The System Research Of Tinidazole Vaginal Delivery

Tinidazole was a new generation of nitroimidazole derivatives. It was a kind of anaerobic bacteria drugs. Tinidazole was the most commonly used drugs for clinical treatment of trichomonas vaginitis and bacterial vaginosis. Common formulations were injection, tablets, capsules and the like. However, water-soluble of tinidazole was poor and systemic administration made oral drug absorption and poor bioavailability. The common form of tinidazole suppository had many problems: prone to stimulus sensitization, uneven release. In this paper, the tinidazole vaginal administration of was systematically researched. Compare the study of tinidazole long-acting sustained-release suppository, vaginal gels, vaginal sustained-release tablets to get less irritating and release dosage form more uniform.The tinidazole preformulation study was firstly investigated in this paper. The formulation and technology of vaginal sustained-release suppository, gels and tablets were researched. Three dosage forms of quality evaluation system and three of the sustained-release preparation of quality control were established for the dissolution method. Three kinds of self-designed sustained-release preparation were carried out in vitro release test and made a preliminary study of the stability of three kinds of sustained-release suppository.A comparative study on the release rate and release mechanism of three formulations was investigated in this paper. The dissolution curve, drug release mechanism and release effect of the three were studied. The results of the research showed that:the suppository and gels accorded with Higuchi equation, which a dual mechanism of diffusion and swelling, and two of these were in the main diffusion mechanism. The tablets were in accordance with the zero order drug release model, which was the double mechanism of diffusion and skeleton dissolution, and the skeleton corrosion is the main mechanism. There were more uniform release characteristics of zero level release. The result of drug release effect comparison study showed that the slow release effect of the tablet was better than the other two, and the sustained-release tablets released more evenly.By stimulating test and allergy test, the effects of the safety of tinidazole long-acting sustained-release suppository, vaginal gels, vaginal sustained-release tablets were studied. Animal test results showed that three dosage forms had not stimulus sensitization, safe and reliable.