Slow-release preparation of cucurbitacin

A sustained-release preparation and technology of gentianin, which is applied to medical preparations containing active ingredients, organic active ingredients, and non-active ingredients of polymer compounds, etc., can solve problems such as inconvenient taking and inability to achieve drug release, and achieve peak reduction Valley phenomenon, reducing fluctuations, and stabilizing the effect of blood drug concentration

Active Publication Date: 2010-07-21
云南蓝绿康药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existing gentianin preparations usually need to be taken 3 times a day, which is inconvenient to take and cannot achieve stable drug release

Method used

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  • Slow-release preparation of cucurbitacin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] composition:

[0027] Snow gallin 18g

[0028] Ethylcellulose 36g

[0029] Stearic acid 54g

[0030] Hydroxypropyl Cellulose 9g

[0031] Dextrin 22g

[0032] Micronized silica gel 3.2g

[0033] Magnesium stearate 0.9g

[0034] Preparation method: Take 54g of stearic acid, 6g of hydroxypropyl cellulose, and 18g of gentianin, pulverize them, pass through a 100-mesh sieve, disperse them evenly in ethyl acetate, and evaporate the solvent to dryness. Crush and pass through an 80-mesh sieve. Another 36g of ethyl cellulose and 3g of hydroxypropyl cellulose were mixed and pulverized, passed through an 80-mesh sieve, added 22g of dextrin passed through an 80-mesh sieve and medicinal powder containing gentianin, mixed evenly, and granulated with 95% ethanol , dried, and granulated through a 40-mesh sieve. Add 3.2 g of micropowder silica gel and 0.9 g of magnesium stearate, mix and press into tablets to make slow-release tablets each containing 18 mg of gentianin.

Embodiment 2

[0036] composition:

[0037] Sustained release portion Immediate release portion

[0038] Snow gallin 18g 6g

[0039] Hydroxypropyl Methyl Cellulose 50g

[0040] Macrogol 1600 20g

[0041] Triethanolamine 6g

[0042] Sodium stearate 5g 30g

[0043] Lactose 50g

[0044] Microcrystalline Cellulose 18g

[0045] Medicinal Calcium Carbonate 10g

[0046] Magnesium stearate 0.7g 0.5g

[0047] Preparation method:

[0048]1. Sustained-release part: Take 46g of hydroxypropyl methylcellulose, 20g of polyethylene glycol, 6g of triethanolamine, 5g of sodium stearate, and 18g of gentianin, mix them well, pulverize them, and pass through a 100-mesh sieve. Another 4 g of hydroxypropyl methylcellulose was prepared into a 3% solution with an appropriate amount of ethanol, granulated, dried, granulated with a 40-mesh sieve, added with 0.7 g of magnesium stearate, and mixed uniformly.

[0049] 2. The quick-release part: take 6g of gentianin, 30g of sodium stearate, ...

Embodiment 3

[0052] composition:

[0053] Sustained release portion Immediate release portion

[0054] Snow gallin 9g 3g

[0055] Methyl methacrylate 41.5g

[0056] Glyceryl monostearate 20g

[0057] Macrogol 400 7g

[0058] Hydroxypropyl Cellulose 2.2g

[0059] Micronized silica gel 22g

[0060] Magnesium stearate 0.5g 0.3g

[0061] Lactose 22g

[0062] Dextrin 10g

[0063] Starch 5.5g

[0064] Preparation method:

[0065] 1. Preparation of sustained-release pellets:

[0066] Get gentianin 9g, pulverize after mixing micropowder silica gel 22g, cross 100 mesh sieves. Glyceryl monostearate 20g, after heating and melting at 70-75°C, add 35g methyl methacrylate and 7g polyethylene glycol 400, mix well, and keep warm. Add pectin-containing medicinal powder, fully stir and mix, and gradually lower the temperature, adjust the stirring speed, when granules are formed, add 0.5g of magnesium stearate, continue to stir, and make round pellets with a particle size of 0....

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Abstract

The invention relates to a slow-release preparation of cucurbitacin, a natural antibiotic. The slow-release preparation is in the special dosage form and is a membrane controlled-release or / and skeleton-release oral preparation formed by the following components in percentage by weight: 5-20% of cucurbitacin, 30-65% of water insoluble polymers for medicine, 5-25% of water soluble polymers for medicine and 15-45% of conventional adjuvants. The preparation can slow down release of cucurbitacin from the medicinal preparation, thus reducing peak valley of medicine absorption and being beneficial to maintaining steady plasma concentration. In particular, when the medicine release mode combining quick release and slow release is adopted, the quick-release part of cucurbitacin is quickly released after oral administration, thus being beneficial to building the plasma concentration meeting treatment requirement, while the slow-release part of cucurbitacin can provide comparatively steady plasma concentration in the following period, thus reducing fluctuation of plasma concentration and being more beneficial to disease treatment.

Description

[0001] This application is a divisional application of 200710065677.3. The filing date of the original application is February 13, 2007. The application number is 200710065677.3. technical field [0002] The invention relates to a sustained-release preparation of a special dosage form of natural antibacterial drug gentianin. Background technique [0003] Cucurbitacin is a mixture of Cucurbitacin IIa and Cucurbitacin IIb extracted from Cucurbitaceae Cucurbitacin. Pharmacological studies have shown that gentianin has the functions of clearing away heat and detoxifying, antibacterial and anti-inflammatory. It has been reported that gentianin has antibacterial activity against Gram-positive bacteria and negative bacteria, and the MIC of gentianin against gram-positive bacteria is <0.00036~0.75 mg·ml -1 . The MIC for Gram-negative bacteria is 0.0056~1.5mg·ml -1 . Its strength is equivalent to or slightly stronger than chloramphenicol, and it is an excellent natural antibac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61K47/40A61P31/04
Inventor 韩颖任磊王曙彩白丽梅王娟
Owner 云南蓝绿康药业有限公司
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