Inclusion compound of higher fatty alcohol and its prepn

A high-level aliphatic alcohol and clathrate technology, which is applied in the direction of non-active ingredients of polymer compounds, food preparation, active ingredients of hydroxyl compounds, etc., can solve the problem of cyclodextrin inclusion complex reports and pharmacology of octacosanol that have not yet been found. The effect is not easy to exert, poor absorption in the body, etc., to achieve the effect of improving bioavailability, improving dissolution mechanism, and increasing surface area

Inactive Publication Date: 2007-11-07
深圳海创医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The experiment of gavage administration of octacosanol to rats showed that because of its low hydrophilic index, the absorption in the body is poor, and the pharmacological effects are not easy to exert
Chinese patent application 200510076612.X discloses the preparation method of microcapsule powder of octacosanol, but no report on cyclodextrin inclusion compound of octacosanol has been found

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 β-CD is preparation of octacosanol clathrate of clathrate material

[0026] This example examines the preparation of octacosanol clathrates in which β-CD is clathrate material. Dissolve octacosanol in a small amount of ethanol, weigh an appropriate amount of β-CD according to the mass ratio of 1:1, 1:5, 1:10, 1:20, and 1:30, dissolve it in water, and After the start, slowly add the ethanol solution of octacosanol to the aqueous solution of cyclodextrin, ultrasonicate for 30 minutes, freeze-dry in vacuum, grind it finely, and pass through a 60-100 mesh sieve to obtain the octacosanol clathrate. At the same time, a blank experiment was carried out, and the dissolution rate of octacosanol in artificial gastric juice, distilled water, and phosphate was detected according to the method described in the instructions. The results are shown in Table 1.

[0027]

[0028] This example shows that the preparation of octacosanol β-CD inclusion compound by ultras...

Embodiment 2

[0029] Example 2 Preparation of octacosanol β-CD inclusion compound by different methods

[0030] This example investigates the preparation of octacosanol β-CD inclusion compound by different preparation methods. Mix octacosanol β-CD with β-CD at a mass ratio of 80% by mass, and prepare octacosanol β-CD according to different preparation methods such as saturated solution method, ultrasonic method and grinding method CD clathrate. At the same time, a blank experiment was carried out, and the dissolution rate of octacosanol in artificial gastric juice, distilled water, and phosphate was detected according to the method described in the instructions. The results are shown in Table 2.

[0031] Preparation

[0032] This example shows that the ultrasonic method is slightly better than the other three methods, and the ultrasonic method is preferred in this case. This example also shows that octacosanol in the β-CD inclusion compound prepared by the three methods has a g...

Embodiment 3

[0033] Example 3 Preparation of Higher Fatty Alcohol Inclusion Compounds Using Hydroxypropyl-β-CD as Inclusion Materials

[0034] This example examines the preparation of octacosanol inclusion compound with hydroxypropyl-β-CD as the inclusion material. Dissolve octacosanol with 80% higher fatty alcohol in a small amount of ethanol, and weigh hydroxyprene in proportions of 1:1, 1:5, 1:10, 1:20, 1:30 An appropriate amount of base-β-CD, dissolved in water, slowly added octacosanol ethanol to the aqueous solution of hydroxypropyl-β-CD after the start of ultrasonication, ultrasonicated for 30 minutes, vacuum freeze-dried, and grinded finely, after 60-100 mesh sieve to obtain octacosanol. After determination, the mass percentage of octacosanol in the clathrate is 2% to 40%. At the same time, a blank experiment is carried out to detect the dissolution rate of octacosanol in artificial gastric juice, distilled water, and phosphate according to the method described in the manual. The...

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PUM

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Abstract

The present invention relates to medicinal intermediate containing higher fatty alcohol and its preparation process. The medicinal intermediate is inclusion compound containing octacosyl alcohol in 0.65-50 wt% and cyclodextrin or cyclodextrin derivative. It is prepared through a grinding process, an ultrasonic process or a saturated water solution process. The higher fatty alcohol including compound has obviously raised dissolution of octacosyl alcohol in leaching medium and thus high bioavailability. It may be further prepared into tablet, suspension or other solid or liquid preparation forms for clinical application of octacosyl alcohol.

Description

technical field [0001] The invention relates to a pharmaceutical intermediate and a preparation method thereof. Specifically, it relates to clathrates containing higher fatty alcohols, especially octacosanol, and a preparation method. Furthermore, the present invention also relates to a pharmaceutical preparation prepared from the clathrate. Background technique [0002] Octacosanol is a straight-chain high-carbon fatty alcohol, mainly found in wheat germ oil, rice bran oil, beeswax, and the skins of fruits such as sugar cane, apples, and grapes. Octacosanol with commercial use is mainly obtained from raw materials such as rice bran wax, cane wax, and beeswax. Octacosanol has significant physiological activities such as lowering blood lipids and anti-fatigue, and can be used as cardiovascular disease drugs, health food, and sports functional drinks, and has good application potential. However, since octacosanol is a macromolecular fat-soluble substance, its physical shape...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/045A61K47/40A61K9/08A61K9/10A61K9/16A61K9/20A61K9/48A61P3/06A61P9/10A61P39/06A23L1/30A23L33/10
Inventor 文震赵金华姚光辉吕修梅张德福薛焰
Owner 深圳海创医药科技发展有限公司
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