Metronidazole-clotrimazole-chlorhexidine acetate vaginal expansive suppository controlled-release preparation and preparation method thereof

A technology for vaginal expansion suppositories and controlled-release preparations, which is applied in the directions of suppository delivery, topical antibacterial agents, and medical preparations of inactive ingredients, etc., can solve the problem of failure to achieve zero-order release, low bioavailability, and poor solubility of active ingredients, etc. problems, to achieve the effect of preventing the outflow of liquid medicine, preventing secondary infection, and reducing irritation

Active Publication Date: 2014-04-23
哈尔滨田美药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Shuangzotai suppository has always had various technical problems, and most of them have been solved; for example, the applicant of the present application, Harbin Oouti Pharmaceutical Co., Ltd., disclosed a Shuangzotai vaginal expansion suppository and its preparation method in Chinese patent CN103284996 , the expansion plug contains an expansion carrier, and the expansion plug is an inner and outer double-layer expansion plug, the inner layer is a slow-release layer, and the outer layer is an immediate-release layer; this application realizes the slow release of active ingredients by adding an absorption retardant Effect; the applicant has obtained through further tests that the release of the expansion suppository disclosed in this patent application is not stable, does not achieve zero-order release, and the release rate of the drug is uncontrollable; and the solubility of the active ingredients in the expansion plug is not good, Its bioavailability is low, which affects the efficacy of the expansion plug; and the expansion plug should not be stored for a long time

Method used

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  • Metronidazole-clotrimazole-chlorhexidine acetate vaginal expansive suppository controlled-release preparation and preparation method thereof
  • Metronidazole-clotrimazole-chlorhexidine acetate vaginal expansive suppository controlled-release preparation and preparation method thereof
  • Metronidazole-clotrimazole-chlorhexidine acetate vaginal expansive suppository controlled-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058]

[0059] Preparation:

[0060] 1) Preparation of the plug core coated on the surface of the expanded carrier:

[0061] a. Polyoxyethylene monostearate, Tween 60 and hydrogenated rosin oil are placed in a water bath for heating and melting to obtain a melt;

[0062] B. take metronidazole, clotrimazole and chlorhexidine acetate of recipe quantity, pulverize, add in the melt that step a makes, mix homogeneously, make mixture;

[0063] c. Pour the mixture prepared in step b into the plug mold, insert the sliver, cool and shape it, and make a plug core coated on the surface of the expanded carrier;

[0064] 2) Preparation of expansion suppository controlled-release preparation:

[0065] d. Dissolve alginic acid and polypropylene dextran in ethanol, and add diacetyl monoglyceride under stirring to prepare a homogeneous ethanol solution;

[0066] e. Place the plug core prepared in step c and coated on the surface of the expanded carrier in a coating pan, spray the coati...

Embodiment 2

[0069]

[0070] Preparation method: According to the method of Example 1, 100 spherical expansion suppository controlled-release preparations were prepared, each weighing about 1.3g, and the coating weight increased by 2%.

Embodiment 3

[0072]

[0073] Preparation:

[0074] 1) Preparation of the plug core coated on the surface of the expanded carrier:

[0075] a. Polyethylene glycol 4000 and hydrogenated castor oil are placed in a water bath for heating and melting to obtain a melt;

[0076] B. take metronidazole, clotrimazole and chlorhexidine acetate of recipe quantity, pulverize, mix with propylene glycol monopalmitic acid diester, make mixture;

[0077] c. adding the mixture prepared in step b to the melt obtained in step a, and mixing evenly to obtain a mixture;

[0078] d. Pour the mixture prepared in step c into a plug mold, insert a sliver, cool and shape, and make a plug core coated on the surface of the expanded carrier;

[0079] 2) Preparation of expansion suppository controlled-release preparation:

[0080] e. Dissolving alginic acid and polyvinyl butyral in ethanol, adding dipropyl sebacate under stirring to make ethanol homogeneous solution;

[0081] f. Place the plug core prepared in st...

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Abstract

The invention relates to a metronidazole-clotrimazole-chlorhexidine acetate vaginal expansive suppository controlled-release preparation and a preparation method thereof. The metronidazole-clotrimazole-chlorhexidine acetate vaginal expansive suppository controlled-release preparation comprises a suppository core and a controlled-release coating at the outer layer of the suppository core, wherein the controlled-release coating consists of a special coating material and a plasticizer, so that the expansive suppository controlled-release preparation has a zero-order stable release effect; moreover, by using the controlled-release coating, the expansive suppository controlled-release preparation can be stabilized, and the irritation of the controlled-release preparation on the vagina can be lowered; furthermore, by adopting seven types of unique leading technologies, the metronidazole-clotrimazole-chlorhexidine acetate vaginal expansive suppository controlled-release preparation has the beneficial effects of preventing a liquid medicament from flowing outwards, preventing secondary infection, and the like.

Description

technical field [0001] The invention belongs to the field of vaginal suppositories, in particular to a controlled-release preparation of Shuangzotai vaginal expansive suppository and a preparation method thereof. Background technique [0002] Shuangzotai suppository, included in the 2010 edition of Chinese Pharmacopoeia, is made of 200g of metronidazole, 160g of clotrimazole, 8g of chlorhexidine acetate, appropriate amount of lanolin, appropriate amount of paraffin and appropriate amount of semi-synthetic fatty acid glyceride; The curative effect of the suppository has been clinically proven for many years, and it is widely used in bacterial vaginosis, candida vulvovaginosis, trichomonal vaginitis and other mixed infectious vaginitis. However, Shuangzotai suppository has always had various technical problems, and most of them have been solved; for example, the applicant of the present application, Harbin Oouti Pharmaceutical Co., Ltd., disclosed a Shuangzotai vaginal expansi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4174A61K9/02A61K47/36A61K47/14A61K47/12A61P31/02A61P15/02A61P33/02A61K31/4164A61K31/155
Inventor 邱学良邱明世
Owner 哈尔滨田美药业股份有限公司
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