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Solid dispersion of higher fatty alcohol and its prepn

A high-grade fatty alcohol and solid dispersion technology, which is applied in food preparation, medical preparations of non-active ingredients, liquid delivery, etc., can solve the problem of undiscovered solid dispersion reports of octacosanol, difficulty in exerting pharmacological effects, Low hydrophilic index and other problems, to achieve the effect of improving bioavailability, improving dissolution mechanism, and increasing wettability

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
Patent application 200510076612.X discloses the preparation method of the microcapsule powder of octacosanol, but has not yet found the report of the solid dispersion of octacosanol

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1 PEG6000 is the preparation of the octacosanol solid dispersion of carrier

[0028] This example examines the preparation of PEG6000 dispersions with different mass ratios of octacosanol and carrier.

[0029] Mix octacosanol monomer with PEG6000 at a mass ratio of 1:1, 1:5, 1:10, 1:20, and 1:30, dissolve in ethanol, stir, mix evenly, and rotate to evaporate, Ethanol is evaporated, cooled, dried in a vacuum drier, pulverized, ground, and passed through a 60-100 mesh sieve to obtain a solid dispersion of octacosanol PEG6000. Dissolution testing: testing by the above method, the results are shown in Table 1.

[0030]

[0031] This example shows that the preparation of octacosanol PEG6000 solid dispersion by solvent method can significantly improve the solubility and dissolution of octacosanol in different water-soluble dissolution media compared with octacosanol monomer. Rate. The mass ratio of octacosanol to carrier has a great influence on the di...

Embodiment 2

[0032] Example 2 Preparation of octacosanol PEG6000 solid dispersion by different methods

[0033] This example investigates the preparation of octacosanol PEG6000 solid dispersion by different preparation methods. The octacosanol-containing monomer is mixed with PEG6000 at a mass ratio of 1:10, and the octacosanol PEG6000 solid dispersion is prepared by different preparation methods such as grinding method, spray drying method, melting method, and solvent method. At the same time, a blank experiment was carried out, and the dissolution rate of octacosanol monomer 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.

[0034] Preparation

[0035]This example shows that the spray drying method is slightly better than the other three methods, and the spray drying method is preferred in this example. This example also shows that octacosanol in the PEG solid disp...

Embodiment 3

[0036] Example 3 Preparation of Higher Fatty Alcohol Solid Dispersions with Different Kinds of PEG as Carriers

[0037] This example examines the preparation of solid dispersions of higher fatty alcohols with different PEG carrier materials. Mix higher fatty alcohols containing 80% octacosanol in a mass ratio of 1:10 with PEG4000, PEG6000, PEG12000, PEG20000, PEG6000-PEG12000 mixture (mass ratio 1:1), dissolve or suspend in ethanol In the solution, the mixed solution was ultrasonicated for 15 minutes, and then spray-dried. The spray-drying conditions were: the inlet air temperature was 45°C, the feed rate was 30mL / min, the atomizer speed was 50HZ, and the pressure difference of the cyclone separator was 50mm water column. , The resulting dry powder is passed through a 60-100 mesh sieve to obtain a solid dispersion of octacosanol. At the same time, a blank experiment was carried out, and the dissolution rate of octacosanol monomer in artificial gastric juice, distilled water, ...

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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 solid dispersion containing octacosyl alcohol in 0.65-50 wt%, and technologically, the present invention features that octacosyl alcohol is dispersed homogeneously in water soluble carrier to prepare the solid dispersion. The higher fatty alcohol solid dispersion 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 a solid dispersion containing higher fatty alcohols, especially octacosanol, and a preparation method; further, the present invention also relates to a pharmaceutical preparation prepared from the solid dispersion. 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 phys...

Claims

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Application Information

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IPC IPC(8): A61K31/045A61K9/08A61K9/10A61K9/16A61K9/20A61K9/48A61K47/34A61P3/06A61P9/00A61P39/06A23L1/30A23L33/10A23L33/105A61K47/10A61K47/12A61K47/22A61K47/26A61K47/32
Inventor 赵金华文震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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