Method for controlling residue of organic solvent in thymic peptide alpha1 microballoon

An organic solvent, thymosin technology, applied in the field of medicine, can solve the problems of fusion or rupture, microsphere adhesion, leakage or outflow of thymosin α1, etc., to achieve the effect of maintaining a complete shape and a stable process

Active Publication Date: 2010-06-30
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 mult

Method used

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  • Method for controlling residue of organic solvent in thymic peptide alpha1 microballoon
  • Method for controlling residue of organic solvent in thymic peptide alpha1 microballoon

Examples

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preparation example Construction

[0038] 1. Preparation of inspection samples

[0039] Prescription 1 (release time 4 weeks)

[0040] Ta1 1.0g

[0041] PLGA(0.15~0.25dl / g)(50 / 50) 36.0g

[0042] Selected organic solvent: dichloromethane

[0043] Preparation process: add the prescribed amount of Ta1 into 30ml of pH 7.4 phosphate buffer solution at room temperature, dissolve it completely, and obtain the aqueous phase for later use;

[0044] 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;

[0045] 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;

[0046] 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% Add 200ml of NaCl aqueous solution to obtain double...

Embodiment 1

[0090] Embodiment 1 The present invention controls the method for residual organic solvent in thymosin α1PLGA microspheres

[0091] Ta1 1.0g

[0092] PLGA(0.15~0.25dl / g)(50 / 50) 38.0g

[0093] Preparation Process

[0094] Add the prescribed amount of Ta1 to 30ml of pH 7.4 phosphate buffer at room temperature to dissolve completely to obtain the aqueous phase for later use;

[0095] 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;

[0096]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;

[0097] 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

[0098] Embodiment 2 The present invention controls the method for residual organic solvent in thymosin α1PLGA microspheres

[0099] Ta1 1.0g

[0100] PLGA(0.24~0.56dl / g)(50 / 50) 32.0g

[0101] Preparation Process

[0102] Add the prescribed amount of Ta1 to 30ml of pH 7.4 phosphate buffer at room temperature to dissolve completely to obtain the aqueous phase for later use;

[0103] 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;

[0104] 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;

[0105] Cool 1600ml of aqueous solution containing 2% PVA and 3% NaCl to below 10°C, adjust the speed of the mixer to 500-1000 rpm, 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 hou...

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Abstract

The invention provides a method for controlling residue of organic solvent in thymic peptide alpha1 microvballoon, including that thymic peptide alpha1 PLGA microballoon emulsion or multiple emulsion obtained by preparation is stirred under the conditions that temperature is 15-42 DEG C and rotating speed is 20-3000r/min. The method for controlling residue of organic solvent in thymic peptide alpha1 microballoon of the invention is efficient and controllable, stable in technology and safe and reasonable, can effectively control the residue problem of organic solvent such as dichloromethane and meanwhile can maintain the form of microballoon to be complete.

Description

technical field [0001] 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 [0002] 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: [0003] AC-Ser-Asp-Alα-Alα-Vαl-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-lys-Glu-Lys-Lys-Glu-Vαl-Vαl-Glu- Glu-Alα-Glu-Asn_-OH [0004] Molecular formula: C 129 h 215 N 33 o 55 [0005] Molecular weight: 3108.37 [0006] Due to the short half-life of the existing thymosin α1 preparations and long treatment time, frequent administration is required, which has the disadvantages of poor patient compliance and low bioavailability. At present, microsphere preparations are used to prepar...

Claims

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Application Information

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IPC IPC(8): A61K38/17A61K9/16A61K47/34A61P37/04A61P1/16
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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