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Diacerein sustained-release microspheres and preparation method thereof

A technology of diacerein and sustained-release microspheres is applied in the directions of microcapsules, pharmaceutical formulations, medical preparations of inactive ingredients, etc. Reduce the number of administrations, the preparation method is simple, and the effect is good reproducibility

Active Publication Date: 2020-04-24
北京太洋药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, there are no diacerein sustained-release microspheres in the prior art, especially long-acting diacerein sustained-release microspheres. Research on a new drug delivery system for diacerein can effectively shorten the onset time, Improving the local drug concentration, reducing the side effects of systemic medication, and improving the shortcomings of oral preparations have significant clinical significance. How to effectively shorten the onset time of the drug delivery system and improve the shortcoming of diacerein's slow onset of action is a current research topic. a problem of

Method used

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  • Diacerein sustained-release microspheres and preparation method thereof
  • Diacerein sustained-release microspheres and preparation method thereof
  • Diacerein sustained-release microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0059] Preparation of blank microspheres

[0060] Lactic acid-glycolic acid copolymer (PLGA) was dissolved in dichloromethane in a certain proportion as the organic phase; polyvinyl alcohol (PVA) aqueous solution was used as the water phase; the organic phase was added to the water phase and ultrasonically emulsified intermittently for 20s with an ultrasonic cell pulverizer , to form O / W emulsion; stir at room temperature for 2-3 hours to volatilize dichloromethane, centrifuge at 4000r / min for 20 minutes to separate the particles, wash the precipitate with deionized water 3 times, observe the formation of microspheres with an optical microscope, and dry them in vacuum at 50°C to obtain Blank microspheres, specifically as Image 6 shown.

[0061] Preparation of Diacerein Sustained Release Microspheres

Embodiment 1～3

[0062] Examples 1-3 investigate the effect of emulsifier concentration on drug loading and encapsulation efficiency of microspheres

[0063] Dissolve 200 mg of diacerein in 3 mL of dimethyl sulfoxide, dilute to 10 mL with dichloromethane to obtain a diacerein solution with a concentration of 20 mg / mL; dissolve lactic acid-glycolic acid copolymer (PLGA) in dichloromethane, The concentration is 30mg / mL, diacerein solution and PLGA solution are mixed as the organic phase, the mass ratio of diacerein to PLGA is 1:5; the concentrations are 0.5%, 1%, 2% (w / v) respectively The aqueous solution of polyvinyl alcohol (PVA) is used as the water phase; the volume ratio of the organic phase / water phase is 1:10, the organic phase is added to the water phase, and the ultrasonic emulsification is intermittently performed for 20s with a cell pulverizer to form an O / W emulsion; at room temperature Stir for 2-3 hours to volatilize dichloromethane, centrifuge at 4000r / min for 20 minutes to separa...

Embodiment 4～6

[0071] Examples 4-6 investigate the effect of the mass ratio of the drug to the carrier on the drug loading and encapsulation efficiency of the microspheres

[0072] The specific experimental process refers to Examples 1-3, wherein the concentration of PLGA is 30mg / mL, the volume ratio of organic phase / water phase is 1:10, the concentration of PVA aqueous solution is 1%, and the mass ratio of diacerein and PLGA is 1 respectively. :5, 1:10, 1:20 to prepare diacerein sustained-release microspheres. The specific results are shown in Table 2 below:

[0073] The influence of table 2 diacerein and PLGA mass ratio

[0074] Example Diacerein to PLGA mass ratio Drug loading(%) Encapsulation rate (%) 4 1:5 9.82 41.74 5 1:10 4.89 49.57 6 1:20 3.61 54.23

[0075] The results showed that the mass ratio of drug to carrier had a significant impact on the encapsulation efficiency. As the amount of carrier increases, the dosage ratio decreases, drug ...

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Abstract

The invention provides a diacerein sustained-release microsphere and a preparation method thereof, comprising diacerein, lactic acid-glycolic acid copolymer and polyvinyl alcohol; the drug loading of the diacerein sustained-release microsphere is 3-3 5%, the encapsulation rate is 50-60%, and the particle size is 2-10 μm. The preparation process is: dissolving diacerein in a mixed solvent of dimethyl sulfoxide and dichloromethane to obtain a diacerein solution; dissolving lactic acid-glycolic acid copolymer in an organic solvent to obtain a PLGA solution; mixing the aforementioned solutions as an organic Phase, the polyvinyl alcohol aqueous solution is used as the water phase, and the organic phase is added to the water phase to mix and emulsify to form an O / W emulsion; stir to evaporate the organic solvent, centrifuge, precipitate, and dry to prepare diacerein sustained-release microspheres. The diacerein sustained-release microspheres prepared by the present invention have a long sustained-release period, can shorten the onset time of the drug delivery system, improve the shortcoming of slow onset of oral diacerein, increase local drug concentration, and reduce systemic medication. side effect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a diacerein sustained-release microsphere and a preparation method thereof, in particular to a diacerein sustained-release microsphere for intra-articular injection and a preparation method thereof. Background technique [0002] Osteoarthritis (OA) is a chronic joint disease characterized by degeneration and destruction of articular cartilage and bone hyperplasia. The disease occurs frequently after middle age. Preliminary surveys in China show that the overall prevalence of osteoarthritis is 15%, the prevalence of people aged 40 is 10% to 17%, and that of people over 60 is 50%. And among people over the age of 75, 80% have osteoarthritis. Clinically, joint swelling and pain, bone hyperplasia and limited mobility are the most common. 80% of patients with osteoarthritis have limited activities, and 25% of patients with osteoarthritis cannot complete the main...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K31/222A61K47/34A61P19/02
CPCA61K9/5031A61K31/222
Inventor 李晓芳秦凌浩郭波红易军谭杰文钱慧仪
Owner 北京太洋药业股份有限公司