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吲哚啉类生物碱药物固体剂型的研发。

Development of solid, dosage forms of medicinal drugs from indoline group alkaloids.

作者信息

Gagua N, Vachnadze V, Alavidze N, Berashvili D, Bakuridze A

机构信息

Tbilisi State Medical University, Georgia.

出版信息

Georgian Med News. 2011 Nov;11(200):112-7.

Abstract

According to biopharmaceutical investigations, the regimen of the tablets of alkaloid containing new galenic preparation of indoline and indole group - Vinkabral, Vingerbin has been developed. Also, the preparation technology was worked out and it has been defined that optimal method of tabletting new galenic formulations, such as Vincabral and Vingerbin is direct pressing by using polifunctional additional formulations - Proslov SMCC (siliced methylceluslose) and Glikonat Sodium of Starch. Their influence on the technological characteristics are studied, so as the proportion of additional compounds are defined. The influence of technological parameters on technological characteristics of the tablets Vinkabral, Vingerbin were investigated and optimal conditions were selected: optimal humidity was 1.5-3.0%, Optimal compression power-105-120 mpa. The kinetics of the release of active substance - alkaloids from the tablets of Vinkabral and Vingerbin was studied using the methods of "rotary basket" in sour, neutral and alkaline area during the mix time 50 rt/min and 100 rt/min. The 90% of active substance releases in sour area during 75 minutes in 100 rt/min mix up condition.

摘要

根据生物制药研究,已研发出含吲哚啉和吲哚基团新盖伦制剂——长春胺缓释片(Vinkabral)、长春西汀(Vingerbin)的片剂给药方案。此外,还制定了制剂工艺,并确定新盖伦制剂(如长春胺缓释片和长春西汀)压片的最佳方法是使用多功能辅料——预胶化淀粉(Proslov SMCC)和淀粉甘氨酸钠直接压片。研究了它们对工艺特性的影响,并确定了辅料的比例。研究了工艺参数对长春胺缓释片、长春西汀片剂工艺特性的影响,并选择了最佳条件:最佳湿度为1.5 - 3.0%,最佳压片力为105 - 120兆帕。采用“旋转篮法”,在50转/分钟和100转/分钟的搅拌速度下,研究了长春胺缓释片和长春西汀片剂中活性物质——生物碱在酸性、中性和碱性环境中的释放动力学。在100转/分钟搅拌条件下,90%的活性物质在酸性环境中75分钟内释放。

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