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Pranlukast solid dispersion and preparation method thereof

A solid dispersion and carrier technology, applied in the directions of active ingredients of heterocyclic compounds, drug combinations, respiratory diseases, etc., can solve the problems of low bioavailability, poor viscosity and water solubility, achieve good reproducibility, reduce pollution, reduce The effect of energy consumption

Inactive Publication Date: 2014-04-30
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Pranlukast is a drug with very strong viscosity and poor water solubility, and its bioavailability is low when administered orally. Patients need to take a large amount of drugs to cause economic losses. It is urgent to develop a preparation that improves the oral absorption rate.

Method used

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  • Pranlukast solid dispersion and preparation method thereof
  • Pranlukast solid dispersion and preparation method thereof
  • Pranlukast solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Pranlukast 10% lactose 50% microcrystalline cellulose 39% Colloidal silica 0.5% Magnesium stearate 0.5%

[0021] Preparation Process:

[0022] The vilazodone hydrochloride, lactose, and microcrystalline cellulose passed through an 80-mesh sieve are uniformly mixed, and then colloidal silicon dioxide and magnesium stearate are added and mixed to form tablets with a weight of about 200 mg.

[0023]

Embodiment 2

[0025]

[0026] Preparation Process:

[0027] Put PEG6000 in a 70°C water bath and heat to melt. Dissolve pranlukast in dichloromethane-methanol solution containing surfactant, dissolve it completely by heating, add this solution into the melted solid medium, and mix well. The solvent of the above mixture is dried by spray drying or vacuum drying. After cooling, place it in a mortar and grind it properly to obtain the solid dispersion of pranlukast. The obtained solid dispersion was added with lactose, MCC, and magnesium stearate, mixed uniformly, and then pressed into tablets, with a tablet weight of about 200 mg.

[0028]

Embodiment 3

[0030]

[0031] Preparation Process:

[0032] Put hydroxypropyl cellulose in a 70°C water bath and heat to melt. Dissolve pranlukast with dichloromethane-methanol solution containing sorbitan ester, dissolve it completely by heating, add this solution into the melted solid medium, and mix well. The solvent of the above mixture is dried by spray drying or vacuum drying. After cooling, place it in a mortar and grind it properly to obtain the solid dispersion of pranlukast. The obtained solid dispersion was added with lactose, MCC, and magnesium stearate, mixed uniformly, and then pressed into tablets, with a tablet weight of about 200 mg.

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Abstract

The invention relates to pranlukast solid dispersion and a preparation method thereof, belonging to the field of pharmaceutical preparations. Particularly, the invention provides solid dispersion and a pharmaceutical composition. The solid dispersion is composed of pranlukast, a water-soluble polymer and a surface active agent; and the pharmaceutical composition is composed of pharmaceutically acceptable carriers. The solid dispersion disclosed by the invention is capable of increasing solubility of medicines, improving viscidity of pranlukast and prompting absorption, and therefore, dissolution rates and bioavailability of medicines are increased.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a solid dispersion composition of prankast capable of improving the dissolution rate and bioavailability of medicines and a preparation method thereof. Background technique [0002] Pranlukast (chemical name 4-oxo-8-[4-(4-phenylbutoxy)benzamido]-2-(tetrazol-5-yl)-4H-1benzopyran hemihydrate Compound) is a strong antagonist against leukotriene C4 (LTC4) and leukotriene D4 (LTD4), and is used as a therapeutic agent for bronchial asthma and allergic rhinitis, and has a wide range of applications. [0003] Pranlukast is a drug with very strong viscosity and poor water solubility. Its oral bioavailability is low, and patients need to take a large amount of drugs to cause economic losses. There is an urgent need to develop a preparation that improves the oral absorption rate. [0004] Therefore preparing solid preparations such as tablets, capsules, granules, and powders...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/41A61P11/06A61P11/02A61P37/08
Inventor 鲍晶晶刁媛媛傅雪猛郭夏
Owner BEIJING VENTUREPHARM BIOTECH
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