Ibuprofen fat emulsion injection and preparation method thereof

A technology for injection and fat emulsion, which is applied in the fields of emulsion delivery, oil/fat/wax non-active ingredients, pharmaceutical formulations, etc. It can solve the problems of less adverse reactions, large irritation, poor stability, etc., and achieve convenient clinical medication, The effect of avoiding cross-contamination

Inactive Publication Date: 2014-03-12
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] The present invention aims at the inherent characteristics of ibuprofen. On the one hand, the advantages of strong antipyretic and analgesic effects and less adverse reactions of ibupr

Method used

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  • Ibuprofen fat emulsion injection and preparation method thereof
  • Ibuprofen fat emulsion injection and preparation method thereof
  • Ibuprofen fat emulsion injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: the selection of oil type and consumption for injection

[0036] To prepare drug-loaded fat emulsion, the prerequisite is that the main drug should have a certain amount of solubility in oil for injection. Otherwise, a stable drug-loaded fat emulsion cannot be prepared. The ibuprofen fat emulsion injection of the present invention is intended to be a drug-loaded fat emulsion for long-term storage, and should be stable within 2 years at least. Therefore, it is necessary to ensure that the selected oil for injection has sufficient solubility for ibuprofen.

[0037] Weigh an appropriate amount of ibuprofen respectively, and place it in caprylic triglyceride for injection, soybean oil for injection and a mixture of the two at 70° C. to make 5 mg / g, 10 mg / g, 20 mg / g, 30mg / g, 40mg / g, 50mg / g concentration, heat and stir, observe the dissolved state. Store the dissolved drug solution under refrigeration at 4-6°C for 72 hours, conduct a low-temperature challenge...

Embodiment 2

[0057] Embodiment 2: Determination of drug loading

[0058] Due to the characteristics of ibuprofen itself, we chose caprylic capric triglyceride for injection or combined with soybean oil for injection as the oil for injection, and the dosage is 10-20% (g / ml). In the selected oil for injection, the solubility of ibuprofen is 20mg / ml-40mg / ml. According to the solubility and clinical dosage, for the convenience of clinical medication, we propose that the drug loading of ibuprofen is 0.1%-40mg / ml. 0.8% g / ml.

Embodiment 3

[0059] Embodiment 3: the selection of refined lecithin

[0060]Most of the fat emulsions currently used clinically and reported in research use refined lecithin as the emulsifier, and the type and specification of lecithin are not clearly defined. Through experiments, we found that not all refined lecithins are suitable for the preparation of ibuprofen fat emulsion injection, and some refined lecithins cannot prepare stable ibuprofen fat emulsion injection at all, which may be related to the ibuprofen itself. related to physical and chemical properties. Therefore, we separately tested soybean lecithin S80 (purchased from Shanghai Taiwei Pharmaceutical Co., Ltd.), egg yolk lecithin PL-100M (purchased from Shanghai Aiweite Pharmaceutical Technology Co., Ltd.), egg yolk lecithin E80 (purchased from Shanghai Dongshang Industrial Co., Ltd.) Co., Ltd.), egg yolk lecithin DS-PL95E (purchased from South Korea Doosan Company), egg yolk lecithin PC-98T (purchased from Shanghai Aiweite ...

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Abstract

The invention relates to the technology of pharmaceutical preparation. The invention provides an ibuprofen fat emulsion injection which comprises ibuprofen, injection oil, refined lecithin, glycerol, a stabilizing agent, a pH regulator and injection water. Through animal experiments, the pain easing effect of the ibuprofen fat emulsion injection is 1.59-4.31 times that of the commercially available ibuprofen injection, the antipyretic and anti-inflammatory effects can also be obviously improved, and the ibuprofen fat emulsion injection has certain long-acting effect. Proved by long-time stability experiments, the quality of the ibuprofen fat emulsion injection at normal temperature has no obvious change within two years. The invention provides the ibuprofen fat emulsion injection which can be intravenous, stable, safe, and high-efficiency.

Description

technical field [0001] The invention relates to pharmaceutical preparation technology, in particular to an ibuprofen fat emulsion injection and a preparation method thereof. Background technique [0002] Ibuprofen (IBUPROFEN, chemical name: 2-methyl-4-(2-methylpropyl) phenylacetic acid) is one of the most commonly used non-steroidal antipyretic analgesics. This product is soluble in ethanol, acetone, chloroform or ether, almost insoluble in water. Ibuprofen was first listed in the UK in 1968. It has significant curative effect in antipyretic and analgesic, and has low toxicity, so the market expands rapidly. Due to the better curative effect and less adverse reactions of ibuprofen, the U.S. and the U.K. successively approved the transfer of ibuprofen from prescription drugs to over-the-counter drugs. [0003] At present, the existing clinical ibuprofen preparations are tablets, capsules, dry suspensions, granules, drops, etc., but they are all oral preparations, which cann...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/192A61K47/44A61K47/24A61P29/00
Inventor 陈建明高保安张广军刘文丽邓莉陈丽娜张元声周琴琴严博吴婵余侬
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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