug delivery systems.

摘要

控制最小有效剂量,减少给予的强效药物的数量和剂量是原位形成凝胶制剂中先进药物输送的独特特征。通过使用 FDA 批准的可生物降解的 PLGA(聚-d,l-乳酸-共-乙醇酸)聚合物对控释系统进行优化,可以提高疗效、一致性,并增加现有注射疗法的应用。本研究旨在开发盐酸丁丙诺啡的不同原位形成植入物(ISFI)制剂,用于治疗吸毒者、急性和慢性疼痛。比较了含有和不含有吐温 80 的不同 ISFI 膜的药物释放情况。动力学方程遵循 Korsmeyer-Peppas 模型,因为图显示出高度线性。使用差示扫描量热法(DSC)研究了这种添加剂对聚合物性质的影响,并通过 X 射线衍射(XRD)和扫描电子显微镜(SEM)研究了膜结构。数据表明,吐温 80 通过扩散机制改变了药物释放模式,并显著降低了玻璃化转变温度(T g)。相反转后结晶度降低,有助于药物从膜中溶解。改性膜的孔隙率与释放曲线一致。这些发现表明,可以开发四种不同的原位形成植入物制剂,以在延长的时间内释放不同剂量的盐酸丁丙诺啡。此外,这种表面活性剂可以作为一种有吸引力的添加剂,用于调节基于 PLGA 的膜药物输送系统中药物的释放速率。

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