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Anti-parasitical medicine in situ setting slow release injection and preparation method thereof

A slow-release injection and anti-parasitic technology, which is applied in directions such as pharmaceutical formulations, anti-infectives, and drug combinations, can solve the problems of low drug loading, complicated preparation processes, and low safety of materials used, and achieves a simple preparation method, The effect of good stability and simplified prescription

Active Publication Date: 2018-03-20
中国疾病预防控制中心寄生虫病预防控制所国家热带病研究中心
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The technical problem to be solved by the present invention is to overcome the technical problems of the existing anti-parasitic drug preparations such as low drug loading, low safety of materials used, complicated preparation process, etc., and provide an anti-parasitic drug in-situ solidified slow-release Injection and preparation method thereof

Method used

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  • Anti-parasitical medicine in situ setting slow release injection and preparation method thereof
  • Anti-parasitical medicine in situ setting slow release injection and preparation method thereof
  • Anti-parasitical medicine in situ setting slow release injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Different types of polymers were selected to prepare in situ solidified sustained-release injections of antiparasitic drugs with different release periods.

[0064] Drug selection of praziquantel and L-praziquantel, niclosamide, benzimidazoles (including albendazole, mebendazole, flubendazole, fenbendazole and oxfendazole) and ivermectin For the prime, select PLGA, PCL, PTMC as the release skeleton, and its weight-average molecular weight is 16000, and measure the release rate of the drug.

[0065] The preparation method of in-situ solidified sustained-release injection of antiparasitic drugs is as follows: Weigh 0.4 g of the drug, add 0.4 g each of PLGA, PCL and PTMC, and 0.8 mL of NMP, and vortex until the polymer material is completely dissolved to obtain a solution or a mixture. Suspension.

[0066] Take 0.2 mL of in-situ solidified slow-release injection of anti-parasitic drugs, add 15 mL of deionized water, place in a shaker at 37°C, take samples regularly, and tak...

Embodiment 2

[0069] In situ solidified sustained-release injections of anti-parasitic drugs were prepared with different formulation ratios, wherein the polymer used was PCL, the dispersant was NMP, and the preparation method was the same as in Example 1.

[0070] Taking polymer molecular weight (A), polymer-to-drug ratio (B), and solvent concentration (C) as investigation factors, gel viscosity, water solidification time, and drug release time in vitro as response indicators, the factors and level parameters are shown in Table 1. 15 prescriptions were obtained by Box-Behnken design in the Design Expert 8.0 software, prepared different prescriptions of in-situ solidified sustained-release injections of antiparasitic drugs (3 parallels), and carried out in vitro release tests, the results are shown in figure 2 a- figure 2 f (in the figure, prescription 1-15 corresponds to sample number 1-15), wherein, figure 2 a-2c data analysis with Sigma Plot, figure 2 e-2f uses Excel for data analy...

Embodiment 3

[0078] The release time was adjusted by combining PLGA with different molecular weights.

[0079] Two kinds of PLGA, PLGA with a molecular weight of 150,000 (LA / GA mass ratio: 90 / 10) and PLGA with a molecular weight of 16,000 (LA / GA mass ratio: 75 / 25), were used as the skeleton material in different proportions. The ratio between the degradation rate of the polymer material to control the drug release time.

[0080] Select PLGA (90 / 10) with a molecular weight of 150,000 and PLGA (75 / 25) with a molecular weight of 16,000, respectively according to the weight ratio of 100 / 0, 90 / 10, 80 / 20, 70 / 30, 50 / 50, 30 / 70, 20 / 80 and 10 / 90 are used in combination, see Table 2.

[0081] Table 2 The combination ratio of two PLGAs

[0082] Sample serial number

PLGA (90 / 10, Mw=150,000)

PLGA (75 / 25, Mw=16,000)

Link 1

100

0

couplet 2

90

10

Link 3

80

20

Link 4

70

30

Link 5

50

50

Link 6

30

70

Link ...

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Abstract

The invention discloses an anti-parasitical medicine in situ setting slow release injection and a preparation method thereof. The injection comprises the following components in ratio: 1-80g of an anti-parasitic disease medicine, 1-100g of a biodegradable high polymer material, 2-300mL of a dispersion medium and 0-50g of a solubilizer, wherein the content of the anti-parasitic disease medicine is1-800mg / mL. The injection can maintain long-term control effect when being medicated to a medicated object only once, the medicated object is protected from being infected by pathogens, propagation ofparasitic diseases can be economically and effectively controlled, material safety is high, prescription of a commercially available anti-parasitic disease medicine is simplified, compliance of the medicated object is improved, and control cost is reduced. Meanwhile, subcutaneous injection slow release injection is prepared by innovatively using a molluscicide, namely niclosamide, of the WHO, andthe effect of preventing schistosoma japonicum infection is achieved. The anti-parasitical medicine in situ setting slow release injection is simple in the preparation method, has good stability andis easy to use and popularize.

Description

technical field [0001] The invention relates to an anti-parasitic medicine in-situ solidified slow-release injection and a preparation method thereof. Background technique [0002] At present, the sustained-release preparations of antiparasitic drugs at home and abroad mainly include oral sustained-release preparations, transdermal sustained-release preparations, implantable sustained-release preparations and sustained-release preparations for injection. [0003] For oral sustained-release preparations, since the daily oral dosage of anti-parasitic drugs is relatively large, and continuous sustained release is required, the dosage of excipients is larger, and generally made into boluses, such as: Paratect Bolus, a rumen bolus that has been marketed by Pfizer. , which can release the drug continuously for up to 90 days; Merial Animal Health Limited’s concentrate (Ivomec SR Bolus) bolus of ivermectin can release the drug continuously for up to 135 days; fenbendazole for the pr...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/26A61K47/32A61K47/34A61K31/4184A61K31/4985A61K31/609A61K31/7048A61P33/02A61P33/12A61P33/10
CPCA61K47/34A61K9/0019A61K9/08A61K31/4184A61K31/4985A61K31/609A61K31/7048A61K9/10A61K9/0004A61K45/00A61K47/22Y02A50/30
Inventor 姜斌张皓冰周晓农陶奕薛剑涂珍伍卫平李石柱徐莉莉贾铁武霍乐乐杨诗杰刘妮魏玉芬李军建
Owner 中国疾病预防控制中心寄生虫病预防控制所国家热带病研究中心
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