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Medicinal preparation and preparation method thereof

A pharmaceutical preparation and pharmacy technology, applied in the field of pharmaceutical preparations and their preparation, can solve the problems of water insolubility, increased ALT or AST, increased liver burden, etc., and achieve the effects of reducing the dosage, improving the curative effect, and reducing the metabolic burden on the liver

Pending Publication Date: 2020-06-30
JIANGSU SIMCERE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] 3-methyl-1-phenyl-2-pyrazolin-5-one has hepatotoxicity, and it is indicated in the drug instructions that the incidence of liver adverse reactions in patients after medication exceeds 5%; 3-butyl-1(3H )-isobenzofuranone soft capsules have obvious first-pass effect when taken orally. The absolute bioavailability is about 6-7%, the maximum is not more than 10%, and the remaining 90% is metabolized by the liver. The two-week course of treatment is 600 mg per day. Dosage, about 550 mg of the main drug is decomposed in the liver in the first pass, virtually increasing the burden on the liver, causing liver damage and resulting in increased ALT or AST
However, since butylphthalide is an oily compound, it must be prepared into an injection to solve its water-insoluble problem

Method used

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  • Medicinal preparation and preparation method thereof
  • Medicinal preparation and preparation method thereof
  • Medicinal preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] 3-Methyl-1-phenyl-2-pyrazolin-5-one 10g, 3-Butyl-1(3H)-isobenzofuranone 12.5g, D-camphor 3g, sulfobutylbeta Sodium cyclodextrin 300g, propylene glycol 414.4g, sodium metabisulfite 5g, appropriate amount of 1mol / L hydrochloric acid.

[0074] Preparation:

[0075] Step 1, preparation of 3-butyl-1(3H)-isobenzofuranone medicinal solution:

[0076] ①Take 10L of water for injection, heat it to 30°C, slowly add the prescribed amount of sulfobutylbeta cyclodextrin sodium into it, stir until completely dissolved, and prepare the sulfobutylbeta cyclodextrin solution;

[0077] ②While stirring, slowly add the prescribed amount of raw material 3-butyl-1(3H)-isobenzofuranone, stir until the solution is clear and transparent, add water for injection to 30L, and prepare 3-butyl-1(3H) -isobenzofuranone solution, for subsequent use.

[0078] Step 2. Preparation of triple compound injection containing 3-methyl-1-phenyl-2-pyrazolin-5-one, 3-butyl-1(3H)-isobenzofuranone and dexbornyl alc...

Embodiment 2

[0085] 3-methyl-1-phenyl-2-pyrazolin-5-one 5g, 3-butyl-1(3H)-isobenzofuranone 12.5g, dexbornyl alcohol 3g, sulfobutylbeta Cyclodextrin sodium 600g, propylene glycol 363.5g, sodium metabisulfite 7.5g, 1mol / L sodium hydroxide aqueous solution in proper amount.

[0086] Preparation

[0087] Step 1, preparation of 3-butyl-1(3H)-isobenzofuranone medicinal solution:

[0088] ①Take 12L of water for injection, heat it to 25°C, slowly add the prescribed amount of sulfobutylbeta cyclodextrin sodium into it, stir until completely dissolved, and prepare the sulfobutylbeta cyclodextrin solution;

[0089] ②While stirring, slowly add the prescribed amount of raw material 3-butyl-1(3H)-isobenzofuranone, stir until the solution is clear and transparent, add water for injection to 30L, and prepare 3-butyl-1(3H) -isobenzofuranone solution, for subsequent use.

[0090]Step 2. Preparation of triple compound injection containing 3-methyl-1-phenyl-2-pyrazolin-5-one, 3-butyl-1(3H)-isobenzofuranone...

Embodiment 3

[0097] 3-methyl-1-phenyl-2-pyrazolin-5-one 5g, 3-butyl-1(3H)-isobenzofuranone 6.25g, dexbornyl alcohol 6g, sulfobutylbeta Cyclodextrin sodium 500g, propylene glycol 515.6g, sodium metabisulfite 6.3g, 1mol / L hydrochloric acid in proper amount.

[0098] Preparation

[0099] Step 1, preparation of 3-butyl-1(3H)-isobenzofuranone medicinal solution:

[0100] ①Take 9L of water for injection, heat it to 35°C, slowly add the prescribed amount of sulfobutylbeta cyclodextrin sodium into it, stir until completely dissolved, and prepare the sulfobutylbeta cyclodextrin solution;

[0101] ②While stirring, slowly add the prescribed amount of raw material 3-butyl-1(3H)-isobenzofuranone, stir until the solution is clear and transparent, add water for injection to 30L, and prepare 3-butyl-1(3H) -isobenzofuranone solution, for subsequent use.

[0102] Step 2. Preparation of triple compound injection containing 3-methyl-1-phenyl-2-pyrazolin-5-one, 3-butyl-1(3H)-isobenzofuranone and dexbornyl a...

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Abstract

The invention discloses a medicinal preparation and a preparation method thereof. The medicinal preparation contains 5-methyl-2-phenyl-1,2-dihydropyrazol-3-one, 3-butylisobenzofuran-1(3H)-one and camphol, as well as pharmaceutically-acceptable auxiliary materials, and a preparation formulation is injection liquid or a freeze-dried agent. The injection liquid provided by the invention can obviouslyreduce the medicine administration dosage of 5-methyl-2-phenyl-1,2-dihydropyrazol-3-one; and besides, the 3-butylisobenzofuran-1(3H)-one is administrated in the form of injection, compared with an orally-taken manner, the form of injection can notably reduce the medicine administration dosage, so that liver metabolism burden can be reduced, and the medicinal preparation has the advantages of being low in medicine administration dosage, stable in properties, low in incidence rate of adverse reactions of the liver and the like.

Description

technical field [0001] The invention belongs to the technical field of anti-cerebrovascular disease, and relates to a pharmaceutical preparation and a preparation method thereof. Background technique [0002] 3-Methyl-1-phenyl-2-pyrazolin-5-one is a brain protectant (free radical scavenger) used to improve neurological symptoms, activities of daily living and function caused by acute cerebral infarction obstacle. Its structure is as follows: [0003] [0004] Clinical studies suggest that N-acetylaspartic acid (NAA) is a specific marker of surviving nerve cells, and its content decreases sharply in the early stage of cerebral infarction. The administration of 3-methyl-1-phenyl-2-pyrazolin-5-one to patients in the acute stage of cerebral infarction can inhibit the decrease of local cerebral blood flow around the infarction, and make the NAA content in the brain 28 days after the onset compared with glycerin control. group significantly increased. Preclinical studies su...

Claims

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Application Information

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IPC IPC(8): A61K31/415A61K31/365A61K31/045A61K9/08A61K47/69A61K47/10A61P9/10A61P25/00
CPCA61K31/415A61K31/365A61K31/045A61K9/08A61K9/0019A61K47/6951A61K47/10A61P9/10A61P25/00A61K2300/00
Inventor 钱勇张汉武任晋生
Owner JIANGSU SIMCERE PHARMA
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