Herba epimedii aglycone or cyclo-herba epimedii aglycone phospholipid compound and preparation method thereof

A technology for cyclic icariin and astrogenin phospholipids, which is applied in the field of pharmaceutical preparations, can solve the problems of poor water solubility, fat solubility, and low bioavailability, achieve high drug loading, simple preparation process, and overcome loading The effect of low dose

Inactive Publication Date: 2010-02-03
贾晓斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thereby solving the shortcomings of their poor wat...

Method used

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  • Herba epimedii aglycone or cyclo-herba epimedii aglycone phospholipid compound and preparation method thereof
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  • Herba epimedii aglycone or cyclo-herba epimedii aglycone phospholipid compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1. In vitro dissolution test of icarigenin, cycloicarigenin raw materials and their phospholipid complexes

[0054] Take icariin or cycloicariin raw material drug and soybean lecithin, their mass ratio is 1:0.5 or 1:5 plus 50 times the mass of absolute ethanol, heat and reflux for 1 hour, the yellow Slightly sticky powder, conduct equilibrium solubility and in vitro dissolution tests.

[0055] Equilibrium solubility experiment:

[0056] Three batches of prepared mixtures and complexes of icariin, cycloicariin and soybean phospholipid were weighed according to the drug / phospholipid mass ratio of 1:0.5 and 1:5 respectively, and the measured average equilibrium solubility is shown in the table below.

[0057] Equilibrium solubility table of icariin, cyclic icariin and soybean lecithin mixture and complex

[0058] ethanol

water

n-octanol

IT

5.30mg / mL

insoluble

4.77mg / mL

IT / phospholipid (1:0.5 mixture

9.51mg / mL

...

Embodiment 2

[0066] Example 2. Preparation of icarigenin phospholipid complex

[0067] Weigh 20g of icariin, 40g of soybean lecithin, add 500mL of ethanol, reflux at 50°C for 1h, until the reaction solution is clear, evaporate the solvent, and dry the solid in vacuum to obtain a yellow solid, which is crushed through an 80-mesh sieve to obtain Epimedium Huogenin phospholipid complex, the resulting product has no new absorption peaks after ultraviolet spectrum scanning, see Figure 6 ; Infrared spectrum see Figure 10 , the results showed that the infrared spectrum analysis spectrum of the icariin phospholipid complex was not consistent with the infrared spectrum analysis spectrum of the mixture. The infrared spectrum of the physical mixture basically retains the characteristic absorption peaks of the drug and phospholipids. It is a simple superposition of the infrared chromatographic peaks of icariin and phospholipids. There is no interaction between the two, and icariin remains in cryst...

Embodiment 3

[0068] Example 3. Preparation of Icarigenin Phospholipid Complex

[0069] Weigh 20g of icariin, 10g of lecithin, add 500mL of methanol, stir at 15°C for 6h until the reaction solution is clear, evaporate the solvent, and dry the solid in vacuum to obtain a yellow solid, which is crushed through a 80-mesh sieve to obtain Epimedium Aurigenin phospholipid complex, its ultraviolet scanning spectrum is the same as implementation example 2, see Figure 13 . Take 30 g of the prepared phospholipid complex, add 40 g of microcrystalline cellulose, 30 g of starch, and 5 g of sodium carboxymethyl starch, wet granulate with 95% ethanol as a wetting agent, dry, add 0.5 g of magnesium stearate, and press into tablets , to get 1000 tablets.

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Abstract

The invention relates to a herba epimedii aglycone phospholipid compound or a cyclo-herba epimedii aglycone phospholipid compound, which is characterized by being composed of herba epimedii aglycone or cyclo-herba epimedii aglycone and phospholipid, wherein the mass ratio of the herba epimedii aglycone or the cyclo-herba epimedii aglycone and the phospholipid is 1:0.5 to 5. The phospholipid in theherba epimedii aglycone phospholipid compound or the cyclo-herba epimedii aglycone phospholipid compound has the positive function on treating the osteoporosis, and the medicine and the phospholipidin the phospholipid compound of the herba epimedii aglycone or cyclo-herba epimedii aglycone medicine has the synergic function on treating the osteoporosis; after the phospholipid and the herba epimedii aglycone or the cyclo-herba epimedii aglycone are prepared into the compound, the dissolvability thereof is improved greatly, and the disadvantages of poor water solubility and fat solubility andlow bioavailability are solved; the herba epimedii aglycone phospholipid compound or the cyclo-herba epimedii aglycone phospholipid compound has simple preparation process and moderate reaction condition, and is suitable to industrialized big production. The invention discloses a preparation method thereof.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical preparations, and relates to the preparation technology of icariin, cycloicariin phospholipid complex and preparations thereof. Background technique: [0002] Osteoporosis is a worldwide disease. With the aging society, osteoporosis has been listed as one of the three major senile diseases. Flavonoids in Epimedium have anti-osteoporosis activity, and icariin, icariside I, icariside II, epimedin B, and epimedin C all have the effect of increasing bone marrow matrix. Cell calcification, and the role of promoting osteoblast proliferation and mineralization (Cai Manling, Ji Hui, Liu Yue, et al. Effects of five epimedium flavonoids on osteoblasts cultured in vitro[J]. Chinese Pharmacology Communication, 2004 , 21 (3): 13.), Epimedium flavonoid glycosides have steric hindrance due to the presence of glycosidic bonds, which weakens their anti-osteoporosis activity, and icariin has the strongest anti-osteo...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K47/24A61P19/10
Inventor 贾晓斌贾东升孙娥
Owner 贾晓斌
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