El-Kamel Amal, Sokar Magda, Naggar Viviane, Al Gamal Safaa
Department of Pharmaceutics, Faculty of Pharmacy, King Saud University, Kingdom of Saudi Arabia.
AAPS PharmSci. 2002;4(4):E44. doi: 10.1208/ps040444.
Metronidazole was formulated in mucoadhesive vaginal tablets by directly compressing the natural cationic polymer chitosan, loosely cross-linked with glutaraldehyde, together with sodium alginate with or without microcrystalline cellulose (MCC). Sodium carboxymethylcellulose (CMC) was added to some of the formulations. The drug content in tablets was 20%. Drug dissolution rate studies from tablets were carried out in buffer pH 4.8 and distilled water. Swelling indices and adhesion forces were also measured for all formulations. The formula (FIII) containing 6% chitosan, 24% sodium alginate, 30% sodium CMC, and 20% MCC showed adequate release properties in both media and gave lower values of swelling index compared with the other examined formulations. FIII also proved to have good adhesion properties with minimum applied weights. Moreover, its release properties (% dissolution efficiency, DE) in buffer pH 4.8, as well as release mechanism (n values), were negligibly affected by aging. Thus, this formula may be considered a good candidate for vaginal mucoadhesive dosage forms.
甲硝唑通过直接压制天然阳离子聚合物壳聚糖制成黏膜黏附阴道片,壳聚糖与戊二醛轻度交联,并与海藻酸钠一起加入或不加入微晶纤维素(MCC)。部分制剂中添加了羧甲基纤维素钠(CMC)。片剂中的药物含量为20%。在pH 4.8的缓冲液和蒸馏水中进行了片剂的药物溶出速率研究。还测量了所有制剂的溶胀指数和黏附力。含有6%壳聚糖、24%海藻酸钠、30% CMC和20% MCC的配方(FIII)在两种介质中均显示出足够的释放特性,与其他受试配方相比,溶胀指数值较低。FIII还被证明在最小施加重量下具有良好的黏附性能。此外,其在pH 4.8缓冲液中的释放特性(%溶出效率,DE)以及释放机制(n值)受老化的影响可忽略不计。因此,该配方可被视为阴道黏膜黏附剂型的良好候选配方。