Medicine composition containing lipoprotein-associated phospholipase A2 inhibitors and application thereof

A reductase inhibitor and related technology, applied in the field of medicine, can solve the problems of poor myocardial infarction and other problems

Active Publication Date: 2015-08-19
HEBEI DONGKANG BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0021] In phase II clinical trials, darapladib can significantly inhibit the growth of necrotic core volume of atherosclerotic plaques. The clinical effect of delaying myocardial infarction alone is not good

Method used

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  • Medicine composition containing lipoprotein-associated phospholipase A2 inhibitors and application thereof
  • Medicine composition containing lipoprotein-associated phospholipase A2 inhibitors and application thereof
  • Medicine composition containing lipoprotein-associated phospholipase A2 inhibitors and application thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0050] Experimental Example 1: Pharmacological effects of lovastatin + Darapladib

[0051] 1. Animals and groups: 105 healthy NIH 8-week-old male mice were divided into 7 groups, 15 in each group, of which:

[0052] Group 1 was the normal control group, fed with distilled water;

[0053] Group 2 was the high-fat model group, which was given high-cholesterol emulsion by intragastric administration;

[0054] Group 3 was the lovastatin group, which received lovastatin 4 mg / kg orally;

[0055] Group 4 is the Darapladib group, and Darapladib 30mg / kg is administered orally;

[0056] Group 5 was lovastatin+Darapladib middle-dose group: lovastatin 4mg / kg and Darapladib 30mg / kg by intragastric administration.

[0057] Group 6 was lovastatin+Darapladib low-dose group: lovastatin 2mg / kg and Darapladib 20mg / kg by intragastric administration.

[0058] Group 7 was the lovastatin+Darapladib high-dose group: lovastatin 6 mg / kg and Darapladib 40 mg / kg by intragastric administration.

[00...

Embodiment 2

[0070] Example 2: Darapladib and lovastatin tablets

[0071] 1. Prescription (1000 tablets)

[0072] composition

Weight (g)

percentage (%)

Darapladib

80

31.68

lovastatin

10

3.96

microcrystalline cellulose

100

39.60

Crospovidone

4

1.58

lactose

50

19.80

povidone

6

2.38

purified water

50

—

Magnesium stearate

2.5

0.99

[0073] total

252.5

100.00

[0074] Remarks: Water used as a solvent evaporates when it is finally dried, and is not included in the prescription composition, so it is not counted.

[0075] 2. Preparation process

[0076] 1) Weigh each component according to the prescription, take Darapladib, lovastatin, microcrystalline cellulose, crospovidone and lactose, mix them evenly, and set aside.

[0077] 2) Take the prescribed amount of povidone and dissolve it in an appropriate amount of purified water...

experiment example 3

[0079] Experimental example 3 Pharmacological effects of fenofibrate + Darapladib

[0080] 1. Animals and Grouping A total of 70 NIH mice, half male and half male, were divided into 7 groups with 10 mice in each group, of which:

[0081] Group 1 is the normal control group, NIH 5-month-old non-modeled normal mice;

[0082] Group 2, Group 3, Group 4, Group 5, Group 6, and Group 7 were 5-month-old obese mice, Group 2 was the model control group; Group 3 was the fenofibrate group, and 50 mg / kg of fenofibrate was administered orally ; Group 4 is Darapladib group, Darapladib 26mg / kg by intragastric administration; Group 5 is fenofibrate + Darapladib medium dose group, intragastric administration of fenofibrate + Darapladib 76mg / kg, of which fenofibrate 50mg / kg (please verify ); Group 6 was the fenofibrate+Darapladib low-dose group, fenofibrate+Darapladib 60mg / kg by oral administration, of which fenofibrate 40mg / kg; Group 7 was the fenofibrate+Darapladib high-dose group, gavage St...

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PUM

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Abstract

The invention relates to a medicine composition containing lipoprotein-associated phospholipase A2 inhibitors and application of the medicine composition, and belongs to the technical field of medicine. The medicine composition consists of lipoprotein-associated phospholipase A2 inhibitors and one or several kinds of the following ingredients including HMG-CoA (3-hydroxyl-3-methylglutaryl CoA) reductase inhibitors, cholesterol and triglyceride metabolism influence medicine, cholesterol absorption influence medicine, polysaccharide lipid-lowering medicine, gastrointestinal lipase inhibitors or butylphenyl phthaleine. The medicine composition provided by the invention has the surprising curative effect in the aspect of treating atherosclerotic diseases, and the surprising curative effect cannot be achieved by previous lipid-lowering medicine.

Description

technical field [0001] The invention relates to a pharmaceutical composition and its application, in particular to a pharmaceutical composition containing a lipoprotein-associated phospholipase A2 inhibitor and its application, belonging to the technical field of medicine. Background technique [0002] Atherosclerosis (atherosclerosis) is a common and most important type of vascular sclerosis. The lesions mainly occur in the aorta, coronary artery and cerebral artery, and also occur in the renal artery and mesenteric artery. Its pathological changes involve the intima, subintima and media of arteries. Lipids accumulate at the lesion site and invade intracellular or subintimal intercellular spaces, leading to smooth muscle cell and connective tissue hyperplasia, hemorrhage, thrombosis, and calcinosis. Due to the obvious accumulation of lipids inside and outside the cells, the appearance of lipids in the arterial intima is yellow atheroma, so it becomes atherosclerosis. Athe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61P9/10
Inventor 刘福利夏丽韩思哲田普森王佩贤孙立亚刘超檀萌
Owner HEBEI DONGKANG BIOTECH CO LTD
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