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Thymus pentapeptide slow-release microshpere formulation for injection and its preparation method

A technology for sustained-release microspheres and injections, which can be used in medical preparations containing active ingredients, antiviral agents, pharmaceutical formulations, etc., and can solve the problems of low bioavailability, large toxic and side effects, and poor patient compliance.

Inactive Publication Date: 2006-12-13
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Existing thymosin preparation, because the biological half-life of thymosin substance is very short, so its bioavailability in blood is very low and side effect is bigger (as: individual patient has drowsiness, fatigue after using, long-term injection patient complies with poor sex)

Method used

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  • Thymus pentapeptide slow-release microshpere formulation for injection and its preparation method
  • Thymus pentapeptide slow-release microshpere formulation for injection and its preparation method
  • Thymus pentapeptide slow-release microshpere formulation for injection and its preparation method

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Experimental program
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Effect test

Embodiment 1

[0056] Embodiment 1: Thymopentin Microspheres Prepared by Double Emulsion Method

[0057] 50mg thymopentin was dissolved in 0.5ml gelatin aqueous solution, 500mg polylactide-glycolide (lactide:glycolide=50:50) (molecular weight is 11000) was dissolved in 5ml dichloromethane, the two Combined, the high-speed homogenizer was stirred at a high speed of 10,000 rpm for 3 minutes to form a W / O emulsion, and the W / O emulsion was poured into 500ml of the external water phase containing 0.2% polyvinyl alcohol to form a W / O / W double emulsion. Stir at a low speed of 500 rpm for 4 hours, volatilize the organic solvent, centrifuge, wash 3 times with distilled water, and freeze-dry for 20 hours to obtain a white powder with good fluidity, the encapsulation rate is 76%, and the particle size range of microspheres is 5~ 80μm, the average particle size is 27.1μm, and the appearance is round, such as figure 1 shown.

Embodiment 2

[0058] Embodiment 2: Double emulsion method prepares thymopentin microspheres

[0059] 100mg thymopentin was dissolved in 1.5ml gelatin aqueous solution, 1.0g polylactide-glycolide (lactide:glycolide=75:25) (molecular weight is 11000) was dissolved in 12ml dichloromethane, dichloromethane The two are combined, and the high-speed homogenizer is stirred at a high speed of 10,000 rpm for 5 minutes to form a W / O emulsion, and the W / O emulsion is poured into 1000ml of the external water phase containing 0.2% polyvinyl alcohol to form a W / O / W double emulsion , stirred at a low speed of 500 rpm for 4 hours, volatilized the organic solvent, centrifuged, washed 3 times with distilled water, and freeze-dried for 20 hours to obtain a white powder with good fluidity. The encapsulation rate was 76%, and the measured particle size was 5~ 120μm, average particle size 32.5μm, such as figure 2 shown.

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PUM

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Abstract

The invention relates the thymus five-peptide slow release microsphere and preparing method. The slow release microsphere comprises 0.5-30wt% thymus five-peptide, 70-99.5wt% degradable high polymer findings. The molecular weight of high polymer findings is 5,000-500,000Dalton. The method can use W / O / W method, S / O / O method and spray-drying method. The particle mean size of the slow release microsphere is 5-40 mum, the encapsulated rate is more than 75%. The slow release microsphere has the advantages of long medicinal crop, less frequency, improving bioavailability and reducing side effects.

Description

technical field [0001] The invention relates to a slow-release microsphere for thymopentin injection and a preparation method thereof. Background technique [0002] Thymopentin (Thymopoietin 32-36, TP-5) is the active fragment of thymopoietin, which is composed of five amino acids, arginine, lysine, aspartic acid, valine and tyrosine, combined in the order of amide bonds Formed, with a definite molecular formula and molecular weight. [0003] The chemical structural formula of Thymopentin is as follows: [0004] [0005] Abbreviation: H 2 N-Arg-Lys-Asp-Val-Tyr-OH [0006] Molecular formula: C 30 h 49 N 9 o 9 [0007] Molecular weight: 679.8 [0008] A large number of clinical studies at home and abroad have proved that thymopentin has the function of inducing and promoting the differentiation, maturation and activation of T lymphocytes and their subsets, regulating the proportion of T lymphocytes, and making CD + 4 / CD + 8 Tends to normal; regulates and enhan...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K9/16A61P1/16A61P31/14A61P37/02A61P11/06A61P35/00
Inventor 梅兴国刘克良艾国梁远军
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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