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Ritodrine liposome and its prepn

A liposome and ritodrine technology, applied in the field of medicine, can solve the problem of low bioavailability and achieve the effect of improving curative effect

Inactive Publication Date: 2006-05-17
胡才忠
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ritodrine polylactic acid nanoparticle freeze-dried injection; bioavailability is low, but there is no recommendation for making ritodrine into liposomes and proliposomes

Method used

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  • Ritodrine liposome and its prepn

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Preparation of ritodrine liposomes by ethanol injection: take soybean phospholipids, cholesterol, VE and add absolute ethanol to dissolve them, inject them into ritodrine aqueous solution, stir at high speed at constant temperature, evaporate under reduced pressure to remove ethanol, pass through a microporous membrane for sizing, that is Deritodrine liposomes have an encapsulation efficiency of 73.8%.

Embodiment 2

[0014] Preparation of ritodrine liposomes by film dispersion method: get soybean phospholipids, cholesterol, VE dissolved in 150ml eggplant-shaped bottle with 15ml chloroform, form a film under reduced pressure on a rotary thin film evaporator and remove all organic solvents, add 10ml ritodrine The aqueous solution is hydrated, passed through a microporous membrane for granulation, and the ritodrine liposome is obtained, and the encapsulation efficiency can reach 67.1%.

Embodiment 3

[0016] Preparation of ritodrine liposomes by reverse-phase evaporation: Weigh soybean lecithin, cholesterol, VE and add 5ml chloroform to dissolve, then add 10ml ether, then add 15ml ritodrine in phosphate buffer, bath ultrasonic to make uniform For single-phase system, remove chloroform ether by vacuum evaporation until gel is formed, continue to evaporate under reduced pressure for 5 to 10 minutes, and vortex until the aqueous suspension, that is, liposome, is formed. The encapsulation efficiency can reach 49.5%.

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Abstract

The present invention is ritodrine liposome with high absorption, high bioavailability and high stability and its preparation. The ritodrine liposome or ritodrine liposome precursor is prepared with ritodrine and phosphatide, cholesterol, supporting agent and other supplementary material. It has phosphatide / medicine weight ratio of 0.1-40, and is prepared through ethanol injecting process, film dispersion process, inverse evaporation process, extruding process or mechanical process. The supporting agent may be sorbitol, mannitol, cane sugar, etc. and has ratio to phosphatide of 0.01-400. The ritodrine liposome is beta2-adrenine receptor excitomotor capable of exciting beta2 receptor in uterine smooth muscle to inhibit the contraction of uterine smooth muscle, reduce uterine activity and prolong gestational period.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a ritodrine liposome (including proliposome) and a preparation method thereof. Background technique [0002] Ritodrine (Ritodrine) Alias: Hydroxybenzyl Hydroxyephedrine, Ritodrine, YUTOPAR Structural Formula: [0003] [0004] Ritodrine is beta 2 Adrenoceptor agonists that stimulate beta in uterine smooth muscle 2 Receptors, inhibit the contraction of uterine smooth muscle, reduce uterine activity and prolong pregnancy. Currently marketed preparations are tablets: 10mg per tablet. Injection: 50mg (5ml) each. A randomized multi-center study of xintongding and ritodrine in the treatment of premature birth. Foreign Medicine. Obstetrics and Gynecology Volume 1998, Issue 04. Jiang Guoqing and Wang Sumei commented on the efficacy of xintongding and ritodrine in the treatment of premature birth, perinatal outcomes and effects on pregnant women A randomized multicenter study of ...

Claims

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Application Information

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IPC IPC(8): A61K31/137A61K9/127A61P15/06
Inventor 胡才忠
Owner 胡才忠
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