Flurbiprofen axetil medium-chain and long-chain fat emulsion and preparation method thereof

A flurbiprofen axetil, medium and long chain technology, which is applied in the field of flurbiprofen axetil medium and long chain fat emulsion and preparation, and can solve the problems of inability to administer intravenously, difficult flurbiprofen, strong pain and the like

Inactive Publication Date: 2011-01-12
北京中海康医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, flurbiprofen is insoluble in water, and its sodium salt has strong pain when injected, so it cannot be given intravenously.

Method used

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  • Flurbiprofen axetil medium-chain and long-chain fat emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] prescription

[0032] Flurbiprofen axetil 10g

[0033] Refined soybean oil 100g

[0034] Egg yolk lecithin 12g

[0035] Glycerin 22.5g

[0036] Disodium hydrogen phosphate appropriate amount

[0037]

[0038] Add water for injection to 1000ml

[0039] Process:

[0040] (1) Preparation of water phase: add glycerin to water to dissolve, heat to 75°C, and set aside;

[0041] (2) Preparation of the oil phase: heat the refined soybean oil to 75°C, add egg yolk lecithin (with a phosphatidylcholine content of more than 80%) to dissolve, add flurbiprofen axetil, and stir to dissolve;

[0042] (3) Preparation of colostrum: Add the oil phase of step (2) into the water phase of step (1), at a temperature of 75° C., high-speed shear dispersion, shear speed of 8000 rpm, and time of 15 minutes to form colostrum;

[0043] (4) pH value adjustment: quickly cool down the colostrum in step (3) to below 30°C, and adjust the pH value to 4.5-6.5 wi...

Embodiment 2

[0048] prescription:

[0049] Flurbiprofen axetil 10g

[0050] Refined soybean oil 50g

[0051] Medium Chain Triglycerides 50g

[0052] Egg yolk lecithin 12g

[0053] Glycerin 22.5g

[0054] Disodium hydrogen phosphate appropriate amount

[0055]

[0056] Add water for injection to 1000ml

[0057] Process:

[0058] (1) Preparation of water phase: add glycerin to water to dissolve, heat to 75°C, and set aside;

[0059] (2) Preparation of the oil phase: heat refined soybean oil and medium-chain triglycerides to 75°C, add egg yolk lecithin (with a phosphatidylcholine content of more than 80%) to dissolve, add flurbiprofen axetil, and stir to make it dissolve;

[0060] (3) Preparation of colostrum: Add the oil phase of step (2) into the water phase of step (1), at a temperature of 75° C., high-speed shear dispersion, shear speed of 8000 rpm, and time of 15 minutes to form colostrum;

[0061] (4) pH value adjustment: quickly cool down the...

Embodiment 3

[0065] The influence of embodiment 3 on rabbit blood lipid

[0066] Take 12 healthy male Japanese long-eared rabbits, weighing 2.0-2.5Kg, and divide them into two groups at random, 6 in each group. The first group is given the fat emulsion of Example 1, and the second group is given the fat emulsion of Example 2. The administration dose is 50mg / kg, and the administration speed is 0.5mg / s.

[0067] The administration method was puncture and catheterization through the ear vein of rabbits. If there was blood back in the indwelling needle and a small amount of normal saline was injected without resistance, it indicated that the catheterization was successful. After the catheterization was successful, the puncture needle was fixed with a suture needle, and intravenous injection was performed at a constant speed. and pre-infusion (T 0 ), 1 hour after infusion (T 1 ), 3 hours (T 2 ), 6 hours (T 3 2ml of venous blood was drawn at each time point for blood lipid detection. Trigly...

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PUM

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Abstract

The invention relates to a flurbiprofen axetil medium-chain and long-chain fat emulsion and a preparation method thereof. The fat emulsion comprises flurbiprofen axetil, long-chain oil for injection, medium-chain oil for injection, emulsifier, isotonic agent, pH regulator and water for injection, wherein the weight-volume percentage of the flurbiprofen axetil is 0.5-5%(w / v), the weight-volume percentage of the long-chain oil for injection is 5-10%(w / v), the weight-volume percentage of the medium-chain oil for injection is 5-10%(w / v), and the weight-volume percentage of the isotonic agent is 1-5%(w / v).

Description

technical field [0001] The invention relates to a medium-long-chain fat emulsion of flurbiprofen axetil and a preparation method thereof. Background technique [0002] Flurbiprofen axetil, its chemical name is: (±) 2-(2-fluoro-4-biphenyl)propanoic acid-1-acetoxyethyl ester [0003] Its structural formula is: [0004] [0005] Molecular formula: C 19 h 19 FO 4 [0006] Molecular weight: 330.36 [0007] Flurbiprofen belongs to non-steroidal anti-inflammatory drugs, the mechanism of action is mainly to inhibit the activity of cyclooxygenase in the arachidonic acid cascade cascade, thereby inhibiting the synthesis of prostaglandins that cause pain and inflammatory reactions, and play an analgesic role . Its analgesic effect is stronger than that of aspirin, and even surpasses the new analgesic. However, flurbiprofen is insoluble in water, and its sodium salt has severe pain when injected, so it cannot be administered intravenously. Flurbiprofen axetil is a prodrug pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/222A61P29/00
Inventor 黄海宋华先马红萍张占军孙欣程宇刘启悦
Owner 北京中海康医药科技发展有限公司
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