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Lafutidine gastric-retention controlled-release composite

A lafutidine and controlled release technology, which is applied in the direction of drug combination, non-active ingredients of polymer compounds, drug delivery, etc., can solve the problems of incomplete absorption, low bioavailability, and limited clinical application of common oral dosage forms

Active Publication Date: 2010-12-22
SHANDONG QIDU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003]Because lafutidine is a poorly soluble drug, it has a high solubility in acidic water and a small solubility in neutral and alkaline water, so that the absorption of common oral dosage forms is not complete , low bioavailability, limited clinical application

Method used

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  • Lafutidine gastric-retention controlled-release composite

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1 (wet granule tabletting method)

[0047]

[0048] Preparation:

[0049] (1) Pulverize the raw materials and pass them through a 100-mesh sieve for later use.

[0050] (2) take the HPMC of recipe quantity K15M , stearic acid and microcrystalline cellulose are uniformly mixed to obtain a mixed controlled-release material.

[0051] (3) Using the "equivalent incremental" method, fully mix the prescribed amount of lafutidine with the mixed controlled-release material, add an appropriate amount of 70% ethanol solution to make soft material, pass through a 20-mesh sieve for granulation, and heat at 50-60°C dry.

[0052] (4) Pass the dry granules through a 20-mesh sieve and mix them evenly with sodium bicarbonate and magnesium stearate, determine the weight of the tablet, and press the tablet to control the hardness of the tablet to 60-80N.

[0053] Carry out in vitro floating test and in vitro release test according to the tablet prepared in Example 1, test...

Embodiment 2

[0057] Embodiment 2 (dry granule tabletting method)

[0058] Component Weight (mg / tablet) % (g / g)

[0059] Lafutidine 20 11.30

[0060] HPMC K15M 60 33.90

[0061] EC(20cp) 20 11.30

[0062] Stearic acid 40 22.60

[0063] Sodium bicarbonate 20 11.30

[0064] Microcrystalline cellulose 15 8.47

[0065] Magnesium stearate 2 1.13

[0066] Preparation:

[0067] (1) Pulverize the raw materials and pass them through a 100-mesh sieve for later use.

[0068] (2) take the HPMC of recipe quantity K15M , stearic acid, sodium bicarbonate and microcrystalline cellulose are uniformly mixed to obtain a mixed controlled-release material.

[0069] (3) Using the "equivalent incremental" method, fully mix the prescribed amount of lafutidine with the mixed controlled-release material, and dry granulate.

[0070] (4) Pass the granules through a 20-mesh sieve and mix them evenly with magnesium stearate, determine the weight of the tablet, compress the tablet, and control the hardness of...

Embodiment 3

[0075] Embodiment 3 (powder direct compression tablet)

[0076] Component Weight (mg / tablet) % (g / g)

[0077] Lafutidine 20 11.30

[0078] HPMC K15M 60 33.90

[0079] EC(20cp) 20 11.30

[0080] Stearic acid 40 22.60

[0081] Sodium bicarbonate 20 11.30

[0082] Microcrystalline cellulose 15 8.47

[0083] Magnesium stearate 2 1.13

[0084] Preparation:

[0085] (1) Pulverize the raw materials and pass them through a 60-mesh sieve for later use.

[0086] (2) take the HPMC of recipe quantity K15M , stearic acid, sodium bicarbonate and microcrystalline cellulose are uniformly mixed to obtain a mixed controlled-release material.

[0087] (3) Using the "equivalent incremental" method, fully mix the prescribed amount of lafutidine with the mixed controlled-release material.

[0088] Determine the tablet weight, compress the tablet, and control the tablet hardness to 60-80N.

[0089] Carry out in vitro floating test and in vitro release test according to the tablet prepar...

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Abstract

The invention relates to a lafutidine gastric-retention controlled-release composite belonging to the field of pharmaceutic preparations. The lafutidine gastric-retention controlled-release composite is characterized by comprising the following components in percentage by weight: 5%-20% of the lafutidine, 10%-40% of framework materials, 10%-30% of assistant bleaching agents, 5%-15% of foaming agents, 5%-15% of filling agents and 0.5%-10% of lubricating agents. The composite has reasonability and simple preparation process; compared with same pharmaceuticals, the lafutidine gastric-retention controlled-release composite has little dose, good tolerance, little side effect, and the like; and in addition, compared with the conventional tablets, the lafutidine gastric-retention controlled-release composite enhances the solubility of lafutidine, prolongs the action time (prolonged from 2-3 hours to 5-6 hours) on the upper parts of a stomach and a small intestine, promotes the absorption, enhances the bioavailability, reduces the pharmaceutical usage times, achieves the maximum treatment effect through minimum doses, reduces the concentration change of peaks and valleys and has good patient compliance.

Description

technical field [0001] The invention relates to a lafutidine gastric retention controlled release composition and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Lafutidine (Lafutidine) is a new type of second-generation histamine H 2 Receptor antagonists, which noncompetitively block H 2 Receptor antagonist, which has dual functions of anti-gastric acid secretion and gastric mucosal protection, was approved for marketing in Japan for the first time in April 2000, and the marketing dosage form is tablet, each tablet is 5mg or 10mg. In phase II clinical research, oral administration of 5-10 mg of this product, twice a day, can significantly accelerate the healing of gastric and duodenal ulcers. Healthy volunteers take 5-10 mg of this product orally, which can inhibit gastric acid secretion stimulated by gastrin or at night. Lafutidine, famotidine, and ranitidine have similar doses to the experimental gastri...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/22A61K9/52A61K31/4545A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P1/04A61K47/10
Inventor 冯波崔美兰董旭李后涛刘杰吕吉祥齐英涛高希波张建勇范建伟
Owner SHANDONG QIDU PHARMA
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