Method for preparing hydrophilic drug microsphere through spray drying process

A hydrophilic drug, spray-drying technology, applied in pharmaceutical formulations, organic active ingredients, medical preparations with non-active ingredients, etc. It is difficult to mass-produce and other problems, and achieves the effect of overcoming a large volume of oily substances and a large amount of volatile solvents for washing, rounding the shape, and reducing organic residues.

Active Publication Date: 2011-11-02
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, Th

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
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Example Embodiment

[0039] Example 1 Preparation of doxorubicin hydrochloride sustained-release microspheres

[0040] Ingredients prescription:

[0041]

[0042]

[0043] The preparation process is as follows:

[0044] (1) Configure spray liquid

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

[0046] (2) One package of raw materials

[0047] Disperse doxorubicin hydrochloride evenly in sesame oil containing Span80 to make S / O 1 Type suspension.

[0048] (3) Homogeneous emulsification of spray liquid

[0049] Add the suspension obtained in (2) to the spray solution obtained in (1) for homogenization and emulsification. The homogenization temperature is 50°C, the speed of the high-speed shear homogenizer is 14000 rpm, and the time is 6 min. S / O 1 / O 2 Type spray emulsion;

[0050] (4) Spray drying: spray drying the above-mentioned spray emulsion at an inlet temperature of 160°C, an outlet temperature of 80°C, a feeding speed of 10mL / min, and a ...

Example Embodiment

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

[0053] Ingredients prescription:

[0054]

[0055] The preparation process is as follows:

[0056] (1) Configure spray liquid

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

[0058] (2) One package of raw materials

[0059] Disperse 5-Fluorouracil evenly in peanut oil containing Span80 to form S / O 1 Type suspension.

[0060] (3) Homogeneous emulsification of spray liquid

[0061] The suspension obtained in (2) was added to the spray liquid obtained in (1) for homogenization and emulsification. The homogenization temperature was 50°C, the speed of the high-speed shear homogenizer was 10,000 rpm, and the time was 9 min. S / O 1 / O 2 Type spray emulsion.

[0062] (4) Spray drying: spray drying the above-mentioned spray emulsion, the inlet temperature is 145°C, the outlet temperature is 50°C, ...

Example Embodiment

[0064] Example 3 Preparation of metformin hydrochloride sustained-release microspheres

[0065] Ingredients prescription:

[0066]

[0067] The preparation process is as follows:

[0068] (1) Configure spray liquid

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

[0070] (2) One package of raw materials

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

[0072] (3) Homogeneous emulsification of spray liquid

[0073] Add the suspension obtained in (2) to the spray liquid obtained in (1) for homogenization and emulsification, at a homogenization temperature of 50°C, a high-speed shear homogenizer at a speed of 20,000 rpm, and a time of 4 min, to obtain S / O 1 / O 2 Type spray emulsion.

[0074] (4) Spray drying

[0075] The spray emulsion is spray-dried, the inlet air temperature is 155°C, the outlet air temperature is 60°C, the feeding speed is 10 ...

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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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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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