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Liquid crystal nanoparticle transdermal agent and preparation method thereof

A kind of technology of nanoparticles and transdermal agent

Active Publication Date: 2014-08-13
GUANGDONG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Wherein, liposome patch mostly is phospholipid liposome, but the lipid material that commonly used phospholipid liposome uses is all sensitive to heat, acid, alkali and esterase, and stability is relatively poor.
In addition, the microemulsion in the microemulsion gel is prone to delamination and demulsification, and the stability is not good
Therefore, the instability of liposome and microemulsion gel hinders the clinical application of liposome and microemulsion drug delivery system
Moreover, the transdermal absorption rate of the sinomenine transdermal smear drug preparation in the prior art is relatively slow, the onset is slow, and the therapeutic effect is not ideal.

Method used

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  • Liquid crystal nanoparticle transdermal agent and preparation method thereof
  • Liquid crystal nanoparticle transdermal agent and preparation method thereof
  • Liquid crystal nanoparticle transdermal agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] A liquid crystal nanoparticle transdermal agent, the raw material components include sinomenine, glycerol monooleate (component A), poloxamer 407 (component B) and water (component C); The mass content is 1%; the mass ratio of component A to component B is 9:1, and the mass relationship of component A, component B and component C satisfies (A+B) / (A+B+C) *100%=10%;

[0032] The preparation method of the above-mentioned liquid crystal nanoparticle transdermal agent, it comprises the following steps: weighing 0.3g sinomenine, 2.7g glycerol monooleate, 0.3g poloxamer 407 and 26.7g water according to the above formula, Phinerine, glyceryl monooleate and poloxamer 407 are heated and melted in a 60°C water bath, and mixed thoroughly to obtain a mixed solution, which is added dropwise to water, then ultrasonically dispersed, and then subjected to high pressure after ultrasonically dispersed homogeneous, the liquid crystal nanoparticle transdermal agent is obtained.

Embodiment 2

[0034] A liquid crystal nanoparticle transdermal agent, the raw material components include sinomenine hydrochloride, phytantriol and glycerol monooleate (component A), poloxamer 407 (component B) and water (component C) The mass content of sinomenine hydrochloride is 1%; the mass ratio of component A to component B is 9:1, and the mass relationship between component A, component B and component C satisfies (A+B) / ( A+B+C)*100%=10%;

[0035] The preparation method of the above-mentioned liquid crystal nanoparticle transdermal agent, it comprises the following steps: weighing 0.3g sinomenine hydrochloride, 1.35g phytantriol, 1.35g monoolein glyceride, 0.3g poloxamer 407 and 26.7g of water, dissolve sinomenine hydrochloride in water to obtain a mixed solution, mix phytantriol, glycerol monooleate and poloxamer 407, heat and melt in a 60°C water bath, and add dropwise to the above mixed solution After ultrasonic dispersion, and then high-pressure homogenization after ultrasonic d...

Embodiment 3

[0037] A liquid crystal nanoparticle transdermal agent, the raw material components include sinomenine mesylate salt, phytantriol (component A), poloxamer 407 (component B) and phosphate buffer (component C ); the mass content of sinomenine mesylate salt is 2%; the mass ratio of component A to component B is 1:1, and the mass relationship of component A, component B and component C satisfies (A+ B) / (A+B+C)*100%=1%;

[0038]The preparation method of the above-mentioned liquid crystal nanoparticle transdermal agent comprises the following steps: weighing 1.2g sinomenine mesylate salt, 0.3g phytantriol, 0.3g poloxamer 407 and 59.4g phosphoric acid according to the above formula Salt buffer solution, dissolving sinomenine mesylate salt and poloxamer 407 in phosphate buffer solution to obtain a mixed solution, heating and melting phytantriol in a water bath at 60°C, adding it dropwise to the above mixed solution, and then performing Ultrasonic dispersion, followed by high-pressure...

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Abstract

The invention relates to the technical field of pharmaceutical preparations, in particular to a liquid crystal nanoparticle transdermal agent and a preparation method thereof. Liquid crystal nanoparticle transdermal agent, its raw material components include drug, liquid crystal material (component A), stabilizer (component B) and dispersion medium (component C); the mass content of the drug is 0.1%~2% ;The mass ratio of component A to component B is 1:1~9:1, and the mass relationship of component A, component B and component C satisfies (A+B) / (A+B+C)* 100%=1%~10%. The liquid crystal nanoparticle transdermal agent of the present invention has the advantages of fast transdermal absorption rate, fast onset of action, good therapeutic effect and good product stability, and it has very light irritation to the skin, no allergic and toxic reactions to the skin, and It has the characteristics of good safety, small side effects and convenient use. The preparation method of the liquid crystal nano particle transdermal agent of the invention is simple and the production cost is low.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a liquid crystal nanoparticle transdermal agent and a preparation method thereof. Background technique [0002] As an emerging field in pharmacy, transdermal drug delivery preparations have become a research hotspot at home and abroad in recent years, and have developed rapidly. The advantages of transdermal administration are as follows: it can avoid the first-pass effect of the gastrointestinal tract and liver, has the advantages of stable blood drug concentration, convenient administration, etc., and has obvious advantages in reducing adverse reactions, improving therapeutic index and drug compliance . Transdermal drug delivery refers to a type of drug delivery method in which drugs pass through the skin at a certain rate, enter the systemic circulation after being absorbed by capillaries, and produce systemic or local therapeutic effects. There are two m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/485A61K31/473A61K31/616A61K47/34A61P29/00A61P19/02A61K47/10
Inventor 彭新生周艳芳王勤于琼周艳星薛曼田园胡敏余娟定
Owner GUANGDONG MEDICAL UNIV