Development Of Novel Vaginal Sustained-release Progesterone Gel

The purpose of research is to study and determine the composition, preparation procedure, quality control of sustained-release progesterone gel and toxicity, mucous membrane irritation; to investigate the stability of the gel, and to found the base for further clinical research.On the base of the formula and adjuvant's property of correlative product in abroad, the formula of sustained-release progesterone gel was determined. Using dynamic viscosity and in vitro release as index, the composition and preparation procedure of progesterone gel were optimized. Using Chinese Pharmacopeia as reference, the method to examine related substance and content of sustained-release progesterone gel was determined, and quality Criteria was established. According to Chinese Pharmacopeia, influential factor test, accelerating test and long-term test were studied. Sustained-release progesterone gel was administrated multiple to rabbit per vagina, observating whether death or side effect was caused, the maximum dosage was calculated and the toxicity was ascertained. Using substrate and sodium chloride as control, adverse effect and recovery of the sustained-release progesterone gel after administrated to rabbit were observated, and the mucous membrane irritation are ascertained.The formula of the vaginal sustained-release progesterone gel was determined. The composition and preparation procedure of gel are optimized, and there are no differences of release between sample and control. The quality criteria of sustained-release progesterone gel was established. The test of toxicity manifested that the preparation didn't cause acute toxicity and systemic toxicity. The experiment of irritation of rabbit's vagina indicated the preparation didn't cause acute pathological change.The optimized composition was reasonable and the preparation procedure was convenient and reliable. It can be industrialized. The quality criteria was simple, accurate and feasible. The preparation is stable, non-toxic, non-irritate, safe and reliable. The clinical trial should be further researched.