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Controlled-release composition for producing sustained-release preparation containing udenafil

A technology of Udenafil and sustained-release preparations, applied in the field of controlled-release compositions, to achieve the effects of reducing drug-related side effects, improving particle stickiness, and reducing deviations between individuals

Inactive Publication Date: 2012-01-04
DONG A PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Republic of Korea Laid-Open Patent Publication No. 2004-83492 discloses an osmotic delivery system, Republic of Korea Laid-Open Patent Publication No. 2002-70330 discloses a hydrogel-based pharmaceutical dosage form, and International Laid-Open Patent Publication No. 2007 / 057762 discloses a controlled-release formulation. , but the controlled-release preparation needs to be coated with an insoluble water-permeable coating after multiple tablet compression processes, and finally undergoes complicated and critical processes such as laser perforation

Method used

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  • Controlled-release composition for producing sustained-release preparation containing udenafil
  • Controlled-release composition for producing sustained-release preparation containing udenafil
  • Controlled-release composition for producing sustained-release preparation containing udenafil

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～4

[0050] The present invention is used to prepare the controlled-release composition containing udenafil sustained-release preparation and its preparation Preparation of the agent

[0051] 1) Manufacture of adsorbent particles for the preparation of controlled release compositions

[0052] Using the components of Examples 1 to 4 described in Table 1 below, adsorbent particles for the production of udenafil controlled-release compositions were produced.

[0053] Specifically, after dissolving Udenafil and citric acid with an appropriate amount of water, the silicon dioxide was then put into a high-speed mixer and the previously prepared Udenafil-citric acid solution was slowly dropped in, the ingredients Adsorbed evenly on the silica surface. The adsorbed particles are put into a high-speed dryer, dried at a temperature of 60 degrees for 30 minutes, and then pulverized.

[0054] 【Table 1】

[0055] Unit: g

[0056]

[0057] 2) Preparation of controlled release composit...

Embodiment 5-12

[0063] The present invention uses various polymers for the preparation of sustained-release formulations containing Udenafil Controlled-release compositions and preparations of formulations

[0064] After the adsorption particles were prepared according to the method of 1) of Example 1 to Example 4, Udenafil was prepared in the same manner as 2) and 3) of Example 1 to Example 4 according to the composition described in Table 3 below. Controlled release formulations and as Examples 5 to 12.

[0065] 【table 3】

[0066]

experiment example 1

[0075] Observation of particle fluidity

[0076] In order to confirm whether granules suitable for the preparation of controlled-release preparations could be formed, the granulation degree of the granules produced in 1) of Examples 1 to 4 and the granules produced in Comparative Examples 1 and 2 was visually evaluated using Pharmatest Co., Ltd. The PTG-S3 measures the time for 100 ml of particles to pass through a hole of a certain size and evaluates the particle flowability after drying.

[0077] As shown in Table 6, in Examples 1 to 4 of the present invention in which the Udenafil-citric acid solution was adsorbed and granulated by silica, the particles were in good shape and had good fluidity after drying; However, when granulation was carried out using a general excipient for granules as in Comparative Examples 1 and 2, it was difficult to granulate because of stickiness, and the fluidity after drying was also poor.

[0078] 【Table 6】

[0079] unit

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Abstract

The present invention relates to a controlled-release composition for producing a sustained-release preparation containing udenafil. More particularly, the present invention relates to a controlled-release composition for producing a sustained-release preparation containing udenafil, said composition comprising (A) udenafil and a pharmaceutically acceptable salt, (B) a solubility modulator, (C) an adsorbent, and (D) a hydrophilic polymer. The controlled-release composition for producing a sustained-release preparation containing udenafil according to the present invention releases drugs constantly regardless of the pH level in the gastrointestinal tract, and thus freely controls the drug release time within the range of 3 to 24 hours, and reduces the variability in the effect of drugs among individuals. In addition, the composition of the present invention can be produced into a sustained-release preparation which has an optimum condition for expressing the effect of drugs in the treatment of diseases such as pulmonary arterial hypertension, hepatic portal vein hypertension, benign prostatic hyperplasia, and the like, which can be treated by udenafil and which requires the administration of drugs over a long period of time. Further, the composition of the present invention can control the release of drugs in accordance with the time taken for the absorption thereof when said drugs are applied to a living body, and thus can be valuably used in preventing and treating erectile dysfunction.

Description

【Technical field】 [0001] The present invention relates to a controlled-release composition for preparing a sustained-release preparation containing udenafil. 【Background technique】 [0002] A pyrazolopyrimidinone compound (3-(1-methyl-7-oxo-3-propyl-4,7-dihydro-1H-pyrazolo[4,3-d) represented by the following Chemical Formula 1 ]pyrimidin-5-yl)-N-[2-(1-methylpyrrolidin-2-yl)ethyl]-4-propoxybenzenesulfonamide (3-(1-methyl-7-oxo-3 -propyl-4,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-N-[2-(1-methylpyrrolidin-2-yl)ethyl]-4-propoxybenzenesulfona mide), following "Udenafil" for short) is a phosphodiesterase type 5 inhibitor (hereinafter referred to as "PDE-5 inhibitor"), and is also a commercially available treatment for erectile dysfunction (erectile dysfunction). Taste. [0003] <Chemical formula 1> [0004] [0005] As a drug, Udenafil has strong inhibitory activity against PDE-5 and excellent selectivity, rapid absorption, high bioavailability and large volume of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/519A61K9/22
CPCA61K9/2054A61K31/519A61K9/2031A61P9/12A61P11/00A61P13/00A61P13/08A61P15/10A61K9/20A61K47/50
Inventor 刘武姬车奉晋金桢薰张善瑀韩相德
Owner DONG A PHARMA
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