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Composition with methylprednisolone palmitate as active component for treating local inflammation

A kind of technology of methylprednisolone and palmitate, applied in the field of medicine

Inactive Publication Date: 2009-04-22
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The derivatives of methylprednisolone are mainly its medicinal esters, and the derivatives of methylprednisolone in the prior art are mainly methylprednisolone acetate, methylprednisolone acetate, methylprednisolone sulfonate, methylprednisolone succinic acid Sodium, etc., there is no report that methylprednisolone is prepared into palmitate and used for injection to treat local inflammation

Method used

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  • Composition with methylprednisolone palmitate as active component for treating local inflammation
  • Composition with methylprednisolone palmitate as active component for treating local inflammation
  • Composition with methylprednisolone palmitate as active component for treating local inflammation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 (lyophilized emulsion)

[0040] Methylprednisolone palmitate 2.5g (Methylprednisolone is about 1.5g),

[0041] Soy Lecithin 10g

[0042] Anhydrous sodium bisulfite 0.01g

[0043] The remaining amount of water for injection to 100ml

[0044] Process:

[0045] 1) In the preparation equipment, dissolve 2.5 g of methylprednisolone palmitate in an appropriate amount of ethanol;

[0046] 2) Mix 10g of soybean lecithin for injection with an appropriate amount of water for injection, and add 0.01g of vitamin C

[0047] 3) Add the mixture obtained in 2) into the mixture obtained in 1) under the condition of stirring, after stirring at 20°C, pass through a homogenizer to homogenize the solution repeatedly to obtain a uniform solution, and prepare 100ml of liquid medicine , add 6g of glucose as a freeze-drying protective agent, pass through a 0.22μm microporous membrane to sterilize, and pack aseptically under 100 grades.

[0048] 4) remove moisture through free...

Embodiment 2

[0050] Embodiment 2 (lyophilized emulsion)

[0051] Methylprednisolone palmitate 1.7g (about 1g methylprednisolone)

[0052] Egg yolk lecithin 2g

[0053] Tea oil for injection 2g

[0054] Anhydrous sodium bisulfite 0.01g

[0055] Ethylparaben 0.01g

[0056] Glucose 5g

[0057] Water for injection to 100ml

[0058] craft

[0059] 1) In the preparation equipment, 1.7 g of methylprednisolone palmitate was dissolved in 2 g of tea oil for injection;

[0060] 2) Mix 2 g of egg yolk lecithin for injection with an appropriate amount of water for injection, and add 0.01 g of ethylparaben and 0.01 g of anhydrous sodium bisulfite.

[0061] 3) Add the mixture obtained in step 1) to the mixture obtained in step (2) under stirring conditions, stir and pass through a homogenizer at 40°C, homogenize the solution repeatedly to obtain a uniform solution, and adjust the pH to 6 with potassium acetate ~7, Add glucose as a freeze-drying protective agent to prepare 100ml of liquid medicine...

Embodiment 3

[0064] Embodiment 3 (lyophilized emulsion)

[0065] Methylprednisolone palmitate 4g (about 2.5g methylprednisolone)

[0066] Poloxamer 4g

[0067] Olive oil for injection 10g

[0068] Anhydrous sodium sulfite 0.1g, dibutyl hydroxytoluene 0.5g

[0069] Water for injection to 100ml

[0070] craft

[0071] 1) In the preparation equipment, 4 g of methylprednisolone palmitate is dissolved in 10 g of olive oil for injection;

[0072] 2) Mix 4 g of poloxamer with appropriate amount of water for injection, and add 0.1 g of anhydrous sodium sulfite and 0.5 g of dibutyl hydroxytoluene.

[0073] 3) Add the mixture obtained in step 1) to the mixture obtained in step (2) under stirring conditions, stir and pass through a homogenizer at 40°C, homogenize the solution repeatedly to obtain a uniform solution, add 8g of glucose as a freeze-drying protective agent , to prepare 100ml of liquid medicine, pass through a 0.22μm microporous membrane to sterilize, and pack aseptically under 100 ...

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Abstract

The invention relates to a drug composition for treating local inflammation, which uses methylprednisolone palmitate as an active composition. The drug composition consists of the methylprednisolone palmitate as the active composition and an inactive composition suitable for local injection, and is used for treating local inflammation of people or mammal through local injection.

Description

Technical field: [0001] The invention relates to the technical field of medicine, and relates to the application of methylprednisolone palmitate in the preparation of medicines for treating local inflammation Background technique: [0002] Rheumatoid arthritis (RA) and osteoarthritis (OA) are common chronic inflammatory joint diseases. At present, the drugs for treating such diseases are mainly steroids and non-steroids. Due to the definite curative effect of steroids, they are necessary for the treatment of severe patients, and their role is irreplaceable by non-steroids. At present, the dosage forms of steroid drugs on the market are mainly divided into two categories, one is solution type (including freeze-dried powder injection) injection, and the other is suspension injection. The former can be "intravenously injected", "intramuscularly injected" and "joint cavity injected", but the elimination speed is fast, and the effective concentration cannot be maintained in the ...

Claims

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Application Information

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IPC IPC(8): C07J5/00A61K31/57A61K9/107A61P29/00
Inventor 郝于田卢彦昌李静韩英陈松
Owner TIANJIN JINYAO GRP
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