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Controlled-release preparation containing cilostazol and process for the preparation thereof

A technology of cilostazol and controlled-release preparations, which is applied in the field of controlled-release preparations containing cilostazol and its preparation, which can solve the problems of complex preparation methods, irregular absorption rates, and difficulty in taking drugs for patients

Inactive Publication Date: 2010-01-27
AMOREPACIFIC CORP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this dosage form has the following problems: the rapid release of the drug in the lower small intestine and colon can cause mucosal damage; the absorption rate of the poorly soluble drug becomes irregular in the lower small intestine and colon where the water content is low; The method of its preparation is very complicated; and the large daily dose of the dosage form makes it difficult for patients to take the drug

Method used

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  • Controlled-release preparation containing cilostazol and process for the preparation thereof
  • Controlled-release preparation containing cilostazol and process for the preparation thereof
  • Controlled-release preparation containing cilostazol and process for the preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 and comparative example 1 to 3

[0056] Example 1 and Comparative Examples 1 to 3: Preparation of Matrix Tablets Containing Cilostazol

[0057] Using the ingredients shown in Table 1, the cilostazol matrix tablets of Example 1 and Comparative Examples 1 to 3 were prepared as follows.

[0058] Table 1

[0059] Element

[0060] A mixture of cilostazol, sodium lauryl sulfate, croscarmellose sodium or crospovidone, and lactose was granulated, and an ethanol solution of hydroxypropylcellulose was added thereto and mixed. The resulting granules were classified using a 14-mesh sieve, dried, and the granules passed through were further classified using a 18-mesh sieve, and the granules passed through the sieve were mixed with: polyethylene oxide (molecular weight: 5,000,000) and light anhydrous silicon acid (Comparative Examples 1 to 3); or polyethylene oxide (molecular weight: 5,000,000), light anhydrous silicic acid, citric acid, and sodium bicarbonate (Example 1). After magnesium stearate was added th...

Embodiment 2 to 11

[0073] Examples 2 to 11: Preparation of matrix tablets comprising cilostazol

[0074] Cilostazol matrix tablets of Examples 2 to 11 were prepared as follows using the ingredients shown in Tables 4a and 4b.

[0075] Table 4a

[0076] Element

[0077] citric acid

[0078] Table 4b

[0079]

[0080] A mixture of cilostazol, sodium lauryl sulfate, croscarmellose sodium or crospovidone, and lactose was granulated, an ethanol solution of hydroxypropylcellulose-L was added thereto, and mix. The obtained granules were classified using a 14-mesh sieve, dried and further classified using a 18-mesh sieve, and the granules passed through the sieve were mixed with the following: polyethylene oxide (molecular weight: 5,000,000), light anhydrous silicic acid, lemon acids and sodium bicarbonate. After magnesium stearate was added thereto, the resulting mixture was lubricated and formulated into tablets using a compounder to obtain a controlled release dosage...

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Abstract

The present invention relates to a controlled-release formulation comprising cilostazol and a method for preparing said formultion. The inventive controlled-release formulation comprising cilostazol or a pharmaceutically acceptable salt thereof, a solubilizing agent, a swelling agent, a swell-controlling agent and a gas generating material has advantages in that it maintains a constant cilostazol level in the blood through a slow release while it resides in the stomach and intestines over a long period of time, thereby increasing the absorption of cilostazol in the small intestine, the major absorption site of cilostazol, as well as minimizing adverse effects caused by rapid release and making it easy for a patient to take the drug.

Description

technical field [0001] The present invention relates to controlled release dosage forms comprising cilostazol and processes for the preparation of said dosage forms. Background technique [0002] Cilostazol is a typical intracellular cAMP PDE (cyclic AMP phosphodiesterase) inhibitor, and it has been known that it reduces platelet aggregation and dilates arteries by inhibiting PDE activity, and plays an important role in the inhibition of blood coagulation, promotion of central blood circulation, anti- It plays an important role in inflammation and anti-ulcer effects, 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 of the limited absorption time in the contr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/20A61K47/34A61K9/36A61K31/47
CPCA61K9/2013A61K9/2077A61K9/2054A61K9/205A61K9/2018A61K31/4709A61K31/47A61K9/0007A61K9/2027A61K9/2009A61K9/0065A61K9/2031A61P7/02A61P9/08A61P9/10A61P11/06A61P29/00A61P43/00A61K9/20
Inventor 朴晋佑申光炫宾圣娥李爀裴埈浩全焘容
Owner AMOREPACIFIC CORP
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