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Pharmaceutical composite formulation comprising hmg-oa reductase inhibitor and aspirin

A reductase inhibitor and aspirin technology is applied in the field of pharmaceutical compound preparations containing HMG-COA reductase inhibitors and aspirin, and can solve the problems of affecting the degradation of HMG-CoA reductase inhibitors and hindering the quality verification of compound preparations.

Inactive Publication Date: 2013-09-04
HANMI SCI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the quality verification of combination preparations, it was observed that aspirin (or salicylic acid derived from aspirin) affects the degradation of HMG-CoA reductase inhibitors under acidic conditions, which hinders accurate quality verification of combination preparations

Method used

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  • Pharmaceutical composite formulation comprising hmg-oa reductase inhibitor and aspirin
  • Pharmaceutical composite formulation comprising hmg-oa reductase inhibitor and aspirin
  • Pharmaceutical composite formulation comprising hmg-oa reductase inhibitor and aspirin

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0071] Preparation Example 1: Preparation of Atorvastatin Granules

[0072] According to the components described in Table 1, atorvastatin calcium (Dr. Reddy's Laboratories Ltd., India), croscarmellose sodium (DMV International) and magnesium carbonate (Tomita, Japan) were mixed. The mixture was then kneaded with a binding solution of HPC and polysorbate 80 (Croda, USA) dissolved in water, dried, and subsequently sieved through a 40 mesh (passable size of particles, sieve size 425 μm) mesh to obtain wet granules, followed by mixing the resultant and magnesium stearate to prepare atorvastatin granules. The average particle size of the particles thus obtained was determined by a particle size image analyzer (Qicpic, Sympatec, X50), which was 400 μm.

[0073]

[0074] Components of atorvastatin granules (unit: mg)

[0075] components

preparation Embodiment 2

[0076] Preparation Example 2: Preparation of the first aspirin pellets

[0077] Aspirin (Spectrum Chemical, USA), hydroxypropylmethylcellulose (HPMC) (Shinetsu, Japan), citric acid, polyethylene glycol, and talc were dissolved in water and acetone according to the components described in Table 2. mixture to obtain a coating solution containing aspirin. The coating solution thus obtained was sprayed onto microcrystalline spherical beads (Pharmatrans Sanaq, Switherland) in a fluidized bed coater (NQ-125, Fujipaudal, Japan) to obtain aspirin-containing pellets. In Preparation Examples 2-1 to 2-3, various particles were prepared by respectively using MCC101 (bead diameter 50 μm), MCC102 (bead diameter 100 μm), and MCC200 (bead diameter 180 μm) as microcrystalline spherical beads diameter pellets.

[0078]

[0079] Components of the first aspirin pellet (unit: mg)

[0080]

[0081]

preparation Embodiment 3

[0082] Preparation Example 3: Preparation of Second Aspirin Pellets with Enteric Coating Layer

[0083] According to the components described in Table 3, the first aspirin pellets prepared in Preparation Example 2 were coated with an enteric coating layer. Hydroxypropyl methylcellulose phthalate (HPMCP) (Shinetsu, Japan), Myvacet, talc, and TiO 2 Dissolve and disperse in a mixture of ethanol and acetone to prepare an enteric coating solution. The enteric coating solution was sprayed onto the first aspirin pellets prepared in Preparation Example 2 in a fluidized bed coater (NQ-125, Fujipaudal, Japan). The resultant was then dried to obtain pellets having an enteric coating layer (Preparation Examples 3-1 to 3-3).

[0084]

[0085] Composition of the second aspirin pellet with enteric coating layer (unit: mg)

[0086]

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Abstract

Provided is a pharmaceutical composite formulation for preventing or treating cardiovascular diseases, which comprises (1) a first particle comprising an HMG-CoA reductase inhibitor and a basic additive; and (2) a second particle comprising a core containing aspirin and an enteric coating layer coated on said core, wherein the difference in the average diameters of said first and second particles is 100 [mu]m to 800 [mu]m; a method for preparing same; and a method of validating the quality of same. The pharmaceutical composite formulation according to the present invention can improve the stability of an active ingredient and prevent adverse impacts between the active ingredients to thereby enable an accurate quality validation of the pharmaceutical composite formulation.

Description

technical field [0001] The present invention relates to a pharmaceutical compound preparation comprising an HMG-CoA reductase inhibitor and aspirin for the prevention or treatment of cardiovascular diseases, which has improved stability and allows accurate quality verification. Background technique [0002] Hyperlipidemia represents a condition in which the level of lipids (such as cholesterol, triglycerides, etc.) in the plasma is abnormally elevated. Hyperlipidemia, especially hypercholesterolemia, induces arterial thrombosis, leading to arteriosclerosis, in which the walls of arteries become thickened due to the accumulation of lipids. Arteriosclerosis is clinically important because it can lead to cardiovascular diseases such as ischemic heart disease, angina pectoris, and myocardial infarction. Arteriosclerosis can be prevented by treating hypercholesterolemia because the latter is closely and highly related to the former. [0003] Hyperlipidemia, or elevated levels o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K9/24A61K31/60A61P9/00
CPCA61K31/22A61K31/366A61K31/40A61K31/405A61K31/47A61K31/505A61K31/616A61K45/06A61K9/1611A61K9/1676A61K9/4808A61K9/5042A61K9/5047A61K9/5078A61K9/5084A61P3/06A61P43/00A61P7/02A61P9/00A61P9/10A61K2300/00A61K9/16G01N33/15
Inventor 金用镒罗荣俊崔俊荣金珉贞禹钟守朴宰贤
Owner HANMI SCI CO LTD