Dimenhydrinate is a therapeutic agent used for the treatment of nausea and vomiting. A conventional dose of dimenhydrinate is 50 mg per 8 h. Once-daily controlled release tablets of dimenhydrinate were formulated intended to treat emesis. The tablets were formulated using hydrophilic polymers Methocel® and hydrophobic polymers Ethocel® and subsequently analyzed for pre-compression and post-compression characteristics, % moisture uptake, dissolution profiles and release behavior of the drug. Identification of active ingredient and compatibility of blends were analyzed through FT-IR. Drug release kinetics of dimenhydrinate was assessed at pH 1.2, 4.5 and 6.8. The results of release profiles were evaluated for different kinetic models including model dependent and model independent. The optimized formulation K100M 30% showed ideal pre-compression properties and in vitro characteristics. Tablets exhibited a controlled drug release pattern due to the formation of a viscous gel layer followed by erosion. Furthermore, zero-order best described the release pattern with the value of r2 ˃ 0.99. Once-daily tablets released 98–100% drug in 24 h. Significantly more concentration and higher viscosity grade of hydrophilic polymer ensured the required pattern of drug release.

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不同粘度等级的 Methocel 和 Ethocel 聚合物对开发控释茶苯海明骨架片的影响

茶苯海明是一种用于治疗恶心和呕吐的治疗剂。茶苯海明的常规剂量为每 8 小时 50 毫克。每天一次的茶苯海明控释片剂旨在治疗呕吐。片剂使用亲水性聚合物 Methocel® 和疏水性聚合物 Ethocel® 配制，随后分析了压片前和压片后的特性、吸湿百分比、溶出曲线和药物的释放行为。通过 FT-IR 分析活性成分的鉴定和混合物的相容性。在 pH 1.2、4.5 和 6.8 下评估茶苯海明的药物释放动力学。针对不同的动力学模型评估释放曲线的结果，包括模型依赖和模型独立。优化的配方 K100M 30% 显示出理想的预压缩特性和体外特性。由于形成粘性凝胶层，随后被侵蚀，片剂表现出受控的药物释放模式。此外，零阶最好地描述了释放模式，r2 ˃ 0.99 的值。每日一次的片剂在 24 小时内释放 98-100% 的药物。显着更高浓度和更高粘度等级的亲水聚合物确保了所需的药物释放模式。