Miconazole nitrate vaginal expansion suppository and its preparation method and detection method

Abstract

The invention relates to a miconazole nitrate vaginal expansive suppository and a preparation method and a detection method thereof. The expansive suppository comprises a drug-containing matrix and an expansion carrier formed by miconazole nitrate and a matrix; miconazole nitrate and a specific solid dispersion carrier Make solid dispersion, can improve the stability of suppository, and the dissolution rate of active ingredient, improve the bioavailability of suppository; The film coating of described expansion suppository outer layer can play prolonging suppository to the action time of vagina, improves The role of suppository stability; and the miconazole nitrate vaginal expansion suppository provided by the present invention adopts seven original leading technologies, and has the beneficial effects of preventing liquid outflow, high stability, long-lasting curative effect, and preventing secondary infection.

Description

technical field [0001] The invention belongs to the field of vaginal suppositories, in particular to a miconazole nitrate vaginal expansive suppository and a preparation method and detection method thereof. Background technique [0002] Miconazole nitrate, chemical name 1-[2-(2,4-dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]-1H-imidazole nitrate , whose structure is as follows: [0003] [0004] Miconazole nitrate is a white or off-white crystal or crystalline powder, slightly soluble in methanol, slightly soluble in ethanol, insoluble in water or ether; miconazole nitrate is an antifungal drug that can interfere with cytochrome P- The activity of 450 inhibits the biosynthesis of ergosterol, the main sterol in the fungal cell membrane, damages the fungal cell membrane and changes its permeability, resulting in the leakage of intracellular substances; it can also inhibit the biosynthesis of triacylglycerol and phospholipids of fungi, inhibit The activity of oxida...

AI Technical Summary

Problems solved by technology

[0005] Miconazole nitrate is poorly absorbed orally, and after topical administration, it mainly stays in the lesion, and it absorbs less into the body; CN1346634 discloses a kind of miconazole nitrate ointment; CN101474188 discloses a kind of miconazole nitrate cream, and these two products mainly It is for external use on the skin, and special tools are required for vaginal administration, which is inconvenient to use and cannot well meet the needs of patients; therefore, miconazole nitrate suppositories are easily accepted by patients when administered vaginally, and have significant curative effects and are widely used

[0006] Zhang Fan et al. (Zhang Fan, Zhang Xianzhou, Lin Huizhen. Preparation and quality control of miconazole nitrate vaginal suppository [J], Modern Applied Pharmacy, 1991, 8(5): 23) disclosed a combination of miconazole nitrate vitamin AD, vitamin E, Vaginal suppositories made of lactic acid, 34 type mixed fatty acid glycerides, and 36 type mixed fatty acid glycerides, the solubility of miconazole nitrate in the suppository is poor, and the stability is low, which affects the curative effect of the suppository; Xing Shuli, etc. (Xing Shu Li, Sun Yingdong, Ding Changling, et al. Preparation and treatment control of miconazole nitrate hollow effervescent suppository[J], Chinese Hospital Pharmaceutical Impurities, 2012,32(1):62-63) disclosed that miconazole nitrate, lemon acid, sodium bicarbonate, semi-synthetic fatty acid glycerides and an appropriate amount of water to make the hollow effervescent suppository, the hollow effervescent suppository has increased the absorption area of ​​the medicine, but the amount of miconazole nitrate in the hollow effervescent suppository Poor solubility and poor dissolution rate lead to low bioavailability of the suppository; the moisture contained in the suppository will affect the stability of the suppository; in the prior art, in order to increase the stability and solubility of the active ingredient, the commonly used technical means are Add stabilizers and absorption accelerators, but the addition of excipients will affect the properties of the matrix, which is not conducive to the release of active ingredients, and is not conducive to the formation of suppositories; and ordinary miconazole nitrate suppositories are still difficult to clean and easily pollute clothes. ; The contact surface between the active ingredient and the human body is small, resulting in insufficient absorption, failure to exert the best curative effect of the formula and other technical problems

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