Mangla Bhumika, Jain Anurekha, Malik Deepinder Singh
Faculty of Pharmaceutical Science, Jayoti Vidyapeeth Women University, Jaipur,. India.
Chitkara College of Pharmacy, Chitkara University, Punjab,. India.
Recent Pat Antiinfect Drug Discov. 2020 Nov 11. doi: 10.2174/1574891X15999201111200523.
To formulate and preliminary evaluated polysaccharide based mucoadhesive floating tablets of Cinnarizine.
Gastro-retentive drug delivery systems has proved to be a successful approach to enhance the gastric residence with site specific targeting for achieving local or generalized effect. Various patents has also been filed globally employing gastro-retentive approach.
The study is designed to explore the mucoadhesive and low density characteristics of corn fibre gum (CFG) for preparation of gastro-retentive floating tablets of cinnarizine.
Floating tablets were prepared by direct compression technique using different concentrations of CFG (45, 50, 60% w/w). The formulated floating tablet batches were evaluated for their hardness, friability, drug content, floating duration/ lag time, swelling behavior, bioadhesive strength and in vitro drug release.
Mucoadhesive strength was found to increase with an increment in the polysaccharide concentration. Swelling index was found to increase both with the increase in CFG concentration and with duration for which tablet remains in medium. The in vitro drug release studies indicated decrease in drug release (91% to 77%) with the increase in polymer concentration. The release data was further fitted to various kinetic models which revealed the drug release to be in accordance with Zero-order and Higuchi models, indicating polymer to exhibit the swellable matrix forming abilities. The value of n (between 0.458 and 0.997) from Korsemeyer Peppas model depicted the possibility of drug to follow more than one mechanism of release from the formulation i.e. diffusion and erosion. Stability studies revealed the preparations to retain their integrity and pharmaceutical characteristics at variable storage conditions.
Thus from the research findings, CFG could be concluded to possess potential binder, release retardant and mucoadhesive characteristics which could be successfully employed for the formulation of gastro-retentive floating tablets.
制备并初步评价桂利嗪多糖基黏膜黏附性胃内漂浮片。
胃滞留型给药系统已被证明是一种成功的方法，可延长药物在胃内的停留时间，并实现局部或全身作用的靶向给药。全球也已提交了多项采用胃滞留方法的专利。
本研究旨在探索玉米纤维胶（CFG）的黏膜黏附性和低密度特性，以制备桂利嗪胃内漂浮片。
采用直接压片技术，使用不同浓度的CFG（45%、50%、60% w/w）制备漂浮片。对制备的漂浮片批次进行硬度、脆碎度、药物含量、漂浮持续时间/滞后时间、溶胀行为、生物黏附强度和体外药物释放评价。
发现黏膜黏附强度随多糖浓度的增加而增加。溶胀指数随CFG浓度的增加以及片剂在介质中停留时间的延长而增加。体外药物释放研究表明，随着聚合物浓度的增加，药物释放减少（从91%降至77%）。释放数据进一步拟合各种动力学模型，结果表明药物释放符合零级和Higuchi模型，表明聚合物具有形成可溶胀基质的能力。Korsemeyer Peppas模型中的n值（介于0.458和0.997之间）表明药物从制剂中释放可能遵循多种机制，即扩散和溶蚀。稳定性研究表明，制剂在不同储存条件下保持其完整性和药学特性。
因此，从研究结果可以得出结论，CFG具有潜在的黏合剂、释放阻滞剂和黏膜黏附特性，可成功用于制备胃内漂浮片。
