Method for preparing hydrophilic drug microsphere through spray drying process

A hydrophilic drug and spray-drying technology, which is applied in the direction of pharmaceutical formulations, organic active ingredients, medical preparations of non-active ingredients, etc., can solve the problem of low encapsulation efficiency of hydrophilic drugs, short sustained release time of drugs Difficult to produce in large quantities, etc., to overcome the large volume of oily substances and a large number of volatile solvents to wash, round the shape, and reduce the effect of organic residues

Active Publication Date: 2013-05-22
武汉回盛生物科技股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the solvent evaporation method has the following disadvantages: the prepared microspheres are easy to agglomerate, so it is difficult to produce in large quantities; a large amount of organic solvent is required in the preparation process, and it is difficult to remove the residual organic solvent in the prepared microspheres; the steps are complicated, The system needs to strictly control the temperature, viscosity and other conditions of the microemulsion; the encapsulation efficiency of hydrophilic drugs is very low
The microsphere preparation prepared by traditional spray drying method is mostly one-step encapsulation, which not only has obvious burst release effect, but also has a short sustained release time of the drug

Method used

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  • Method for preparing hydrophilic drug microsphere through spray drying process
  • Method for preparing hydrophilic drug microsphere through spray drying process
  • Method for preparing hydrophilic drug microsphere through spray drying process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039]The preparation of embodiment 1 doxorubicin hydrochloride sustained-release microspheres

[0040] Raw material prescription:

[0041]

[0042]

[0043] The preparation process is as follows:

[0044] (1) Configure spray liquid

[0045] Dissolve the acrylic resin II in the ethanol solution, then add glyceryl monostearate and castor oil and stir evenly;

[0046] (2) Primary package of raw materials

[0047] Uniformly disperse doxorubicin hydrochloride in sesame oil containing Span80 to prepare S / O 1 type suspension.

[0048] (3) Homogeneous emulsification of spray liquid

[0049] Add the suspension prepared in (2) to the spray liquid obtained in (1) for homogeneous emulsification, the homogenization temperature is 50 °C, the speed of the high-speed shear homogenizer is 14000 rpm, and the time is 6 minutes to obtain S / o 1 / O 2 type spray emulsion;

[0050] (4) Spray drying: Spray dry the above-mentioned spray emulsion, the air inlet temperature is 160°C, the...

Embodiment 2

[0052] Example 2 Preparation of 5-fluorouracil sustained-release microspheres

[0053] Raw material prescription:

[0054]

[0055] The preparation process is as follows:

[0056] (1) Configure spray liquid

[0057] Dissolve acrylic resin Eudragit L100 and acrylic resin Eudragit S100 in ethanol solution, then add glyceryl monostearate and castor oil and stir well.

[0058] (2) Primary package of raw materials

[0059] Disperse 5-fluorouracil evenly in peanut oil containing Span80 to make S / O 1 type suspension.

[0060] (3) Homogeneous emulsification of spray liquid

[0061] Add the suspension prepared in (2) to the spray liquid obtained in (1) for homogeneous emulsification, the homogenization temperature is 50°C, the speed of the high-speed shear homogenizer is 10000 rpm, and the time is 9min, to obtain S / o 1 / O 2 type spray emulsion.

[0062] (4) Spray drying: Spray dry the above-mentioned spray emulsion, the air inlet temperature is 145°C, the air outlet temper...

Embodiment 3

[0064] The preparation of embodiment 3 metformin hydrochloride sustained-release microspheres

[0065] Raw material prescription:

[0066]

[0067] The preparation process is as follows:

[0068] (1) Configure spray liquid

[0069] Dissolve acrylic resin Eudragit L100 in ethanol solution, then add glyceryl monostearate and castor oil and stir well.

[0070] (2) Primary package of raw materials

[0071] Disperse metformin hydrochloride evenly in sesame oil containing Span80, and prepare S / O 1 type suspension.

[0072] (3) Homogeneous emulsification of spray liquid

[0073] Add the suspension prepared in (2) to the spray liquid obtained in (1) for homogeneous emulsification, the homogenization temperature is 50°C, the speed of the high-speed shear homogenizer is 20000 rpm, and the time is 4min, to obtain S / o 1 / O 2 type spray emulsion.

[0074] (4) spray drying

[0075] The above-mentioned spray emulsion was spray-dried, the inlet air temperature was 155°C, the out...

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Abstract

The invention relates to the technical field of preparation of hydrophilic drug microspheres, in particular discloses a method for preparing a hydrophilic drug microsphere through a spray drying process. The method comprises preparation steps of: uniformly dispersing hydrophilic drug powder into an isolation oil phase to form an S / O1 type suspension, and then slowly adding into a spray solution (O2) which contains a macromolecular carrier, an anti-sticking agent and a plasticizing agent, homogeneously emulsifying to form an S / O1 / O2 type spray emulsion, decompressing and drying at 60 DEG C or less through a spray drying technology after collecting the microspheres in a cyclone separator, and screening with a sieve of 80 meshes so as to prepare the hydrophilic drug twice-embedded sustained-release microsphere. The microsphere prepared by spray drying have the advantages of round shape, smooth surface, good mobility, uniform grain size distribution, high encapsulating rate, capability ofeffectively controlling burst release, and accordance with the characteristics of a long-acting preparation; and the method has the advantages of reducing consumption of a great quantity of oil substances and volatile organic solvents , greatly shortening drying time and being remarkable in effect, and is applicable to industrial production.

Description

technical field [0001] The invention relates to the technical field of preparation of hydrophilic drug microspheres, in particular to a method for preparing hydrophilic drug microspheres by a spray drying method. This method is suitable for the preparation of controlled release drugs. Background technique [0002] Controlled drug release is a new technology developed in the 1980s and a new field of pharmacology. The drug controlled release system refers to embedding the drug in a certain polymer excipient. Since the dissolution and diffusion speed of the drug are limited by different excipients and preparation processes, the drug is released slowly, continuously and stably through the erosion and hydrolysis of the polymer. effect. One of the purposes of designing drug sustained-release preparations is to prolong the action time of the drug as much as possible or to achieve the desired long action time; the other is to reduce the local tissue or blood concentration and pote...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/32A61K47/34A61K47/38A61K31/155A61K31/513A61K31/704
Inventor 张卫元张永丹陈翠兰刘国庆
Owner 武汉回盛生物科技股份有限公司
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