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Mefloquine fat emulsion composition and method for preparing the same

A technology for mefloquine fat and composition, applied in the field of fat emulsion composition, can solve the problems of toxic and side effects, complex preparation process, low bioavailability and the like, and achieve the effects of reducing toxic and side effects, reducing adverse reactions and increasing stability

Inactive Publication Date: 2009-07-08
NORTHWESTERN POLYTECHNICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to overcome the deficiencies of low bioavailability, toxic and side effects, and complicated preparation process in the prior art, the present invention provides a mefloquine fat emulsion composition, which can enhance the anti-inflammatory effect of mefloquine by utilizing the property of fat emulsion to inhibit the growth of Plasmodium. Malaria effect, improve its bioavailability, and reduce its toxic side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: 20mg mefloquine is put into 0.5mL dehydrated alcohol and fully dissolved into a solution, this solution is mixed with 20g soybean oil for injection, and 2.5g egg yolk lecithin for injection, 0.02g anti- Oxidant Vitamin E, mixed at 60°C to form an oil phase mixture. Mix 170mL of water for injection and 2.5g of glycerol at 70°C to form an aqueous phase mixture. Under the protection of nitrogen, mix the water phase mixture and the oil phase mixture, at 80°C, disperse at a high speed of 3000r / min, and then mechanically stir for 60 minutes to make colostrum. After adjusting the pH to 7.0, homogenize 7 times under the condition of 105MPa. , to obtain a uniform milky solution; the above-mentioned milky solution is filtered, sealed with nitrogen gas, sterilized at 115°C for 40min, and stored below 25°C.

[0020] After testing, the bioavailability of mefloquine in the mefloquine fat emulsion composition prepared in this example is 80%.

Embodiment 2

[0021] Embodiment 2: 50mg mefloquine is put into 0.6mL isopropanol and fully dissolved into a solution, this solution is mixed with 20g camellia oil for injection, and 2.5g soybean lecithin for injection, 0.02g antibacterial Oxidant vitamin E, mixed at 65°C to form an oil phase mixture. Mix 170mL of water for injection and 2.5g of xylitol at 70°C to form an aqueous phase mixture. Mix the water phase mixture and the oil phase mixture under the protection of nitrogen. At 75°C, disperse at a high speed of 2800r / min and then mechanically stir for 70 minutes to make colostrum. After adjusting the pH to 7.5, homogenize 9 times under the condition of 90MPa. , to obtain a uniform milky solution; the above-mentioned milky solution is filtered, sealed with nitrogen gas, sterilized at 120°C for 35min, and stored below 25°C.

[0022] After testing, the bioavailability of mefloquine in the mefloquine fat emulsion composition prepared in this example is 81.5%.

Embodiment 3

[0023] Embodiment 3: Put 100mg mefloquine into 1mL dehydrated alcohol and fully dissolve into a solution, mix this solution with 20g sesame oil for injection, add 2.5g egg yolk lecithin for injection, 0.02g antioxidant vitamin E, Mix at 70°C to form an oil phase mixture. Mix 170mL of water for injection and 2.5g of glucose at 75°C to form an aqueous phase mixture. Under the protection of nitrogen, mix the water phase mixture and the oil phase mixture, at 75°C, 3200r / min high-speed dispersion, then mechanically stir for 75min to make colostrum, adjust the pH to 8.0, and homogenize 6 times under the condition of 95MPa , to obtain a uniform milky solution; the above-mentioned milky solution is filtered, sealed with nitrogen gas, sterilized at 125°C for 30 minutes, and stored below 25°C.

[0024] After testing, the bioavailability of mefloquine in the mefloquine fat emulsion composition prepared in this example is 82%.

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PUM

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Abstract

The invention discloses a mefloquine fat emulsion composition which is characterized by containing 0.1-0.5wt% of mefloquine, 10.0-30.0wt% of oil for injection, 0.01-0.35wt% of emulsifier, 0.01-0.4wt% of solubilizer, 0.01-0.25wt% of isotonic agent, 0.007-0.02wt% of vitamin E and the rest of water for injection. The invention also discloses a method for preparing the composition, which comprises the following steps: the mefloquine is put into the solubilizer to be fully dissolved and mixed with the oil for injection, and then the mixed liquor is added with the emulsifier and antioxidant under the condition of nitrogen protection to form oil phase mixture; the water for injection and the isotonic agent are mixed together to form water phase mixture; then under the condition of nitrogen protection, the water phase mixture is mixed with the oil phase mixture, and then is dispersed at high speed and stirred mechanically to be made into lacteous solution; the obtained product is stored after germicidal treatment. As the mefloquine fat emulsion composition has the characteristic of utilizing fat emulsion to inhibit the growth of plasmodium, thus enhancing the antimalarial effect of the mefloquine, increasing the bioavailability of the mefloquine to 80-88% from 30-50% in the prior art, and reducing the toxic side effect.

Description

technical field [0001] The invention relates to a fat emulsion composition, especially a mefloquine fat emulsion composition. It also relates to a preparation method of the mefloquine fat emulsion composition. Background technique [0002] Mefloquine hydrochloride-mefloquine (WR-142490) is a new derivative of 4-quinoline methanol, its molecular formula: C17H16F6N2O·HCl, it can treat drug-resistant Plasmodium infection. [0003] The document "Chinese Patent with Patent Application No. 200580008298.X" discloses a pharmaceutical composition of (+)-erythro-mefloquine, which contains a unit dose of 1-60 mg (+)-erythro-mefloquine. Because it is an oral tablet, the bioavailability is low, about 30-50%. Since mefloquine is slightly soluble in water, it is necessary to use polyoxyethylene castor oil and absolute ethanol as a solubilizing carrier when it is used as an injection preparation clinically. , This will easily lead to the release of histamine and cause severe allergic reac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/113A61J3/00A61K31/4709A61P33/06
CPCY02A50/30
Inventor 马玉樊胡惠静陈涛卢婷利陈云
Owner NORTHWESTERN POLYTECHNICAL UNIV
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