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Drug formulation containing fibrate medicament and process for producing the same

A technology for fibrates and medicines, which is applied in the field of preparations containing fibrates and their preparation, and can solve the problem that the mixing ratio of pitavastatin and fenofibrate is not recorded, the relationship between free fatty acids is not mentioned, and the effect is not fully demonstrated. and other problems, to achieve the effect of reducing the concentration of fibrinogen and inhibiting thrombosis

Inactive Publication Date: 2009-09-16
ASKA PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the mixing ratio of pitavastatin and fenofibrate is not recorded in this document, and the effect of combining the two preparations is not fully shown in the examples, nor is it recorded or suggested that free fatty acid and fibrinogen (independent of cholesterol or risk factors for decreased triglycerides)
[0011] In addition, said patent document does not mention metabolic syndrome or the diseases derived therefrom, especially the relationship between said diseases and free fatty acids

Method used

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  • Drug formulation containing fibrate medicament and process for producing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Embodiment 1 (experimental example)

[0079] Pitavastatin (PIT) was mixed into the feed, and administered to normolipidemic rabbits at a dose of 0.5 mg / kg / day for 4 weeks (PIT administration group). Fenofibrate (FEN) was then mixed into the feed, and administered to normal blood lipid rabbits at a dose of 30 mg / kg / day for 4 weeks (FEN administration group). Then PIT and FEN were mixed into feed and administered to normal blood lipid rabbits for 4 weeks (combined administration group). In the combination administration group, the dosage of PIT was 0.5 mg / kg / day, and the dosage of FEN was 30 mg / kg / day.

[0080] After the last administration, the rabbits were fasted for one day, blood was collected from the ear vein, and treated with ethylenediaminetetraacetic acid (EDTA) to prepare plasma. Total cholesterol (TC) and triglyceride (TG) concentrations in plasma were measured according to an enzymatic method using a detection kit for enzymatic method (manufactured by Wako P...

Embodiment 2

[0082] Embodiment 2 (experimental example)

[0083]Pitavastatin (PIT) was orally administered to normal guinea pigs at a dose of 1 mg / kg / day for 2 weeks (PIT administration group). Fenofibrate (FEN) was orally administered to normal guinea pigs at a dose of 30 mg / kg / day for 2 weeks (FEN administration group). PIT and FEN were then orally administered to normal guinea pigs for 2 weeks (combined administration group). In the combination administration group, the dosage of PIT was 1 mg / kg / day, and the dosage of FEN was 30 mg / kg / day.

[0084] After the last administration, the guinea pigs were fasted for 1 day, and the blood collected from the abdominal aorta was made into plasma as in Example 1, and the TC and TG values ​​were measured, and the cholesterol content in the liver was measured.

[0085] The results showed that TC and TG were significantly decreased in the combined administration group in which both PIT and FEN were administered, compared to the PIT-administered gro...

Embodiment 3

[0086] Embodiment 3 (experimental example)

[0087] Study on the effects of reducing blood lipids in dogs caused by combined administration of fenofibrate (FEN) and pitavastatin (PIT)

[0088] (1) Subject

[0089] Experiments were carried out with dogs (male and male Beagle dogs used for drug research, 11 males and 2 females, aged 27 to 73 months). Dogs were raised in separate cages in an animal room set at room temperature 23±3°C, humidity 50±10%, light period 8:00-20:00 and dark period 20:00-8:00, one per cage. Feed the dog with 300g CD-5M feed (manufactured by Japan CLEA) once a day. Make it ad libitum to drink tap water.

[0090] (2) Tested object and control object

[0091] Fenofibrate (FEN) 20 mg / kg and pitavastatin (PIT) 2 mg / kg were used as test substances.

[0092] (3) experiment

[0093] One day before the start of administration, blood was collected from the anterior wrist radial vein at 4 hours (the 0th day-4 hours) and 24 hours (the 0th day-24 hours) after f...

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Abstract

A preparation (pharmaceutical composition) reducing a concentration of a free fatty acid and / or fibrinogen in the blood is prepared. The preparation contains a statin agent comprising at least a statin compound having a benzopyridine skeleton (e.g., pitavastatin) and a fibrate agent (e.g., fenofibrate). The preparation is useful as a preventive or treating agent for hyper-free fatty acidemia, metabolic syndrome, or type II diabetes.

Description

technical field [0001] The present invention relates to a preparation containing statins and fibrates and a preparation method thereof, which can be used as a preparation for preventing or treating metabolic syndrome, type II diabetes, complications of type II diabetes and the like. Background technique [0002] Statins can inhibit cholesterol synthesis by inhibiting hydroxymethylglutaryl CoA (HMG-CoA) reductase (the rate-limiting enzyme of the cholesterol synthesis pathway), and thus are widely used as agents for the prevention or treatment of hyperlipidemia. Known representative statin drugs include pravastatin, simvastatin, fluvastatin, atorvastatin, lovastatin, cerivastatin, rosuvastatin and the like. These statins are highly effective in reducing the concentration of total cholesterol and low-density lipoprotein-binding (LDL) cholesterol in the blood. However, the effect of lowering blood triglyceride concentration, lowering blood free fatty acid concentration and rais...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/47A61K31/216A61P1/16A61P1/18A61P3/00A61P3/06A61P3/08A61P3/10A61P7/02
CPCA61K31/216A61K31/47A61P1/16A61P1/18A61P3/00A61P3/06A61P3/08A61P7/02A61P3/10
Inventor 金泽一森本雅也谷森直人
Owner ASKA PHARMACEUTICAL CO LTD
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