Hygroscopic auxiliary material-based solid preparation

A solid preparation and hygroscopic technology, which is applied in the field of solid preparations based on easily hygroscopic excipients, can solve the problems of simvastatin raw materials on thermal instability, drug stability, acceleration, etc.

Inactive Publication Date: 2011-02-23
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, if the above-mentioned method for preventing the hydrolysis of meclofenoxate hydrochloride is extended to other solid preparations, there will be the following problems: under acidic conditions, the hydrolysis of some drugs will be accelerated, because the acid has a catalytic effect on the hydrolysis, and it will not be able to prevent the hydrolysis of the solid preparations. hydrolyzed drug hydrolysis
However, there are still at least three deficiencies in the preparation of the above-mentioned simvastatin preparation: ① the content drop of the drug due to hydrolysis is not considered; However, the raw material of simvastatin is unstable to heat, and the use of this process will cause a decrease in content; ③ a large amount of organic solvents are used in the granulation process, and the volatilization of organic solvents may affect the stability of the drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] The components of this example and their mass percentages are: 5% simvastatin, 0.5% BHA, 60.5% lactose, 28% microcrystalline cellulose, 5% croscarmellose sodium and 1% magnesium stearate .

[0020] Wherein: the amount of simvastatin is 5mg, 10mg, 20mg or 40mg.

[0021] The preparation method of this embodiment comprises the following steps:

[0022] (1) Weigh BHA into a glass mortar, gradually add lactose and mix evenly by doubling the grinding method, and pass through a 60-mesh sieve to obtain the mixture ①;

[0023] (2) Then weigh the simvastatin of the prescribed amount and put it into a glass mortar, then add the above-mentioned mixture ① and mix by double grinding method to obtain the mixture ②;

[0024] (3) Weigh lactose equal to the above-mentioned mixture ②, mix with the mixture ② evenly, and pass through a 20-mesh sieve to obtain the mixture ③;

[0025] (4) Mix the mixture ③ with the remaining lactose, microcrystalline cellulose, and croscarmellose sodium in...

Embodiment 2

[0027] The components and their mass percentages in this example are: 5.1% simvastatin, 0.3% BHA, 59.7% lactose, 30.8% microcrystalline cellulose, 5.2% sorbitol and 0.9% magnesium stearate.

[0028] Wherein: the amount of simvastatin is 5mg, 10mg, 20mg or 40mg.

[0029] The preparation method of this embodiment comprises the following steps:

[0030] (1) Weigh BHA into a glass mortar, gradually add lactose and mix evenly by doubling the grinding method, and pass through a 60-mesh sieve to obtain the mixture ①;

[0031] (2) Then weigh the simvastatin of the prescribed amount and put it into a glass mortar, then add the above-mentioned mixture ① and mix by double grinding method to obtain the mixture ②;

[0032] (3) Weigh lactose equal to the above-mentioned mixture ②, mix with the mixture ② evenly, and pass through a 20-mesh sieve to obtain the mixture ③;

[0033] (4) Mix the mixture ③ with the remaining lactose, microcrystalline cellulose, and sorbitol in a mixer, then add m...

Embodiment 3

[0035] The components and their mass percentages of this example are: 4.8% simvastatin, 0.4% BHA, 58.6% lactose, 30% microcrystalline cellulose, 30% microcrystalline cellulose, 5.2% citric acid and magnesium stearate 1 %.

[0036] Wherein: the amount of simvastatin is 5mg, 10mg, 20mg or 40mg.

[0037] The preparation method of this embodiment comprises the following steps:

[0038] (1) Weigh BHA into a glass mortar, gradually add lactose and mix evenly by doubling the grinding method, and pass through a 60-mesh sieve to obtain the mixture ①;

[0039] (2) Then weigh the simvastatin of the prescribed amount and put it into a glass mortar, then add the above-mentioned mixture ① and mix by double grinding method to obtain the mixture ②;

[0040] (3) Weigh lactose equal to the above-mentioned mixture ②, mix with the mixture ② evenly, and pass through a 20-mesh sieve to obtain the mixture ③;

[0041] (4) Mix the mixture ③ with the remaining lactose, microcrystalline cellulose, an...

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PUM

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Abstract

The invention provides a hydroscopic auxiliary material-based solid preparation, which belongs to the technical field of medicament preparation. The solid preparation comprises the following components: 1 to 10 percent of active ingredient, 0.1 to 60 percent of hydroscopic auxiliary material, 0.1 to 2.0 percent of antioxidant, 40 to 75 percent of excipient, 2 to 10 percent of disintegrating agent, 1 to 10 percent of adhesive, and 0.5 to 3 percent of lubricant. The problem can be solved by utilizing a method of adding the hydroscopic auxiliary material, and the contact between a hydroscopic medicament and moisture is reduced so as to reduce the hydrolysis of the hydrolytic medicament in the solid preparation.

Description

technical field [0001] The invention relates to a preparation in the technical field of pharmaceutical preparation, in particular to a solid preparation based on a hygroscopic auxiliary material. Background technique [0002] The basic requirements of pharmaceutical preparations should be safe, effective and stable. Stability refers to the stability of a drug in vitro. If the drug decomposes and deteriorates, it will not only reduce the efficacy of the drug, but some drugs may even produce toxic and side effects. Therefore, the stability of the drug preparation is very important to ensure the safety and effectiveness of the drug preparation. Drugs have different degradation reactions due to different chemical structures. Hydrolysis and oxidation are the two main pathways for drug degradation. Other reactions such as isomerization, polymerization, and decarboxylation also occur in some drugs. [0003] Hydrolysis is the main way of drug degradation, and the drugs that belon...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K47/36A61K47/38A61K47/34A61K47/10A61K47/12A61K9/16A61K47/42A61K47/44A61K9/20A61K9/14A61K47/32A61K47/26A61K47/14
Inventor 郭圣荣陈伟峦郭冬薇沈园园
Owner SHANGHAI JIAO TONG UNIV
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