Alam Mohd Aftab, Ahmad Farhan Jalees, Khan Zeenat Iqbal, Khar Roop Krishen, Ali Mushir
Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, New Delhi-110062, India.
AAPS PharmSciTech. 2007 Dec 14;8(4):E109. doi: 10.1208/pt0804109.
An acid-buffering bioadhesive vaginal tablet was developed for the treatment of genitourinary tract infections. From the bioadhesion experiment and release studies it was found that polycarbophil and sodium carboxymethylcellulose is a good combination for an acid-buffering bioadhesive vaginal tablet. Sodium monocitrate was used as a buffering agent to provide acidic pH (4.4), which is an attribute of a healthy vagina. The effervescent mixture (citric acid and sodium bicarbonate) along with a superdisintegrant (Ac-Di-sol) was used to enhance the swellability of the bioadhesive tablet. The drugs clotrimazole (antifungal) and metronidazole (antiprotozoal as well as an antibacterial) were used in the formulation along with Lactobacillus acidophilus spores to treat mixed vaginal infections. From the ex vivo retention study it was found that the bioadhesive polymers hold the tablet for more than 24 hours inside the vaginal tube. The hardness of the acid-buffering bioadhesive vaginal tablet was optimized, at 4 to 5 kg hardness the swelling was found to be good and the cumulative release profile of the developed tablet was matched with a marketed conventional tablet (Infa-V). The in vitro spreadability of the swelled tablet was comparable to the marketed gel. In the in vitro antimicrobial study it was found that the acid-buffering bioadhesive tablet produces better antimicrobial action than marketed intravaginal drug delivery systems (Infa-V, Candid-V and Canesten 1).
开发了一种用于治疗泌尿生殖道感染的酸缓冲生物粘附阴道片。通过生物粘附实验和释放研究发现，聚卡波非和羧甲基纤维素钠是制备酸缓冲生物粘附阴道片的良好组合。使用柠檬酸一钠作为缓冲剂以提供酸性pH值（4.4），这是健康阴道的一个特征。泡腾混合物（柠檬酸和碳酸氢钠）与超级崩解剂（交联羧甲基纤维素钠）一起用于增强生物粘附片的溶胀性。制剂中使用了克霉唑（抗真菌药）和甲硝唑（抗原虫药以及抗菌药）以及嗜酸乳杆菌孢子来治疗混合性阴道感染。通过体外滞留研究发现，生物粘附聚合物可使该片剂在阴道管内保持超过24小时。对酸缓冲生物粘附阴道片的硬度进行了优化，发现硬度为4至5千克时溶胀效果良好，且所开发片剂的累积释放曲线与市售常规片剂（Infa-V）相匹配。溶胀片的体外铺展性与市售凝胶相当。在体外抗菌研究中发现，酸缓冲生物粘附片比市售阴道给药系统（Infa-V、Candid-V和凯妮汀1）具有更好的抗菌作用。
