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Long-acting liposome preparation for pulmonary drug delivery and preparation method thereof

A technology for pulmonary drug delivery and liposomes, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., and can solve problems such as long action time, poor compliance, and enlargement

Active Publication Date: 2014-05-14
SHENZHEN JYMED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The purpose of the present invention is to prepare long-acting liposome preparations for pulmonary administration of polypeptide drugs for the treatment of cardiovascular diseases, to overcome the shortcomings of existing polypeptide injections, such as poor compliance, inconvenient carrying, and untimely rescue. Pulmonary administration has huge advantages. The absorption area, the lung epithelial cells are extremely thin and have good permeability, and are also permeable to some macromolecules, the clearance of the lower respiratory tract is slow, and the longer residence time of the drug in the lungs can increase its in the alveoli Absorption in the medium, and rapid absorption of pulmonary administration, no liver first-pass effect, can improve bioavailability, long action time, and easy to carry, patients can self-administer medication

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1 Preparation and pharmacokinetic investigation of long-acting liposome aerosol for pulmonary administration of bivalirudin

[0017] Weigh 1 part of bivalirudin, 5 parts of PEG2000-dipalmitoylphosphatidylcholine, 3 parts of cholesterol, dissolve bivalirudin in water to obtain an aqueous phase, and dissolve PEG2000-dipalmitoylphosphatidylcholine and cholesterol Obtain the oil phase in dichloromethane, inject the oil phase into the water phase at an even speed, stir to evaporate the organic solvent, and homogenize the emulsion to obtain long-acting liposomes, put them into a special container, and fill with trichlorofluoromethane to obtain bival Luding long-acting liposome aerosol. The pharmacokinetics of the sample prepared in Example 1 was investigated, and the results showed that its half-life was about 64 minutes and the clearance rate was about 1.2 mL / min / kg, while the marketed bivalirudin for injection had a half-life of about 25 minutes and clearance rate. It...

Embodiment 2

[0018] Example 2 Preparation and pharmacokinetic study of long-acting liposome powder spray for pulmonary administration of bivalirudin

[0019] Weigh 1 part of bivalirudin, 5 parts of PEG2000-dipalmitoylphosphatidylcholine, 3 parts of cholesterol, dissolve bivalirudin in water to obtain an aqueous phase, and dissolve PEG2000-dipalmitoylphosphatidylcholine and cholesterol Obtain the oil phase from ethyl acetate, inject the oil phase into the water phase at a uniform speed, stir and evaporate the organic solvent, and homogenize the emulsion to obtain long-acting liposomes, and obtain long-acting liposome powder mist by spray freeze-drying method. The obtained long-acting liposome preparation is spherical, uniform in particle size, with an average particle size of 5 μm, and the encapsulation rate is as high as 90%. The pharmacokinetics of the sample prepared in Example 2 was investigated, and the results showed that its half-life was about 75 minutes and the clearance rate was abou...

Embodiment 3

[0020] Example 3 Preparation and pharmacokinetic study of long-acting liposome aerosol for pulmonary administration of eptifibatide

[0021] Weigh 5 parts of eptifibatide, 8 parts of PEG1000-dipalmitoylphosphatidylethanolamine, 3 parts of cholesterol, dissolve eptifibatide in water to obtain an aqueous phase, dissolve PEG1000-dipalmitoylphosphatidylethanolamine and cholesterol The oil phase is obtained from methyl chloride, the oil phase is injected into the water phase at an even speed, the organic solvent is evaporated, and the emulsion is homogenized to obtain long-acting liposomes, which are packed into a special container, and filled with trichlorofluoromethane and difluoromethane to obtain Etibatide long-acting liposome aerosol. The pharmacokinetics of the sample prepared in Example 3 was investigated, and the results showed that its half-life was about 6.4h and the clearance rate was about 0.5mL / min / kg, while the half-life of eptifibatide for injection on the market was ab...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and relates to a long-acting liposome preparation for pulmonary drug delivery and a preparation method thereof. Specifically, the preparation takes polyethylene glycol modified liposome as a drug carrier, takes polypeptide drugs for treating cardiovascular diseases as active ingredients, and mainly comprises related peptides such as bivalirudin, eptifibatide, carperitide, nesiritide, romiplostim, and the like. The long-acting liposome preparation prepared according to the invention is high in encapsulation efficiency, easy to use, long in acting time and high in bioavailability.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a long-acting liposome for pulmonary administration and a preparation method thereof. Background technique [0002] Bivalirudin is mainly used to prevent angioplasty in the interventional treatment of unstable angina and ischemic complications before and after. Etibatide is mainly used in the treatment of unstable angina and acute myocardial infarction. Caperitide is mainly used in the treatment of Acute heart failure (including exacerbation of chronic heart failure), Nesiritide is mainly used for patients with acute decompensated congestive heart failure and dyspnea at rest or light activity, to reduce pulmonary capillary wedge pressure and improve Symptoms of dyspnea, Romipristine is mainly a platelet-producing drug for adult patients with splenectomy and unresected chronic immune thrombocytopenic purpura (ITP), and both are polypeptide drugs for the treatment of cardiovascu...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/34A61K38/10A61K38/12A61K38/22A61K39/395A61P9/00A61P9/10A61P9/04
Inventor 姚志勇李新宇支钦马洪季邱焕杰舒遂智李云开
Owner SHENZHEN JYMED TECH
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