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Praziquantel slow-released Implants for animals and preparation method thereof

A technology of slow-release implants and praziquantel, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, which can solve the problems of unfavorable scale-up production, time-consuming heating and cooling operations, and Uncertain drug load and other issues, to achieve the effect of reducing production costs, saving production costs, and improving accuracy

Inactive Publication Date: 2009-07-29
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inclusion of biocompatible materials not only effectively increases the drug loading capacity, but also significantly improves the utilization rate and action time of the drug through subcutaneous implantation or intramuscular injection. However, the preparation of the above-mentioned inclusion preparations is still There are at least two deficiencies: ① a large amount of organic solvents are used in the inclusion process, and the residue of organic solvents will affect the stability of the pharmaceutical preparation; ② it is difficult to ensure that the drug is completely wrapped by the material during the inclusion process. The drug loading is uncertain, and the preparation process is not reproducible
Although this method avoids the use of toxic organic solvents and the preparation method is relatively simple, there are still at least three shortcomings in the above-mentioned sustained-release injections: ①The temperature-raising and cooling operations involved in the preparation process of the sustained-release injections are time-consuming; ②Drug granules It is also difficult to ensure uniform dispersion in aluminum monostearate castor oil gel, thus, the drug loading of the unit preparation after packaging is uncertain; ③ This production method is not conducive to scale-up production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] (1) Weigh 1 kg of praziquantel and 9 kg of biocompatible material PLGA (composed of polylactic acid and polyglycolic acid with a weight ratio of 85:15);

[0024] (2) Put praziquantel and PLGA into an extruder heated to 180° C., stir at a rate of 5 rpm, and extrude through a die with an inner diameter of 1 mm;

[0025] (3) Cool and solidify the blend of medicine and material extruded by the extruder at a temperature of -200°C;

[0026] (4) Cut the blend of the completely cooled and solidified medicine and materials into 1mm medicine sticks to obtain the praziquantel slow-release implant;

[0027] Implementation effect: The slow-release implant prepared by the present invention has no organic solvent residue and accurate dosage. The subcutaneous implantation experiment in rats shows that the implant can release medicine stably and slowly in rats for up to 10 days.

Embodiment 2

[0029] (1) Weigh 4kg of praziquantel and 6kg of biocompatible material polycaprolactone (the weight average molecular weight of polycaprolactone is 50000);

[0030] (2) Put praziquantel and polycaprolactone into an extruder heated to 60° C., stir at a rate of 50 rpm, and extrude through a die with an inner diameter of 5 mm;

[0031] (3) Cool and solidify the blend of medicine and material extruded by the extruder at a temperature of -100°C;

[0032] (4) Cut the blend of the completely cooled and solidified medicine and materials into 20mm medicine sticks to obtain the praziquantel slow-release implant;

[0033] Implementation effect: the slow-release implant prepared by the present invention has no organic solvent residue and accurate dosage. The subcutaneous implantation experiment in rats shows that the implant can release medicine stably and slowly in rats for up to 90 days.

Embodiment 3

[0035] (1) Weigh 7kg of praziquantel and 3kg of biocompatible material ethylene / vinyl acetate copolymer (the weight average molecular weight of ethylene / vinyl acetate copolymer is 60000);

[0036] (2) Put praziquantel and ethylene / vinyl acetate copolymer into an extruder heated to 60° C., stir at a rate of 100 rpm, and extrude through a die with an inner diameter of 10 mm;

[0037] (3) Cool and solidify the blend of medicine and material extruded by the extruder at a temperature of 0°C;

[0038] (4) Cut the blend of the completely cooled and solidified medicine and materials into 60mm medicine sticks to obtain the praziquantel slow-release implant;

[0039] Implementation effect: the sustained-release implant prepared by the present invention has no organic solvent residue and accurate dosage. The subcutaneous implantation experiment in rats shows that the implant can release medicine stably and slowly in rats for up to 120 days.

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Abstract

The invention relates to a veterinary praziquantel slow-release implant in the field of veterinary drug and a method for preparing the same. The slow-release implant comprises the following compositions in percentage by weight: 10 to 70 percent of praziquantel, 30 to 90 percent of a biocompatible material and 0 to 60 percent of a hydrophilic release regulator; the method for preparing the slow-release implant comprises the following steps: the praziquantel, the biocompatible material and the hydrophilic release regulator are weighed according to weight mixture ratio, thrown into an extruder, stirred and extruded out by a neck ring mold; a mixture of the extruded drug and material is cooled and solidified; and the fully cooled and solidified mixture of the drug and material is cut into drug bars so as to obtain the praziquantel slow-release implant. The method avoids the use of an organic solvent in the process of the preparation production and ensures the precision of the content of the preparation drug and the repeatability of preparation production.

Description

technical field [0001] The invention relates to a sustained-release implant in the field of pharmaceutical technology and a preparation method thereof, in particular to a sustained-release praziquantel implant for animals and a preparation method thereof. Background technique [0002] Schistosomiasis and tapeworm are zoonotic parasitic diseases. In particular, schistosomiasis has been on the rise in recent years, which has attracted great attention from the country. When livestock are seriously infected, it often leads to emaciation of the affected animal. If the prevention and control is not timely, it is easy to cause the death of the affected animal and seriously affect the healthy development of animal husbandry. In order to control the above-mentioned parasitic diseases, at present, ordinary praziquantel tablets are mainly administered orally to achieve deworming. However, this treatment has only a temporary curative effect and no long-term preventive effect. In addi...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/34A61K47/32A61K47/36A61K47/42A61K31/498A61P33/12A61P33/14
Inventor 郭圣荣程亮
Owner SHANGHAI JIAO TONG UNIV
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