Etomidate fat emulsion concentrated solution, preparation method and application thereof

A technology of etomidate and fat emulsion, applied in the directions of emulsion delivery, oil/fat/wax inactive ingredients, pharmaceutical formulations, etc., can solve the problems of oil-water stratification, inability to perform clarity detection, complex preparation process, etc.

Inactive Publication Date: 2015-06-17
天津迈迪瑞康生物医药科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Etomidate fat emulsion is the same as common fat emulsion preparations, and there are the deficiencies of poor stability and complicated preparation process: those skilled in the art understand that fat emulsion preparations such as etomidate fat emulsions appear as opaque milky white liquids in appearance , can not be tested for clarity; oil-water stratification, coagulation, flocculation and other phenomena are prone to occur during product storage; the preparation process involves colostrum preparation, high-pressure homogenization, and the process is unstable, and the temperature, emulsification time and production equipment all affect product quality. impact, resulting in uneven milk grains; and, existing fat emulsions require specialized equipment to be sterilized under high pressure

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  • Etomidate fat emulsion concentrated solution, preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0150] Embodiment 1: the preparation of etomidate fat emulsion concentrate sample 1

[0151] Its composition is as follows:

[0152] Etomidate 2.5g

[0153] Medium-chain fatty acid glycerides (Capmul MCM, Abitec) 25g

[0154] 30g soybean oil

[0155] 1,2-propanediol 9 grams

[0156] Soy Lecithin (Epikuron 170, Degussa) 10g

[0157] Polyglyceryl Oleate 3 g

[0158] Tween 80 9 grams

[0159] Polyethylene glycol lauryl hydroxystearate (Solutol HS 15, BASF) 11 g

[0160] Sodium Oleate 0.2g

[0161] Vitamin E 0.3g

[0162] The preparation method of this etomidate fat emulsion concentrate is as follows:

[0163] 1) At 20°C, add the above-mentioned weight of soybean lecithin and polyglycerol oleate into medium-chain fatty acid glycerides and soybean oil, and stir at 20,000 rpm until a transparent and clear solution is formed;

[0164] 2) Add the above-mentioned weight of 1,2-propanediol and etomidate to the product of step 1) at 20°C, and keep stirring at 200rpm until...

Embodiment 2

[0167] Embodiment 2: the preparation of etomidate fat emulsion concentrate sample 2

[0168] Its composition is as follows:

[0169] Etomidate 1.5g

[0170] Medium chain fatty acid triglycerides (Crodamol, GTCC) 70g

[0171] 1,2-Propanediol 8g

[0172] Soy Lecithin (Epikuron 170, Degussa) 7.5g

[0173] Polyglyceryl Oleate 1 g

[0174] Tocopheryl Polyethylene Glycol Succinate 4g

[0175] Tween 80 3.7g

[0176] Polyethylene glycol lauryl hydroxystearate (Solutol HS 15, BASF) 4 g

[0177] Vitamin E 0.3 grams

[0178] The preparation method of this etomidate fat emulsion concentrate is as follows:

[0179] 1) At 45°C, add the above-mentioned weight of soybean lecithin and polyglycerol oleate to medium-chain fatty acid triglycerides, and stir at 2000 rpm until a transparent and clear solution is formed;

[0180] 2) Add the above-mentioned weight of 1,2-propanediol and etomidate to the product of step 1) at 35°C, and keep stirring at 1000rpm until the whole system is ...

Embodiment 3

[0183] Embodiment 3: the preparation of etomidate fat emulsion concentrate sample 3

[0184] Its composition is as follows:

[0185] Etomidate 2g

[0186] Caprylic Capric Glycerides (Miglyol 812, SASOL) 65g

[0187] 1,2-Propanediol 12g

[0188] Soy Lecithin (Epikuron 170, Degussa) 12g

[0189] Tween 80 3 grams

[0190] Polyethylene glycol lauryl hydroxystearate (Solutol HS 15, BASF) 5.5 g

[0191] Sodium Oleate 0.3g

[0192] Vitamin A 0.2g

[0193] The preparation method of this etomidate fat emulsion concentrate is as follows:

[0194] 1) At 30°C, add the above-mentioned weight of soybean lecithin to caprylic capric glyceride, and stir at 10,000 rpm until a transparent and clear solution is formed;

[0195] 2) Add the above-mentioned weight of 1,2-propanediol and etomidate to the product of step 1) at 45°C, and continue stirring at 1000 rpm until the whole system is transparent;

[0196] 3) Add the above-mentioned weight of Tween 80, polyethylene glycol lauryl hy...

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Abstract

An etomidate fat emulsion concentrated solution, a preparation method and an application thereof belong to the field of pharmacology and pharmaceutics. According to the invention, the defect that a traditional fat emulsion preparation technology is complex and stability is poor is overcome. The preparation technology provided by the invention is simple; the general physical stirring process is only needed; and no homogenization technology is required. A product prepared in the invention can be sterilized through a 0.22-micron microfiltration membrane; in clinical use, the product can be spontaneously emulsified after diluted by the use of an aqueous solution such as normal saline or a glucose solution, etc. and slightly oscillated; and under optimized conditions, average particle size is about 0.2 micron, and injection fat emulsion characteristics are fully embodied. The product has good fluidity, will not be retained on the wall, is single-phase, transparent and clear in appearance, can undergo clarification detection, will not cause preparation stratification after multigelation and is used in clinical uses such as induction of general anesthesia, short-time operative anesthesia and the like.

Description

technical field [0001] The invention belongs to the field of pharmacy and pharmacy, and relates to etomidate fat emulsion concentrate, its preparation method and application. Background technique [0002] Etomidate is a general hypnotic intravenous anesthetic known to have no cardiovascular effects. Etomidate has poor solubility under physiological conditions (pKa 4.2). In order to increase its solubility, two pharmaceutical preparations currently used in clinical practice are respectively dissolving etomidate in 35% propylene glycol to make 0.2% etomidate injection liquid; and etomidate fat emulsion prepared with fat emulsion as carrier. Studies by Doenicke A and others have shown that compared with etomidate injection, etomidate fat emulsion can greatly reduce the free hemoglobin concentration in patients (Doenicke A, Roizen MF, Hoernecke R, et al. (1997) British Journal of Anaesthesia . 79(3): 386-388), thereby reducing side effects such as injection pain and vascular d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/4174A61K47/34A61K47/44A61K47/24A61K47/22A61K47/10A61P23/00A61K47/14
Inventor 杨杰其他发明人请求不公开姓名
Owner 天津迈迪瑞康生物医药科技有限公司
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