Ahmad Farhan Jalees, Alam Mohd Aftab, Khan Zeenat Iqbal, Khar Roop Krishen, Ali Mushir
Department of Pharmaceutics, Hamdard University, New Delhi-110062, India.
Acta Pharm. 2008 Dec;58(4):407-19. doi: 10.2478/v10007-008-0023-2.
An acid buffering bioadhesive vaginal (ABBV) gel was developed for the treatment of mixed vaginal infections. Different bioadhesive polymers were evaluated on the basis of their bioadhesive strength, stability and drug release properties. Bioadhesion and release studies showed that guar gum, xanthan gum and hydroxypropyl methylcelullose K4M formed a good combination of bioadhesive polymers to develop the ABBV gel. Monosodium citrate was used as an acid buffering agent to provide acidic pH (4.4). The drugs clotrimazole (antifungal) and metronidazole (antiprotozoal as well as antibacterial) were used in the formulation along with Lactobacillus spores to treat mixed vaginal infections. The ex vivo retention study showed that the bioadhesive polymers hold the gel for 12-13 hours inside the vaginal tube. Results of the in vitro antimicrobial study indicated that the ABBV gel had better antimicrobial action than the commercial intravaginal drug delivery systems and retention was prolonged in an ex vivo retention experiment.
一种用于治疗混合性阴道感染的酸性缓冲生物粘附性阴道（ABBV）凝胶被研发出来。基于不同生物粘附性聚合物的生物粘附强度、稳定性和药物释放特性对其进行了评估。生物粘附和释放研究表明，瓜尔胶、黄原胶和羟丙基甲基纤维素K4M形成了一种良好的生物粘附性聚合物组合，用于研发ABBV凝胶。柠檬酸钠用作酸性缓冲剂以提供酸性pH值（4.4）。配方中使用了克霉唑（抗真菌药）和甲硝唑（抗原虫药以及抗菌药）以及乳酸杆菌孢子来治疗混合性阴道感染。体外滞留研究表明，生物粘附性聚合物可使凝胶在阴道管内保持12至13小时。体外抗菌研究结果表明，ABBV凝胶比市售阴道给药系统具有更好的抗菌作用，并且在体外滞留实验中滞留时间延长。
