酮康唑生物黏附性阴道片的制备与体外评价

 目的制备酮康唑生物黏附性阴道片,并对其体外性质进行评价。方法在考察Carbopol934P,974P,HPMC K4M和HPC等生物黏附材料的黏附性质的基础上,用Carbopol934P分别配以HPMC和HPC作黏附剂,加入泡腾剂增加药物释放,设计5种酮康唑黏附片处方,比较不同处方之间的溶胀速率、黏附力、体外释放等指标。结果5种自制黏附片均有生物黏附及缓释效果,其体外释放符合Fick′s扩散机制。结论设计的酮康唑生物黏附性阴道片制备工艺简便,具有黏膜黏附和缓释特点,有望用于治疗妇女的阴道念珠菌感染。

Preparation and Evaluation of Bioadhesive Vaginal Tablets of Ketoconazole in Vitro

OBJECTIVE To prepare and evaluate a new bioadhesive vaginal tablets of ketoeonazole in vitro. METHODS The bioadhesive strength and swelling behaviour of Carbopol934P,974P, HPMC K4M and HPC were studied. Five formulations of bioadhesive vaginal tablets of ketoeonazole were prepared by the mixtures of Carbopol934P with HPMC K4M or HPC as bioadhesive materials. Effervescent agents were added into every formulation to enhance the dissolution of ketoconazole. The values of bioadhesive strength, swelling rate and dissolution were compared among the different formulations. RESULTS The vaginal tablets were bioadhesive and extended-release. In vitro dissolution of ketoconazole was fitted with Fick diffusion mechanism. CONCLUSION The preparation of bioadbesive vaginal tablet is simple and all the formulations had properties of bioadhesion and sustained-release. This study seems to be a step forwad in the ongoing research for the treatment of mycotic infections.