Composition for improving dissolution rate of benzamide gastric motility drug and application of composition

A technology of benzamides and gastric motility, which is applied in the direction of drug combinations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of poor dissolution, achieve high dissolution, improve curative effect, and good The effect of stability

Inactive Publication Date: 2014-11-19
SHANGHAI CHENPON PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The present invention aims to provide a solution to the problem of poor dissolution of existing benzamide gastric motility drugs, thereby reducing the sensitivity of the drug to pH when it is dissolved in the medium, and realizing the non-pH value of this type of drug. Dependent release, improving drug dissolution

Method used

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  • Composition for improving dissolution rate of benzamide gastric motility drug and application of composition
  • Composition for improving dissolution rate of benzamide gastric motility drug and application of composition
  • Composition for improving dissolution rate of benzamide gastric motility drug and application of composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Prepare a composition capsule that improves the dissolution rate of benzamide gastric motility drugs, specifically capsules containing mosapride citrate, the specific amount of raw materials of the composition is as shown in Table 1:

[0055] Table 1, the composition raw material list of preparation mosapride citrate capsule

[0056] composition raw material

Content mg / grain

Mosapride citrate

5.3

Mannitol

90.2

Hypromellose

10

Hydroxypropyl methylcellulose RT5 (HPMC RT5)

8

fumaric acid

8

Micropowder silica gel

0.5

[0057] The preparation steps are as follows:

[0058] Pass the mosapride citrate bulk drug through a 200-mesh sieve, and other excipients through a 80-mesh sieve;

[0059] Dissolve 5 mg of hydroxypropyl methylcellulose in 100 ml of purified water, add the raw material drug into the solution, put the rest of the materials into a fluidized bed granulator and mix for 3 minutes...

Embodiment 2

[0062] Prepare a composition tablet that improves the dissolution rate of benzamide gastric motility drugs, specifically a tablet containing cisapride, and the specific consumption of the raw materials of the composition is as shown in Table 2:

[0063] Table 2, the composition raw material list of preparation cisapride tablet

[0064] composition raw material

Content mg / tablet

Cisapride

6

malic acid

8

[0065] Cyclodextrin

92

Hydroxypropylmethylcellulose

8

carboxymethyl cellulose

10

Talc powder

3

Micro silica gel

4

[0066] The preparation steps are as follows:

[0067] The above-mentioned components are uniformly mixed, and each component is compressed by a general wet granule compression method, and the tablet obtained by compression is coated with a protective film to obtain the desired tablet containing cisapride.

Embodiment 3

[0069] Prepare a composition tablet that improves the dissolution rate of benzamide gastric motility drugs, specifically a tablet containing metoclopramide, and the specific amount of raw materials of the composition is as shown in Table 3:

[0070] Table 3, the composition raw material list of preparation metoclopramide tablet

[0071] composition raw material

Content mg / tablet

Metoclopramide hydrochloride

6

aspartic acid

5

Sorbic acid

3

Cyclodextrin

92

Copolymer of polyvinylpyrrolidone and vinyl chloride

8

Sodium carboxymethyl starch

10

Talc powder

3

Micro silica gel

4

[0072] The preparation steps are as follows:

[0073] The above-mentioned ingredients are uniformly mixed, and the ingredients are compressed and manufactured by the general direct powder compression method, and the tablets obtained by the compression manufacturing are coated with a slow-release film t...

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Abstract

The invention discloses a composition for improving a dissolution rate of a benzamide gastric motility drug. The composition specifically comprises a benzamide gastric motility drug containing at least one amino and/or ammonium salts thereof as well as at least one organic acid. The composition disclosed by the invention generates a local acidic microenvironment after being dissolved, and therefore, the influence of a pH value of a medium on the dissolution rate of the active ingredients is slight, and non-pH dependence dissolution is realized. Therefore, a high dissolution rate also can be realized under the condition that pH value in a digestive tract greatly changes, so that the influence of differences in diet or constitution on the curative effect of the drug is reduced, the dissolution rate of active ingredients of the drug can be effectively improved, and the bioavailability is improved. The composition is low in production cost and easy to use and can realize non-pH dependence release of the active ingredients of the drug. Moreover, a prescription of the composition disclosed by the invention does not comprise a surfactant, and the composition is suitable for a patient sensitive to the surfactant.

Description

technical field [0001] The invention relates to an oral pharmaceutical composition, in particular to an oral pharmaceutical composition capable of improving the sensitivity of the drug dissolution rate to pH value, thereby increasing the drug dissolution rate and application thereof. Background technique [0002] The gastrointestinal tract is one of the important parts of the digestive system. The gastrointestinal tract can digest and absorb the food ingested by the human body. Among them, the stomach is the most important part of the human digestive tract and an important part of the human body’s nutrient absorption. The small intestine Various digestive juices are also secreted in the stomach, which can carry out secondary digestion and absorption of food processed by the stomach, and transport the digested substances to the large intestine. [0003] The human stomach can secrete acidic digestive juice to help digest and absorb food. The gastric juice mainly includes hydro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/5375A61K47/12A61P1/14
Inventor 孟建强廖志勇曹云杜狄峥
Owner SHANGHAI CHENPON PHARM TECH CO LTD
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