Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, India.
Drug Dev Ind Pharm. 2012 Jun;38(6):706-17. doi: 10.3109/03639045.2011.623167. Epub 2011 Oct 19.
To obtain controlled release of captopril in the stomach, coated, mucoadhesive donut-shaped tablets were designed.
Donut-shaped tablet were made of different ratios of diluents to polymer or combination of polymers by direct compression method. Top and bottom portions of the tablet were coated with water-insoluble polymer followed by mucoadhesive coating. Time of water penetration, measurement of tensile strength, mucoadhesion studies (static ex vivo and ex vivo wash-off) were taken into account for characterization of respective films. In vitro study has been performed at different dissolution mediums. Optimized batches were also prepared by wet granulation. Stability studies of optimized batches have been performed.
The results of time of water penetration and tensile strength indicated positive response against water impermeation. Mucoadhesive studies showed that film thickness of 0.12 mm was good for retention of tablet at stomach. At pH 1.2, optimized batch of tablet made with hydroxypropyl methyl cellulose (HPMC) E15 as binder showed 80% w/w drug release within 4–5 h with maximum average release of 97.49% w/w. Similarly, maximum average releases of 96.36% w/w and 95.47% w/w were obtained with nearly same dissolution patterns using combination of HPMC E5 and HPMC E50 and sodium salt of carboxy methyl cellulose (NaCMC) 500–600 cPs instead of HPMC E15. The release profiles in the distilled water and pH 4.5 followed the above pattern except deviation at pH 6.8. Stability studies were not positive for all combinations.
Coated, mucoadhesive donut-shaped tablet is good for controlled release of drug in the stomach.
为了在胃部实现卡托普利的控制释放，设计了包衣、粘膜粘附的甜甜圈形片剂。
通过直接压缩法，用不同比例的稀释剂与聚合物或聚合物组合制成甜甜圈形片剂。片剂的顶部和底部用不溶于水的聚合物包衣，然后用粘膜粘附涂层进行包衣。考虑到各自薄膜的特性，对水穿透时间、拉伸强度测量、粘膜粘附研究（静态离体和离体冲洗）进行了测量。在不同的溶解介质中进行了体外研究。还通过湿法制粒制备了优化的批次。对优化的批次进行了稳定性研究。
水穿透时间和拉伸强度的结果表明对水渗透有积极的响应。粘膜粘附研究表明，厚度为 0.12mm 的薄膜有利于片剂在胃中的保留。在 pH 1.2 下，用羟丙基甲基纤维素（HPMC）E15 作为粘合剂制成的优化片剂在 4-5 小时内释放 80%w/w 的药物，最大平均释放量为 97.49%w/w。同样，使用 HPMC E5 和 HPMC E50 的组合以及羧甲基纤维素钠（NaCMC）500-600 cPs 代替 HPMC E15 时，也获得了几乎相同的溶解模式，最大平均释放量分别为 96.36%w/w 和 95.47%w/w。在蒸馏水和 pH 4.5 中的释放曲线遵循上述模式，除了在 pH 6.8 时存在偏差。所有组合的稳定性研究都不是阳性的。
包衣、粘膜粘附的甜甜圈形片剂有利于药物在胃部的控制释放。
