Tinidazole expandable vaginal suppository, and preparation method and detection method thereof

Abstract

The invention relates to a tinidazole expandable vaginal suppository, and a preparation method and a detection method thereof. The expandable vaginal suppository comprises tinidazole, a matrix and an expansion carrier. After micronization treatment, tinidazole gains increased dissolution rate, so as to increase bioavailability of the suppository. A resin compound formed by the resin with micronized tinidazole can improve stability of the suppository, and a technology of medicament long-acting layered release is employed to prolong effect time of tinidazole on the vagina, extend therapeutic effect and maintain the specific acid environment and self-cleaning function of the vagina; and the pregelatinized starch can promote the mixing of each component in the suppository and improve the stability of the suppository. The tinidazole expandable vaginal suppository employs seven unique advanced technologies and has beneficial effects of prevention of outflow liquid, high stability, lasting curative effect and prevention of secondary infection.

Description

Technical field [0001] The invention belongs to the field of vaginal suppositories, and particularly relates to a tinidazole vaginal expansion suppository and a preparation method and a detection method thereof. Background technique [0002] Tinidazole, whose chemical name is 2-methyl-1-[2-(ethylsulfonyl)ethyl]-5-nitro-1H imidazole, has the following structural formula: [0003] [0004] Tinidazole is a white to light yellow crystal or crystalline powder, which is soluble in acetone or chloroform, and slightly soluble in water or ethanol. [0005] Tinidazole is a new generation of anti-anaerobic and antiprotozoal drugs after metronidazole. It has higher efficacy and better tolerance than metronidazole. It is mainly used for anaerobic vaginitis and trichomonal vaginitis. The commonly used dosage forms are mainly tablets, injections and suppositories, but tablets and injections often cause adverse reactions in the digestive system; therefore, tinidazole suppositories are more widely u...

AI Technical Summary

Problems solved by technology

Commonly used dosage forms are mainly tablets, injections and suppositories, but tablets and injections often cause adverse reactions in the digestive system; therefore, tinidazole suppositories are more widely used; Technology Research [J], Modern Medicine and Health, 2005,21 (23): 3335-3336) discloses an effervescent suppository made of tinidazole, mixed fatty acid glycerides, citric acid and sodium hydroxide; Chongde (Yang Chongde. Tinidazole Suppository Preparation and Content Determination [J], China Pharmaceutical Industry, 1999, 8(9): 29-30) discloses a preparation of tinidazole, gelatin, glycerin and water suppositories; in the suppository prescriptions disclosed by Shi Lei and Yang Chongde, the water solubility of tinidazole is poor, resulting in low bioavailability of tinidazole, thereby affecting its antibacterial efficacy; in order to solve the above technical problems, Wen Shaorong et al. Shao Rong, Wen Xiangxiong. Development and Quality Control of Tinidazole Suppository [J], China Pharmaceutical Industry, 1999, 8(1): 37) discloses the composition of tinidazole, lactic acid, polysorbate 80, semi-synthetic fatty acid The suppository made of glyceride, the suppository has added absorption accelerator polysorbate 80, has increased vagina to the absorption promotion effect of tinidazole, but the effect achieved is still unsatisfactory; CN1278429 discloses a kind of β-ring A controlled-release suppository composed of dextrin and tinidazole, β-cyclodextrin increases the solubility of tinidazole, but the stability of the controlled-release suppository is not good; in the prior art, in order to change the poor dissolution rate of active ingredients The problem is that absorption enhancers are often added, but the addition of absorption enhancers will affect the properties of the matrix; moreover, ordinary tinidazole suppositories are not easy to clean, and are easy to contaminate clothes; the active ingredient has a small contact surface with the human body, resulting in insufficient absorption and lack of performance. Technical issues such as the optimal curative effect of the prescription

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