Cornel extract oral medicine compositions low irritative to gastrointestinal tract and its preparation

A composition, the technology of Cornus officinalis, applied in the direction of drug combination, drug delivery, non-central analgesics, etc., can solve problems affecting the effect of drug application, pain, stomach discomfort, etc.

Inactive Publication Date: 2005-01-19
HUTCHISON MEDIPHARMA ENTERPRISES LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the inventor also found in the research process that the conventional oral dosage form of the extract has obvious stimulating effect on the patient'

Method used

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  • Cornel extract oral medicine compositions low irritative to gastrointestinal tract and its preparation
  • Cornel extract oral medicine compositions low irritative to gastrointestinal tract and its preparation
  • Cornel extract oral medicine compositions low irritative to gastrointestinal tract and its preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation of Cornus officinalis Extract and Determination of Polyphenol Content Therein by Skin Powder Method

[0049]Cornus officinalis 500g, add water 5000mL, decoct 3 times, the degree of decoction is slightly boiled, the decoction time is 2 hours each time, the decoction liquid is filtered, combined, and set aside for later use; The ratio of 1:2 is packed into the column, and then the above-mentioned water decoction is passed through the macroporous adsorption resin column at a flow rate of 20 ml / min. After passing through completely, the resin column is eluted with water, 10% ethanol and 95% ethanol . The eluate was collected and vacuum-dried to obtain 48 g of Cornus officinalis extract.

[0050] Take 2.0076g (W) of the above-mentioned Cornus officinalis extract, dissolve it in 500mL of water, take 25mL of the solution, concentrate it to dryness, and then dry it at 105°C for 3 hours to obtain a solid product, the weight of which is T 1 = 0.0966g.

[...

Embodiment 2

[0054] Example 2 Separation and Identification of Three Active Components of Cornus officinalis

[0055] Isolation and identification of loganin:

[0056] 100g of Cornus officinalis can be soaked three times in 500mL of 95% ethanol, and the extracts can be combined to obtain 10g of concentrate. The concentrate was subjected to vacuum column chromatography and eluted with petroleum ether, chloroform and methanol in sequence. After concentration of methanol eluent, silica gel column chromatography (eluent CH 2 CL 2 / CH 3 OH=6:4), to get loganin 875mg, its Rf value=0.57 (developing agent: 0.1M KH 2 PO 4 : 0.1MH 3 PO 4 :CH 3 CN=7:7:4). Its spectral data are:

[0057] [α] D 25 =-81°(c0.1, H 2 O), UV(λ max , nm) 238 (4.0); IR: (cm -1 , KBr): 3350, 3300, 1715, 1650, 1440, 1300, 1080;

[0058] 1 H NMR (D 2 O, 300MHz) δppm: 7.42 (s, H-3), 5.39 (d, J=3.6Hz, H-1), 4.14 (m, H-7), 3.73 (s, OCH 3 ), 3.05(m, H-5), 2.16(m, H-6a), 2.10(m, H-9), 1.88(m, H-8), 1.73(m, H-6b), 1...

Embodiment 3

[0069] Example 3 HPLC chromatogram and quantitative analysis of Cornus officinalis extract

[0070] Quantitative analysis of Cornus officinalis extract (Example 1) was carried out by HPLC system. Instrument: Agilent 1100, the set wavelength is 240nm, the analytical column is Zorbax SC18 4.6*150mm, and the flow rate is 1ml / min. The mobile phase is CH 3 CN and 0.1% H 3 PO 4 solution. The gradient status is: CH 3 CN increments from 0% to 25% in 50 minutes. During the next 5 minutes, CH 3 CN is incremented to 100%. be attached figure 1 The HPLC chromatogram shown.

[0071] The reference substances of loganin, morroniside, and corniside were all isolated and purified in this laboratory. Through HPLC analysis, the purity is above 96%.

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Abstract

The invention relates to a cornel extract oral medicine compositions low irritative to gastrointestinal tract and its preparation, the oral pharmaceutical composition and preparation of its active constitution, the invention also relates to the process for preparing the oral pharmaceutical composition and preparation.

Description

technical field [0001] The present invention relates to an oral pharmaceutical composition and preparation of traditional Chinese medicine extracts with low gastrointestinal irritation and a preparation method thereof, in particular to an oral pharmaceutical composition and preparation of cornus officinalis extracts with low gastrointestinal irritation and a preparation method thereof . Background technique [0002] Loganin is an iridoid glycoside compound, present in Cornus officinalic Sieb.et Zucc (Li et al., Daozong.Shipin Gongye Keji (2002), 23(10), 45-47.), Hydrangea hortensis (Khalifa et al., Journal of Pharmaceutical Sciences (2001), 28 221-229.), Strychnoscathayensis (Cheng et al., Journal of the Chinese Chemical Society (Taipei, Taiwan) (2001), 48 (2), 235-239) and other plants. According to literature reports, loganin has strong anti-inflammatory activity (Maria del Carmen Recio et al Structural Considerations on the Iridoids as Anti-inflammatory Agents Planta Me...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/7048A61P29/00A61P37/02
Inventor 杜莹潘柯严孝强张维汉赵世萍
Owner HUTCHISON MEDIPHARMA ENTERPRISES LTD
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