Dangi Amish Ashvinkumar, Zalodiya Prakash Bhikhabhai
Department of Pharmaceutics, Suresh Gyan Vihar University, Jaipur, Rajasthan, India.
Int J Pharm Investig. 2012 Oct;2(4):183-8. doi: 10.4103/2230-973X.106989.
The demand for melt-in-mouth tablets (MMTs) has been rapidly growing during the last decade, especially for the elderly and children who have swallowing difficulties, to avoid first-pass metabolism and quick drug entry into the systemic circulation.
In this work, a new approach has been tried to prepare MMTs using a hydrophilic waxy binder [polyethylene glycol (PEG)-6-stearate]. Carvedilol MMTs were prepared by direct compression method using different mucoadhesive polymers such as hydroxypropyl methylcellulose (HPMC), chitosan, and sodium carboxymethyl cellulose (Na-CMC) at various concentrations (range: 0.5-5%) to reduce the flushing action of saliva and to increase mucosal absorption. All the formulations were evaluated for various physiochemical parameters, and the formulations containing the maximum amount of polymer (F4, F7, and F10) were selected for further stability study.
The deaggregation time of the tablets was found to be rapid, and the dissolution test revealed that carvedilol was dissolved from the formulation within the compendia limits. This data confirmed that the polymer concentration (0.5-5%) was within acceptable limits. It was also concluded that avicel PH101, pearlitol SD 200, and croscarmellose sodium (CCS) were the appropriate excipients and formulated in the right proportion.
As a result, mouth dissolving administration of carvedilol formulated with appropriate excipients and especially with chitosan seems a promising alternative to traditional routes.
在过去十年中，口腔崩解片（MMT）的需求迅速增长，特别是对于有吞咽困难的老年人和儿童，以避免首过代谢并使药物快速进入体循环。
在这项工作中，尝试了一种新方法，即使用亲水性蜡质粘合剂[聚乙二醇（PEG）-6-硬脂酸酯]制备口腔崩解片。采用直接压片法，使用不同浓度（范围：0.5 - 5%）的不同粘膜粘附聚合物，如羟丙基甲基纤维素（HPMC）、壳聚糖和羧甲基纤维素钠（Na-CMC）制备卡维地洛口腔崩解片，以减少唾液的冲洗作用并增加粘膜吸收。对所有制剂进行各种理化参数评估，并选择含有最大聚合物量的制剂（F4、F7和F10）进行进一步的稳定性研究。
发现片剂的崩解时间很快，溶出度试验表明卡维地洛从制剂中溶出符合药典规定。该数据证实聚合物浓度（0.5 - 5%）在可接受范围内。还得出结论，微晶纤维素PH101、山梨醇SD 200和交联羧甲基纤维素钠（CCS）是合适的辅料，且配比正确。
因此，用合适辅料特别是壳聚糖配制的卡维地洛口腔崩解给药似乎是传统给药途径的一个有前景的替代方法。
