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Citral submicron emulsion and preparation method thereof

A citral and sub-microemulsion technology, which is applied in pharmaceutical formulations, emulsion delivery, aldehyde active ingredients, etc., can solve problems such as undiscovered citral formulations, few formulations and unstable properties of citral oil. Not easy to change compatibility, promote drug absorption, good compatibility

Active Publication Date: 2014-06-25
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because citral is a terpene compound, it is oily, has poor water solubility, unstable properties, and is volatile and easily oxidized at room temperature, so its application is limited to a certain extent.
[0003] At present, there are few domestic patents on litsea cubeba oil formulations, and no research on citral formulations has been found.

Method used

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  • Citral submicron emulsion and preparation method thereof
  • Citral submicron emulsion and preparation method thereof
  • Citral submicron emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Composition of citral submicron emulsion:

[0024] Citral: emulsifier: glycerin: ultrapure water = 1:0.5:0.25:2 (volume ratio), the emulsifier is a mixture of Tween 80: Span 80 = 1:2 (volume ratio), and the amount of lecithin is The volumetric dosage of citral is 0.005g / ml.

[0025] Preparation method: at 25°C, take 0.33ml Tween 80, 0.66ml Span 80, 0.5ml glycerin, and 10mg lecithin, stir and mix at a speed of 10000r / min, add 2ml citral to form an oil phase, Add 4ml of ultrapure water to the above oil phase, and stir it for 4min at a speed of 15500r / min in an emulsifier (model IKA T18, manufacturer: IKA Group Co., Ltd., Germany) to obtain oil-in-water (O / W) type citral submicron emulsion.

[0026] Performance test of citral submicron emulsion:

[0027] (1) Determination of encapsulation efficiency of citral submicron emulsion:

[0028] Mainly use GC-MS (model 7890A GC-5975C MSD, manufacturer: Agilent, USA), conditions: chromatographic column HP-5MS5%Phenyl Methyl Si...

Embodiment 2

[0043] Composition of citral submicron emulsion:

[0044] Citral: emulsifier: polyethylene glycol: ultrapure water = 1:1:0.25:2 (volume ratio), the emulsifier is a mixture of Tween 80: Span 80 = 1:3 (volume ratio), lecithin The mass dosage is 0.01g / ml based on the volumetric dosage of citral.

[0045] The preparation method is the same as in Example 1, and the temperature condition is 20°C. The performance test method of embodiment 2 citral submicron emulsion is the same as embodiment 1. The average encapsulation efficiency of three batches of citral submicron emulsions was measured to be 87%, the polydispersity index PDI was 0.204, the average particle size was 269nm, the average Zeta potential was -27.6mV, and the stability constant K E The value is 0.20. The results of the stability test showed that the three batches of citral submicroemulsion had good stability.

Embodiment 3

[0047] Composition of citral submicron emulsion:

[0048] Citral: emulsifier: glycerin: ultrapure water=1:2:0.25:2 (volume ratio), the emulsifier is a mixture of Tween 80: Span 80=1:1 (volume ratio), and the amount of lecithin is The volumetric dosage of citral is 0.005g / ml.

[0049] The preparation method is the same as in Example 1, and the temperature condition is 10°C. Embodiment 3 The performance testing method of the citral submicron emulsion is the same as that in Embodiment 1. The average encapsulation efficiency of three batches of citral submicron emulsions was measured to be 83%, the polydispersity index PDI was 0.219, the average particle size was 260nm, the average Zeta potential was -26.5mV, and the stability constant K E The value is 0.29. The results of the stability test showed that the three batches of citral submicroemulsion had better stability.

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Abstract

The invention discloses a citral submicron emulsion and a preparation method thereof. The preparation method comprises following steps of mixing an emulgator, a co-emulsifier and a stabilizer at 10-30DEG C, stirring uniformly, dripping citral while stirring so as to form an oil phase, and then adding ultrapure water so as to prepare the citral submicron emulsion, wherein the volume ratio of citral to the emulgator to the co-emulsifier to ultrapure water is 1:(0.5-3):(0.25-1):(1.5-5), and the mass dosage of stabilizer is 0.005-0.02g / ml according to the volume dosage of citral. The oil-in-water type submicron emulsion has small particle size, is uniform in particle distribution and has good stability, nasal spraying or aerosol inhalation can promote absorption of the drug and increase local drug concentration, and the citral submicron emulsion can remarkably relieve the syndrome of an asthma rat when being atomized on the rat, thus laying a foundation for clinical application of citral.

Description

(1) Technical field [0001] The invention relates to a submicron emulsion and its preparation, in particular to a citral submicroemulsion and a preparation method thereof. The submicron emulsion has an anti-asthma effect and can be administered by nasal spray or atomization. (2) Background technology [0002] Citral (citral), molecular formula C 10 h 16 O, is a kind of monoterpene compound with lemon flavor extracted from the fruit of Litsea cubeba, a plant of the genus Zingiberaceae. It contains two cis-trans isomers of α-citral and β-citral. They are all active ingredients of citral (Luo Man, Jiang Like. GC-MS analysis of Litsea cubeba essential oil components in Anhui Huangshan Mountain [J]. Crop Research, 2006,3:256-258.), the citral described in this patent Refers to the composition of α-citral and β-citral cis-trans isomers. Citral is the main raw material for the synthesis of various spices and an important intermediate in the pharmaceutical industry. Studies have ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/12A61K31/11A61K47/34A61K47/10A61P11/06
Inventor 丁兴红钱俊华张艳
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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