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Complex formulation comprising aspirin coated with barrier containing hydrophobic additive, and hmg-coa reductase inhibitor

A technology of reductase inhibitor and hydrophobic additive, applied in the field of compound preparation, can solve problems such as adverse side effects, occurrence of gastric ulcer or gastric bleeding, adverse interaction and the like

Inactive Publication Date: 2012-10-17
HANMI SCI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Meanwhile, aspirin may exhibit adverse side effects such as gastric ulcer or gastric bleeding when it is released in the gastrointestinal tract, and when both aspirin and HMG-CoA reductase inhibitors are simultaneously released in the gastrointestinal tract, aspirin may interact with HMG - Adverse interaction with CoA reductase inhibitors

Method used

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  • Complex formulation comprising aspirin coated with barrier containing hydrophobic additive, and hmg-coa reductase inhibitor
  • Complex formulation comprising aspirin coated with barrier containing hydrophobic additive, and hmg-coa reductase inhibitor
  • Complex formulation comprising aspirin coated with barrier containing hydrophobic additive, and hmg-coa reductase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Preparation of Aspirin Pellets and Granules

[0040] Preparation of aspirin pellets

[0041] According to Table 1, aspirin (Spectrum Chemical, US), hydroxypropyl methylcellulose (HPMC; Shinetsu, Japan), citric acid, and talc (Nippon talc, Japan) were dissolved and dispersed in a mixed solution of water and ethanol to A coating solution containing aspirin was prepared. The coating solution was sprayed while fluidizing microcrystalline spherical beads (cellet; Pharmatrans) using a fluidized bed sprayer (NQ-125, Fuji Paudal, Japan) to prepare aspirin pellets.

[0042] Preparation of aspirin granules

[0043] According to Table 1, aspirin, microcrystalline cellulose (Avicel) (FMC biopolymer, US), citric acid and mannitol were mixed and kneaded using hydroxypropylmethylcellulose (HPC) dissolved in water and ethanol, followed by Extruded using an extruder (MG-55, Dalton, Japan). Then, the extruded product was spheronized using a spheronizer (Q-230T, Dal...

Embodiment 2 to 7

[0046] Examples 2 to 7: Coating with barrier agent containing hydrophobic additive (1)

[0047] According to Table 2, the aspirin pellets or granules of Example 1 were coated with a barrier agent containing hydrophobic additives of various compositions. Specifically, HPMC, acetylated monoglyceride ( Kerry bio-sCience, US), talc, titanium dioxide (TiO 2 ) and hydrophobic additives (carnauba wax or ethylcellulose (EC, Colorcon)) were dissolved and dispersed in a mixed solution of water and ethanol to prepare a barrier agent coating solution. Then, each coating solution was sprayed while fluidizing aspirin pellets or granules (cellet; Pharmatrans) using a fluidized bed spraying machine (NQ-125, Fuji Paudal, Japan) to prepare aspirin pellets coated with a barrier agent. grain.

[0048]

[0049]

Embodiment 8 and comparative Embodiment 4

[0054] Example 8 and Comparative Example 4: Coating with barrier agent containing hydrophobic additive (2)

[0055] According to the same method as in Example 2 to Example 7, the pellets of Example and Comparative Example 3 were coated with a barrier agent containing a hydrophobic additive as shown in Table 4, respectively.

[0056]

[0057]

[0058]

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Abstract

Provided is a complex formulation for the prevention or treatment of cardiovascular diseases, comprising: a) aspirin coated with a barrier containing a hydrophobic additive; and b) an HMG-CoA reductase inhibitor, which has improved storage stability by preventing the deterioration in the stability of HMG-CoA reductase which is caused by salicylic acid, thereby being used in the treatment of hypertension and hypercholesterolemia.

Description

technical field [0001] The present invention relates to a compound preparation for preventing or treating cardiovascular diseases, comprising a) aspirin coated with a barrier containing a hydrophobic additive, and b) an HMG-CoA reductase inhibitor. Background technique [0002] Hyperlipidemia is a condition in which the levels of lipids (such as cholesterol, triglycerides, etc.) in the plasma are abnormally elevated. Hyperlipidemia, especially hypercholesterolemia, induces arterial thrombosis and leads to arteriosclerosis. Arteriosclerosis refers to the thick accumulation of lipids in blood vessels. It is clinically important because it contributes to cardiovascular diseases such as ischemic heart disease, angina pectoris and myocardial infarction. Prevention of arteriosclerosis can be achieved by treating hypercholesterolemia which is highly related to it. [0003] HMG-CoA reductase inhibitors have been used to treat hyperlipidemia for decades. Such compounds are known t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/60A61K31/505A61K31/40A61P9/00
CPCA61K9/1652A61K31/505A61K31/616A61K9/5063A61K31/40A61K9/5084A61K45/06A61P3/06A61P7/02A61P9/00A61P9/10A61P9/12A61P43/00A61K2300/00
Inventor 禹钟守朴宰贤金用镒罗荣俊崔俊荣李润娥
Owner HANMI SCI CO LTD