Khosam oil suppository

A technology of bruce chinensis oil and oil suppository, applied in the directions of suppository delivery, antiviral agent, plant raw material, etc., can solve the problems of shock, no research report, death, etc., and achieves reduction of toxic and side effects, stable blood drug concentration, bioavailability high degree of effect

Active Publication Date: 2012-08-22
上海庸善健康科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The most widely used formulations of javanica javanica oil are mainly injections and oral solutions, but years of production and clinical practice have proved that these two preparations have certain defects
For example, the process of javanica javanica oil emulsion injection is unstable, and the temperature, emulsification time and production equipment can all affect the product quality and cause uneven emulsion particles; oil and water stratification, cracking, phase inversion, and easy to occur during product storage. Flocculation and decay and other phenomena make it unusable, and it is greatly affected by the environment in actual use, and often fails or has unqualified properties within the validity period.
The Chinese patent "Preparation Method of Emulsified Pharmaceutical Composition Containing Brucea Brucea Oil" (publication number CN 101683367A) stated that the commercially available Brucea Brucea Oil Emulsion Injection failed the hemolysis test after being stored for 6 months under specified conditions. The hemolytic reaction in the human body can lead to a sharp drop in hemoglobin in the human body. In mild cases, it is accompanied by symptoms such as chills, fever, chills, hives, headache or dizziness; urine, can lead to shock and death, there is a big safety hazard
Some people have loaded Brucea javanica oil with glycerin gelatin or balsamic butter to make traditional common suppositories for local treatment (Zhang Ruhua et al., Journal of Shenyang Pharmaceutical College, 1978, 10:7-10), but there is no follow-up research report
And this kind common suppository can't control drug release, can't give full play to the therapeutic effect of javanica javanica oil

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Brucea javanica oil is loaded in the in situ (in vivo) gel matrix in the form of microcapsules

[0026] One, the preparation of Brucea javanica oil microcapsule

[0027] Take 2.5 g of gum arabic, add 6 mL of distilled water to grind evenly, add 1 g of javanica javanica oil dropwise, grind to make colostrum, add 60 mL of distilled water, dilute, and set aside (a); take 2.5 g of gelatin, add 60 mL of distilled water, Stir well and set aside for (b). Mix the above a and b, stir at 50°C, add 10% acetic acid to adjust the pH value to 3-4 (c). Pour 100 mL of distilled water into c, stir in an ice bath to 10°C, add 6 mL of 36% formaldehyde, stir for 15 min, add 20% NaOH to adjust the pH value to 8-9, stir for 1 h, stand still, filter, and wash with water until no aldehyde Taste, dried into microcapsules. Gained Brucea javanica oil microcapsules are spherical (see figure 1 ), the particle size is 3-15 μm, and the stability is good.

[0028] 2. Determinatio...

Embodiment

[0082] Example 2 Brucea javanica oil loaded in a water-soluble matrix in the form of microcapsules

[0083] Take 4 g of PEG6000, heat and melt at 60°C, add 4 g of PEG400 and mix evenly, then add the javanica javanica oil microcapsules prepared according to Example 1, stir well, fill in a bolt mold and cool, shape, and demould to obtain .

[0084] Example 3 Brucea javanica oil loaded in oily matrix in the form of microcapsules

[0085] Take 10 g of gum arabic, add 30 mL of distilled water, grind evenly, add 10 g of javanica javanica oil dropwise, grind to make colostrum, add 300 mL of distilled water, dilute, and set aside (a); take 10 g of gelatin, add 300 mL of distilled water, Stir well and set aside for (b). Mix the above a and b, stir at 50°C, add 10% acetic acid to adjust the pH value to 3-4 (c). Pour 500 mL of distilled water into c, stir in an ice bath to 10°C, add 30 mL of 36% formaldehyde, stir for 15 min, add 20% NaOH to adjust the pH value to 8-9, stir for 1 ...

Embodiment 4

[0087] Example 4 Brucea javanica oil is loaded in a water-soluble matrix in the form of liposomes

[0088] Take 1 g of javanica javanica oil, 10 g of soybean lecithin and 1 g of cholesterol, dissolve them in 200 mL of absolute ethanol, place them in an eggplant-shaped bottle, and use a rotary evaporator to evaporate the organic solvent in a water bath at 60 °C to form a homogeneous mass on the wall of the bottle. Lipid film. Add 10 mL of phosphate buffered saline solution PBS (pH 7.4) into the bottle, rotate to wash the membrane, and obtain liposome suspension for later use.

[0089] Take 60 g of PEG6000, heat and melt at 60°C, add 20 g of PEG400 and mix evenly, then add the liposome prepared above under constant stirring, mix evenly, fill it in a plug mold and cool it, shape it, and demould it.

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Abstract

The invention discloses a khosam oil suppository. An active component of khosam oil of the khosam oil suppository of the invention is loaded in a matrix in a form of particles. The khosam oil suppository of the invention has the advantages of both suppositories and particles, not only is suitable for rectal administration or vaginal administration to generate local and systemic effect, can effectively prevent adverse reactions of khosam oil, but also can control the drug release speed, give full play to the drug curative effect, and significantly improve patient compliance, and has significant treatment superiority when compared with commercially available khosam oil products and traditional common khosam oil suppositories.

Description

technical field [0001] The invention relates to the technical field of traditional Chinese medicine pharmacy, in particular to a suppository containing javanica javanica oil. Background technique [0002] Brucea javanica, also known as old javanica and flavescens, was first recorded in the "Compendium of Materia Medica Supplements" written by Zhao Xuemin in the Qing Dynasty. It is bitter and poisonous. Brucea javanica (L.) The dry ripe fruit of Merr. Produced in my country's Guangdong, Hunan, Guangxi, Fujian and other places, the main functions are heat clearing, dampness, insecticide, detoxification, and corrosion of warts. The ingredients contained in Brucea javanica can be divided into two parts: water-soluble and fat-soluble (Bruce javanica oil). The water-soluble components are mainly a series of tetracyclic triterpenoids, which are toxic. Brucea javanica oil contains triolein (which is hydrolyzed to oleic acid), other types of bound fatty acids, and non-esterified ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/185A61K9/02A61P35/00A61P1/04A61P1/00A61P31/20A61P17/12A61P13/08A61P15/00A61P3/06A61K131/00
Inventor 陈钢温露
Owner 上海庸善健康科技发展有限公司
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