A kind of sustained-release terpinene-4-alcohol microemulsion and preparation method thereof

A terpinene and sustained-release technology, which is applied in the field of sustained-release terpinene-4-ol microemulsion and its preparation, can solve the problem of difficult administration of terpinene-4-ol, terpinene-4-ol The problem of low water solubility of alcohol, to achieve the effect of improving water solubility and solving drug delivery difficulties

Inactive Publication Date: 2017-08-25
CHONGQING ACADEMY OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved in the present invention is that the water solubility of terpinene-4-ol is extremely low, which brings difficulties to the administration of terpinene-4-ol

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] The selection of embodiment 1 composite emulsifier

[0015] Get polyoxyethylene hydrogenated castor oil, oleic acid, Tween, polyethylene glycol-400, clove oil, Triton X-100, lecithin in proportion (w / w) 9.5:0.5 (as a control), 9: 1. 8.5:1.5, 8:2, 7.5:2.5, 7:3, 6.5:3.5, 6:4, 5.5:4.5, 5:5 are mixed in pairs respectively, the total amount is 200mg, and then add 100ml of water at 60r / Min speed stirring, observe the emulsification phenomenon. Visually evaluate its self-microemulsification efficiency (from the time of forming microemulsion and microemulsion morphology), and find that the microemulsion formed by polyoxyethylene hydrogenated castor oil and clove oil takes a short time and the microemulsion is clear and slightly blue. Good stability. Microemulsions formed by other combinations cannot take care of both at the same time.

Embodiment 2

[0016] Co-emulsifier and compound emulsifier of embodiment 2

[0017] Get ethanol, propylene glycol or butanol and the composite emulsifier in the example 1 in proportion (w / w) 9.5:0.5,9:1,8.5:1.5,8:2,7.5:2.5,7:3,6.5:3.5, Mix 6:4, 5.5:4.5, and 5:5 (as a control) respectively, the total amount is 200mg, then add 100ml of water and stir at a speed of 60r / min to observe the emulsification phenomenon. Evaluate self-microemulsification efficiency by visual inspection, find that the microemulsion formed with propylene glycol and the composite emulsifier in Example 1 is transparent and slightly blue-white in about 1.2 minutes; The microemulsion was transparent and slightly bluish-white in about 1.5 minutes; the microemulsion formed by ethanol and the composite emulsifier in Example 1 had the shortest time, about 0.7 minutes, and was clear and slightly bluish, with good uniformity.

Embodiment 3

[0018] The preparation of embodiment 3 sustained-release terpinen-4-ol microemulsions

[0019] Take terpinen-4-ol (0.7%), compound emulsifier (0.9%), and co-emulsifier (0.6%) respectively, mix according to the above ratio, stir at room temperature to make it evenly mixed, and then add the remaining proportion of water , and vortexed for 10-20 minutes to obtain a slow-release terpinen-4-ol microemulsion, which was clear. The changes of the microemulsion were tested respectively under the following three environments: normal temperature for 3 months, 40°C for 1 month and 4500lx light for 15 days. The experimental results found that the microemulsion was still clear and uniform under the above three environments. No precipitation, good stability.

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Abstract

The invention belongs to the technical field of microemulsion preparation, particularly relates to a sustained-release terpinene-4-alcohol microemulsion and a preparation method thereof, and aims at solving the technical problems that terpinene-4-alcohol is extremely low in water solubility and brings difficulty for drug delivery. According to the technical scheme provided by the invention, the sustained-release terpinene-4-alcohol microemulsion is prepared from the following components in percentage by weight: 0.9%-2.7% of a compound emulsifier, 0.3%-0.6% of a co-emulsifier, 0.7%-1.2% of terpinene-4-alcohol and the balance of water. The invention further provides a preparation method of the sustained-release terpinene-4-alcohol microemulsion. The water solubility of terpinene-4-alcohol is improved; the microemulsion has a sustained release effect; and a new way is provided for drug delivery of the terpinene-4-alcohol.

Description

technical field [0001] The invention belongs to the technical field of microemulsion preparation, and in particular relates to a slow-release terpinene-4-ol microemulsion and a preparation method thereof. Background technique [0002] Terpinen-4-ol (chemical formula C 10 h 18 O) is a colorless oily liquid, slightly soluble in water, has anti-inflammatory, detoxification, antibacterial and other functions, especially has a strong antibacterial effect on fungi, common pathogenic bacteria and drug-resistant bacteria. Terpinen-4-ol has good safety and antibacterial properties, especially the antibacterial effect on drug-resistant bacteria has certain development prospects. Due to the extremely low water solubility of terpinen-4-ol, it is difficult to administer terpinen-4-ol. With the continuous improvement of preparation technology, not only can more new dosage forms be developed, but also it is expected to further reduce its toxicity and fully exert its antibacterial activi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/045A61P29/00A61P39/02A61P31/04A61P31/10A61K47/44
Inventor 秦建波李滨王玉
Owner CHONGQING ACADEMY OF SCI & TECH
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