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Controlled release preparation containing cilostazoland process for the preparation thereof

A controlled-release preparation, the technology of cilostazol, which is applied in the field of controlled-release preparations of cilostazol, can solve the problems of large daily dose, inconvenience for patients to take comfortably, and complicated preparation methods

Inactive Publication Date: 2010-01-20
AMOREPACIFIC CORP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these dosage forms have problems that the preparation method is very complicated, and the daily dose required for the dosage form becomes too large to be convenient for patients to take the medicine comfortably

Method used

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  • Controlled release preparation containing cilostazoland process for the preparation thereof
  • Controlled release preparation containing cilostazoland process for the preparation thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0017] Preparation of drug granules

[0018] In step (1) according to the present invention, cilostazol or a pharmaceutically acceptable salt thereof is mixed with a solubilizer, and the resulting mixture is subjected to a solid dispersion method to obtain particles in which the drug is uniformly dispersed.

[0019] The solid dispersion method can be any conventional melting or solvent method. Where the melting method is used, solubilized drug particles can be prepared by mixing cilostazol with a solubilizing agent, heating the mixture until either the cilostazol or the solubilizing agent does not melt to result in cilostazol The temperature of the molecular level mixing of azole and solubilizing agent, slow cooling of the mixture to form solid clusters, and processing of the solid clusters to obtain particles of the desired size. When the solvent method is used, the surface of the cilostazol-containing particles is modified by a solubilizing agent, which can be prepared by ...

Embodiment 1 to 9

[0055] Examples 1 to 9: Preparation of Tablets of Cilostazol-(1)

[0056] Put cilostazol in a high-speed planetary swing mixer, and slowly add sodium lauryl sulfate and hydroxypropylcellulose-L dissolved in ethanol to cilostazol undergoing high-speed rotation to obtain granules . Subsequently, the granules thus obtained are mixed with hydroxypropylmethylcellulose, croscarmellose sodium or crospovidone, lactose, microcrystalline cellulose and calcium hydrogen phosphate, and further added to the mixture Add hydroxypropylcellulose-L dissolved in ethanol. The resulting mixture was washed and passed through a 14-mesh sieve to obtain granules, which were dried, further filtered through a 18-mesh sieve, and a magnesium stearate lubricant was added thereto. Then, the resulting mixture is compressed to obtain tablets. The amount of each component used is shown in Table 1.

[0057] Table 1

[0058]

Embodiment 10

[0066] Example 10: Preparation of tablets containing cilostazol-(3)

[0067] Cilostazol was mixed with sodium lauryl sulfate dissolved in ethanol, and the mixture was dried to form a solid mass. The material was milled and passed through a 20 mesh screen to obtain granules. Subsequently, the particles were mixed with microcrystalline cellulose and propylene glycol alginate, and hydroxypropylcellulose-L dissolved in ethanol was further added to the mixture. The resulting mixture was washed and passed through a 14-mesh sieve to obtain granules, which were dried, further filtered through a 18-mesh sieve, and a magnesium stearate lubricant was added thereto. Then, the resulting mixture is compressed to obtain tablets. The amount of each component used is shown in Table 3.

[0068] table 3

[0069] Composition (mg)

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Abstract

A controlled release preparation which comprises particles containing cilostazol or its pharmaceutically acceptable salt dispersed in a solubilizing agent and an erodible material encasing said particles which is capable of forming a hydrogel, can maintain a constant level of cilostazol in the blood through its slow release during its prolonged residence time in the stomach and intestines, thereby minimizing adverse effects caused by rapid release of the drug or solubilizing agent.

Description

technical field [0001] The present invention relates to controlled release formulations of cilostazol and methods of preparing said formulations. Background technique [0002] Cilostazol is a typical intracellular cAMP PDE (cyclic AMP phosphodiesterase) inhibitor, and it has been known that it inhibits platelet aggregation and dilates arteries by inhibiting PDE activity. It plays an important role in anti-inflammatory and anti-ulcer effects, lowering blood pressure, prevention and treatment of asthma and cerebral infarction, and improvement of cerebral circulation. [0003] Cilostazol has poor water solubility (1 μg / ml or less), and it has been demonstrated that orally administered cilostazol is absorbed primarily in the upper gastrointestinal (GI) tract and its absorption occurs as it moves to the lower GI tract reduce. Because the conventional controlled-release dosage form of cilostazol has a limitation on the absorption time at the desired absorption site, the current ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10
CPCA61K9/2013A61K9/1694A61K9/1635A61K9/205A61K9/1652A61K9/2018A61K31/4709A61K9/2077A61K9/2027A61K9/2009A61K9/2054A61P7/02A61P9/10A61K9/10A61K9/16
Inventor 朴晋佑申光炫权珉贞裴埈浩全焘容
Owner AMOREPACIFIC CORP
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