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Flurbiprofen axetil emulsion for injection and preparation method thereof

A technology for flurbiprofen axetil and injection is applied in the field of flurbiprofen axetil injection emulsion and its preparation, which can solve problems such as unfavorable drug efficacy, influence on drug targeting effect, etc., so as to improve drug encapsulation efficiency and improve Emulsifying effect, milk uniform effect

Active Publication Date: 2019-01-18
WUHAN DOCAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the key index that affects the correlation between in vivo and in vitro of flurbiprofen axetil injection emulsion—drug entrapment rate is ignored, which will affect the targeting effect of the drug entering the body, which is not conducive to the exertion of drug efficacy

Method used

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  • Flurbiprofen axetil emulsion for injection and preparation method thereof
  • Flurbiprofen axetil emulsion for injection and preparation method thereof
  • Flurbiprofen axetil emulsion for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] The present embodiment provides a kind of flurbiprofen axetil injection emulsion, and its prescription is as follows:

[0067]

[0068]

[0069] The preparation method is as follows:

[0070] (1) Stir and mix the prescribed amount of flurbiprofen axetil, refined soybean oil, egg yolk lecithin, and dioleoylphosphatidylserine at 60° C. for 30 minutes under nitrogen-filled conditions to obtain a uniform oil phase (122.1 g) for later use;

[0071] (2) Stir and mix the glycerin and water for injection in the prescribed amount, and heat to 60°C for later use;

[0072] (3) Under the protection of nitrogen, 48.8g of the oil phase of step (1) was sheared and mixed with the water phase of step (2) at 4000rpm for 10min to obtain crude milk A; crude milk A was sheared with 36.6g of the oil phase of step (1) at 6000rpm again Cut and mix for 10 minutes to obtain crude milk B; shear and mix crude milk B with 36.6 g of the oil phase of step (1) at 8000 rpm for 20 minutes again t...

Embodiment 2

[0076] The present embodiment provides a kind of flurbiprofen axetil injection emulsion, and its prescription is as follows:

[0077]

[0078] The preparation method is as follows:

[0079] (1) Stir and mix the prescribed amount of flurbiprofen axetil, olive oil, soybean lecithin, and dipalmitoylphosphatidic acid at 65° C. for 20 minutes under nitrogen-filled conditions to obtain a uniform oil phase (156 g) for subsequent use;

[0080] (2) Stir and mix the sucrose and water for injection of the prescribed amount evenly, and heat to 65°C for later use;

[0081] (3) Under the protection of nitrogen, 78g of the oil phase of step (1) was sheared and mixed with the water phase of step (2) at 5000rpm for 15min to obtain crude milk A; crude milk A was again sheared and mixed with 39g of the oil phase of step (1) at 7000rpm 15min to obtain crude milk B; crude milk B was sheared and mixed with 39g of the oil phase of step (1) at 9000rpm for 30min again to obtain colostrum;

[0082...

Embodiment 3

[0085] The present embodiment provides a kind of flurbiprofen axetil injection emulsion, and its prescription is as follows:

[0086]

[0087] The preparation method is as follows:

[0088] (1) Stir and mix the prescribed amount of flurbiprofen axetil, medium-chain triglycerides, refined soybean oil, macrogol stearate, and sphingomyelin at 70°C for 15 minutes under nitrogen filling to obtain a uniform Oil phase (125.8g) is standby;

[0089] (2) Stir and mix the prescribed amount of mannitol and water for injection evenly, and heat to 70°C for later use;

[0090] (3) Under the protection of nitrogen, 75.5g of the oil phase of step (1) was sheared and mixed with the water phase of step (2) at 6000rpm for 20min to obtain crude milk A; crude milk A was sheared again with 25g of the oil phase of step (1) at 8000rpm Mix for 20 minutes to obtain crude milk B; shear and mix crude milk B with 25 g of the oil phase of step (1) at 10000 rpm for 30 minutes again to obtain colostrum; ...

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Abstract

The invention provides a flurbiprofen axetil emulsion for injection and a preparation method thereof. The preparation method comprises the following steps: under the protection of nitrogen, the oil phase is added into the aqueous phase step by step and shearing and mixing for many times to obtain colostrum; 40-60wt% of total oil phase is added into that water phase, shear and mixing are carried out for 10-30min to obtain crude emulsion A, wherein the crude emulsion A is obtained by adding 40-60 wt% of total oil phase into the water phase and mixing for 10-30min; 20-30wt% of total oil phase isadded into that crude emulsion A, and the crude emulsion B is obtained by shear and mixing for 10-30min; Shearing and mixing the crude emulsion B and the remaining oil phase for 10 to 30 minutes; Theoil phase includes flurbiprofen esters, oil phase solvents, emulsifiers and stabilizers, and the aqueous phase includes water for injection and / or osmotic pressure regulators. Under the precondition of the presence of the stabilizer in the oil phase, the invention adopts the oil phase step-by-step and multiple emulsification technology, which can effectively improve the emulsification effect, makethe particle size of the obtained emulsion more uniform, the encapsulation efficiency of the drug higher, and the targeting of the drug to the wound tissue better.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a flurbiprofen axetil injection emulsion and a preparation method thereof. Background technique [0002] Flurbiprofen axetil is a prodrug of flurbiprofen, used for postoperative and cancer analgesia. Flurbiprofen axetil injection emulsion is a new type of targeted analgesic with fat emulsion (or called lipid microspheres) as the carrier. Released from the milk granules, it is rapidly hydrolyzed by carboxyl esterase to produce flurbiprofen, and flurbiprofen inhibits cyclooxygenase in the process of arachidonic acid metabolism and inhibits the synthesis of prostaglandins to exert analgesic effect . This drug-loaded emulsion has stronger drug efficacy, faster onset and longer duration, and is less likely to cause adverse reactions such as gastric mucosal damage. It has been widely used in clinical practice. [0003] The preparation process of flurbiprofen axetil injecti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/24A61K31/222A61P29/00
CPCA61K9/0019A61K9/107A61K31/222A61K47/24A61P29/00A61K9/1075A61K31/192A61K47/10A61K47/26
Inventor 黄岭张晓花宋金春尹磊
Owner WUHAN DOCAN PHARMA
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