Sevoflurane venous microemulsion and preparation method thereof

A technology of intravenous microemulsion and sevoflurane, applied in the field of medicine, can solve problems such as low cost, and achieve the effects of easy acceptance, improved treatment effect, and simple and easy preparation method

Inactive Publication Date: 2010-08-04
XUZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As far as we know, there has not been found a low-cost, rapid general anesthesia, strong controllability, no toxic and side effects, safe and effective intravenous injection of volatile sevoflurane microemulsion and its preparation method

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Take 0.55 g of sevoflurane, add 4.4 g of medium-chain triglycerides for injection, and stir rapidly; mix 16.3 g of emulsifier polyoxyethylene castor oil (Cremophor ELP) and co-emulsifier polyethylene glycol-400 (PEG- 400) 5.0g was heated, stirred and mixed, then cooled to 25°C, and sevoflurane and medium-chain triglycerides were added to the emulsifier to obtain an oil phase; 84ml of water for injection was measured, and 2.0g of glycerin and 0.005g of tocopherol were added , stirred to dissolve, and heated to 25°C to obtain an aqueous phase. Stir and mix the oil phase and the water phase in a closed container at 25°C to obtain a microemulsion, adjust its pH to 7.5 with sodium hydroxide solution or hydrochloric acid solution, subpackage, fill with nitrogen, and sterilize at 121°C for 15 minutes to obtain seven Fluoride intravenous microemulsion. The average particle diameter of the microemulsion is (45.8±1.2) nm, the pH is 7.51, the content of sevoflurane is 0.50%, and ...

Embodiment 2

[0036] Get 0.65g of sevoflurane, add 5.2g of medium-chain triglyceride for injection, and stir quickly; mix 20.6g of emulsifier polyoxyethylene castor oil (Cremophor ELP) and co-emulsifier polyethylene glycol-400 (PEG 400 ) 5.0g, heated, stirred and mixed evenly, then cooled to 35°C, added sevoflurane and medium-chain triglycerides to the emulsifier to obtain an oil phase; measured 81ml of water for injection, added 2.0g of glycerin, 0.005g of tocopherol, Stir to dissolve and heat to 35°C to obtain an aqueous phase. Stir and mix the oil phase and the water phase in a closed container at 35°C to obtain a microemulsion, adjust its pH to 7.5 with sodium hydroxide solution or hydrochloric acid solution, subpackage, fill with nitrogen, and sterilize at 121°C for 15 minutes to obtain seven Fluoride intravenous microemulsion. The average particle diameter of the microemulsion is (42.7±0.5) nm, the pH is 7.52, the content of sevoflurane is 0.61%, and other indexes meet the requiremen...

Embodiment 3

[0038] Take 0.81 g of sevoflurane, add 7.2 g of ethyl oleate for injection, and stir rapidly; 30.5 g of the emulsifier polyoxyethylene castor oil (Cremophor ELP) and 8.5 g of the co-emulsifier 1,2-propylene glycol are heated, stirred and mixed After cooling down to 25°C, add sevoflurane and medium-chain triglycerides to the emulsifier to obtain an oil phase; measure 65ml of water for injection, add 2.0g of glycerin and 0.005g of tocopherol, stir to dissolve, and heat to 25 °C to obtain the aqueous phase. Stir and mix the oil phase and the water phase in a closed container at 25°C to obtain a microemulsion, adjust its pH to 7.0 with sodium hydroxide solution or hydrochloric acid solution, subpackage, fill with nitrogen, and sterilize at 121°C for 15 minutes to obtain seven Fluoride intravenous microemulsion. The average particle diameter of the microemulsion is (29.0±1.8) nm, the pH is 7.03, the content of sevoflurane is 0.71%, and other indexes meet the requirements of the in...

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Abstract

The invention relates to a medicinal preparation and a preparation method thereof, in particular to a sevoflurane venous microemulsion and a preparation method thereof, and belongs to the technical field of medicaments. The sevoflurane venous microemulsion is prepared from sevoflurane, oil for injection and auxiliary materials such as emulsifying agent and the like by using the microemulsion preparation technology. The sevoflurane venous microemulsion is clear and transparent liquid, has light blue opalescence, and has Tyndall phenomenon; and the medicament-loading rate is 0.01 to 2.00 percent, the average grain diameter is 10 to 100 nanometers, and the pH is 4.5 to 9.5. On the one hand, the sevoflurane venous microemulsion improves the bioavailability and treatment effect of the sevoflurane by changing an administration route, and on the other hand, the venous microemulsion has targeting and can reduce the toxic or side effect of the medicament; and meanwhile, the volatility of the sevoflurane is reduced to be minimum due to the package of the microemulsion so as to reduce the acrimony of the sevoflurane, alleviate the pain of a patient during injection, make the patient accept easily and improve the administration compliance of the patient.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a sevoflurane intravenous microemulsion and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] The chemical name of sevoflurane is fluoromethyl-isopropyl ether. It is a colorless, transparent, fragrant and non-irritating volatile liquid with a molecular weight of 200.05 and a boiling point of 58.6°C. Sevoflurane is a relatively new inhalational anesthetic, synthesized by Regan in 1968, first reported by Willin et al. in 1971, and evaluated its physical and chemical properties, pharmacological effects and toxicology in 1975. It was first used in Japan in 1992. In 1995, it was approved by the US FDA to go on the market in the United States. Because sevoflurane is not highly water-soluble and fat-soluble, it is now clinically used as an inhalational anesthetic, but it needs to be used through a sp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/08A61P23/00
Inventor 刘毅印晓星庄雪梅刘莉陈效毅张玲刘玲尹翠
Owner XUZHOU MEDICAL COLLEGE
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