A kind of triptorelin sustained-release microparticles and preparation method thereof

A slow-release microparticle and microparticle technology, which is applied in the direction of diseases, antineoplastic drugs, bulk delivery, etc., can solve the problems of sudden release, poor uniformity of microspheres, low drug loading and encapsulation efficiency, and achieve simple process, Good plasticity and good drug loading effect

Active Publication Date: 2018-05-11
SHANGHAI SOHO YIMING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the uniformity of the microspheres (granules) is poor, the drug loading and encapsulation efficiency are low, and burst release phenomenon is prone to occur during the drug release process.

Method used

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  • A kind of triptorelin sustained-release microparticles and preparation method thereof
  • A kind of triptorelin sustained-release microparticles and preparation method thereof
  • A kind of triptorelin sustained-release microparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0026] Example 1-3: Microparticles were prepared according to different types of PLGA, and the release time, drug loading and encapsulation efficiency of the prepared triptorelin microparticles were investigated under the same preparation conditions.

[0027] Weigh 50 mg of triptorelin (4.572%), 1 g of PLGA (95.048%) (see Table 1 for the model of PLGA, different models represent different mass ratios of lactic acid and glycolic acid), 2.1 mg of poloxamer 188 (0.2%) , into the feeding funnel, set the speed of the feeding funnel to 120 rpm, the hot melt extrusion temperature to 80°C, the hot melt extrusion time to 20 minutes, and the crushing and cooling temperature after extrusion to -90°C to collect the crushed particles, Check physical and chemical properties. The test results are shown in Table 1 below.

[0028] Table 1 Microparticles prepared by different types of PLGA

[0029] Example

Embodiment 4-6

[0030] Example 4-6: Microparticles were prepared according to different amounts of PLGA, and the release time, drug loading and encapsulation efficiency of the prepared triptorelin microparticles were investigated under the same preparation conditions.

[0031] Weigh 50 mg of triptorelin, different amounts of PLGA of 75:25 type, poloxamer 188 0.4%, and send them into the feeding funnel, set the feeding funnel speed at 120 rpm, and the hot melt extrusion temperature at 80°C. The hot-melt extrusion time is 20 minutes, the pulverization cooling temperature after extrusion is -90°C, the pulverized particles are collected, and the physical and chemical properties are tested. The test results are shown in Table 2 below.

[0032] Table 2 Microparticles prepared with different ratios of triptorelin and PLGA

[0033] Example

Embodiment 7-15

[0034] Example 7-15: 9 parts of materials were weighed with the prescription ratio of 4.5% triptorelin, 95% PLGA, and 0.5% poloxamer, and prepared by combining the process parameters in the following table 3 respectively. Microparticles were tested for encapsulation efficiency, drug loading, and release time.

[0035] Table 3 Microparticles prepared by different process parameters

[0036]

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Abstract

The invention relates to drug slow-release microparticles, in particular to triptorelin sustained-release microparticles and a preparation method thereof. The composition includes the following components by weight percentage: 0.5%-20% of triptorelin, 79%-99% of PLGA, and 0.1%-1% of poloxamer. The preparation method of the above-mentioned triptorelin sustained-release microparticles of the present invention comprises mixing each component and sending it into a hot-melt extruder, where heating and melting, extrusion and low-temperature pulverization are carried out. The praline sustained-release microparticles of the present invention have good shape, high encapsulation efficiency of the microparticles, good drug loading capacity and stable release. The synthesis process is simple, the product itself is non-toxic, and the product after degradation is non-toxic and stable in quality.

Description

technical field [0001] The invention relates to drug slow-release microparticles, in particular to triptorelin sustained-release microparticles and a preparation method thereof. Background technique [0002] Triptorelin is a synthetic gonadotropin-releasing hormone analog, which can be effectively used for diseases such as prostate cancer, endometriosis, and precocious puberty. Conventional triptorelin preparations have short biological half-life, poor preparation stability, difficult absorption after oral administration, and large side effects after taking the medicine. [0003] Using the biodegradable material PLGA as the skeleton material, the triptorelin drug is encapsulated into microspheres (granules). As a sustained and controlled release preparation, the common preparation techniques include emulsification-liquid drying, spray drying, separation method, etc., the triptorelin microspheres have achieved sustainable drug release. However, the uniformity of the microsp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K38/09A61K47/34A61K47/10A61P35/00A61P15/00A61P15/08
Inventor 吕金芹王文琪赵转霞符雯刘哲鹏崔颀周逸明
Owner SHANGHAI SOHO YIMING PHARMA
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