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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AI-Extracted 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...

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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.

Application Domain

Organic active ingredientsPharmaceutical non-active ingredients +1

Technology Topic

ChemistryOil phase +12

Image

Examples

Experimental program(3)

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 spray pressure of 0.5MPa. After collecting the microspheres in a cyclone, the temperature is 50°C. Dry under reduced pressure for 2 hours, and then pass through an 80-mesh sieve to obtain the product.

[0051] The resulting microspheres have round morphology, smooth surface, good fluidity, and uniform particle size. The average particle size is 79.43 μm, the drug loading is 22.54%, the encapsulation rate is 90%, and the burst release is less than 5%. It lasts for about a month, and the cumulative release in 30 days is about 80%. The in vitro release performance is in line with the characteristics of long-acting preparations. In vitro cumulative drug release curve (37℃) of prepared doxorubicin hydrochloride sustained-release microspheres, see figure 1.

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, the feeding speed is 20mL/min, and the spray pressure is 0.4MPa. After collecting the microspheres in the cyclone, the temperature is 40°C. Dry under reduced pressure for 3 hours, then pass through an 80-mesh sieve to obtain the product.

[0063] The obtained microspheres have round morphology, smooth surface, good fluidity, uniform particle size distribution, with an average particle size of 69.59μm, drug loading of 16.5%, encapsulation efficiency of 95.68%, burst release less than 15%, sustained release microspheres In vitro sustained release for more than 36 days, the in vitro release performance is in line with the characteristics of long-acting preparations. In vitro cumulative drug release curve (37℃) of the prepared 5-fluorouracil sustained-release microspheres, see figure 2.

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 mL/min, and the spray pressure is 0.3 MPa.

[0076] After collecting the microspheres in a cyclone, they were dried under reduced pressure at 45°C for 1 hour, and then passed through an 80-mesh sieve to obtain the product.

[0077] The obtained microspheres have round morphology, smooth surface, good fluidity, uniform particle size distribution, average particle size 79.43μm, drug loading of 19.98%, encapsulation rate of 88%, burst release less than 10%, sustained-release microspheres The in vitro release performance is in line with the characteristics of long-acting preparations. In vitro cumulative drug release curve (37℃) of prepared metformin hydrochloride sustained-release microspheres, see image 3.

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PUM

Property	Measurement	Unit
Particle size	<= 250.0	µm
tensile		MPa
Particle size		Pa
strength	10

Description & Claims & Application Information

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Classification and recommendation of technical efficacy words

Flat surface
Round shape

Method for preparing hydrophilic drug microsphere through spray drying process

AI-Extracted Technical Summary

Problems solved by technology

Abstract

Image

Examples

Example Embodiment

Example Embodiment

Example Embodiment

PUM

Description & Claims & Application Information

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