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Formulation Optimization of Hydrodynamically Balanced Oral Controlled Release Bioadhesive Tablets of Tramadol Hydrochloride

机译:盐酸曲马多水动力平衡口服控释生物粘附片的处方优化

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摘要

The directly compressible floating-bioadhesive tablets of tramadol were formulated using varying amounts Carbopol 971P (CP) and hydroxy-propylmethyl cellulose (HPMC), along with other requisite excipients. In vitro drug release profile, floatational characteristics and ex vivo bioadhesive strength using texture analyzer were determined, and systematically optimized using a 32 central composite design (CCD). The studies indicated successful formulation of gastroretentive compressed matrices with excellent controlled release, mucoadhesion and hydrodynamic balance. Comparison of the dissolution profiles of the optimized formulation, with optimal composition of CP:HPMC :: 80.0:125.0, with that of the marketed controlled release formulation other indicated analogy of drug release performance with each other. Validation of optimization study using eight confirmatory experimental runs indicated very high degree of prognostic ability of CCD with mean ± SEM of −0.06% ± 0.37. Further, the study successfully unravels the effect of the polymers on the selected response variables.
机译:使用不同量的Carbopol 971P(CP)和羟丙基甲基纤维素(HPMC)以及其他必要的赋形剂配制了曲马多可直接压制的漂浮生物粘附片剂。使用质构分析仪确定体外药物释放曲线,漂浮特性和离体生物粘附强度,并使用32个中央复合设计(CCD)对其进行系统优化。研究表明成功配制了具有出色的控释,粘膜粘附和流体力学平衡的胃滞留性压缩基质。比较具有CP:HPMC :: 80.0:125.0的最佳组成的优化制剂的溶出曲线,与市售的控释制剂的溶出曲线进行比较,表明药物释放性能彼此相似。使用八项验证性实验运行对优化研究进行的验证表明,CCD的预后能力非常高,平均值±SEM为-0.06%±0.37。此外,该研究成功地揭示了聚合物对所选响应变量的影响。

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