Slow releasing microsphere preparation of Thymopentin, and prepartion method

A slow-release microsphere preparation and thymus technology, which is applied in pharmaceutical formulations, peptide/protein components, medical preparations containing active ingredients, etc., can solve problems such as low bioavailability, different courses of treatment, and loss of biological activity

Active Publication Date: 2006-12-06
北京博恩特药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] But because the biological half-life of thymopentin is very short (about 30 seconds), it is very easy to be degraded into amino acids by protease and aminopeptidase in plasma and lose its biological activity. Therefore, the half-life of the drug is very short and its bioavailability is low. , and clinical use often requires repeated and long-term injections (depending on the condition, the course of treatment is often different), which is extremely inconvenient to use

Method used

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  • Slow releasing microsphere preparation of Thymopentin, and prepartion method
  • Slow releasing microsphere preparation of Thymopentin, and prepartion method
  • Slow releasing microsphere preparation of Thymopentin, and prepartion method

Examples

Experimental program
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Effect test

experiment example 1

[0026] exist figure 1 In the process, the O phase is weighed according to the proportion and added to the W1 phase, and the crusher is used for thorough crushing. Through microscopic observation, the formation of figure 1 The transparent unstable spherical microspheres in the W1 / O phase.

[0027] exist figure 2 In the experimental example shown, the W1 / O phase was slowly and uniformly injected into the high-speed stirring W2 with a syringe. After the final clathrate, the sample was taken and observed through a microscope. It can be observed that the W1 / O / W2 phase is an opaque spherical microstructure. The diameter of the microsphere is obviously larger than that of the W1 / O phase.

[0028] exist image 3 In another experimental example shown, W1 / O / W2 microspheres are aged by a rotary evaporator to evaporate methylene chloride, the collected microspheres are added with excipients, and a specific lyophilization curve is applied in a lyophilizer Microscopic observation of th...

experiment example 2

[0029] Experimental Example 2: Release of Lactide-Glycolide Copolymer

[0030] See Figure 4 , Figure 5

Description of drawings:

[0031] figure 1 It is a structural diagram of the W1 / O phase of the present invention.

[0032] figure 2 It is the structure diagram of W1 / O / W2 phase.

[0033] image 3 Structural diagram of microspheres.

[0034] Figure 4 Release curve of PLGA50 / 50

[0035] Figure 5 Release curve of PLGA65 / 35

Embodiment 1

[0037] Thymopentin 7.5g Lactide-glycolide copolymer (PLGA) 40g

[0038] Gelatin 0.75g D-mannitol 0.75g

[0039] Thymopentin was fully dissolved in water to make water phase W1, lactide-glycolide copolymer (PLGA) was fully dissolved in dichloromethane to make oil phase O; polyvinyl alcohol (PVA) was fully dissolved in water to make Form water phase W2; add oil phase O to water phase W1, emulsify to form W1 / O phase, then slowly inject into water phase W2 at a uniform speed to form W1 / O / W2 phase, evaporate through rotary evaporation Organic solvent dichloromethane, collect the microspheres, use a specific freeze-drying curve to freeze-dry, and finally make 1000 thymopentin sustained-release microspheres for injection, with a particle size of 1-100um. One injection per month, 4 to 5 mg per injection.

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Abstract

A slow-release thymopeptide-5 microball injection able to be injected once every month is prepared from thymopeptide-5, lactide-glycolide copolymer (PLGA), gelatin and D-mannitol. Its preparing process is also disclosed.

Description

field of invention [0001] The invention relates to a sustained-release microsphere preparation and a preparation method thereof, in particular to a thymopentin sustained-release microsphere preparation and a preparation method thereof. Background technique [0002] Thymopentin (Thymopentin) is a biological pentapeptide that can be synthesized and has significant cellular immune regulation activity. The preparation currently in clinical use is Thymopentin for Injection (Thymopentin for Injection) freeze-dried powder. As a good cellular immune regulation drug, it has been widely used in clinic. Thymopentin can be widely used clinically in malignant tumors of various organs and parts (such as lung cancer, liver cancer, ovarian cancer, kidney cancer, breast cancer, cervical cancer, bone and flesh cancer, digestive system tumors and blood cancers, etc. A large number of Clinical studies have proved that Thymopentin can not only be used for the immunotherapy of malignant tumors,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K9/16A61P35/00
Inventor 黎飞冯前进梁卫郭光明崔晓星周晓庆
Owner 北京博恩特药业有限公司
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