Agarwal Shweta, Murthy R S R
Department of Pharmaceutical Sciences, Faculty of Technology and Engineering, Kalabhavan, M. S. University of Baroda, Vadodara-390 001, India.
Indian J Pharm Sci. 2015 Nov-Dec;77(6):705-14. doi: 10.4103/0250-474x.174993.
Mucoadhesive tablets have emerged as potential candidates for gastroretentive drug delivery providing controlled release along with prolonged gastric residence time. Gastroretentive mucoadhesive tablets could result in increased bioavailability due to prolonged gastric residence time. A hydrophilic matrix system was developed as mucoadhesion is achievable on appropriate wetting and swelling of the polymers used. The polymers were so chosen so as to provide a balance between swelling, mucoadhesion and drug release. The polymers chosen were hydroxypropyl methylcellulose K4M, chitosan, and Carbopol 934. The concentrations of these polymers used has a great impact on the physicochemical properties of the resulting formulation. The tablets were formulated using wet granulation method and tranexamic acid was used as the model drug. The prepared tablets were characterized for size, shape, appearance, hardness, friability, weight variation, swelling, mucoadhesion and in vitro drug release. Several batches of tablets were prepared by varying the ratio of hydroxypropyl methylcellulose K4M and Chitosan. The batches having a greater ratio of chitosan showed higher rate of swelling, greater erosion, less mucoadhesion and faster release rate of the drug whereas the batches having greater ratio of hydroxypropyl methylcellulose K4M showed lesser rate of swelling, less erosion, better mucoadhesion and a smaller drug release rate. The level of carbopol was kept constant in all the batches.
粘膜粘附片已成为胃滞留药物递送的潜在候选者,可实现控释并延长胃内停留时间。由于胃内停留时间延长,胃滞留粘膜粘附片可提高生物利用度。开发了一种亲水性基质系统,因为在所用聚合物适当的润湿和溶胀时可实现粘膜粘附。选择聚合物是为了在溶胀、粘膜粘附和药物释放之间取得平衡。选择的聚合物为羟丙基甲基纤维素K4M、壳聚糖和卡波姆934。这些聚合物的使用浓度对所得制剂的物理化学性质有很大影响。片剂采用湿法制粒法制备,氨甲环酸用作模型药物。对制备的片剂进行尺寸、形状、外观、硬度、脆碎度、重量差异、溶胀、粘膜粘附和体外药物释放等方面的表征。通过改变羟丙基甲基纤维素K4M和壳聚糖的比例制备了几批片剂。壳聚糖比例较高的批次显示出较高的溶胀率、较大的侵蚀、较低的粘膜粘附和较快的药物释放速率,而羟丙基甲基纤维素K4M比例较高的批次显示出较低的溶胀率、较少的侵蚀、较好的粘膜粘附和较小的药物释放速率。所有批次中卡波姆的含量保持恒定。