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Slow-release cilostazol tablet having an improved elution rate and minimal side effects

一种西洛他唑片剂、西洛他唑的技术，应用在非有效成分的医用配制品、含有效成分的医用配制品、丸剂输送等方向，达到长溶出时间、头痛低的效果

Active Publication Date: 2012-07-04
KOREA UNITED PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Conventional cilostazol tablets cause side effects such as headache, tachycardia, and heaviness due to their high dissolution rate immediately after administration

Method used

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  • Slow-release cilostazol tablet having an improved elution rate and minimal side effects
  • Slow-release cilostazol tablet having an improved elution rate and minimal side effects
  • Slow-release cilostazol tablet having an improved elution rate and minimal side effects

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Sustained release tablets were prepared using the following method using the formulation listed in Table 1 below. First, Povidone K-30 and Carbomer (50%) were dispersed and dissolved in ethanol to prepare a binder solution. Next, cilostazol, microcrystalline cellulose, carbomer (50%), and hydroxypropyl methylcellulose were mixed thoroughly using a high-speed mixer, and then granulated in a cylindrical granulator using a binder solution. Made into wet granules. The prepared granules were dried in a drying oven (40° C.) for 12 hours, and then passed through a 40-mesh sieve. Afterwards, light anhydrous silicic acid and magnesium stearate were further mixed with the sieved semi-finished product, and formed into tablets, whereby one tablet could reach the weights listed in Table 1 below. The sustained-release cilostazol tablets prepared as in the following examples with a constant content were subjected to a dissolution test according to the method described in Korean Herb...

Embodiment 2

[0054] The formulations listed in Table 5 below were prepared in the same manner as in Example 1 except that the ingredients listed in Table 5 below were used.

[0055] table 5

[0056]

[0057] Table 6

[0058]

Embodiment 3

[0060] The formulations listed in Table 7 below were prepared in the same manner as in Example 1, except that the ingredients listed in Table 7 below were used.

[0061] Table 7

[0062]

[0063] Table 8

[0064]

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PUM

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Abstract

The present invention relates to a slow-release tablet of cilostazol which is a pharmacologically active component efficacious in the suppression of blood platelet aggregation and the promotion of vascular relaxation by inhibiting phosphodiesterase types; and, more specifically, provided is a slow-release cilostazol tablet of which the elution time is extended such that it can be taken once a day for expediency of drug-taking, and which minimises the occurrence of headache which is a side effect during the taking of cilostazol preparations of the prior art and therefore improves the convenience of drug-taking for women, the elderly and children. Also provided is a slow-release cilostazol tablet which exhibits a stable elution pattern without any variation in the percentage eluted depending on the pH in the stomach in addition to an effect whereby release of the drug is delayed, by using a release-controlling polymer consisting of a mixture of hydroxypropyl methyl cellulose and a carbomer.

Description

technical field [0001] The present invention relates to a sustained-release tablet comprising cilostazol as a pharmacologically active ingredient prepared using a release-controlling polymer, more specifically, the present invention relates to a sustained-release cilostazol tablet, the tablet Enables once-daily dosing and improves tablet convenience by controlling the dissolution rate of stable cilostazol during pH changes to reduce side effects of cilostazol such as headache, heaviness, and tachycardia sex. Background technique [0002] As a quinolinone compound, cilostazol (6-[4-(cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone : Chemical formula 1) has the effect of inhibiting platelet aggregation and promoting vasodilation by inhibiting phosphodiesterase types. In addition, cilostazol is known to prevent diseases such as arteriosclerosis by inhibiting the growth of vascular smooth muscle cells that migrate to vascular endothelial cells. [0003] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/41A61K47/38A61P7/02A61P9/10
CPCA61K9/2054A61K31/4709A61K9/2027A61K9/2095A61K47/38A61K47/32A61P7/02A61P9/10
Inventor 崔然雄闵炳九赵相珉
Owner KOREA UNITED PHARMA
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