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Ozagrel liposomes and preparation method thereof

A liposome and lipid technology, which is applied in the field of medicine, can solve the problems of short residence time in the body, shorten the administration time, and poor patient compliance, and achieve the effects of prolonging the residence time in the body, targeting, and controlling drug release

Inactive Publication Date: 2009-04-29
李淑斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to solve the problems of the first-pass effect, poor stability, short residence time in the body, long administration time and poor patient compliance in the existing preparations of ozagrel, the present invention prepares ozagrel into liposomes, and controls the suitable particle size Size, so that liposomes escape the uptake of the mononuclear phagocytic system, increase the residence time of the systemic circulation, so that the effective concentration of the drug in the blood can be maintained for a long time, and it can be concentrated in the target site to the maximum extent, reducing the administration time

Method used

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  • Ozagrel liposomes and preparation method thereof
  • Ozagrel liposomes and preparation method thereof
  • Ozagrel liposomes and preparation method thereof

Examples

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Effect test

Embodiment 1

[0029] Take 5g of ozagrel, 30g of soybean lecithin, 30g of cholesterol, 200mL of chloroform, and add pH7.4 phosphate buffer to 1000mL. Put the above ozagrel, soybean lecithin, and cholesterol into a round-bottomed flask and fully dissolve them with chloroform, and place them in a constant temperature water bath at 20-40°C for rotary steaming under reduced pressure, so that the lipids form a uniform film at the bottom of the flask. Pour pH 7.4 phosphate buffer into the above-mentioned flask, hydrate, shake, then adjust the volume to 1000mL with pH 7.4 phosphate buffer, and homogenize 6 times through 750bar high-pressure emulsification to obtain a liposome suspension; or Add 200 g of glucose to the ozagrel liposome suspension, and freeze-dry to obtain ozagrel liposome solid powder.

Embodiment 2

[0031] Take 10g of ozagrel, 50g of egg yolk lecithin, 50g of cholesterol, and add pH7.4 phosphate buffer to 1000mL.

[0032] Dissolve the above-mentioned ozagrel, egg yolk lecithin, and cholesterol in an appropriate amount of ethanol, slowly inject into 800mL of pH7.4 phosphate buffer, remove the residual ethanol under reduced pressure, use the buffer to make up to 1000mL, and homogenize through 700bar high-pressure milk for 7 or 200 g of lactose was added to the above-mentioned ozagrel liposome suspension, and lyophilized to obtain ozagrel liposome solid powder.

Embodiment 3

[0034] Take 7.5g of ozagrel, 60g of dipalmitoylphosphatidylcholine, 50g of poloxamer F68, 50g of cholesterol, and add pH7.4 phosphate buffer to 1000mL.

[0035] Take ozagrel, dipalmitoylphosphatidylcholine, poloxamer F68, and cholesterol, melt and mix until clear, drop into the pH7.4 phosphate buffer solution heated to 65°C under stirring, keep warm, after 500w, accumulate Ultrasonic dispersion for 5 minutes to prepare ozagrel liposome suspension; or add 100 g of trehalose to the above ozagrel liposome suspension, and spray dry to obtain ozagrel liposome solid powder. Spray drying conditions: inlet temperature 160°C, outlet temperature 91°C, air volume 100%, flow rate 0.01%, yield 40.8%.

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Abstract

The invention provides an ozagrel liposome and a preparation method thereof. The Ozagrel liposome consists of ozagrel which is an active substance, lipid used for preparing the liposome, a buffer solution and a propping agent. The preparation method can improve the stability of the ozagrel and is characterized by high drug-load rate and good stability. Experiments prove that the ozagrel liposome prepared by the preparation method of the invention can prolong the in-vivo retention time of the ozagrel which is the active substance, avoid first pass effect, enhance the targeting performance of the ozagrel liposome to blood platelets and endothelial cells in blood vessels, improve curative effect and increase the adaptability of patients, has simple preparation process and low cost and is suitable for industrialized large scale production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an ozagrel liposome and a preparation method thereof. Background technique [0002] Ozagrel is the world's first specific thromboxane (TXA2) synthetase inhibitor, and its action site is platelets and vascular endothelial cells. Pharmacological studies have shown that this product can strongly inhibit the activity of TXA2 synthetase, thereby inhibiting platelet aggregation, and at the same time increase the concentration of prostacyclin PGI2, dilate blood vessels, increase blood flow, effectively inhibit the formation of cerebral thrombosis, and make the already formed thrombus rely on blood balance It dissolves itself when the relationship is broken, and achieves the effect of treating cerebral infarction. There are three common forms of ozagrel: free carboxylic acid form, sodium salt form and hydrochloride form. Among them, the dissolution properties of the latter two are sim...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4164A61P7/02
Inventor 李淑斌段鹏杰刘丹鲍洁
Owner 李淑斌
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