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Complex formulation of 3-hydroxy-3-methyl glutaryl coa reductase inhibitor and antihypertensive agent, and process for preparing same

A reductase inhibitor and anti-hypertensive technology, applied in pill delivery, drug combination, pharmaceutical formula, etc., can solve the problems that the therapeutic effect cannot be maintained for a long time, liver toxicity, etc.

Inactive Publication Date: 2007-12-19
HANMI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Caduet  (Pfizer), a commercially available atrovastatin-amlodipine combination dosage form, has the problem of rapid release of both drugs causing hepatotoxicity, while its therapeutic effect cannot be maintained for a long time

Method used

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  • Complex formulation of 3-hydroxy-3-methyl glutaryl coa reductase inhibitor and antihypertensive agent, and process for preparing same
  • Complex formulation of 3-hydroxy-3-methyl glutaryl coa reductase inhibitor and antihypertensive agent, and process for preparing same
  • Complex formulation of 3-hydroxy-3-methyl glutaryl coa reductase inhibitor and antihypertensive agent, and process for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 to 3 and comparative example 1

[0062] Examples 1 to 3 and Comparative Example 1: Preparation of Solid Dispersion

[0063]Simvastatin (Hanmi Fine Chemical Co., Ltd., Korea), MYRJ (ICI, USA), HPMC 2910 (viscosity: 3 to 15cps, Shin-Etsu, Japan), BHT (UENO Fine Chemical, USA) and light Quality anhydrous silicic acid (as a dispersant) was dissolved in a mixture of ethanol and dichloromethane according to the amounts described in Table 1, and each resulting mixture was spray-dried to obtain particles with an average particle size of 100 μm or less. solid dispersion. The solid dispersions of Examples 1 to 3 and Comparative Example 1 thus obtained are shown in Table 1.

[0064]

[0065] components

Embodiment 4 to 8

[0066] Examples 4 to 8: Preparation of sustained-release dosage forms for oral administration

[0067] According to the amounts described in Tables 2 to 4, respectively utilizing simvastatin, lovastatin or fluvastatin as active ingredients, together with MYRJ, HPMC 2910, BHT, and light anhydrous silicic acid, the procedure of Example 1 was repeated to obtain A solid dispersion is obtained. Then, each solid dispersion was mixed with xanthan gum (Kelco, USA), locust bean gum (Cesalpinia, Italy), propylene glycol alginate (ISP, USA), HPMC 2208 (viscosity: 4,000 to 100,000 cps, Shin -Etsu, Japan) and erythorbic acid were mixed for about 30 minutes; and sucrose fatty acid ester and light anhydrous silicic acid powder (finer than 40 mesh) were added and mixed for 5 minutes. Each of the resulting mixtures was molded into a block using a molding assembly, and the block was pulverized into particles having a mesh size ranging from 20 to 80. The granules are then formulated into tab...

Embodiment 9 to 11

[0074] Examples 9 to 11: Preparation of combination dosage forms for oral administration

[0075] Each sustained-release dosage form obtained in Examples 5, 7 and 8 was coated with Opadry  AMB (Colorcon) film. Amlodipine camphorsulfonate (Hanmi Fine Chemical Co., Ltd., Korea), HPMC 2910 (viscosity: 3 to 15 cps) and acetylated monoglyceride (Myvacet) were dissolved respectively according to the amounts described in Table 5 In a mixture of ethanol and dichloromethane, it was applied to the film-coated formulations described above.

[0076]

[0077] components

(mg / tablet)

Example 9

Example 10

Example 11

Sustained-release dosage form core

Example 5

Example 7

Example 8

Active into

Minute

Ammonium D-camphorsulfonate

Clodipine

7.9

7.9

7.9

coating agent

HPMC 2910

10

10

10

plasticizer

Myvacet

1.6

1.6

1.6

stabilizer ...

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Abstract

A complex formulation for oral administration comprising a sustained release formulation of an HMG-CoA reductase inhibitor and a film layer for rapid release of an anti-hypertensive agent, the film layer being coated on the sustained release formulation, can achieve improved therapeutic effects of the anti-hypertensive agent by promptly releasing it, while maintaining a constant drug level of the HMG-CoA reductase inhibitor in blood through a slow release. Accordingly, the complex formulation is useful for preventing and treating diseases such as hyperlipidemia, atherosclerosis, hypertension and cardiovascular disease.

Description

field of invention [0001] The present invention relates to a combined dosage form for oral administration comprising a sustained release dosage form of a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor and a rapid release film layer of an antihypertensive agent; and its preparation method. Background of the invention [0002] Hypercholesterolemia, a representative example of hyperlipidemia, is caused by elevated serum LDL (low-density lipoprotein)-cholesterol and total cholesterol levels, and in serum by reducing lipids especially LDL-cholesterol Treating hypercholesterolemia at low levels can reduce the risk of cardiovascular disorders leading to delayed progression of arteriosclerosis (American diabetes association, Diabetic care, 23 (suppl.), S57-565, 2000). Therefore, there have been many studies on lipid-lowering therapy to delay the progression of arteriosclerosis or alleviate arteriosclerosis in order to reduce the risk of cardiovascular disorders...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/366
CPCA61K31/366A61K9/205A61K9/209A61K31/4422A61K45/06A61P3/06A61P9/12A61K2300/00A61K9/00A61K31/44
Inventor 禹钟守池文爀金用镒
Owner HANMI PHARMA
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