Triptorelin slow-release micro particles and preparation method thereof

A technology of slow-release microparticles and microparticles, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Low-level problems, to achieve good plasticity, simple process, good drug loading effect

Active Publication Date: 2016-01-27
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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  • Triptorelin slow-release micro particles and preparation method thereof
  • Triptorelin slow-release micro particles and preparation method thereof
  • Triptorelin slow-release micro particles 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), poloxamer 1882.1 mg (0.2%), Feed into the feeding hopper, set the feeding hopper speed to 120 rpm, hot-melt extrusion temperature to 80°C, hot-melt extrusion time to 20 minutes, crushing and cooling temperature after extrusion to -90°C, collect the crushed particles, and detect 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 PLGA model Drug loading encapsulation rate release time Example 1 85:15 PLGA 6.4%...

Embodiment 4-6

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

[0031]Take triptorelin 50mg, different amounts of PLGA of 75:25 type, poloxamer 1880.4%, send into the feeding funnel, set the feeding funnel rotating speed as 120 rev / min, hot melt extrusion temperature is 80 ℃, heat The melt-extrusion time was 20 minutes, and the pulverization cooling temperature after extrusion was -90°C. The pulverized particles were collected and their physical and chemical properties were tested. The test results are shown in Table 2 below.

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

[0033] Example Triptorelin PLGA Drug loading encapsulation rate Example 4 50mg (7.66%) 0.6g（91.94%） 6.2% 74.1% Example 5 50mg (5.86%) 0.8g（93.74...

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 medicinal low-release micro particles and in particular relates to triptorelin slow-release micro particles and a preparation method thereof. The triptorelin slow-release micro particles comprise the following components in percentage by weight: 0.5-20% of triptorelin, 79-99% of PLGA and 0.1-1% of poloxamer. The preparation method of the triptorelin slow-release micro particles comprises the steps of mixing all the components, then putting the mixture into a hot melt extruder, and performing heating melting, extrusion and low-temperature crushing in the hot melt extruder. The triptorelin slow-release micro particles provided by the invention are good in shape, high in entrapment efficiency, good in drug loading capacity and stable in releasing. Moreover, the triptorelin slow-release micro particles are simple in synthetic process, are harmless, generate nontoxic products after degradation, and are 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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IPC IPC(8): A61K9/16A61K38/09A61K47/34A61P35/00A61P15/00A61P15/08
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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