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Method for improving encapsulation yield of water-soluble drug microsphere drug-loading system

A technology for water-soluble drugs and drug-carrying systems, applied in the field of medicine, can solve the problems of obvious burst release phenomenon of microspheres, short in vitro release time, low drug encapsulation rate, etc., and achieves good fluidity, complete shape and stable preparation process. Effect

Inactive Publication Date: 2018-01-05
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Abstract
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Problems solved by technology

[0003] The available emulsification solvent volatilization method for preparing water-soluble drug microspheres includes three methods. The first method is water-in-oil (W / O) emulsification solvent volatilization method, but when using this method to prepare water-soluble drug sustained-release microspheres, Due to the water solubility of the drug, a large amount of loss is caused during the preparation process, and the drug encapsulation efficiency is very low
The second method is the oil-in-oil (O / O) emulsified solvent evaporation method. Although the microspheres with high encapsulation efficiency and drug loading capacity are obtained, the burst release phenomenon of the microspheres is obvious, the release time in vitro is short, and the sustained-release effect is relatively short. Difference
Since the drug is freely dispersed in the inner aqueous phase, the water-soluble drug is easily released during the preparation process, resulting in a low encapsulation efficiency of the prepared microspheres

Method used

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  • Method for improving encapsulation yield of water-soluble drug microsphere drug-loading system
  • Method for improving encapsulation yield of water-soluble drug microsphere drug-loading system
  • Method for improving encapsulation yield of water-soluble drug microsphere drug-loading system

Examples

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Embodiment 1

[0030] This example uses the method of the present invention to prepare microspheres whose carrier material is ethyl cellulose and the model drug metformin hydrochloride, and mainly investigates the influence of different gelatin concentrations on the encapsulation yield.

[0031] The drug concentration is 10%, and the oil phase is a dichloromethane solution saturated with metformin aqueous solution, wherein the concentration of ethyl cellulose is 10%, and the volume ratio of the inner water phase to the oil phase is 1:40. The water phase is 1% PVA, and its volume ratio to colostrum is 10:1, emulsified using a high-shear dispersing emulsifier. The gelatin concentrations were selected to be 0%, 15%, 20%, 25%, and 30%, respectively, and the encapsulation yield and drug loading of metformin hydrochloride microspheres were shown in Table 1. It can be seen that the encapsulation yield and drug loading are the highest when the gelatin concentration is 20%. figure 1 It is a 64-fold ...

Embodiment 2

[0035] In this example, the method of the present invention is used to prepare microspheres whose carrier material is PLGA and the model drug metformin hydrochloride.

[0036] The drug concentration is 10%, the oil phase adopts the dichloromethane solution saturated with metformin aqueous solution, wherein the PLGA concentration is 25%, the volume ratio of the inner water phase and the oil phase is 1:40, and the ultrasonic cell pulverizer is used for ultrasonication, and the outer water phase is 1% PVA, its volume ratio to colostrum is 10:1, emulsified using a high shear dispersing emulsifier. The gelatin concentration was selected as 20%, and the encapsulation yield and drug loading of metformin hydrochloride microspheres were 75.91% and 2.01%, respectively.

Embodiment 3

[0038] In this example, microspheres in which the carrier material is PLGA and the model drug is atropine sulfate are prepared by the method of the present invention.

[0039] The drug concentration is 10%, the oil phase adopts dichloromethane solution, wherein the PLGA concentration is 25%, the volume ratio of the inner water phase and the oil phase is 1:40, and the ultrasonic cell pulverizer is used for ultrasonication, and the outer water phase is 1%PVA. Its volume ratio to colostrum is 10:1, and it is emulsified using a high-shear dispersing emulsifier. When the concentration of gelatin is 20%, the encapsulation yield and drug loading of atropine sulfate microspheres are 77.36% and 3.65%.

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Abstract

The purpose of the present invention is to provide a method for improving the encapsulation yield of the water-soluble drug microsphere drug-carrying system. Based on the existing double-emulsion method (W / O / W), the present invention adds gelatin with a mass fraction of 15% to 30% to the inner water-phase drug-containing solution forming the double-emulsion. The invention improves the encapsulation yield of the water-soluble drug microsphere drug-carrying system.

Description

technical field [0001] The invention relates to a method for improving the encapsulation yield of a water-soluble drug microsphere drug-loading system, which belongs to the technical field of medicine. Background technique [0002] Micro-sphere technology is a new process and new technology applied in drug delivery system in the past 30 years. Microsphere (microsphere) refers to the particle dispersion system formed by drug dispersion or adsorption in polymer or polymer matrix. Microsphere preparations have the following advantages: ① cover up the adverse characteristics of the drug and reduce the irritation of the drug; ② improve the stability of the drug; ③ change the properties of the drug; Microencapsulation of living cells or biologically active substances; ⑥ avoiding the first-pass effect; ⑦ targeted. Microsphere preparations can greatly improve the convenience and compliance of patients with medication, and have shown advantages in clinical practice. They are a dosa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K9/19A61K31/155A61K31/704A61K31/46
Inventor 高子彬胡佳孙勇军陈玺谢英花吴亚楠赵亚楠
Owner HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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