Phaechamud T, Mueannoom W, Tuntarawongsa S, Chitrattha S
Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon, Pathom-73000, Thailand.
Indian J Pharm Sci. 2010 Mar;72(2):173-83. doi: 10.4103/0250-474X.65026.
The aim of this research was to investigate the technique for preparation of coated valproic acid and sodium valproate sustained-release matrix tablets. Different diluents were tested and selected as the effective absorbent for oily valproic acid. Effect of the amount of absorbent and hydroxypropylmethylcellulose on drug release from valproic acid-sodium valproate matrix tablets prepared with wet granulation technique was evaluated in pH change system. Colloidal silicon dioxide effectively adsorbed liquid valproic acid during wet granulation and granule preparation. The amounts of colloidal silicon dioxide and hydroxypropylmethylcellulose employed in tablet formulations affected drug release from the tablets. The drug release was prominently sustained for over 12 h using hydroxypropylmethylcellulose-based hydrophilic matrix system. The mechanism of drug release through the matrix polymer was a diffusion control. The drug release profile of the developed matrix tablet was similar to Depakine Chrono(®), providing the values of similarity factor (f2) and difference factor (f1) of 85.56 and 2.37, respectively. Eudragit(®) L 30 D-55 was used as effective subcoating material for core matrix tablets before over coating with hydroxypropylmethylcellulose film with organic base solvent. Drug release profile of coated matrix tablet was almost similar to that of Depakine Chrono(®).
本研究的目的是探究丙戊酸和丙戊酸钠缓释骨架片的包衣制备技术。测试了不同的稀释剂,并选择其作为油性丙戊酸的有效吸收剂。在pH变化体系中,评估了吸收剂和羟丙基甲基纤维素的用量对采用湿法制粒技术制备的丙戊酸 - 丙戊酸钠骨架片药物释放的影响。在湿法制粒和颗粒制备过程中,胶体二氧化硅有效地吸附了液态丙戊酸。片剂配方中使用的胶体二氧化硅和羟丙基甲基纤维素的量影响了片剂的药物释放。使用基于羟丙基甲基纤维素的亲水性骨架系统,药物释放显著持续超过12小时。药物通过骨架聚合物的释放机制为扩散控制。所研制的骨架片的药物释放曲线与德巴金缓释片(Depakine Chrono(®))相似,相似因子(f2)和差异因子(f1)的值分别为85.56和2.37。在使用有机碱溶剂的羟丙基甲基纤维素薄膜进行包衣之前,优特奇(Eudragit(®))L 30 D - 55被用作核心骨架片的有效底包衣材料。包衣骨架片的药物释放曲线与德巴金缓释片(Depakine Chrono(®))几乎相似。