Medicinal composition of methanesulfonic acid arbidol oral solid preparation

A solid preparation and composition technology, applied in the field of oral pharmaceutical preparations, can solve the problems of slow dissolution of preparations and affect absorption, and achieve the effects of good dispersion state, convenient taking and reasonable formula

Active Publication Date: 2012-02-22
HUBEI LIYI PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The physical and chemical properties of Arbidol hydrochloride are characterized by its almost insoluble in water (1g of this product cannot be dissolved in 10000mL of water), and the dissolution of the preparation is slow, which may affect its absorption in the body

Method used

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  • Medicinal composition of methanesulfonic acid arbidol oral solid preparation
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  • Medicinal composition of methanesulfonic acid arbidol oral solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 20

[0158] A kind of synthetic method of Arbidol mesylate, its steps are as follows:

[0159] 1) Preparation of 3-methylamino-butenoic acid ethyl ester

[0160] Put 150.0 g of ethyl acetoacetate into the reaction bottle, add 160 mL of 40 wt % methylamine aqueous solution dropwise under stirring at 25 ° C, after the drop is complete, continue to stir and react at this temperature for 3 hours, let stand to separate layers, and wash the lower organic layer with water , and dried to obtain intermediate (B) 157.6g, yield: 95.5%.

[0161] 2) Preparation of 1,2-dimethyl-5-oxindole-3-carboxyethyl ester

[0162] Dissolve 124.0g of p-benzoquinone in 1200mL of acetone in a reaction flask, stir evenly, heat to 30°C, add 150.0g of intermediate (B) dropwise under stirring, and continue to react for 2 hours. 2 / 3 of the solvent was cooled to 0-5° C., filtered to obtain a solid, and dried to obtain 90.1 g of intermediate (C), yield: 36.9%.

[0163]3) Preparation of 6-bromo-2-bromomethyl-5-oxind...

Embodiment 21

[0173] A kind of synthetic method of Arbidol mesylate, its steps are as follows:

[0174] 1) Preparation of 3-methylamino-butenoic acid ethyl ester

[0175] Put 100 g of ethyl acetoacetate into the reaction bottle, add 120 mL of 40 wt % methylamine aqueous solution dropwise under stirring at 30 ° C, after the drop is completed, continue to stir and react at this temperature for 3 hours, let stand to separate layers, and wash the lower organic layer with water. Dry to obtain intermediate (B) 99.0 g, yield: 90.0%.

[0176] 2) Preparation of 1,2-dimethyl-5-oxindole-3-carboxyethyl ester

[0177] Dissolve 74.7g of p-benzoquinone in 700mL of acetone in a reaction flask, stir evenly, heat to 40°C, add 90.0g of intermediate (B) dropwise under stirring, and continue to react for 2 hours. 2 / 3 of the solvent was cooled to 0-5° C., filtered to obtain a solid, and dried to obtain 52.3 g of intermediate (C), yield: 37.7%.

[0178] 3) Preparation of 6-bromo-2-bromomethyl-5-oxindole-3-carb...

Embodiment 22

[0187] A kind of synthetic method of Arbidol mesylate, its steps are as follows:

[0188] 1) Preparation of 3-methylamino-butenoic acid ethyl ester

[0189] Put 153.2 g of ethyl acetoacetate into the reaction bottle, add 180 mL of 40 wt % methylamine aqueous solution dropwise under stirring at 35 ° C, after the drop is complete, continue to stir and react at this temperature for 3 hours, let stand to separate layers, and wash the lower organic layer with water , and dried to obtain intermediate (B) 161.9g, yield: 96.14%.

[0190] 2) Preparation of 1,2-dimethyl-5-oxindole-3-carboxyethyl ester

[0191] Dissolve 132.9g of p-benzoquinone in 1300mL of acetone in a reaction flask, stir evenly, heat to 45°C, add 160.0g of intermediate (B) dropwise under stirring, and continue to react for 2 hours. 2 / 3 of the solvent. After cooling to 0-5°C, the solid was obtained by filtration and dried to obtain 91.2 g of intermediate (C), yield: 35.0%.

[0192] 3) Preparation of 6-bromo-2-bromo...

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Abstract

The invention relates to the technical field of medicinal oral solid preparations, in particular to a medicinal composition of a methanesulfonic acid arbidol oral solid preparation serving as an anti-influenza virus medicament. The composition exists in the form of film-coated tablets, dispersible tablets, chewable tablets, capsules or particles; the film-coated tablets, dispersible tablets, chewable tablets, capsules or particles consist of an effective dosage of methanesulfonic acid arbidol and excipient; and the excipient contains organic acid for enhancing the stability of the medicinal composition, and contains more than three of a diluent, a bonding agent, a disintegrating agent, a flavoring agent and a lubricant. The medicinal composition has the advantages of stable mass, reasonable formula, application of nontoxic excipient, high safety, small using amount of auxiliary materials, capability of meeting the requirement of the oral solid preparation, quick dissolving of all dosage forms, medicament dissolving rate over 85 percent within 15 minutes, contribution to in-vivo absorption of the oral solid preparation and guarantee of better curative effect.

Description

technical field [0001] The invention relates to the technical field of oral pharmaceutical preparations, in particular to a pharmaceutical composition of an anti-influenza virus drug Arbidol mesylate oral solid preparation. Background technique [0002] At present, the antiviral chemical drugs used clinically in China mainly include arbidol hydrochloride, ribavirin, amantadine, rimantadine, oseltamivir, zanamivir, etc. Among them, ribavirin is active against influenza A and B viruses in large doses, but has teratogenic and mutagenic toxicity of nucleoside drugs, which can cause anemia and immunosuppression. Amantadine and rimantadine are only effective against influenza A, and are prone to drug resistance. Such drugs can also cause central nervous system toxicity, thereby reducing the clinical use value. The neuraminidase inhibitors oseltamivir and zanamivir are effective but expensive. [0003] Arbidol hydrochloride and its oral solid preparations (tablets, capsules, dis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4045A61K47/12A61P31/16C07D209/42C07C309/04C07C303/32
Inventor 樊迎春吴海燕史自东李瑛吴迪王菁烨
Owner HUBEI LIYI PHARM TECH CO LTD
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