Thymus gland peptide alpha1sustained-release microsphere preparation for injection and preparation thereof

A technology for sustained-release microsphere preparations and thymosin, which is applied to medical preparations with inactive ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, can solve the problems of reduced encapsulation rate, waste of cost, loss, etc. The effect of stable release, reduced administration frequency and low burst release rate

Active Publication Date: 2008-08-20
CHENGDU DIAO JIUHONG PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To achieve a short release effect of 10-15 days or 10-25 days, the viscosity of PLGA needs to be reduced, but the reduction of viscosity is bound to reduce the encapsulation efficiency, and a large amount of expensive thymosin α 1 Will be lost in water, causing huge waste and rising costs

Method used

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  • Thymus gland peptide alpha1sustained-release microsphere preparation for injection and preparation thereof
  • Thymus gland peptide alpha1sustained-release microsphere preparation for injection and preparation thereof
  • Thymus gland peptide alpha1sustained-release microsphere preparation for injection and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Example 1: Thymosin α for injection prepared by drying method in double emulsion-liquid 1 slow release microspheres

[0064] Thymosin alpha 100mg 1 , 0.7g of PEG-6000 was dissolved in 6ml of pH7.4 phosphate buffer, 6g of polyglycolide-lactide (glycolide:lactide=50:50) (intrinsic viscosity 0.45dl / g: 0.55dl / g=2: 3) and be dissolved in 130ml of dichloromethane, the water phase is poured into the oil phase under the effect of high-shear homogenizer rotating speed 2000r / m, emulsify under 2500r / m rotating speed -8min to get w / o emulsion, pour the w / o emulsion into 1000ml ice-bath containing 2%PVA, 1%NaCl external aqueous solution, stirring speed 700r / m, time 2-3 minutes, then add 1500ml The external aqueous phase solution was stirred at a stirring speed of 550r / m for 4 hours, the organic solvent was evaporated, filtered with suction, washed 3 times with distilled water, and freeze-dried for 4 days to obtain a white powder with good fluidity. The encapsulation efficiency wa...

Embodiment 2

[0065] Example 2: Preparation of Thymosin α for Injection by Drying Method in Double Emulsion-Liquid 1 sustained-release microspheres

[0066] Thymosin alpha 100mg 1 The mannitol of 1.5g is dissolved in the phosphate buffered saline solution of the pH7.4 of 6ml, the polyglycolide-lactide of 6g (glycolide: lactide=50: 50, intrinsic viscosity 0.35dl / g: 0.89 dl / g=1:3) was dissolved in 130ml of dichloromethane, the water phase was poured into the oil phase under the action of a high-shear homogenizer at a speed of 2000r / m, and emulsified at a speed of 2500r / m for 5-8min to obtain w / o emulsion, pour the w / o emulsion into 1000ml ice-bath containing 2%PVA, 1%NaCl external water phase solution, stirring speed 700r / m, time 2-3 minutes, then add 1500ml external water phase solution , the stirring speed was 550r / m, the stirring time was 4 hours, the organic solvent was evaporated, suction filtered, washed 3 times with distilled water, and freeze-dried to obtain a white powder with goo...

Embodiment 3

[0067] Example 3: Preparation of thymosin α for injection by dry method in double emulsion-liquid 1 sustained-release microspheres

[0068] Thymosin alpha 500mg 1Dissolve in 20ml of pH7.4 phosphate buffer, 33g of polyglycolide-lactide (glycolide:lactide=50:50, intrinsic viscosity 0.65dl / g:0.80dl / g=1 : 1) and PEG-60003g were dissolved in 600ml of dichloromethane, the water phase was poured into the oil phase under the effect of high-shear homogenizer rotating speed 2000r / m, emulsified under 2500r / m rotating speed for 5-8min to obtain w / o Emulsion, pour w / o emulsion into 4000ml ice-bath containing 2%PVA, 1%NaCl external water phase solution, stirring speed 700r / m, time 2-3 minutes, then add 1000ml external water phase solution, The stirring speed was 550r / m and the stirring time was 5 hours. The organic solvent was evaporated, suction filtered, washed 3 times with distilled water, and freeze-dried to obtain a white powder with good fluidity. The average particle size of the ...

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Abstract

The invention provides a slow release microsphere agents, comprising thymosin Alpha 1 of 0.5% to 10% of the microsphere weight, degradable pharmaceutical macromolecular accessories with a molecular weight of 5,000 to 500,000 Dalton and of 70% to 99.5% of the macroshpere weight, and 0% to 10% of other pharmaceutically acceptable accessories. The invention also provides the preparation method of the slow release microsphere agents. The slow release microsphere agent of thymosin Alpha 1 for injection has the advantages that the poison and side effect of thymosin Alpha 1 is reduced; the bioavailability is enhanced; times for drug taking is reduced and the drug can be conveniently taken by patients.

Description

technical field [0001] The invention relates to a thymosin alpha for injection 1 A sustained-release microsphere preparation belongs to the field of medicines. Background technique [0002] thymosin alpha 1 (thymosin α 1 , referred to as T α 1 ) is a polypeptide with immune function and is mostly used in the treatment of viral hepatitis clinically. Its amino acid sequence is [0003] A C-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-lys-Glu-Lys-Lys-Glu-Val-Val-Glu -Glu-Ala-Glu-Asn_-OH [0004] Molecular formula: C 129 h 215 N 33 o 55- [0005] Molecular weight: 3108.37 [0006] Existing Tα 1 Due to short half-life and long treatment time, preparations require frequent administration, poor patient compliance and low bioavailability. [0007] Thymosin alpha 1 There are many reports on microspheres, such as: He Yi et al., Preparation and Release Performance of Thymosin Polylactic Acid Microspheres, Chinese Journal of Pharmaceutical Industry, 2006...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/17A61K9/16A61K47/32A61K47/34A61K47/36A61P37/02A61K47/10A61K47/42
Inventor 叶兵刘金花李伯刚刘忠荣及元乔
Owner CHENGDU DIAO JIUHONG PHARMA FACTORY
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