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Racecadotril liposome solid preparation

A technology for racecadotril and solid preparation, applied in the field of medicine, can solve the problems of affecting the speed and effect of drug treatment, not improving the solubility of active ingredients, low solubility of racecadotril, etc., so as to improve the bioavailability and reduce the Toxic and side effects, the effect of improving solubility

Inactive Publication Date: 2011-07-27
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent document CN101442990A discloses a novel administration form of racecadotril, which consists of racecadotril, lactose monohydrate, carmellose calcium, hydroxypropyl cellulose, microcrystalline cellulose, pregelatinized Composed of starch and magnesium stearate, wet granulation to produce racecadotril tablets, the tablets and dry suspensions prepared by the above patents did not improve the solubility of the active ingredients, resulting in low dissolution and slow absorption , affecting the curative effect
[0006] The preparations of racecadotril currently on the market include capsules, tablets and granules, all of which are administered orally. Due to the low solubility of racecadotril and relatively low bioavailability, the drug's Absorption and distribution are slow, which affects the treatment speed and effect of the drug

Method used

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  • Racecadotril liposome solid preparation
  • Racecadotril liposome solid preparation
  • Racecadotril liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of racemic cardotril liposome tablets

[0043] Prescription (1000 tablets)

[0044]

[0045]

[0046] Preparation Process

[0047] (1) Dissolve 10g racecadotril, 25g soybean lecithin, 25g hydrogenated egg yolk lecithin, 18g cholesterol and 6g Tween 80 in 800ml mixed solvent of ethanol and isopropanol with a volume ratio of 2:1 to obtain Lipid solution

[0048] (2) Put the above-mentioned lipid solution in a pear-shaped bottle, and spin-evaporate in a constant temperature water bath at 55°C to remove the mixed solvent to form a uniform lipid film;

[0049] (3) Prepare 500ml of phosphate buffer solution with pH 6.0, add it to a pear-shaped bottle and shake it gently to elute the lipid membrane and disperse it in the hydration medium to dissolve, to obtain a liposome suspension;

[0050] (4) Pour the above suspension into the APV2000 milk homogenizer, and continue milk homogenization under a pressure of 0.5Mpa;

[0051] (5) Filter the above suspension with a 0.4...

Embodiment 2

[0055] Example 2 Preparation of racemic cardotril liposome particles

[0056] Prescription (1000 bags)

[0057]

[0058]

[0059] Preparation Process

[0060] (1) Dissolve 30g of racecadotril, 120g of soybean lecithin, 120g of hydrogenated egg yolk lecithin, 100g of cholesterol and 45g of Tween 80 in 2000ml of a mixed solvent of ethanol and isopropanol with a volume ratio of 2:1 to obtain Lipid solution

[0061] (2) Put the above-mentioned lipid solution in a pear-shaped bottle, and spin-evaporate in a constant temperature water bath at 45°C to remove the mixed solvent to form a uniform lipid film;

[0062] (3) Prepare 1000ml of phosphate buffer solution with pH 6.0, add it to a pear-shaped bottle and shake it gently to elute the lipid membrane and disperse it in the hydration medium to dissolve, to obtain a liposome suspension;

[0063] (4) Pour the above suspension into the APV2000 milk homogenizer, and continue milk homogenization under a pressure of 2.8Mpa;

[0064] (5) Filter the ab...

Embodiment 3

[0066] (7) Bagging to prepare racecadotril liposome granules. Example 3 Preparation of racemic cardotril liposome capsules

[0067] Prescription (1000 capsules)

[0068]

[0069]

[0070] Preparation Process

[0071] (1) Dissolve 100 g of racecadotril, 600 g of soybean lecithin, 600 g of hydrogenated egg yolk lecithin, 500 g of cholesterol and 200 g of Tween 80 in 10000 ml of a mixed solvent of ethanol and isopropanol with a volume ratio of 2:1 to obtain Lipid solution

[0072] (2) Put the above-mentioned lipid solution in a pear-shaped bottle and spin-evaporate in a constant temperature water bath at 50°C to remove the mixed solvent to form a uniform lipid film;

[0073] (3) Prepare 5000ml of phosphate buffer solution with pH 6.0, add it to a pear-shaped bottle and shake it gently to elute the lipid membrane and disperse it in the hydration medium to dissolve, to obtain a liposome suspension;

[0074] (4) Pour the above suspension into the APV2000 milk homogenizer, and continuously ho...

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Abstract

The invention discloses a racecadotril liposome solid preparation. The racecadotril liposome is prepared from racecadotril, soy lecithin, hydrogenated egg lecithin, cholesterol and tween 80 in the weight ratio of 1:2-8: 2-8:1.5-6:0.5-3; and the solid preparation is prepared from the racecadotril liposome and other pharmaceutically common auxiliary materials. The other pharmaceutically common auxiliary materials comprise filler, a disintegrating agent, a sweetener, an adhesive and a lubricant. The racecadotril liposome solid preparation improves the dissolubility of the racecadotril so as to improve bioavailability; a medicament is absorbed and distributed in a body fast; a curative effect is improved obviously; and the product quality of the preparation is improved and the toxic and side effects are reduced.

Description

Technical field [0001] The invention relates to a new solid preparation of racecadotril, in particular to a solid preparation of racecadotril liposome, belonging to the technical field of medicine. Background technique [0002] Racecadotril, the chemical name is N-[(R,S)-3-acetylmercapto-2-benzylpropionyl)]glycine benzyl ester, molecular formula C 21 H 23 NO 4 S, molecular weight 385.48, structural formula: [0003] [0004] Racecadotril is a prodrug, which is easily absorbed from the gastrointestinal tract due to its lipophilicity. Racecadotril is metabolized by tissue lipase in the gastrointestinal tract into its active ingredient. This active metabolite is an effective inhibitor of enkephalin, which can protect endogenous enkephalin from damage, thus prolonging the physiological Antisecretory effect, which enables rapid control of the excessive secretion of water and electrolytes during diarrhea. After oral administration, the inhibitory effect of racecadotril enkephalinase is...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/265A61K47/34A61K47/36A61K47/38A61P1/12A61K47/26
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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