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A solid pharmaceutical formulation

A formulation and drug technology, applied in the field of sustained-release solid pharmaceutical formulations, can solve the problems of not so good drug release performance and reducing the firmness of solid formulations

Inactive Publication Date: 2011-07-06
OTSUKA PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has the disadvantage of reducing solid formulation firmness and the drug release properties of administered starch-containing formulations are not so good

Method used

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  • A solid pharmaceutical formulation
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Corn starch (trade name: "Nisshoku Corn Starch", manufactured by Nippon Shokuhin Kako K.K.) (90 g), crystalline cellulose (trade name: "CEOLUS PH301", manufactured by Asahi Kasei Corporation) (30 g), hydroxypropyl acetate Athylmethylcellulose succinate (trade name: "AS-HF", manufactured by Shin-Etsu Chemical Co., Ltd.) (30 g) and cilostazol (manufactured by Otsuka Pharmaceutical Co., Ltd.) (150 g ) was mixed, the mixture was put into an accelerated kneader (model: NSK-150, manufactured by Okada Seiko K.K.), and then 37.5 mL of 4% polysorbate 80 aqueous solution (containing 1.5 g Polysorbate 80) and purified water (92.5 g) to obtain a starting composition (starting composition example 1).

[0070] The starting composition was subjected to extrusion granulation with an extrusion granulator equipped with a dome die (hole diameter: 0.6 mm, DomeGran DG-L1, manufactured by DALTON Co. LTD.) to obtain wet granules. The wet granules were treated with a spheroidizer (Murmerizer ...

Embodiment 2

[0073] Corn starch (trade name: "Nisshoku Corn Starch", manufactured by Nippon Shokuhin Kako K.K.) (90 g), crystalline cellulose (trade name: "CEOLUS PH301", manufactured by Asahi Kasei Corporation) (30 g), hydroxypropyl acetate Athylmethylcellulose succinate (trade name: "AS-HF", manufactured by Shin-Etsu Chemical Co., Ltd.) (30 g) and cilostazol (manufactured by Otsuka Pharmaceutical Co., Ltd.) (150 g ) was mixed, the mixture was put into an accelerated kneader (model: NSK-150, manufactured by Okada Seiko K.K.), and then 37.5 mL of 4% polysorbate 80 aqueous solution (containing 1.5 g Polysorbate 80) and purified water (67.5 g) to obtain a starting composition (starting composition example 2).

[0074] The starting composition was subjected to extrusion granulation with an extrusion granulator equipped with a dome die (hole diameter: 0.6 mm, DomeGran DG-L1, manufactured by DALTON Co. LTD.) to obtain wet granules. The wet granules were treated with a spheroidizer (Murmerizer ...

Embodiment 3

[0077] Corn starch (trade name: "Nisshoku Corn Starch", manufactured by Nippon Shokuhin Kako K.K.) (69 g), crystalline cellulose (trade name: "CEOLUS PH301", manufactured by Asahi Kasei Corporation) (51 g), methacrylic acid Copolymer L (trade name: "Eudragit L100", manufactured by EVONIK) (30 g) and cilostazol (manufactured by Otsuka Pharmaceutical Co., Ltd.) (150 g) were mixed, and the mixture was put into an accelerating kneader (model: NSK-150, manufactured by Okada Seiko K.K.), and purified water (130 g) was added thereto with stirring to obtain a starting composition (starting composition example 3).

[0078] The starting composition was subjected to extrusion granulation with an extrusion granulator equipped with a dome die (hole diameter: 0.6 mm, DomeGran DG-L1, manufactured by DALTON Co. LTD.) to obtain wet granules. The wet granules were treated with a spheroidizer (Murmerizer QJ-400, manufactured by DALTON Co. LTD.) to adjust the shape and size of the granules, there...

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Abstract

The present invention relates to a sustained-release solid pharmaceutical formulation comprising (a) an active medical ingredient, (b) a pre-gelatinized starch in an amount of 10 to 90 % by weight based on the whole weight of the formulation and (c) one or more kinds of enteric ingredients.

Description

technical field [0001] The present invention relates to a solid pharmaceutical formulation. More specifically, it relates to a sustained release solid pharmaceutical formulation comprising (a) an active pharmaceutical ingredient, in particular cilostazol, (b) a pregelatinized starch in an amount of 10-90% by weight, based on The total weight of the formulation, and (c) one or more enteric ingredients. Background of the invention [0002] Sustained-release solid pharmaceutical formulations are useful formulations because it is possible to control the blood concentration of the active ingredient, to modify the dosing conditions (e.g. reduce the frequency of dosing), to increase the active ingredient (which has a short duration in living organisms). half-life), to reduce the side effects of the active ingredient (whose concentration difference between the minimum blood concentration and the side effect onset concentration is small), etc. [0003] Cilostazol is 6-[4-(1-cyclohe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4709
CPCA61K9/1652A61K9/1694A61K31/4709A61K9/1635A61P11/06A61P29/00A61P7/02A61P9/00A61P9/10A61P9/12A61P9/14
Inventor 向井正志
Owner OTSUKA PHARM CO LTD
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