Celecoxib porous microspheres for articular cavity injection and preparation method of celecoxib porous microspheres

A technology of celecoxib and porous microspheres, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc. problem, to achieve the effect of simple preparation process, rapid deposition prevention, and maintenance of long-term swelling

Active Publication Date: 2021-06-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The drug loading of microspheres is directly related to the designed clinical dosage. Generally, the higher the drug loading, the lower the dosage, and the encapsulation efficiency is more suitable for evaluating the preparation process level. Generally, the higher the encapsulation efficiency, the better the process. In the process of preparing microspheres by emulsified solvent evaporation method, increasing the ratio of polymer to drug can effectively prevent the drug from leaking into the external phase and obtain a higher encapsulation efficiency, but at the same time it will also lead to a lower drug loading in the microspheres. Low

Method used

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  • Celecoxib porous microspheres for articular cavity injection and preparation method of celecoxib porous microspheres
  • Celecoxib porous microspheres for articular cavity injection and preparation method of celecoxib porous microspheres
  • Celecoxib porous microspheres for articular cavity injection and preparation method of celecoxib porous microspheres

Examples

Experimental program
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Effect test

Embodiment 1

[0037] Preparation of celecoxib PLGA microspheres

[0038] Weigh 0.18g PLGA7525, dissolve 60mg celecoxib (CEL) in 3mL dichloromethane as the organic phase, slowly drop into continuously stirred 30mL concentration of 2% PVA (w / v) aqueous solution, use a high-speed disperser at room temperature for 15 After emulsification at 7000rpm at ~25°C for 5min, pour 50mL of pure water into the above emulsion, stir magnetically at room temperature for 3h at 15-25°C, collect the microspheres by centrifugation, wash with pure water, and freeze-dry to obtain celecoxib PLGA Microspheres.

Embodiment 2～9

[0040] See Table 1 for the prescription.

[0041] The prescription of table 1 embodiment 2~9 celecoxib PLGA microsphere

[0042]

[0043] The microsphere preparation steps of Examples 2-9 are the same as Example 1.

Embodiment 10

[0045] Take by weighing 0.18g PLGA7525, 60mg CEL is dissolved in the mixed solvent (both volume ratio 20:1) 3mL of dichloromethane and ethyl acetate as the organic phase, slowly drip into the 30mL concentration of 2%PVA (w / v) Aqueous solution, use a high-speed disperser to emulsify at 7000rpm at room temperature 15-25°C for 5 minutes, pour 50mL of pure water into the above emulsion, stir magnetically at room temperature 15-25°C for 3 hours, centrifuge to collect the microspheres, wash with pure water, Freeze-dry to obtain celecoxib PLGA porous microspheres.

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PUM

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Abstract

The invention discloses a medicine release speed controllable celecoxib porous microsphere for articular cavity injection and a preparation method of the celecoxib porous microsphere, and belongs to the technical field of pharmaceutical preparations. The porous microspheres are prepared from celecoxib and a high polymer material PLGA (poly (lactic-co-glycolic acid)); and the porous microspheres enable celecoxib to have a specific drug release characteristic, so that the drug can rapidly and effectively act on an inflammation part in a short time to play a rapid analgesic role, the drug can be slowly released in a later period to maintain the long-term detumescence and inflammation inhibition drug effects, the drug administration frequency is reduced, and the compliance of a patient is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a celecoxib porous microsphere for intra-articular injection with controllable drug release rate and a preparation method thereof. Background technique [0002] Rheumatoid arthritis (RA) is a chronic, unexplained, systemic autoimmune disease characterized by joint invasion, mainly manifested as synovitis, and the diseased joints are mainly manifested by inflammatory cells Infiltration, hyperplasia of the synovium, pannus formation and resulting cartilage and bone damage. If it is not treated in time, it can lead to joint deformity and loss of function, and the disability rate is high. There is currently no cure for this disease. The principle of RA treatment is to reduce joint inflammation and reduce rheumatic activity to prevent joint damage, disease progression and long-term disability. [0003] The drugs currently used to treat rheumatoid arth...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/00A61K31/635A61K47/34A61P19/02A61P29/00
CPCA61K9/1647A61K9/0024A61K9/0002A61K31/635A61P19/02A61P29/00
Inventor 姚静樊万君张佳音王宸
Owner CHINA PHARM UNIV
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