Optimization of Formula and Preparation Process of Metronidazole Vaginal Thermosensitive in situ Gel by Orthogonal Tests / 中国药师

ABSTRACT

Objective: To optimize the formula and preparation process of metronidazole thermosensitive in situ gel.Methods: The temperature of gelation and 24-h cumulative release were used as the evaluation indices, and the orthogonal tests were carried out to investigate the amounts of poloxamer 407 (P407), poloxamer 188 (P188), sodium alginate and polyethylene glycol 4000 (PEG 4000) to screen the best formula of thermosensitive in situ gel.The in vitro release of metronidazole thermosensitive in situ gel was determined by HPLC and compared with that of commercially available gel.Results: The optimum formula of thermosensitive in situ gel was P407 of 20%, P188 of 18%, sodium alginate of 0.1% and PEG 4000 of 1.5%.The release rate of metronidazole thermosensitive in situ gel was high, and the temperature of gelation was suitable.Compared with that of the commercially available gel, the vaginal retention of the in situ gel was significantly improved.Conclusion: The formula of the in situ gel is reasonable and the preparation process is feasible.