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.
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[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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