Andrographolide cyclodextrin inclusion compound, preparation method and application thereof

A technology of cyclodextrin inclusion compound and andrographolide, which is applied in the field of medicine, can solve the problems of limiting the application of andrographolide, instability, and inability to take it orally, so as to reduce the possibility of external interference, enhance stability, and improve solubility. Improved effect

Inactive Publication Date: 2012-02-08
CITY UNIVERSITY OF HONG KONG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, diterpenes are generally poorly soluble in water
Therefore, andrographolide, despite its high medical value, cannot be used orally because poor water solubility prevents it from being well absorbed

Method used

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  • Andrographolide cyclodextrin inclusion compound, preparation method and application thereof
  • Andrographolide cyclodextrin inclusion compound, preparation method and application thereof
  • Andrographolide cyclodextrin inclusion compound, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1: the preparation of solid system

[0058] This example provides the preparation of a physical mixture of andrographolide and cyclodextrin and the preparation of a typical andrographolide-cyclodextrin inclusion compound of the present invention.

[0059] A physical mixture of andrographolide and cyclodextrin was prepared by rolling and mixing andrographolide and cyclodextrin for 15 minutes at a mixing molar ratio of andrographolide and cyclodextrin of 1:1 and 1:2.

[0060] The inclusion compound of andrographolide-cyclodextrin and the inclusion compound of andrographolide-cyclodextrin-polymer were prepared by spray drying. The andrographolide-cyclodextrin binary system was prepared as follows: the drug and the cyclodextrin in a molar ratio of 1:1 or 1:2 were dissolved in 50% ethanol (300ml of 50% ethanol solution contained 250mg of andrographolide), Sonicate the solution for 1h. Andrographolide-cyclodextrin-polymer ternary system was prepared as follows:...

experiment example 2

[0062] Experimental Example 2: Phase Solubility Study

[0063] Phase solubility studies were determined according to the method of Higuchi and Connors (T. Higuchi et al., Adv. Anal. Chem. Inst. 4 (1965) 117-121). Excess andrographolide was added to 10 ml of water or an aqueous solution containing various concentrations of the following cyclodextrins: β-cyclodextrin (0 to 16 mM), 2-hydroxypropyl β-cyclodextrin (0 to 20 mM) and Gamma cyclodextrin CD (0 to 20 mM). The suspension was shaken vigorously at 25 °C for 3 days. After reaching equilibrium, the samples were filtered through a 0.45 micron filter and diluted appropriately. The concentration of andrographolide was determined by ultraviolet spectrophotometry at a wavelength of UV 230nm (Hewlett Packard 8425A, Germany). Repeat the test 3 times. The apparent stability constant (K C ):

[0064]

[0065] where S 0 is the water solubility of andrographolide.

[0066] The phase solubility diagram of andrographolide in ...

experiment example 3

[0067] Experimental Example 3: Particle Size and Particle Size Distribution

[0068] The particle size of the sample powder was measured by a laser diffraction analyzer (MasterSizer 2000, Malvern Instrument, UK) using dry dispersion at a pressure of 3.5 bar. Repeat the measurement 3 times to get the average value. The results are expressed as the volume median diameter d(v; 0.5), where d refers to the diameter at 50% of the entire volume distribution.

[0069] The particle size of the spray-dried samples was determined by laser diffraction. The sample powder is dispersed by compressed air, which is then passed through a focused laser beam. Table 1 shows the particle size distribution of spray-dried granules produced with different andrographolide-CD ratios and under different operating conditions. Spray-dried particles with volume diameters in the range of 0.684-2.504 μΜ were successfully prepared. The results show that the drug-CD molar ratio does not affect the particl...

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Abstract

The present invention provides an andrographolide cyclodextrin inclusion compound. The basic components of the andrographolide cyclodextrin inclusion compound comprise: a) andrographolide, and b) pharmaceutically-acceptable cyclodextrin. The inclusion compound is prepared through carrying out spray drying for the CD and the andrographolide, wherein the entrance temperature is 100-200 DEG C, the material feeding speed is less than or equal to 20 ml/min, a molar ratio of the CD to the andrographolide is more than or equal to 1:1. The present invention further provides a preparation method for the inclusion compound, and an application of the inclusion compound. The inclusion compound provided by the present invention has excellent solubility, excellent drug stability and excellent bioavailability. With the method provided by the present invention, the inclusion compound of the andrographolide and the cyclodextrin or the inclusion compound of other plant compounds and the cyclodextrin can be prepared, wherein the inclusion compound has the particle size from micrometer to submicron, such that the bioavailability and the stability of the andrographolide are increased, a new delivery system for the diterpene plant compound is provided.

Description

technical field [0001] The invention belongs to the technical field of medicine. Specifically, the present invention relates to andrographolide cyclodextrin inclusion compound, its preparation method and application. Background technique [0002] It is well known in the art that poor solubility of a biologically active compound hinders the biological efficacy and therapeutic value of the compound as reflected in its bioavailability. Despite the increasing understanding of the reasons for the poor bioavailability of compounds in recent years and a series of methods to improve the solubility of some poorly soluble compounds have been disclosed, most plant compounds undergo hydrolysis under neutral and alkaline conditions, Therefore, the bioavailability and efficacy of these molecules are greatly reduced in the alkaline environment of the GI tract. [0003] Andrographolide (Andro) is the main active ingredient in Andrographis paniculata (Burm.f), a plant of the Acanthaceae fa...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/365A61P1/16A61P31/04A61P37/04A61P35/00
Inventor 张汉扬赖慧冰
Owner CITY UNIVERSITY OF HONG KONG
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