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Pharmaceutical formulation comprising microcapusles of statins suspended in alkyl esters of polyunsaturated fatty acids (PUFA)

A technology of unsaturated fatty acids and pharmaceutical preparations, which is applied in the field of pharmaceutical preparations containing microcapsules of statins suspended in alkyl esters of polyunsaturated fatty acids (PUFA), which can solve problems such as stability issues

Inactive Publication Date: 2007-09-26
GP PHARM +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] WO 02 / 100394 and WO 03 / 103640 describe pharmaceutical compositions in which pure statin nanoparticles without any protective coating are dispersed in a pharmaceutically acceptable oil, but if the temperature of the system exceeds 40°C during preparation, the Types of formulations have stability issues for statins, which are present in most oral formulations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: prepare the microcapsule of simvastatin with gelatin and carboxymethyl cellulose by complex coacervation method

[0036] Solution A: A 1% aqueous solution of gelatin was prepared, and the pH was adjusted to be equal to or greater than 7.

[0037] Solution B: A 1% aqueous solution of sodium carboxymethylcellulose was prepared, and the pH was adjusted to be equal to or greater than 7.

[0038] Mix 100mL of solution A and 100mL of solution B, and heat to 40°C. 1.2 g of simvastatin powder was dispersed in the mixture. When all powder had dispersed and no lumps were observed, acetic acid was added to adjust the pH to 4.0. Stirring was maintained at 40°C for 1 hour, then the solution was cooled to 10°C and this temperature was maintained for an additional hour. Add 1 mL of 50% glutaraldehyde in water.

[0039] The resulting suspension was dried by spray drying to obtain a microcapsule powder containing 37% simvastatin.

[0040] The microcapsule powder was d...

Embodiment 2

[0041] Example 2: Preparation of microcapsules of simvastatin with gelatin by single coacervation method

[0042] A 1% aqueous solution of gelatin was prepared.

[0043] Take 100 mL of the above solution, and disperse 1 g of simvastatin powder therein. When all of the simvastatin had dispersed, 30 mL of a saturated aqueous solution of sodium sulfate was added. This was kept under stirring for 1 hour, and 0.5 mL of 50% aqueous glutaraldehyde solution was added.

[0044] The formed microcapsules were collected by filtration, washed with water and dried in a vacuum oven. The content of simvastatin in these microcapsules was 45%.

[0045] The obtained microcapsule powder was directly dispersed in oil containing 70% PUFA methyl ester, wherein the ratio of EPA / DHA in PUFA was 0.8.

Embodiment 3

[0046] Embodiment 3: prepare the microcapsule of lovastatin with polyethylene glycol

[0047] A 10% polyethylene glycol aqueous solution was prepared by using polyethylene glycol with a molecular weight of 35000 (PEG-35000).

[0048] 6 g of lovastatin were dispersed in the solution by vigorous stirring.

[0049] When a fine dispersion free of lumps was obtained, the solution was dried by spray drying.

[0050] The resulting microencapsulated powder contained 40% lovastatin, which was directly dispersed in an oil containing 85% ethyl esters of PUFAs with an EPA / DHA ratio of 1 in the PUFAs.

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PUM

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Abstract

The invention relates to a pharmaceutical composition comprising a suspension consisting of an oil with a high concentration of alkyl esters of polyunsaturated fatty acids (PUFA) and to microcapsules comprising at least one polymer and a statin.

Description

field of invention [0001] The present invention describes a new pharmaceutical composition for administering statins and its preparation method. Background of the invention [0002] Statins have shown efficacy in primary and secondary prevention of cardiovascular disease in numerous clinical studies. Recent evidence suggests that the clinical benefit obtained with statin therapy may be related to a reduction in markers of systemic inflammation (Ridker P.M., et al.; N. Engl, JMed. 344:1959-65, 2001 ) more than a reduction in cholesterol levels. Although a direct link between statins and anti-inflammatory mechanisms in reducing cardiovascular events has not been demonstrated, recent studies have shown that treatment with statins improves plaque stability in patients undergoing endarterectomy And reduce the inflammatory response of arteries (Crisby M., et al.; Circulation 103:926-33, 2001). Furthermore, treatment with statins in experimental models reduced the expression of i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/50A61K31/20A61P3/06
CPCA61K9/5057A61K9/1652A61K9/5047A61K31/20A61K9/4858A61K9/1641A61K9/4808A61P29/00A61P3/00A61P3/06A61P9/10A61K9/10A61K9/50
Inventor P·卡米纳蒂A·帕兰特
Owner GP PHARM