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用于药物包衣的新型松香衍生物的评估

Evaluation of new rosin derivatives for pharmaceutical coating.

作者信息

Satturwar P M, Fulzele S V, Panyam J, Mandaogade P M, Mundhada D R, Gogte B B, Labhasetwar V, Dorle A K

机构信息

Department of Pharmaceutical Sciences, Nagpur University Campus, Amravati Road, Nagpur 440 010, India.

出版信息

Int J Pharm. 2004 Feb 11;270(1-2):27-36. doi: 10.1016/j.ijpharm.2003.10.021.

Abstract

Rosin and Rosin-based polymers have diversified drug delivery applications achieving sustained/controlled release profiles. In this manuscript, two new Rosin derivatives were synthesized and evaluated for physicochemical properties, molecular weight, polydispersity and glass transition temperature. Plasticizer-free films prepared by solvent evaporation were tested for surface morphology, water vapour transmission and mechanical properties (tensile strength, percent elongation and modulus of elasticity). The films showed low tensile strength and high percent elongation values achieving smooth and uniform surface. The derivatives were further characterized for film coating by evaluating the release of a model drug (diclofenac sodium) from pellets coated with the rosin derivatives as retarding membrane. Drug release was sustained up to 10 h due to 10% (w/w) coat built up with the new rosin derivatives. Increase in coat-built-up further facilitated sustained release from coated forms. Film coating could be achieved without agglomeration of the pellets within a reasonable operating time. The present study proposes novel film forming materials with potential use in sustained drug delivery.

摘要

松香及基于松香的聚合物在药物递送应用方面具有多样性,可实现持续/控释特性。在本论文中,合成了两种新型松香衍生物,并对其物理化学性质、分子量、多分散性及玻璃化转变温度进行了评估。通过溶剂蒸发制备的无增塑剂薄膜,对其表面形态、水蒸气透过率及机械性能(拉伸强度、伸长率百分比及弹性模量)进行了测试。这些薄膜显示出低拉伸强度和高伸长率百分比值,表面光滑且均匀。通过评估模型药物(双氯芬酸钠)从涂有松香衍生物作为阻滞膜的微丸中的释放情况,对这些衍生物进行了薄膜包衣的进一步表征。由于用新型松香衍生物构建了10%(w/w)的包衣,药物释放可持续长达10小时。包衣量的增加进一步促进了包衣剂型的持续释放。在合理的操作时间内,可实现薄膜包衣而微丸不发生团聚。本研究提出了具有在持续药物递送中潜在应用价值的新型成膜材料。

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