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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 not improving the solubility of active ingredients, affecting the speed and effect of drug treatment, 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: 2012-08-01
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] The preparation of embodiment 1 racecadotril liposome sheet

[0043] Prescription (1000 tablets)

[0044]

[0045]

[0046] Preparation Process

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

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

[0049] (3) Prepare 500 ml of phosphate buffer solution with a pH value of 6.0, add it to a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolution to obtain a liposome suspension;

[0050] (4) Pour the above suspension into the APV2000 homogenizer, and continuously homogenize under the pressure of 0.5Mpa;

[0051] (5) Th...

Embodiment 2

[0055] The preparation of embodiment 2 racecadotril liposome particles

[0056] Prescription (1000 bags)

[0057]

[0058]

[0059] Preparation Process

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

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

[0062] (3) Prepare 1000ml of phosphate buffer solution with a pH value of 6.0, add it to a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolution, to obtain a liposome suspension;

[0063] (4) Pour the above suspension into the APV2000 milk homogenizer, and continuously milk evenly under the pressure of 2.8...

Embodiment 3

[0066] (7) Packing into bags to prepare racecadotril liposome granules. The preparation of embodiment 3 racecadotril liposome capsules

[0067] Prescription (1000 capsules)

[0068]

[0069]

[0070] Preparation Process

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

[0072] (2) Place the above-mentioned lipid solution in a pear-shaped bottle, and remove the mixed solvent by rotary evaporation in a constant temperature water bath at 50° C. to form a uniform lipid film;

[0073] (3) Prepare 5000ml of phosphate buffer solution with a pH value of 6.0, add it to a pear-shaped bottle and shake gently, so that the lipid film is eluted and dispersed in a hydration medium for dissolving to obtain a liposome suspension;

[0074] (4) Pour the above suspension into the APV2000 milk homo...

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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, which belongs to the technical field of medicine. Background technique [0002] Racecadotril, 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 that is readily absorbed from the gastrointestinal tract due to its lipophilicity. Racecadotril is metabolized into its active ingredient by tissue lipase in the gastrointestinal tract. This active metabolite is an effective inhibitor of enkephalinase, which can protect endogenous enkephalin from destruction, thus prolonging the physiological The effect of antisecretory effect, which makes the excessive secretion of water and electrolytes in diarrhea can be quickly controlled. After oral administration, the inhibitory ef...

Claims

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Application Information

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