天然高分子基质片盐酸曲唑酮的研制与评价

Jeetendra Kushwaha, D. Chaturvedi, M. Verma, K. Tiwari, Neelesh Anuragi
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引用次数: 0

摘要

创新药物的并发症和营销成本的增加使人们更加关注缓释(SR)或控释(CR)给药系统的开发。盐酸曲唑酮(TRZ)是一种众所周知的化合物,被用作抗抑郁药,属于选择性血清素再摄取抑制剂(SARI)。本研究的目的是研制口服TRZ缓释片并对其进行评价。评估预压缩参数。对其进行压后参数评价,如厚度、硬度、平均重量、脆性和体外释放研究。傅里叶变换红外光谱未观察到TRZ与辅料之间的相互作用。本研究成功地提高了TRZ口服治疗的疗效,因为药物释放时间延长了12小时,从而减少了给药频率,提高了患者的依从性。研究还揭示了HPMC K-15、高尔胶和PVP K30作为基质片控速聚合物的适用性。单用HPMC亲水性基质不能有效控制TRZ的释放12 h,而与瓜尔胶联用可减缓药物的释放,因此可成功用于制备基质片sr。优化后的F-8在溶出12 h内释放度最高达99.12%。F-8的释放动力学数据为一级释放动力学(R2 = 0.980)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
FORMULATION DEVELOPMENT AND EVALUATION OF MATRIX TABLET TRAZODONE HYDROCHLORIDE USING NATURAL POLYMER
Increased complications and costs of marketing of innovative drugs focused greater attention to the development of sustained release (SR) or controlled release (CR) drug delivery systems. Trazodone Hydrochloride (TRZ) is a well-known chemical compound that is used as an antidepressant that belongs to a selective serotonin reuptake inhibitor (SARI). The objective of present work was to develop and evaluated oral sustained release matrix tablet of TRZ. Pre-compression parameters were evaluated. The tablets were evaluated for post-compression parameters such as thickness, hardness, average weight, friability and In vitro release studies. No interactions were observed between TRZ and excipients from the Fourier transform infrared spectroscopy. The present research work was successful in improving the efficacy TRZ oral therapy as the drug release was extended for 12 hours thus reducing dosing frequency thereby improving patient compliance. The study also revealed the applicability of HPMC K-15, Gaur gum and PVP K30 as rate-controlling polymers in matrix tablets. The hydrophilic matrix of HPMC alone cannot control the release TRZ effective for 12 h while when combined with guar gum, may slow down the release of the drug and therefore, can be successfully employed for the formulation of matrix tablets SR. It may be concluded from the study that; the optimized formulation F-8 was shown maximum drug release 99.12 % in 12 h of dissolution. The release kinetic data of formulation F-8 shown first order release kinetics (R2 = 0.980).
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