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Temperature-sensitive in-situ gel preparation composition for anticular injection and preparation method thereof

An in-situ gel and composition technology, applied in the field of pharmaceutical preparations, can solve the problems of diclofenac sodium with short half-life, large side effects, gastrointestinal tract and kidney side effects, etc., to facilitate industrial production, improve compliance, and improve drug efficacy Effect

Inactive Publication Date: 2015-04-29
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the long-term medication required by the patient, and the short plasma half-life of diclofenac sodium in the human body (t 1 / 2 =1.5h), need frequent administration, often cause gastrointestinal and kidney side effects
Moreover, administration methods such as oral administration, rectal administration, intramuscular injection, and intravenous injection cannot change its systemic drug distribution, and long-term application has serious side effects.

Method used

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  • Temperature-sensitive in-situ gel preparation composition for anticular injection and preparation method thereof
  • Temperature-sensitive in-situ gel preparation composition for anticular injection and preparation method thereof
  • Temperature-sensitive in-situ gel preparation composition for anticular injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment 1

[0028] Weigh 0.2 g of diclofenac sodium and dissolve it in 10 mg / mL poloxamer 407 solution, add 0.2 g of sodium alginate and stir for 1 hour until completely dissolved, then add 30 mL of liquid paraffin containing 2.5% emulsifier, and stir with a high-speed disperser at 4000 rpm 3min, make emulsion A. Add 5mL of 25% calcium chloride solution to 15mL of liquid paraffin containing 2.5% emulsifier, and stir with a high-speed disperser at 4000rpm for 3min to prepare emulsion B. Add emulsion B dropwise to emulsion A, stir magnetically for 30 minutes to complete the cross-linking reaction, separate the microspheres by suction filtration, and freeze-dry to obtain drug-loaded sodium alginate microsphere freeze-dried powder. The particle size of the drug-loaded sodium alginate microsphere is 1-20 μm, and the drug-loaded amount is about 25%.

[0029] Chitosan (0.02g) was dissolved in 1mL glacial acetic acid solution (0.1M), and under the condition of stirring in an ice-water bath, β-so...

specific Embodiment 2

[0030]Weigh 0.2 g of diclofenac sodium and dissolve it in 10 mg / mL poloxamer 407 solution, add 0.2 g of sodium alginate and stir for 1 hour until completely dissolved, then add 30 mL of liquid paraffin containing 2.5% emulsifier, and stir with a high-speed disperser at 4000 rpm 3min, make emulsion A. Add 5mL of 25% calcium chloride solution to 15mL of liquid paraffin containing 2.5% emulsifier, and stir with a high-speed disperser at 4000rpm for 3min to prepare emulsion B. Add emulsion B dropwise to emulsion A, stir magnetically for 30 minutes to complete the cross-linking reaction, separate the microspheres by suction filtration, and freeze-dry to obtain drug-loaded sodium alginate microsphere freeze-dried powder. The particle size of the drug-loaded sodium alginate microsphere is 1-20 μm, and the drug-loaded amount is about 25%.

[0031] Chitosan (0.02g) was dissolved in 1mL glacial acetic acid solution (0.1M), and under the condition of stirring in an ice-water bath, β-sod...

specific Embodiment 3

[0032] The temperature-sensitive in situ gel formulation composition for joint cavity injection obtained in Specific Example 1 of the present invention was subjected to an in vitro drug release test, and the results of its in vitro drug release curve are shown in the attached figure 2 shown.

[0033] Test method: Accurately measure 1mL of the composition obtained in Example 1, add it to a 10mL stoppered test tube, and place it in a water bath at 37±1°C for 1 hour. 37±1°C, shaking in a 100rpm shaker. Take out all the release medium at fixed sampling time points (0.25, 0.5, 1, 2, 4, 6, 8, 12, 24, 36, 48, 60, 72, 96, 120h), and add the same volume of fresh release medium . Filter through a 0.45 μm filter membrane, take the filtrate, measure the absorbance at a wavelength of 275 nm according to ultraviolet spectrophotometry, and calculate the cumulative drug release rate.

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Abstract

The invention relates to a temperature-sensitive in-situ gel preparation composition for intra-articular injection and a preparation method thereof, and belongs to the field of medicine preparations. The preparation method comprises the following steps: preparing diclofenac sodium-carrying sodium alginate microspheres by combining a microsphere technology with a temperature-sensitive gel technology, and then carrying the medicine-carrying microspheres in a chitosan / beta-sodium glycerophosphate temperature-sensitive in-situ gel system to obtain a diclofenac sodium in-situ gel preparation composition. The composition is in a liquid state at a room temperature, capable of being converted to a semi-solid gel at a body temperature and forming a medicine storeroom at a medication part after being partially injected to enter an articular cavity, and beneficial to slowly releasing the medicine, prolonging the time of staying at the injection part, of the medicine, and enhancing the efficacy. The composition disclosed by the invention can be used for treating arthritis diseases of rheumatism, rheumatoid arthritis, osteoarthritis, synovitis and the like, as well as applicable to both diclofenac sodium and other arthritis treatment medicines of non-steroidal anti-inflammatory medicines, steroid hormone medicines, biological preparations and the like.

Description

technical field [0001] The invention relates to a temperature-sensitive in-situ gel preparation composition for joint cavity injection and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] With my country's economic development and population aging, the incidence of joint inflammatory diseases such as rheumatism, rheumatoid arthritis and osteoarthritis is getting higher and higher, and it is showing a younger trend. Arthritis is a chronic disease, clinically manifested as joint redness, swelling, heat, pain, dysfunction and joint deformity, severe cases lead to joint disability, and further development of the disease will involve internal organs, affecting the quality of life of patients, giving patients physical, It takes a lot of psychological and financial burden. [0003] At present, the best treatment for arthritis is early diagnosis and intervention, but there is no cure for the irreversible joint damage...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/36A61K31/196A61P19/02A61P29/00
Inventor 吴正红秦晓雪祁小乐钦佳怡李文艳
Owner CHINA PHARM UNIV
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