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Hemsleyadin sustained-release preparation

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: 2008-08-20
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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  • Hemsleyadin sustained-release preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] composition:

[0026] Snow gallin 18g

[0027] Ethylcellulose 36g

[0028] Stearic acid 54g

[0029] Hydroxypropyl Cellulose 9g

[0030] Dextrin 22g

[0031] Micronized silica gel 3.2g

[0032] Magnesium stearate 0.9g

[0033] 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. Take another 36g of ethyl cellulose and 3g of hydroxypropyl cellulose, grind them after mixing, pass through an 80-mesh sieve, add 22g of dextrin passed through an 80-mesh sieve and medicinal powder containing gentianin, mix well, and granulate 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

[0035] composition:

[0036] Sustained release portion Immediate release portion

[0037] Snow gallin 18g 6g

[0038] Hydroxypropyl Methyl Cellulose 50g

[0039] Macrogol 1600 20g

[0040] Triethanolamine 6g

[0041] Sodium stearate 5g 30g

[0042] Lactose 50g

[0043] Microcrystalline Cellulose 18g

[0044] Medicinal Calcium Carbonate 10g

[0045] Magnesium stearate 0.7g 0.5g

[0046] Preparation method:

[0047] 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 propyl 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.

[0048]2. Quick-release part: take 6g of gentianin, 30g of sodium stearate, 50g of lacto...

Embodiment 3

[0051] composition:

[0052] Sustained release portion Immediate release portion

[0053] Snow gallin 9g 3g

[0054] Methyl methacrylate 41.5g

[0055] Glyceryl monostearate 20g

[0056] Macrogol 400 7g

[0057] Hydroxypropyl Cellulose 2.2g

[0058] Micronized silica gel 22g

[0059] Magnesium stearate 0.5g 0.3g

[0060] Lactose 22g

[0061] Dextrin 10g

[0062] Starch 5.5g

[0063] Preparation method:

[0064] 1. Preparation of sustained-release pellets:

[0065] Get 9g of gentianin and 22g of micropowder silica gel after mixing, pulverize, and cross a 100-mesh sieve. Glyceryl monostearate 20g, heat and melt at 70-75°C, add 35g methyl methacrylate, 7g polyethylene glycol 400, mix well, 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, and continue stirring to make round pellets with a particle size of...

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Abstract

The invention relates to a special sustained-release preparation of natural antibiotics curcurbitacin, in particular to a membrane controlled or / and matrix release oral preparation with the composition as follows: curcurbitacin 5 to 20%, water insoluble medical macromolecular material 30 to 65%, water soluble medical macromolecular material 5 to 25%, and conventional auxiliary material 15 to 45%. The special sustained-release preparation of natural antibiotics curcurbitacin has the advantages of retarding the release of curcurbitacin from drug preparation, reducing the peak and peak valley for drug absorption, facilitating stable plasma drug concentration, and especially facilitating the disease treatment when the sustained release is combined with rapid release since the rapid release part can be rapidly released to produce the plasma drug concentration required for treatment as soon as possible, while the sustained release part can subsequently provide stable plasma drug concentration and reduce the fluctuation of plasma drug concentration.

Description

technical field [0001] The invention relates to a sustained-release preparation of a special dosage form of natural antibacterial drug gentianin. Background technique [0002] 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 antibacterial drug. Another study showed that the minimum inhibitory concentration of gentianin to influenza virus was about 2.5 mg·ml -1 , suggesting that pectin has the effect of anti-...

Claims

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Application Information

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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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