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Process for producing a pharmaceutical solid preparation containing a poorly soluble drug

a technology of solid preparation and drug, which is applied in the field of pharmaceutical solid preparation containing a poorly soluble drug, can solve the problems of organic solvent residue, environmental pollution by organic solvents, and safety in operation, and achieve excellent improvement of drug dissolution, improved dissolution, and improved dissolution

Inactive Publication Date: 2005-07-21
SHIN ETSU CHEM IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0009] According to the present invention, a solid solution preparation of a poorly soluble drug can be simply prepared using the existing equipment and without use of an organic solvent. Also, preparation of the present invention has the improved dissolution of a poorly soluble drug compared to the solid dispersion obtained by the conventional physically mixed method, and has solubility equivalent to the solid dispersion obtained by the conventional solvent method.

Problems solved by technology

However, in this solvent method, because organic solvents such as dichloromethane, acetone and alcohol are frequently used, considerable problems have arisen, including problems of organic solvents residue in products, environmental pollution by organic solvents and safety in operation, and corporate problems such as capital investment required to avoid such concerns.

Method used

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  • Process for producing a pharmaceutical solid preparation containing a poorly soluble drug
  • Process for producing a pharmaceutical solid preparation containing a poorly soluble drug

Examples

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example 1

[0032] The poorly soluble drug, nifedipine (10 g)(supplied by Daito Co., Ltd.) was dissolved in a mixture solution of the plasticizer, polyethylene glycol 400 (96 g) and triethyl citrate (4 g) to make Spray A solution. As the water-soluble polymer solution, a dispersion made of 6 g of talc, 0.2 g of sodium lauryl sulfate and 107.1 g of purified water for 20 g of hydroxypropylmethylcellulose acetate succinate (HPMCAS)(AS-MF: supplied by Shin-Etsu Chemical Co. Ltd.) was prepared to make Spray B solution. Lactose (200 g) (lactose 200M: supplied by DMV Co., Ltd.) was fluidized in a fluidized-bed granulation machine (equipment name: Multiplex: supplied by Freund Industrial Co., Ltd.: Multiplex MP-01), and both Spray A and B solutions were sprayed to granulate in a manner of side spraying using three fluid nozzles (spray gun) shown in FIG. 1. Spray A solution, Spray B solution and compressed air were supplied to three fluid nozzles by a tube pump from the outside. Solutions A and B and co...

example 2

[0043] Granulation was carried out to obtain the nifedipine containing preparation in the same manner as that in Example 1, except that the aqueous solution of the water-soluble polymer was made by dissolving 20 g of hydroxypropylmethylcellulose (TC-5R: supplied by Shin-Etsu Chemical Co. Ltd.) in 180 g of purified water to render Spray B solution.

example 3

[0044] Granulation was carried out to obtain the nifedipine containing preparation in the same manner as that in Example 1, except that 200 g of lactose in Example 1 were replaced with the mixed powder of 170 g of lactose and 30 g of Hydrated Silicon-Dioxide (Carplex #80: supplied by Shionogi & Co. Ltd.).

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Abstract

Among the conventional processes for producing solid dispersion, the solid dispersion obtained by a solvent method is excellent in terms of solubility and bioavailability of a poorly soluble drug. However, due to frequent uses of organic solvents in the solvent method, problems have arisen such as organic solvent residue in products, environmental pollution and operational safety as well as corporate problems such as capital investment and the like required to avoid such events. The present invention provides a process for preparing pharmaceutical solid preparations without use of organic solvents frequently used in conventional solvent methods. Specifically, the present invention provides a process for producing a pharmaceutical solid preparation, which is formulated by spraying a solution wherein a poorly soluble drug is dissolved in a plasticizer, and an aqueous solution and / or water dispersion of a water-soluble polymer from nozzle outlets simultaneously and separately in the process for producing the pharmaceutical solid preparation.

Description

BACKGROUND OF THE INVENTION [0001] 1. Field of the Invention [0002] The present invention relates to a pharmaceutical solid preparation containing a poorly soluble drug for the purpose of improvement of dissolution and a process for the production thereof, and more particularly, to the pharmaceutical solid preparation obtained by delivering and discharging / spraying an aqueous solution and / or a water dispersion of a water soluble polymer as well as a plasticizer solution wherein a poorly soluble drug is dissolved, from nozzle outlets simultaneously and separately, and the process for the production thereof. [0003] 2. Description of the Invention [0004] In light of efficiency and safety, it has been regarded as important that significantly high bioavailability is set in the designs for pharmaceutical solid preparations. One of important factors which affect bioavailability of medicines includes solubility of drugs, and numerous studies have been carried out regarding the relationship ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61J3/06A61K9/14A61K9/16A61K31/4422A61K47/10A61K47/14A61K47/32A61K47/38
CPCA61K9/1676A61K9/143A61K9/145A61K9/1652A61K9/1617A61K9/1623A61K9/146
Inventor TANNO, FUMIENISHIYAMA, YUICHI
Owner SHIN ETSU CHEM IND CO LTD
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