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A kind of L-carnitine base emulsion and its preparation method and medicine
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A technology of L-carnitine and emulsion, applied in the field of microemulsion, can solve the problems of difficult delivery, poor solubility, difficult transdermal delivery, etc., and achieve the effects of improving absorption effect, biological activity and efficacy retention, and good solubility
Active Publication Date: 2021-08-03
HARBIN INST OF TECH SHENZHEN GRADUATE SCHOOL
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However, transdermal delivery is difficult due to insolubility or slight solubility of poorly soluble drugs in water and most organic solvents
It is well known that many poorly soluble promising drugs never enter clinical trials due to their poor solubility and delivery difficulties
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Embodiment 1
[0073] The preparation method of the present embodiment L-carnitine malate microemulsion comprises the following steps:
[0074] Under a nitrogenatmosphere, dissolve 0.01mol of malic acid in 10mL of water in the reactor, dissolve 0.01mol of L-carnitine in 10mL of water, and add dropwise into the reactor in which malic acid is dissolved, heat to 40°C, and ionize into Salt reaction for 12 hours;
[0075] After the reaction is complete, concentrate the solution to 1 / 10 of the reaction solution under vacuum conditions, distill and crystallize under reduced pressure, and obtain the L-carnitine base ion salt crystal product through filtration and washing, and dry it in a vacuum oven for 48 hours to obtain the purity More than 99% L-carnitine malate 2.84g, yield 96.27%, to obtain L-carnitine base ion salt.
[0076] At room temperature, mix the emulsifier Tween 80 and co-emulsifier Span 20 in a molar ratio of 1:1, 1:2, 2:1, mix thoroughly with a magnetic stirrer to mix the emulsifie...
Embodiment 2
[0079] The preparation method of the present embodiment L-carnitine citrate ion salt microemulsion comprises the following steps:
[0080]Under a nitrogenatmosphere, dissolve 0.01 mol of citric acid in 10 mL of aqueous solution in the reactor, and dissolve 0.01 mol of L-carnitine in 10 mL of water, and add dropwise into the reactor in which citric acid is dissolved, heat to 40°C, and ionize into Salt reaction for 12 hours;
[0081] After completion of the reaction, concentrate the solution to 1 / 6 of the reaction solution under vacuum conditions, freeze and crystallize, and obtain the L-carnitine citrate ion salt crystal product through filtration and washing separation, and dry it in a vacuum oven for 48 hours to obtain a product with a purity exceeding 99% L-carnitine citrate ion salt 3.42g, yield 96.88%.
[0082] At room temperature, mix the emulsifier Tween 80 and co-emulsifier Span 20 in a molar ratio of 1:1, 1:2, 2:1, mix thoroughly with a magnetic stirrer to mix the em...
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Abstract
The invention discloses an L-carnitine-based emulsion, a preparation method and medicine. The preparation method of the L-carnitine-based emulsion comprises: adding an organic acid and L-carnitine into water to obtain a L-carnitine-based ionsalt solution; mixing an emulsifier with a co-emulsifier to obtain a mixed emulsifier; The mixed emulsifier is mixed with the oil phase and the L-carnitine base ionsalt solution to obtain the L-carnitine base emulsion. The L-carnitine-based emulsion prepared by the method for preparing the L-carnitine-based emulsion of the present invention has the characteristics of good biocompatibility and better solubility for insoluble drugs.
Description
technical field [0001] The invention relates to the technical field of microemulsions, in particular to an L-carnitine-based emulsion, a preparation method and a medicine. Background technique [0002] In recent years, non-aqueous microemulsions containing ionic liquids have begun to be used in drug delivery systems. Compared with traditional aqueous microemulsions, the most prominent advantage of ionic liquid-oil microemulsions is thermal stability. As a new type of drugdelivery system, microemulsion has the advantages of increasing the solubility of drugs, improving the stability of drugs and avoiding the first-pass effect. It is an excellent way for drug delivery. [0003] In the ionic liquid-oil microemulsion, the ionic liquid can be used as the polar phase solvent of the microemulsion, and can also be used as the surfactant of the microemulsion. Compared with traditional drug delivery strategies (oral, injection), transdermal drug delivery has many advantages, such as...
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