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Preparation method and application of medicament-cyclodextrin inclusion compound self-emulsifying composition

A technology of cyclodextrin inclusion complex and composition, which is applied in directions such as pharmaceutical formulations, medical preparations of inactive ingredients, and emulsion delivery, can solve the problems of difficult preparation of preparations, low bioavailability and the like, and achieves a simple preparation process. Ease of operation, good emulsifying performance, and low cost of production

Inactive Publication Date: 2011-06-29
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] In drug research, it is found that nearly 40% of drugs are insoluble in water, which easily leads to problems such as difficult preparation of preparations and low bioavailability. A hot spot and a difficult point

Method used

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  • Preparation method and application of medicament-cyclodextrin inclusion compound self-emulsifying composition
  • Preparation method and application of medicament-cyclodextrin inclusion compound self-emulsifying composition
  • Preparation method and application of medicament-cyclodextrin inclusion compound self-emulsifying composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Preparation and content determination of methotrexate-β-cyclodextrin inclusion compound

[0040] Weigh 7mmol β-cyclodextrin and 1mmol methotrexate in a mortar, add an appropriate amount of ammonia water containing 35% NH4OH, grind for 30min, dry in a vacuum oven for 12h to obtain a solid powder, add appropriate amount of water, and centrifuge to remove the precipitate ( free drug), the supernatant was taken, and vacuum-dried to obtain the methotrexate-cyclodextrin inclusion compound.

[0041] Methotrexate content was determined by HPLC (LC-2010C, Shimadzu, Japan) method. The mobile phase is methanol: water=75:25 (v / v), and the chromatographic column is Lichrospher C 18 (150×4.6μm), the column particle size is 5μm. The flow rate was 1.0 mL / min, the detection wavelength was 227 nm (SPD-10A, UV detector, Shimadzu, Japan), the column temperature was 30° C., and the injected sample volume was 20 μl. The drug loading amount of the sample was calculated by formul...

Embodiment 2

[0043] Example 2: Preparation and Content Determination of Retinoic Acid-β-Cyclodextrin Inclusion Compound

[0044] Weigh 10mmol β-cyclodextrin and 1mmol retinoic acid in a mortar, add an appropriate amount of ammonia water containing 35% NH4OH, grind for 30min, dry in a vacuum oven for 12h to obtain a solid powder, add appropriate amount of water, and centrifuge to remove the precipitate (free drug ), take the supernatant, and vacuum-dry to obtain retinoic acid-cyclodextrin inclusion compound.

[0045]The content determination was carried out by HPLC (LC-2010C, Shimadzu, Japan) method. The mobile phase is methanol: water: formic acid=95:5:0.5 (v / v), and the chromatographic column is Lichrospher C 18 (150×4.6μm), the column particle size is 5μm. The flow rate was 1.0 mL / min, the detection wavelength was 345 nm (SPD-10A, UV detector, Shimadzu, Japan), the column temperature was 25° C., and the injected sample volume was 20 μl. The encapsulation efficiency of the sample was c...

Embodiment 3

[0046] Example 3: Preparation and content determination of simvastatin-hydroxypropyl-β-cyclodextrin inclusion compound

[0047] Weigh 5mmol hydroxypropyl-β-cyclodextrin and 1mmol rosuvastatin, add 10ml water, stir magnetically at 37°C for 72h, after reaching stability, centrifuge the sample, pass the supernatant through the membrane (to remove free drug), freeze dry to obtain simvastatin-cyclodextrin inclusion complex.

[0048] The content determination was carried out by HPLC (LC-2010C, Shimadzu, Japan) method. The mobile phase is 0.025mol L -1 Sodium dihydrogen phosphate solution (p H=4.5)-acetonitrile (35:65) (v / v), the chromatographic column is Lichrospher C 18 (150×4.6 μm). The flow rate was 1.0 mL / min, the detection wavelength was 238 nm (SPD-10A, UV detector, Shimadzu, Japan), the column temperature was 40°C, and the injected sample volume was 20 μl. The encapsulation efficiency of the sample was calculated by formula (1). As a result of calculation, the encapsulat...

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Abstract

The invention discloses a preparation method and application of a medicament-cyclodextrin inclusion compound self-emulsifying composition. The composition is prepared through the following steps: preparing a medicament-cyclodextrin inclusion compound by combining a medicament and cyclodextrin; mixing the medicament-cyclodextrin inclusion compound, an oil phase, an emulsifier, an assistant emulsifier, a stabilizer and an additive; and completely dissolving the materials through magnetic stirring or ultrasonic; and uniformly mixing. The composition has the advantages that the defects of low solubility of poorly water-soluble drugs, low bioavailability, low drug-loading rate and the like are overcome, the medicament stability is greatly improved, the problems of poor emulsifier stability, large storage volume and the like caused by a water phase are solved, and the effect of sustaining medicament release can be achieved. The preparation method has the advantages of simplicity, developed process, high yield of the composition and suitability for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a method and application of a cyclodextrin inclusion compound prepared as a pharmaceutical carrier into a microemulsion. Background technique [0002] In drug research, it is found that nearly 40% of drugs are insoluble in water, which easily leads to problems such as difficult preparation of preparations and low bioavailability. A hot and difficult point. [0003] Cyclodextrin is non-toxic, tasteless, and easily hydrolyzed into glucose in the body, and its unique cavity structure can form inclusion complex structures with many drugs, which solves the problem of drug solubility and accelerates drug absorption. Improve bioavailability, in addition, it can also increase drug stability, reduce gastrointestinal side effects of drugs, reduce irritation, effectively cover up the bad taste of drugs and other advantages. [0004] Microemulsion (ME) is a clear and thermodynamica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/48A61K47/61
Inventor 周建平姚静娜迪亚方正杰
Owner CHINA PHARM UNIV
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