Coptidis total alkaloids vaginal suppository

A technology of total alkaloids and vaginal suppositories, applied in the directions of suppository delivery, drug combination, plant raw materials, etc., to achieve the effects of increasing medication compliance, improving curative effect, and reducing the number of administrations

Active Publication Date: 2018-06-26
宁玉梅
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Coptidis total alkaloids gelatin microspheres can be seen in the existing domestic literature [Jia Yongyan, Yuan Yuxia, Zhou Ning, etc. Optimization of the preparation process of Coptidis total alkaloids gelatin microspheres[J], Chinese Journal of Experimental Formulas, 2013, 19(11) :11-13.], pH-dependent total alkaloids of Coptis chinensis colon-targeted pellets [Ling Xiao, Hu Yuanli, Chen Feilong et al. Preparation of pH-dependent total alkaloids of Coptis chinensis colon-targeted pellets and their release properties in vivo and in vitro Evaluation[J]. Chinese Journal of Experimental Formulas, 2014,20(21):24-27.], Coptidis ointment [Guan Zhiyu, Chen Lihua, Wang Sen, etc. Optimization of the preparation process of Coptis ointment [J]. Chinese Journal of Experimental Formulas, 2012,18(17):36-38.] and other oral or transdermal preparations, no related vaginal preparations

Method used

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  • Coptidis total alkaloids vaginal suppository
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  • Coptidis total alkaloids vaginal suppository

Examples

Experimental program
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Effect test

preparation example Construction

[0035] The preparation method of Coptis chinensis total alkaloids of the present invention is as follows: taking Coptis chinensis Chinese herbal medicine (Milian, Yalian or Yunlian) and pulverizing to a particle size of 20 mesh to 60 mesh, decocting and extracting 2 to 3 times by 8 to 12 times the weight, Each time for 1 to 2 hours, the water decoction of Coptidis Rhizoma was obtained, concentrated under reduced pressure at 60 to 70°C, centrifuged at 4000 to 6000 rpm for 6 to 15 minutes, and the supernatant was added to distilled water to obtain Coptidis Coptidis water extract, in which the total alkaloid content of Coptidis Rhizome was 26~27mg / mL. Pack the treated D101 resin into a 1:9 column (4cm×36cm) by wet method, take 1.2BV of the above-mentioned Coptidis rhizome water extract and load it at 2BV / h, remove impurities with 2BV of pure water, and wash with 2BV of 60% ethanol Remove, collect eluate, carry out spray drying according to the conditions of inlet temperature 180 ...

Embodiment 1

[0038] formula:

[0039]

[0040]

[0041] Preparation method: Take gelatin in 773g of distilled water to swell, then add glycerin and total alkaloids of Coptis chinensis in the formulated amount and stir until uniformly dispersed, grind and mix evenly with a colloid mill or homogenizer, adjust to pH 3.8 with citric acid, and then Fill it in a suppository mold coated with oiled liquid paraffin to cool, and cut off the overflowing part to obtain the suppository.

[0042] According to the in vitro dissolution release test, the total alkaloids of Coptidis Rhizoma vaginal suppository were completely released within 2 hours.

Embodiment 2

[0044] formula:

[0045]

[0046] Preparation process: first heat polyethylene glycol at 60°C to melt, then add the total alkaloids of Coptis chinensis in the prescribed amount, grind and mix evenly through a colloid mill or a homogenizer, and then fill it into a plug mold coated with oiled liquid paraffin After cooling, cut off the overflowing part to obtain the suppository.

[0047] According to the in vitro dissolution release test, the total alkaloids of Coptidis Rhizoma vaginal suppository were completely released within 2 hours.

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Abstract

The invention discloses a coptis chinensis total alkaloid vaginal suppository, which is prepared by mixing of the following raw materials by mass: 6%-24% of coptis chinensis alkaloid, and 76%-94% of matrix. And the pH is controlled at 3.8-5.0. Further, the coptis chinensis total alkaloid vaginal suppository is an adhesive suppository, and is prepared by mixing of the following raw materials by mass: 3%-12% of coptis chinensis total alkaloid, 1%-4% of osthole, 1%-4% of aloe polysaccharide, 1%-4% of Hedyotis diffusa total flavone, 1-16% of a bioadhesive agent, and 60%-93% of matrix. The coptis chinensis total alkaloid vaginal suppository is for local medication, the efficacy is concentrated at a part of vagina, thus avoiding the first pass effect and liver, kidney toxicity caused by oral medication, extending the retention time of drug in vagina, at the same time solving the increasingly serious drug resistance and high recurrence rate problems caused by chemical drugs in VVC (vulvovaginal candidiasis) and RVVC (recurrent vulvovaginal candidiasis) treatment, and achieving the purpose of improving the treatment effect.

Description

technical field [0001] The invention relates to a suppository, in particular to a total alkaloid vaginal suppository of coptis. Background technique [0002] Vulvovaginal candidiasis (VVC) is a common vulvovaginal inflammatory disease. In recent years, with the widespread use of clinical antibiotics, the increase of women using oral contraceptives, the increase in the incidence of diabetes and other factors, the incidence and recurrence of VVC have shown an obvious upward trend. According to foreign epidemiological statistics: 5% of VVC patients suffer from 4 or more episodes per year, which is called recurrent vulvovaginal candidiasis (RVVC). Therefore, the recurrence of VVC has become an urgent clinical problem to be solved. [0003] Coptis chinensis Franch., Coptis deltoidea C.Y.Cheng et Hsial or Coptis teeta Wall. have a long history of clinical application in my country. The main ingredients are alkaloids. [0004] Coptidis total alkaloids gelatin microspheres can be...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K36/748A61K9/02A61K47/10A61K47/36A61K47/38A61P15/02A61P31/10A61K31/37A61K31/715
Inventor 宁玉梅丁美红石森林
Owner 宁玉梅
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