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Method for controlling organic solvent residue in thymosin alpha 1 microspheres

A technology of organic solvents and thymosin, applied in antiviral agents, pharmaceutical formulations, peptide/protein components, etc., can solve problems such as fusion or rupture, adhesion of microspheres, loss of burst release of microsphere preparations, energy efficiency of slow and controlled release, etc., to achieve The effect of maintaining complete shape and process stability

Active Publication Date: 2013-11-13
CHENGDU DIAO JIUHONG PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the microsphere preparation process, if the temperature is close to or higher than the glass transition temperature of PLGA, the elasticity of PLGA increases, and when the microspheres contact and collide, the microspheres are prone to fusion or sphere rupture and cause thymosin α1 to leak or flow out; At the same time, due to the temperature rise of the double emulsion, the microspheres form pores, and the pores of multiple microspheres tend to fuse after colliding, resulting in adhesion, fusion or rupture of the microspheres, resulting in serious burst release of the microsphere preparation or loss of slow release. The energy efficiency of controlled release, can not be used as medicine
Therefore, only by increasing the temperature can not reduce the residual organic solvent, nor can it guarantee the quality of the microsphere preparation

Method used

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  • Method for controlling organic solvent residue in thymosin alpha 1 microspheres
  • Method for controlling organic solvent residue in thymosin alpha 1 microspheres
  • Method for controlling organic solvent residue in thymosin alpha 1 microspheres

Examples

Experimental program
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preparation example Construction

[0039] 1. Preparation of inspection samples

[0040] Prescription 1 (release time 4 weeks)

[0041]Ta1 1.0g

[0042] PLGA (0.15~0.25dl / g) (50 / 50) 36.0g

[0043] Selected organic solvent: dichloromethane

[0044] Preparation process: Add the prescribed amount of Ta1 into 30ml of pH7.4 phosphate buffer at room temperature, dissolve it completely, obtain the aqueous phase, and set aside;

[0045] Add the prescribed amount of PLGA into 150ml of dichloromethane at room temperature to dissolve it completely to obtain an oil phase for subsequent use;

[0046] At 10-25°C, adjust the speed of the emulsifier to 2000-2800 rpm, inject the water phase into the oil phase, and emulsify for 5-10 minutes to obtain colostrum (O / W) for later use;

[0047] Cool 800ml of aqueous solution containing 3%PVA and 5%NaCl to below 10°C, adjust the speed of the mixer to 500-1000 rpm, add colostrum, stir for 2 minutes, then add 3%PVA, 5% NaCl aqueous solution 200ml, get double emulsion (W / O / W), keep i...

Embodiment 1

[0089] Embodiment 1 The present invention controls the method for residual organic solvent in thymosin α1PLGA microspheres

[0090] Ta1 1.0g

[0091] PLGA (0.15~0.25dl / g) (50 / 50) 38.0g

[0092] Preparation Process

[0093] Add the prescribed amount of Ta1 into 30ml of pH7.4 phosphate buffer at room temperature to dissolve completely to obtain an aqueous phase for later use;

[0094] Add the prescribed amount of PLGA into 150ml of dichloromethane at room temperature to dissolve it completely to obtain an oil phase for subsequent use;

[0095]At 10-25°C, adjust the speed of the emulsifier to 2000-2800 rpm, inject the water phase into the oil phase, and emulsify for 5-10 minutes to obtain colostrum (O / W) for later use;

[0096] Cool 800ml of aqueous solution containing 3%PVA and 5%NaCl to below 10°C, adjust the speed of the mixer to 500-1000 rpm, add colostrum, stir for 2 minutes, then add 3%PVA, 5% 200ml of NaCl aqueous solution to obtain double emulsion (O / W / O). Stir for ...

Embodiment 2

[0097] Embodiment 2 The present invention controls the method for residual organic solvent in thymosin α1PLGA microspheres

[0098] Ta1 1.0g

[0099] PLGA (0.24~0.56dl / g) (50 / 50) 32.0g

[0100] Preparation Process

[0101] Add the prescribed amount of Ta1 into 30ml of pH7.4 phosphate buffer at room temperature to dissolve completely to obtain an aqueous phase for later use;

[0102] Add the prescribed amount of PLGA into 100ml of ethyl formate at room temperature to dissolve it completely to obtain an oil phase for later use;

[0103] At 10-25°C, adjust the speed of the emulsifier to 2500-3200 rpm, inject the water phase into the oil phase, and emulsify for 5-10 minutes to obtain colostrum (O / W) for later use;

[0104] Cool 1600ml of aqueous solution containing 2%PVA and 3%NaCl to below 10°C, adjust the speed of the mixer to 500-1000rpm, add colostrum, stir for 2 minutes, then add 2%PVA, 3% 400ml of NaCl aqueous solution to obtain double emulsion (O / W / O). Stir for 3 hour...

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Abstract

The invention provides a method for controlling organic solvent residue in thymosin alpha 1PLGA microspheres. The method comprises the following steps: stirring a prepared thymosin alpha 1PLGA microsphere emulsion or multiple emulsion under normal temperature and normal pressure at a speed of 500-1200rpm for 3 hours; stirring the emulsion or multiple emulsion for 2-18 hours under the conditions of vacuum degree of -0.035MP to -0.096MP, a temperature of 26-35 DEG C and rotating speed of 50-800 rpm. The method for controlling organic solvent residue in thymosin alpha 1 microspheres provided by the invention is efficient, controllable, stable in process, safe, reasonable and capable of effectively controlling the residue problem of such organic solvents as dichloromethane and keeping the integral forms of the microspheres at the same time.

Description

[0001] This application is a divisional application of a patent application with an application date of December 23, 2008, an application number of CN200810240539.9, and an invention title of "Method for controlling organic solvent residue in thymosin α1 microspheres". technical field [0002] The invention relates to a preparation process of a pharmaceutical preparation, in particular to a method for controlling the residual amount of an organic solvent in thymosin α1PLGA microspheres, and belongs to the field of medicine. Background technique [0003] Thymosin α1 (thymosin alpha1, referred to as Tα1) is a polypeptide with immune function, which is mostly used clinically for immune enhancement or treatment of viral hepatitis. Its amino acid sequence is: [0004] ΑC-Ser-Αsp-Α1α-Α1α-Vα1-Αsp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Α sp-Leu-lys-Glu-Lys-Lys-Glu-Vα1-Vα1-Glu -Glu-Αlα-Glu-Αsn-OH [0005] Molecular formula: C 129 h 215 N 33 o 55 [0006] Molecular weight: 3108.37 [...

Claims

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Application Information

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IPC IPC(8): A61K38/22A61K9/19A61P37/04A61P1/16A61P31/14A61P31/20
Inventor 叶兵武勇刘金花黄梅鲍锐谢毅毛华
Owner CHENGDU DIAO JIUHONG PHARMA FACTORY
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