Pharmaceutical composition and application of lipoprotein-related phospholipase a2 inhibitor

A correlation, phospholipase technology, applied in the field of medicine, can solve problems such as poor myocardial infarction effect

Active Publication Date: 2018-02-16
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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  • Pharmaceutical composition and application of lipoprotein-related phospholipase a2 inhibitor
  • Pharmaceutical composition and application of lipoprotein-related phospholipase a2 inhibitor
  • Pharmaceutical composition and application of lipoprotein-related phospholipase a2 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

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

[0051] 1. Animals and grouping 105 healthy NIH 8-week-old male mice were randomly 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 administrati...

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 to ma...

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] Groups 2, 3, 4, 5, 6, and 7 were 5-month-old obese mice, and group 2 was the model control group; group 3 was the fenofibrate group, and 50 mg / kg; Group 4 was Darapladib group, Darapladib 26 mg / kg orally; Group 5 was fenofibrate + Darapladib medium dose group, fenofibrate + Darapladib 76 mg / kg orally, of which fenofibrate 50 mg / kg ; Group 6 was fenofibrate + Darapladib low-dose group, fenofibrate + Darapladib 60mg / kg by intragastric administration, of which fenofibrate 40mg / kg; Group 7 was fenofibrate + Darapladib high-dose group, intragastric administration Fenofibrate + Darapladib 90mg / kg, of which fenofibrate 60mg / kg, after continuous gavage for 1 mont...

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PUM

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Abstract

The invention relates to a pharmaceutical composition containing a lipoprotein-related phospholipase A2 inhibitor and its application, belonging to the technical field of medicine. The pharmaceutical composition is composed of a lipoprotein-associated phospholipase A2 inhibitor and one or more of the following components: 3-hydroxy-3 meglutaryl coenzyme A (HMG-CoA) reductase inhibitor, cholesterol and Triglyceride metabolism drugs, drugs that affect cholesterol absorption, polysaccharide lipid-lowering drugs, gastrointestinal lipase inhibitors or butylphthalide. The pharmaceutical composition provided by the invention has unexpected curative effect on the treatment of atherosclerotic diseases, which cannot be achieved by previous lipid-lowering drugs.

Description

technical field [0001] The present 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 the most common and most important type of vascular sclerosis. The lesions mainly occur in the aorta, coronary arteries and cerebral arteries, and also occur in the renal arteries and mesenteric arteries. Its pathological changes involve the intima, subintima and media of arterial vessels. Lipids accumulate at the lesion site and invade the intracellular or subintimal intercellular space, resulting in 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, ...

Claims

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Application Information

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Patent Type & Authority Patents(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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