Idebenone nanometer lipid carrier transdermal absorption preparation and preparation method thereof

A technology for nano lipid carrier and transdermal absorption preparation, which is applied in the field of idebenone nano lipid carrier transdermal absorption preparation and preparation, can solve problems such as technical parameter differences, achieve good skin compatibility and avoid first pass effect, the effect of improving bioavailability

Inactive Publication Date: 2011-06-15
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the nano-lipid carrier of some medicines has been prepared, there are great differences in the technical parameters of the preparation method of the corresponding nano-lipid carrier for different drugs, so there is an urgent need for an idebenone nano-lipid Carrier transdermal absorption preparation and preparation method

Method used

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  • Idebenone nanometer lipid carrier transdermal absorption preparation and preparation method thereof
  • Idebenone nanometer lipid carrier transdermal absorption preparation and preparation method thereof
  • Idebenone nanometer lipid carrier transdermal absorption preparation and preparation method thereof

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Embodiment 1

[0048] Material

[0049] Weigh the prescribed amount of idebenone, glyceryl behenate, caprylic triglyceride, capric triglyceride and poloxamer-188 and mix evenly, heat to 80°C to form a lipid phase; Sodium amphoteric acetate and ultrapure water are mixed evenly at 80°C to form a water phase; under stirring, the lipid phase is slowly added to the water phase at a temperature of 80°C and mixed, and at a temperature of 80°C, it is emulsified at a high speed of 7000r / min Uniformly shear for 2 minutes for preliminary emulsification, and then use an ultrasonic breaker to perform ultrasonic crushing with a power of 200w for 2 minutes; after the above 4 cycles of high-speed milk uniform shearing and ultrasonic crushing, the mixture is gradually cooled to room temperature, and the loaded moxa powder is prepared. Nanostructured Lipid Carriers of Debenzoquinones. The particle diameter of the carrier is 80.1±4.2nm, the encapsulation efficiency is 90.2%-93.4%, and the ζ potential...

Embodiment 2

[0051] Material

[0052] Weigh the prescribed amount of idebenone, glyceryl palmitostearate, squalene and Tween-80 and mix evenly, heat to 70°C to form a lipid phase; mix the prescribed amount of molecularly distilled monoglyceride with ultrapure water Mix evenly at 70°C to form a water phase; under stirring, slowly add the fat phase to the water phase at 70°C and mix, and at 70°C, perform preliminary emulsification with 7000r / min high-speed milk shear for 2min, Afterwards, the primary emulsion was homogenized with a high-pressure homogenizer, the pressure was 400 bar, and the temperature was controlled at 75°C; after 2 cycles, the sample was poured into a silanized glass container and cooled at room temperature to prepare the loaded idebenne Quinone Nanostructured Lipid Carriers (see figure 2 ). The particle size is 40.2±2.3nm, the encapsulation efficiency is 98.3%~99.1%, and the zeta potential is -31.4~-35.5mV. Then add the prescribed amount of pharmaceutically ...

Embodiment 3

[0054] Material

[0055] cetyl palmitate

[0056] Weigh the prescribed amount of idebenone, cetyl palmitate, caprylic triglyceride, capric triglyceride and lecithin and mix evenly, heat to 90°C to form a lipid phase; Pure water is mixed evenly at 90°C to form a water phase; under stirring, the lipid phase is slowly added to the water phase at 90°C and mixed, and at 90°C, the high-speed emulsion shearing at 13000r / min for 8min is used for preliminary Emulsification, and then ultrasonic crushing with 200w power for 8 minutes; after the above three cycles of high-speed emulsion shearing and ultrasonic crushing, the mixture is gradually cooled to room temperature, and the nanostructure loaded with idebenone is made lipid carrier (see figure 1 ). The average particle size of the carrier is 110.2±7.5nm, the encapsulation rate is 80.5%-85.7%, and the zeta potential is -28.0-32.2mV. Then add the prescribed amount of pharmaceutically acceptable auxiliary materials...

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Abstract

The invention discloses an idebenone nanometer lipid carrier transdermal absorption preparation and a preparation method thereof. The preparation method comprises the following steps: mixing idebenone, solid lipid materials, liquid lipid materials and a surface active agent 1 uniformly, and heating until the mixture is turned into a lipid phase; mixing a surface active agent 2 with ultrapure water uniformly so that the mixture is turned into a water phase; adding the lipid phase into the water phase slowly under the condition of keeping the temperature of the lipid phase and the water phase consistent while stirring; homogenizing rapidly, cutting, carrying out primary emulsification, carrying out ultrasonication again, and cooling down, so that a lipid carrier of a nanometer structure loading idebenone is prepared; and adding pharmaceutically acceptable auxiliary materials, so that the idebenone nanometer lipid carrier transdermal absorption preparation is prepared. The particle diameter of the idebenone nanometer lipid carrier transdermal absorption preparation provided by the invention is 40.2-110.2nm, the entrapment rate is 80.5%-99.1%, the zeta potential is minus 25.5-minus 34.4mV, the morphology is stable, an organic solvent is not contained, the idebenone nanometer lipid carrier transdermal absorption preparation has good compatibility with skin and has no irritation, the first pass effect is avoided, and the bioavailability is improved.

Description

technical field [0001] The invention relates to the field of medicine and health product preparations, in particular to an idebenone nano lipid carrier transdermal absorption preparation and a preparation method. Background technique [0002] Idebenone is a synthetic analogue of coenzyme Q10, which has strong antioxidant and free radical scavenging functions, and can selectively activate the mitochondrial respiratory chain cycle of nerve cells to improve glucose utilization and promote ATP production. There are a lot of foundations Experimental and clinical experiments have confirmed that idebenone has a good curative effect in the treatment of mental disorders and language disorders caused by cerebrovascular diseases, brain function and metabolic disorders, as well as in the treatment of senile dementia and in delaying the aging of various tissues and organs of the body. In addition, Chinese patent 00809884.0 discloses and protects a skin preparation for topical application...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P25/18A61P25/28A61K31/122A61P3/00A61P39/06A61K9/127A61P9/10
Inventor 葛志强李蓓
Owner TIANJIN UNIV
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