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A method for preparing polypeptide drug microspheres based on subliquid jet spray technology

A technology of polypeptides and airflow nozzles, which is used in pharmaceutical formulations, microcapsules, nanocapsules, etc., can solve the problems of low spheroidization rate of microspheres, easy aggregation, and difficulty in realization of microspheres, and achieves high yield and drug production. Release uniform and long-lasting effects with low equipment cost

Active Publication Date: 2022-03-25
ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the inventors of the present application have found in the course of their research that it is difficult to realize the preparation of microspheres in this way, and the biggest problem is that when the primary emulsion containing high viscosity (>1000cp) is sprayed into the liquid surface of an aqueous solution (such as PVA), even if Under stirring conditions, a large number of films will inevitably be formed. The polymer solution at the gas-liquid interface is not surrounded by water in time and fully, and the surface of the microspheres is not yet solidified, and it is easy to aggregate (similar to carboxymethyl Sodium cellulose dissolution phenomenon), resulting in extremely low microsphere formation rate

Method used

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  • A method for preparing polypeptide drug microspheres based on subliquid jet spray technology
  • A method for preparing polypeptide drug microspheres based on subliquid jet spray technology
  • A method for preparing polypeptide drug microspheres based on subliquid jet spray technology

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Embodiment approach

[0040] A method for preparing polypeptide drug microspheres based on submerged airflow spray technology, comprising the following steps:

[0041](1) Dissolving the polypeptide water-soluble drug in water to obtain an inner aqueous drug solution with a concentration of 40-55wt%; dissolving the carrier material in an organic solvent to obtain a phase polymer solution with a concentration of 25-40wt% oil; The water-soluble drug is selected from one of leuprolide acetate, triptorelin acetate, goserelin acetate, octreotide, exenatide, lanreotide and pasireotide; the carrier material is PLA or PLGA; the organic solvent is selected from one of dichloromethane, ethyl acetate and chloroform.

[0042] (2) adding the oil phase polymer solution to the inner water phase drug solution, the volume ratio of the inner water phase drug solution and the oil phase polymer solution is controlled to be 1: 11-22, and ultrasonic crushing or shear dispersion forms Colostrum, the colostrum particle si...

Embodiment 1

[0050] (1) dissolving leuprolide acetate in water to obtain an inner water phase with a drug concentration of 50%; dissolving PLGA (7525, Mw13000Da) at the carboxyl end in dichloromethane to obtain an oil with a polymer concentration of 33.3% Mutually;

[0051] (2) adding the above-mentioned oil phase to the inner water phase (volume ratio 12.5:1), controlling the colostrum shearing temperature to be 15°C, and using a high-speed shearing machine at 12000rpm to shear for 10min to form a primary emulsion, and the primary emulsion viscosity is 1541cp (20.83°C);

[0052] (3) setting the airflow velocity to be 130L / min, the above-mentioned initial emulsion is supplied into the liquid inlet of the airflow nozzle at a constant speed with a flow rate of 10mL / min, after the compressed air flow is broken, the bottom of the drying tank in the liquid is sprayed into 15 ℃ from bottom to top In a 0.1% concentration polyvinyl alcohol aqueous solution, under stirring at 300 rpm, a well-dispe...

Embodiment 2

[0059] (1) dissolving leuprolide acetate in water to obtain an inner water phase with a drug concentration of 50%; PLGA (7525, Mw 13000Da) at the carboxyl end is dissolved in dichloromethane to obtain a polymer concentration of 37.5%. oil phase;

[0060] (2) adding the above-mentioned oil phase to the inner water phase (volume ratio 12.5:1), controlling the colostrum shearing temperature to be 17°C, and shearing for 10 min under the condition of a high-speed shearing machine at 12000 rpm to form a primary emulsion, and the initial emulsion viscosity is 2499cp (18.94°C);

[0061] (3) setting the airflow flow rate to be 130L / min, the above-mentioned initial emulsion is supplied into the liquid inlet of the airflow nozzle at a constant speed with a flow rate of 10mL / min, after the compressed air flow is broken, the bottom of the drying tank in the liquid is sprayed into 17 ℃ from bottom to top In a 0.1% concentration polyvinyl alcohol aqueous solution, under stirring at 300 rpm,...

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Abstract

The invention discloses a method for preparing polypeptide drug microspheres based on subliquid airflow spraying technology, which comprises the following steps: (1) dissolving polypeptide water-soluble drugs in water to obtain an inner water phase drug solution; dissolving carrier materials in In an organic solvent, an oil phase polymer solution is obtained; (2) the oil phase polymer solution is added to the internal water phase drug solution, ultrasonically crushed or shear dispersed to form a primary emulsion; (3) the primary emulsion is transported to The liquid inlet of the airflow nozzle located at the bottom of the liquid drying tank, and the gas inlet of the airflow nozzle is opened at the same time to atomize the primary emulsion, and the nozzle opening of the airflow nozzle is sprayed into the liquid from bottom to top into the liquid drying tank. In the aqueous solution of the agent, start the stirring while spraying the primary emulsion to form a double emulsion, and then dry it in the liquid at 15-25°C for 3-5 hours to remove the organic solvent, and obtain the polypeptide drug microspheres. The microspheres produced by the invention have high encapsulation efficiency, spheroidization rate and high production efficiency.

Description

technical field [0001] The invention relates to the technical field of microsphere production, in particular to a method for preparing polypeptide drug microspheres based on the submerged airflow spray technology. Background technique [0002] Microspheres refer to the particle dispersion system formed by dispersing or adsorbing drugs in macromolecules and polymer matrices. Compared with traditional preparations, microspheres can reduce the number of administrations, improve patient compliance, reduce side effects, and improve efficacy. The microsphere formulation technology that can be industrialized must first be able to ensure the controllability of its critical quality attributes (CQAs), such as: microsphere morphology, particle size and particle size distribution, drug loading and encapsulation efficiency, and in vitro release. The good control of CQAs, etc., will greatly promote the development of drugs and technological transformation. Especially for polypeptide and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K38/08A61K38/09A61K38/22A61K38/12A61K47/34A61K47/32
CPCA61K38/09A61K38/08A61K38/22A61K38/12A61K9/5192A61K9/5153A61K9/5138
Inventor 于崆峒蒋朝军刘喜明
Owner ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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