a Department of Pharmaceutics, Faculty of Pharmacy, Deraya University , Minia , Egypt.
b Department of Pharmaceutics, Faculty of Pharmacy, Minia University , Minia , Egypt.
Drug Dev Ind Pharm. 2019 Feb;45(2):244-251. doi: 10.1080/03639045.2018.1529787. Epub 2018 Oct 18.
Attempting to prepare a convenient bioavailable formulation of vitamin B (cyanocobalamin), 17 tablet formulations were prepared by direct compression. Different concentrations of hydroxypropyl methyl cellulose (HPMC), carbopol 971p (CP971p), and chitosan (Cs) were used. The tablets were characterized for thickness, weight, drug content, hardness, friability, surface pH, in vitro drug release, and mucoadhesion. Kinetic analysis of the release data was conducted. Vitamin B bioavailability from the optimized formulations was studied on rabbits by the aid of enzyme-linked immunosorbent assay. Neurotone I.M. injection was used for comparison. HPMC (F1-F4), CP971p (F5-F8), and HPMC/CP971p (F12-F15)-based formulations showed acceptable mechanical properties. The formulated tablets showed maximum swelling indices of 232 ± 0.13. The surface pH values ranged from 5.3 ± 0.03 to 6.6 ± 0.02. Bioadhesive force ranged from 66 ± 0.6 to 150 ± 0.5 mN. Results showed that CP971p-based tablets had superior in vitro drug release, mechanical, and mucoadhesive properties. In vitro release date of selected formulations were fitted well to Peppas model. HPMC/CP971p-based formulations showed bioavailability up to 2.7-folds that of Neurotone I.M. injection.
为了制备方便生物利用的维生素 B(氰钴胺)制剂,通过直接压缩法制备了 17 种片剂制剂。使用了不同浓度的羟丙基甲基纤维素(HPMC)、卡波姆 971p(CP971p)和壳聚糖(Cs)。对片剂的厚度、重量、药物含量、硬度、脆碎度、表面 pH 值、体外药物释放和粘膜粘附进行了表征。对释放数据进行了动力学分析。通过酶联免疫吸附试验(ELISA)在兔子身上研究了优化制剂的维生素 B 生物利用度。使用 Neurotone I.M. 注射液进行比较。基于 HPMC(F1-F4)、CP971p(F5-F8)和 HPMC/CP971p(F12-F15)的制剂具有可接受的机械性能。所制备的片剂显示出最大的溶胀指数为 232±0.13。表面 pH 值范围为 5.3±0.03 至 6.6±0.02。生物粘附力范围为 66±0.6 至 150±0.5 mN。结果表明,CP971p 为基础的片剂具有优越的体外药物释放、机械和粘膜粘附性能。所选制剂的体外释放数据拟合良好 Peppas 模型。基于 HPMC/CP971p 的制剂的生物利用度高达神经酮 I.M. 注射液的 2.7 倍。