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Triamcinolone acetonide acetate sustained release microsphere and preparation method thereof

A technology of triamcinolone acetonide acetate and sustained-release microspheres, which is applied in pharmaceutical formulations, microcapsules, medical preparations with inactive ingredients, etc., can solve the problems of poor patient compliance, short preparation release time, etc., and achieve slow drug loading. Release, reduce drug loss, good form effect

Active Publication Date: 2019-09-17
JIANG SU PHARMAMAXCORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In order to solve the above-mentioned technical problems, the object of the present invention is to provide a triamcinolone acetonide acetate sustained-release microspheres and a preparation method thereof, the preparation method is simple and fast, and can effectively solve the problems of short release time of the preparation and poor patient compliance

Method used

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  • Triamcinolone acetonide acetate sustained release microsphere and preparation method thereof
  • Triamcinolone acetonide acetate sustained release microsphere and preparation method thereof
  • Triamcinolone acetonide acetate sustained release microsphere and preparation method thereof

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Effect test

Embodiment 1

[0033] Weigh 70.8 mg of triamcinolone acetonide acetate and 187.5 mg of PLA dissolved in 7.5 mL of acetone. Under stirring conditions, add the drug-containing PLA solution to 7.5mL of the water phase containing 5% (w / v) stabilizer PVA to form an O / W emulsion, volatilize acetone in the fume hood for 6h, and transfer the microsphere system to 300mL Cured in water for 8h. Stand still after solidification, and after the suspended matter settles to the bottom, remove the upper aqueous solution, collect the microspheres deposited at the bottom, wash with water three times, collect the microspheres by centrifugation, and freeze-dry.

Embodiment 2

[0035] Weigh 70.8mg of triamcinolone acetonide acetate and 187.5mg of PLGA (molar ratio of lactide to glycolide=75:25, Mw=1.2wg / mol), and dissolve them in 7.5mL of dichloromethane. Under stirring conditions, add the PLGA solution containing the drug to 150mL of water phase containing 1% (w / v) stabilizer PVA to form an O / W emulsion, volatilize methylene chloride for 6h in the fume hood, and transfer the microsphere system to Cured in 300mL water for 8h. Stand still after solidification, and after the suspended matter settles to the bottom, remove the upper aqueous solution, collect the microspheres deposited at the bottom, wash with water three times, collect the microspheres by centrifugation, and freeze-dry.

Embodiment 3

[0037] Weigh 70.8mg of triamcinolone acetonide acetate and 187.5mg of PLGA (molar ratio of lactide to glycolide=75:25, Mw=1.2wg / mol), and dissolve them in 7.5mL of ethyl acetate. Under stirring conditions, add the PLGA solution containing the drug to 150mL of water phase containing 1% (w / v) stabilizer PVA to form an O / W emulsion, volatilize methylene chloride for 6h in the fume hood, and transfer the microsphere system to Cured in 300mL water for 8h. Stand still after solidification, and after the suspended matter settles to the bottom, remove the upper aqueous solution, collect the microspheres deposited at the bottom, wash with water three times, collect the microspheres by centrifugation, and freeze-dry.

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Abstract

The invention relates to a triamcinolone acetonide acetate sustained release microsphere and a preparation method thereof. The method comprises the following steps that triamcinolone acetonide acetate and a degradable polymer with a hydrophobic chain segment are dissolved in an organic solvent, and a polymer solution with drugs is obtained; under the stirring condition, the polymer solution with drugs is added to a water phase to form an O / W emulsion, and the organic solvent in the emulsion is removed; the water phase contains a stabilizer, and the proportion of the stabilizer to the water phase is 0.1-5% (w / v); under the stirring condition, the obtained dispersion system is added into water for solidification, and the triamcinolone acetonide acetate sustained release microsphere is obtained. The triamcinolone acetonide acetate sustained release microsphere is proper in particle diameter, round in shape, high in encapsulation efficiency and good in drug loading capacity, and the problems of short release time of a preparation and poor compliance of a patient can be effectively solved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a triamcinolone acetate sustained-release microsphere and a preparation method thereof. Background technique [0002] Triamcinolone acetonide acetate (TAA) is a synthetic fluorine-containing medium- and long-acting adrenal glucocorticoid. It has strong anti-inflammatory and anti-allergic effects and quick onset, which can significantly improve the condition of patients. The anti-inflammatory and anti-allergic effect of triamcinolone acetonide acetate is similar to that of hydrocortisone, and the anti-inflammatory effect is 5 to 20 times that of hydrocortisone. However, triamcinolone acetonide acetate has a strong water and sodium retention effect, and long-term use can lead to adverse reactions such as skin atrophy, telangiectasia, rosacea-like dermatitis, perioral dermatitis, and secondary infection. Therefore, in the process of preparation development, it i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/34A61K31/58A61P29/00A61P37/08A61P17/00A61P11/02A61P11/06A61P19/02A61P19/04
CPCA61K9/5031A61K9/5089A61K31/58A61P11/02A61P11/06A61P17/00A61P19/02A61P19/04A61P29/00A61P37/08
Inventor 曹青日杜欢欢夏亚男
Owner JIANG SU PHARMAMAXCORP
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