Lornoxicam microsphere and preparation method thereof

A technology of lornoxicam and microspheres, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as toxic side effects, short half-life of drugs, and increased pain for patients , to achieve the effect of increasing drug concentration, reducing toxic and side effects, and strong and lasting effect

Inactive Publication Date: 2011-11-09
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] At present, common injections are mainly used for intra-articular injection in clinical practice. Conventional injections for intra-articular administration have the following problems: the half-life of the drug is short, long-term and frequent medication reduces patient compliance, and drug resistance is prone to occur; The rapid leakage of the drug causes systemic absorption, which has serious side effects and increases the pain of the patient

Method used

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  • Lornoxicam microsphere and preparation method thereof
  • Lornoxicam microsphere and preparation method thereof
  • Lornoxicam microsphere and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Embodiment 1: the preparation of lornoxicam microsphere

[0024] Dissolve 80mg of polylactic acid-glycolic acid copolymer in 2mL of dichloromethane to form an organic phase with a concentration of 40mg / mL; suspend 4mg of sustained-release drug in 0.4mL of distilled water to form an inner water phase, and then add the inner water phase dropwise to In the organic phase, shear at high speed for 1 min to obtain colostrum; then use a syringe to inject colostrum into 10 mL of the outer aqueous phase gelatin solution (concentration 40 g / L), shear at high speed for 2 min to obtain W / O / W double emulsion, and stir After 3 hours, the dichloromethane was completely volatilized; centrifuged, discarded the upper liquid, washed 3 to 5 times with distilled water to obtain microspheres, and dried in vacuum for 72 hours to obtain dry powder of lornoxicam microspheres. Wherein, the high-speed shearing speed is 12000r / min.

Embodiment 2

[0025] Embodiment 2: the preparation of lornoxicam microsphere

[0026] Dissolve 80mg of polylactic acid-glycolic acid copolymer in 2mL of dichloromethane to form an organic phase with a concentration of 40mg / mL; suspend 4mg of sustained-release drug in 0.4mL of distilled water to form an inner water phase, and then add the inner water phase dropwise to In the organic phase, shear at high speed for 1 min to obtain colostrum; then use a syringe to inject colostrum into 10 mL of the external aqueous phase polyvinyl alcohol solution (concentration 40 g / L), and shear at high speed for 2 min to obtain W / O / W double emulsion. Stir for 4 hours to completely volatilize the dichloromethane; centrifuge, discard the upper liquid, wash with distilled water for 3 to 5 times to obtain microspheres, and vacuum dry for 90 hours to obtain dry powder of lornoxicam microspheres. Wherein, the high-speed shearing speed is 16000r / min.

Embodiment 3

[0027] Embodiment 3: the preparation of lornoxicam microsphere

[0028] Dissolve 20 mg of polylactic acid-glycolic acid copolymer in 2 mL of dichloromethane to form an organic phase with a concentration of 10 mg / mL; suspend 2 mg of sustained-release drug in 0.4 mL of distilled water to form an inner water phase, and then add the inner water phase dropwise to In the organic phase, high-speed shearing is performed for 5 seconds to obtain colostrum; then the colostrum is injected into 20 mL of gelatin solution (concentration: 20 g / L) with a syringe, and high-speed shearing is performed for 1 min to obtain W / O / W double emulsion, which is then stirred for 2 hours. Completely volatilize the dichloromethane; centrifuge, discard the upper liquid, wash with distilled water for 3 to 5 times to obtain microspheres, and vacuum dry for 48 hours to obtain dry powder of lornoxicam microspheres. Wherein, the high-speed shearing speed is 8000r / min.

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Abstract

The invention discloses Lornoxicam microspheres, in which polylactic acid-glycolic acid copolymer is used as a carrier and Lornoxicam as a sustained-released medicament; the average diameter of the microspheres is 1-15mum, the span thereof is 1-2, and Lornoxicam accounts to 1-15 percent of the whole microsphere mass. The preparation method of the Lornoxicam microspheres is that: polylactic acid-glycolic acid copolymer is dissolved in dichloromethane to form an organic phase; the sustained-released medicament is mixed and suspended in distilled water to form an internal aqueous phase, and thenthe internal aqueous phase is added into the organic phase in a dropwise way, thus a primary emulsion is obtained. Next, the primary emulsion is injected by an injector into an external aqueous phase, and a W / O / W multiple emulsion is obtained, and then stirred to fully evaporate dichloromethane, the multiple emulsion is centrifugated to remove the supernatant liquid, cleaned by distilled water; and then the microspheres are obtained, and the microspheres are dried in vacuum, thus the dried powder of Lornoxicam microsphere is obtained. The microspheres enhances the curative effect of the medicament, reduces the toxicity and side effects, and avoids the shortcomings of long term administration, which has quite good effect on the treatment of arthritis.

Description

technical field [0001] The invention relates to a lornoxicam microsphere and a preparation method thereof. Background technique [0002] Osteoarthritis (OA), also known as osteoarthritis and degenerative osteoarthritis, is the most common disease in arthritis. Changes in joint function. OA is a chronic, degenerative joint disease that occurs mostly after middle age. It has a high incidence rate in middle-aged and elderly people. The joint pain and dysfunction it causes seriously affect the quality of life of patients. With the increase of the world's aging population, the incidence of OA is also increasing year by year. [0003] Lornoxicam is a new member of the Oxicam family, and its action sites include the central nervous system and peripheral pain areas, and it works through multiple mechanisms: ① In the periphery, it inhibits the activity of cyclooxygenase (COX) Synthesis of prostaglandins in the inflammatory area, thereby reducing the concentration of pain mediators...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/542A61K47/34A61K9/14A61P19/02
Inventor 黄桂华石洋毕秀丽张娜窦明金席延卫
Owner SHANDONG UNIV
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