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Long-acting implantation agent of pentapeptide for thymus gland and method of producing the same

An implant and thymus technology, which is applied in the field of thymopentin long-acting implants and its preparation, can solve the problems of thymopentin, complex preparation process, and small molecular weight, etc., and achieve the elimination of burst release effect and simple preparation process , the effect of high encapsulation rate

Inactive Publication Date: 2008-02-27
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low molecular weight and strong hydrophilicity of thymopentin, although its biodegradable microparticle drug delivery system has literature (J Microencapsul.1997, 14: 303-310.) and patent (Chinese invention patent, application number: 200510081540.8; China Invention patent, application number: 200510075584.X; Chinese invention patent, application number: 200510082777.8) report, but there are problems of complex preparation process, and it is difficult to achieve a high encapsulation efficiency and a bottleneck with a significant burst release effect
So far, there have been no reports on thymopentin biodegradable long-acting implants

Method used

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  • Long-acting implantation agent of pentapeptide for thymus gland and method of producing the same
  • Long-acting implantation agent of pentapeptide for thymus gland and method of producing the same
  • Long-acting implantation agent of pentapeptide for thymus gland and method of producing the same

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Experimental program
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Effect test

Embodiment 1

[0023] Weigh 797mg lactic acid-glycolic acid copolymer (PLGA, polymerization ratio 50:50, molecular weight 5000), 200mg polylactic acid (PLA, molecular weight 500000), dissolve in 4ml dichloromethane. Add 1mg Thymopentin, 1mg Mg(OH) 2 and 1 mg of polyethylene glycol, after uniform dispersion, volatilize at 30°C to remove part of the organic solvent, extrude the obtained semi-dry mixture, volatilize to remove the residual solvent, and obtain a cylindrical implant with a diameter of 0.5 mm and a length of 30 mm.

Embodiment 2

[0025] Weigh 545mg PLGA (polymerization ratio 50:50, molecular weight 15000), 448mg PLA (molecular weight 100000), heat to 80°C to soften and mix well, add 5mg thymopentin, 1mg ZnCO 3 and 1 mg of mannitol, stirred to disperse evenly, extruded under heat preservation conditions, and cooled to obtain a cylindrical implant with a diameter of 1 mm and a length of 20 mm.

Embodiment 3

[0027] Weigh 245mg PLGA (polymerization ratio 75:25, molecular weight 30000), 745mg PLA (molecular weight 60000), dissolve in 4ml dichloromethane, add 10mg thymopentin, disperse evenly, remove part of the organic solvent by volatilization at 25°C , the resulting semi-dry mixture was extruded, and the residual solvent was volatilized to remove a cylindrical implant with a diameter of 2 mm and a length of 10 mm.

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Abstract

The invention discloses a long-effective implantation agent of thymic pentapeptide in the drug agent domain, which is characterized by the following: adopting thymic pentapeptide as treating active material and biologically decomposed material as base; making the appearance as fine rob shape or cylinder shape; injecting or surgerying to transplant into body; releasing drug completely without surgery and fetching; obtaining high-packing rate and drug-carrying quantity to approach constant speed to release one to several months; reducing the medical cost; improving the compliance for patients. The invention has simple preparing technique and high safety, which projects he clinical treatment superiority and good applying prospect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a thymopentin long-acting implant and a preparation method thereof. Background technique [0002] Thymopentin is a 5-peptide fragment in the structure of thymopoietin II that has the same biological activity and efficacy. Its common English name is thymopentin, and its chemical structural formula is: [0003] [0004] It is known that thymopentin can induce T cell differentiation and bind to T cell specific receptors to increase the level of intracellular cAMP, thereby inducing a series of intracellular reactions to achieve the effect of promoting and inhibiting the two-way regulation of immune function. Thymopentin is mainly used to improve the immunosuppression caused by radiotherapy and chemotherapy in patients with malignant tumors. Its clinical application also includes: (1) chronic hepatitis B; (2) various primary or secondary T cell defects (3) autoimmune disea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K9/00A61K47/34A61P37/02A61K47/10
Inventor 陆伟跃魏刚金樑
Owner FUDAN UNIV
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