Alprostadil liposome microsphere preparation

A technology of lipid microspheres and dill fat, which is applied in the field of pharmaceutical preparations and can solve the problems of short validity period and poor stability
CN101716147AInactive Publication Date: 2010-06-02BEIJING TIDE PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
BEIJING TIDE PHARMA
Publication Date
2010-06-02
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides an alprostadil liposome microsphere preparation, in particular to an alprostadil liposome microsphere preparation containing a stabilizing agent, wherein the stabilizing agent contains a component A and a component B; the component A is selected from one or more of oleic acid, sodium oleate and cholesterol; the component B is selected from one or more of vitamin E, coenzymes Q10, propylgallate, ascorbyl palmitate and vitamin C. The stabilizing agent can guarantee that alprostadil is in a relatively stable weak acidic environment, prevent the alprostadil from being oxidized and degraded, reduce the interfacial tension of oil phases and water phases of the microsphere preparation, stabilizes phospholipids bimolecular films of liposome microspheres and has the dual functions of improving the chemical stability and the preparation stability of active medicaments so as to greatly reduce the degradation rate of the alprostadil, obviously prolong the validity period and the storage life of medicaments and avoid the defects of adverse reactions, toxic and side effects, inconvenient use, and the like of the traditional alprostadil preparations.
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Description

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, in particular to an alprostadil lipid microsphere preparation, in particular to an alprostadil lipid microsphere preparation containing a stabilizer. Background technique

[0002] Alprostadil (PGE 1 ), also known as prostaglandin E1, the chemical name is (1R, 2R, 3R)-3-hydroxy-2[(E)-(3S)-3-hydroxy-1-octenyl]-5-oxocyclopentyl Alkaneheptanoic acid, which belongs to natural prostaglandin (PG) analogs, is a highly active endogenous physiologically active substance, which can be synthesized in various tissue cells of the human body.

[0003] PGE 1 It has a variety of pharmacological activities: it can significantly expand peripheral and coronary vessels, improve hemodynamics and hemorheology; inhibit platelet aggregation, reduce platelet hyperreactivity and thromboxane A (TXA) levels; inhibit free Ca of vascular smooth muscle cells 2+ , Inhibit the release of norepinephrine from vascular ...

Claims

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