Prabakaran D, Singh Paramjit, Jaganathan K S, Vyas Suresh P
Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Dr. Harisingh Gour University, Sagar MP, 470 003, India.
J Control Release. 2004 Mar 5;95(2):239-48. doi: 10.1016/j.jconrel.2003.11.013.
Sustained release asymmetric membrane capsular systems were developed for simultaneous oral delivery of rifampicin and isoniazid sodium in order to reduce the problems associated with the multi drug therapy of tuberculosis. Dense semipermeable membrane coating capsules were also prepared for the delivery of these drugs by adopting two different filling approaches. In vitro release studies were carried out for both types of systems and the results were compared. Asymmetric membrane capsules provided sustained release of rifampicin associated with initial burst release, where isoniazid release rates were comparatively high due to higher aqueous solubility. Dense semipermeable membrane systems provided controlled release of both drugs but were devoid of initial burst release of isoniazid. To overcome these drawbacks, a modified asymmetric system was developed by adding appropriate amount of hydrophilic polymer mixture with isoniazid. The system provided satisfactory sustained release of rifampicin and isoniazid with initial burst release may be sufficient to achieve minimum effective concentration in blood. In vitro dissolution kinetics of the systems followed first order kinetics and statistical analysis of release rate data proved that modified asymmetric system was better amongst the developed systems.
为了减少与结核病多药疗法相关的问题,开发了用于同时口服利福平和平肼屈嗪钠的缓释不对称膜胶囊系统。还通过采用两种不同的填充方法制备了用于递送这些药物的致密半透膜包衣胶囊。对这两种类型的系统进行了体外释放研究,并对结果进行了比较。不对称膜胶囊提供了与初始突释相关的利福平缓释,而异烟肼的释放速率由于较高的水溶性而相对较高。致密半透膜系统提供了两种药物的控释,但没有异烟肼的初始突释。为了克服这些缺点,通过向异烟肼中添加适量的亲水性聚合物混合物开发了一种改良的不对称系统。该系统提供了利福平和异烟肼令人满意的缓释,初始突释可能足以在血液中达到最低有效浓度。该系统的体外溶出动力学遵循一级动力学,释放速率数据的统计分析证明,改良的不对称系统在已开发的系统中更好。