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Inclusion compound of forsythin and cyclodextrin or cyclodextrin derivative and preparation method of inclusion compound

A technology of forsythia aglycone and cyclodextrin is applied in the directions of active ingredients of heterocyclic compounds, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problem of poor solubility of forsythia aglycone, increase biological Availability and other issues, to achieve the effects of high bioavailability, fast dissolution, and simple process

Pending Publication Date: 2022-07-08
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The object of the present invention is to provide an inclusion compound containing forsythin and its preparation method. The inclusion compound of the present invention can increase the water solubility of forsythin, overcome the defect of poor solubility of forsythin, and increase its bioavailability

Method used

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  • Inclusion compound of forsythin and cyclodextrin or cyclodextrin derivative and preparation method of inclusion compound
  • Inclusion compound of forsythin and cyclodextrin or cyclodextrin derivative and preparation method of inclusion compound
  • Inclusion compound of forsythin and cyclodextrin or cyclodextrin derivative and preparation method of inclusion compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Forsythin: hydroxypropyl-β-cyclodextrin = 1:5.

[0023] Take 4 g of hydroxypropyl-β-cyclodextrin and put it in a beaker, add water to dissolve, put it on a magnetic heating stirrer, and stir at 60 °C, and add 0.8 g of forsythia aglycone. Filtration, freeze-drying of the filtrate to obtain loose powder, namely forsythia aglycone hydroxypropyl-β-cyclodextrin inclusion complex.

Embodiment 2

[0025] Forsythin: hydroxypropyl-β-cyclodextrin = 1:10.

[0026] Take 4 g of hydroxypropyl-β-cyclodextrin and put it in a beaker, add water to dissolve, to obtain solution A; take 2 g of forsythia aglycone, dissolve it with methanol under ultrasonic conditions, to obtain solution B; solution A is ultrasonicated at 40 °C, While adding solution B, after all the addition, continue to ultrasonic for 3h, filter, and dry the filtrate to obtain forsythia aglycone hydroxypropyl-β-cyclodextrin inclusion complex.

Embodiment 3

[0028] Forsythin: dimethyl-β-cyclodextrin = 1:10.

[0029] Take 40 g of dimethyl-β-cyclodextrin and put it in a beaker, add water to dissolve, to obtain solution A; take 4 g of forsythia aglycone, dissolve it with 60% ethanol solution under ultrasonic conditions, to obtain solution B; solution A is at 50 ℃ While sonicating, add solution B, after all the addition, continue sonicating for 1 h, filter, and spray-dry the filtrate to obtain forsythia aglycone β-dimethyl-β-cyclodextrin.

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Abstract

The invention discloses a phillygenin cyclodextrin or cyclodextrin derivative clathrate compound as well as a preparation and a preparation method thereof. The phillygenin is contained in the cyclodextrin or the cyclodextrin derivative, and the weight ratio of the phillygenin to the cyclodextrin or the cyclodextrin derivative is 1: (1-50). According to the inclusion compound of the forsythin cyclodextrin or the cyclodextrin derivative, disclosed by the invention, the solubility and the bioavailability of the forsythin can be effectively improved. The inclusion compound of the forsythin cyclodextrin or cyclodextrin derivative can be used for preparing tablets, capsules, infusion, hydro-acupuncture, powder injection, oral liquid, syrup, granules, dispersible tablets, orally disintegrating tablets and the like.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicines, in particular, the invention relates to an inclusion compound of forsythia aglycone and a cyclodextrin inclusion compound or a cyclodextrin derivative and a preparation and preparation method thereof. Background technique [0002] Forsythia, also known as Eclipta ("Medicinal Properties"), Daqiaozi ("Xinxiu Materia Medica"), is the dried fruit of Forsythia suspense (Thunb.Vah1), a rhinoceros plant. Bitter and slightly cold in taste, it returns to the lung, heart, and small intestine meridians. It has the effects of clearing away heat and detoxifying, reducing swelling and dispersing knots. It is mainly used to treat carbuncle, mammary carbuncle, erysipelas, wind-heat cold, early onset of dampness, high fever and polydipsia, dizziness, and dizziness. Hot shower urine closed. The chemical composition of Forsythia is complex and diverse, among which are mainly phenylethyl alcoh...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/34A61K36/634A61P35/00A61P3/06A61P39/06A61P1/16
CPCA61K31/34A61K47/6951A61K36/634A61P35/00A61P3/06A61P39/06A61P1/16Y02A50/30
Inventor 滕勇荣梁红宝郭田甜
Owner LUNAN PHARMA GROUP CORPORATION
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