Preparation and application of drug powder

Abstract

Belonging to the field of pharmaceutical preparations, the invention provides a preparation method for a drug A (formula 1) powder and its application in oral solid preparations. The method includes: dispersing the crude drugs of drug A in a hydrophilic suspending aid solution, employing wet grinding to reduce the particle size to less than 5 micrometers, adding a spray-drying support agent, and combining spray drying, thus obtaining the drug A powder with an average particle size of less than 20 micrometers. The drug A powder prepared by the invention has high surface hydrophilicity, small particle size and good redispersibility in water. Compared with the crude drugs, the oral solid preparations prepared from the drug A powder and suitable auxiliary materials can significantly improve the dissolution rate. The preparation method for the drug A powder provided by the invention is suitable for industrial production and has high application value. (formula I).

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations and relates to a drug A (2-ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazole-3 -yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid) powder and its preparation and application, specifically through wet grinding combined with spray drying to prepare a surface coated with hydrophilic The suspending agent is covered, and there are water-soluble auxiliary materials between the powders to support the drug A powder, and its application in oral solid preparations. [0002] Background technique [0003] Hypertension is the most common chronic disease and one of the most important predisposing factors for cardiovascular and cerebrovascular diseases. Every year, tens of millions of people in the world suffer from complications such as coronary heart disease, cerebral infarction, chronic renal failure and heart disease due to high blood pressure, and even death in severe cases. [0004...

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Problems solved by technology

[0006] But the above-mentioned method for improving the dissolution rate of drug A all has obvious deficiencies: in CN102793680A, since drug A is a large dose of medicine, a large amount of hydrophilic carrier (drug: carrier=1:4- 1:10), the quality of the prepared solid preparation is relatively large, it is difficult to swallow, and the patient's compliance is poor

In addition, solid dispersions are prone to moisture absorption and aging, which reduces the dissolution rate, and there are still problems such as organic solvent residues

[0007] In CN102580097A, although the jet pulverization can reduce the average particle size of the drug to within 5 μm, compared with the drug A powder with the same particle size prepared in the present invention, the absorption window pH range (pH5.4-6.0) Dissolution rate is low ( figure 1 , figure 2 )

[0008] In CN101528262A, compared with the high-viscosity binder, the dissolution rate of drug A is improved by using the low-viscosity binder after granulation and tableting, but the low-viscosity binder cannot reduce the particle size of drug A, and it is difficult to Avoid Agglomeration of Hydrophobic Drug A During Tabletting

[0009] Those skilled in the art have used a large amount of methods, but still can not overcome the defective of prior art

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