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Wax matrix sustained release formulation containing acidic active ingredient of Garcinia cambogia

A technology of active ingredients and sustained-release agents, applied in the field of traditional Chinese medicine preparations, can solve the problems of oxidative decomposition, lack of stability and effectiveness, etc., and achieve the effects of reducing toxic and side effects, broadening drug routes, and increasing stability

Active Publication Date: 2011-12-14
HENAN JIUSHI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The above patented technology solves the water-soluble problem of gambogic acid and neogambogic acid, but its stability and effectiveness are lacking, and it is easily oxidized and decomposed by the influence of humidity, temperature and light, and it is clinically used as an injection drug. These limitations have brought various obstacles and limitations to the actual production and clinical application of gambogic acid and new gambogic acid

Method used

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  • Wax matrix sustained release formulation containing acidic active ingredient of Garcinia cambogia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Embodiment 1, new gambogic acid hydrogel matrix sheet.

[0045] Formula: Neogambogic Acid 10g, Hypromellose E5M 1.9g, Hypromellose K100M 6.9g, Carmellose Sodium 10.2g, Microcrystalline Cellulose 20g, Magnesium Stearate 2g .

[0046] Preparation: Take the prescribed amount of new gambogic acid and use hydroxypropyl-β cyclodextrin to prepare an inclusion compound in a solvent, then mix it with carboxymethylcellulose sodium, granulate and dry with 95% ethanol, then add HPMC and micro The crystalline cellulose is mixed evenly, granulated, magnesium stearate is added, mixed evenly and pressed into tablets to obtain 200 tablets.

[0047] Tumor suppression experiment

[0048] 1. Experimental tumor strain:

[0049] A: human breast cancer MCF-7,

[0050] B: Human liver cancer BEL-7402,

[0051] C: Human cervical carcinoma HELA.

[0052] 2. Experimental results

[0053] Liver cancer BEL-7402 cells are most sensitive to neogambogic acid sustained-release agent, breast cance...

Embodiment 2

[0055] Embodiment 2, gambogic acid waxy matrix tablet.

[0056] Formula: 10 grams of gambogic acid, 12 grams of stearic acid, 13.2 grams of cetyl alcohol, 6.2 grams of PVP, 11.8 grams of microcrystalline cellulose, 1.1 grams of micronized silica gel, 10 grams of lactose, 5 grams of talc, magnesium stearate 0.3 grams.

[0057] Preparation: Take the prescribed amount of gambogic acid and prepare it into a water-soluble salt first, then dissolve the water-soluble salt in ethanol, then add PVP to dissolve, add micronized silica gel and mix well, add magnesium stearate and cetyl alcohol, and take a water bath Heat to 60°C to melt, add the homogeneous mixture of microcrystalline cellulose, lactose, and talc into the melt, and stir for 1 hour. Afterwards, the viscous mixture was spread on a tray, and left at room temperature for 20 minutes. When agglomerated, it was granulated with a 16-mesh sieve, dried at 30°C, sized, added with magnesium stearate, and compressed into 200 tablets....

Embodiment 3

[0065]Embodiment 3, new gambogic acid gastric retention tablet.

[0066] Formula: 10 grams of neogambogic acid, 10 grams of HPMC, 7 grams of cetyl alcohol, an appropriate amount of PVP, and an appropriate amount of magnesium stearate.

[0067] Preparation: Take the prescribed amount of neogambogic acid and first prepare pellets with coating materials, and then

[0068] Mix the pellets with auxiliary materials HPMC and cetyl alcohol evenly and pass through an 80-mesh sieve, use 10% PVP absolute ethanol solution as a binder to make a soft material, granulate, dry, add magnesium stearate and compress into tablets to obtain 200 tablets.

[0069] Experimental therapeutic effect of 7721 on human liver cancer in nude mice.

[0070] Experimental results: The results showed that the slow-release agent had obvious inhibitory effect on the growth of human liver cancer 7721 solid tumor in nude mice, and had no obvious effect on the weight gain of mice, and its inhibitory effect on the tu...

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Abstract

The present invention relates to a sustained-release preparation containing an acidic active ingredient of garcinia cambogia. It is a sustained-release preparation of gambogic acid, neogambogic acid, arroic acid, etc., which is made of gambogic acid, neogambogic acid, arroic acid, etc., and selected appropriate auxiliary materials and reasonable sustained-release agents. The invented sustained-release preparations of gambogic acid, neogambogic acid and arroic acid have improved the defects of the current new gambogic acid injections, have good solubility and stability, are economical and practical, and have good antitumor effects.

Description

technical field [0001] The invention relates to a traditional Chinese medicine preparation, in particular to a slow-release preparation containing active ingredients such as gambogic acid, neogambogic acid and aruric acid and a preparation method thereof. Background technique [0002] `Garcinia cambogia is a dry resin secreted by Garciniaceae plants. Chinese researchers such as Chen Baoren and Lu Guibao studied the active components of Garcinia cambogia around the 1980s, and initially determined that the active components are mainly gambogic acid, Neogambogic acid, arroic acid, etc. The product is also included in the United States Pharmacopoeia. After that, the research work on the anticancer effect of active ingredients such as gambogic acid continued to deepen. For example, Qu Baoxi et al. have shown through experiments that neogambogic acid has the effect on S 180 , ARS ascites cancer, Lewis lung cancer, leukemia P 388 Solid cancers such as lung adenocarcinoma have g...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K36/185A61K47/38A61P35/00
Inventor 王效山周晶赵煤矿
Owner HENAN JIUSHI PHARMA
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