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Cyclodextrin inclusion compound and preparation method thereof

A technology of cyclodextrin inclusion complex and cyclodextrin, which is applied in the directions of active ingredients of heterocyclic compounds, pharmaceutical combinations, pharmaceutical formulations, etc., can solve the problem that the proportion of eucalyptus oil is small, the pharmaceutical ingredients cannot reach the efficacy, and the formulations, etc.

Active Publication Date: 2021-06-25
BEIJING GRAND JOHAUM PHARMA CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is aimed at the inclusion of eucalyptus oil, and it is impossible to know how the components with different contents in eucalyptus oil affect the inclusion
Moreover, because a large amount of β-cyclodextrin is used during inclusion complex, the proportion of eucalyptus oil in the prepared inclusion compound is relatively small, and even only contains a small amount of eucalyptus oil. The ingredients of traditional Chinese medicine cannot achieve the efficacy and cannot meet the purpose of the preparation

Method used

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  • Cyclodextrin inclusion compound and preparation method thereof
  • Cyclodextrin inclusion compound and preparation method thereof
  • Cyclodextrin inclusion compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 compares the differences in the preparation of cyclodextrin inclusion compounds by different methods, including ultrasonic method and stirring method, specifically including the following:

[0035] Experimental group 1

[0036] Experimental group 1 used ultrasonic method to prepare cyclodextrin inclusion compound containing eucalyptus limonene oil, and the experimental steps were as follows:

[0037] Under the condition of 20° C., 2 g of β-cyclodextrin (β-CD) was weighed and dissolved in 100 mL of purified water to make a supersaturated aqueous solution, and filtered to obtain a saturated aqueous solution. Add 1g of eucalyptus limonene oil (including 0.5g of eucalyptol, 0.38g of limonene and 0.12g of α-pinene), ultrasonically treat at 20°C for 1h, refrigerate overnight, filter with suction, and filter the residue at 40°C Drying under the hood to obtain the cyclodextrin inclusion compound containing eucalyptus limonene oil.

[0038] Experimental group 2

[0...

Embodiment 2

[0047] Example 2 The ultrasonic method was used to prepare cyclodextrin inclusion complexes, and the influence of β-cyclodextrin and eucalyptus limonene oil on the yield of cyclodextrin inclusion complexes under different mass ratio conditions was studied.

[0048] At 20°C, weigh 0.74 g of β-CD and add it into purified water to prepare a supersaturated aqueous solution, and filter to obtain a saturated aqueous solution; then add different amounts of eucalyptus limonene oil (as shown in Table 1 below, where Comprising 50% eucalyptol by weight, 38% limonene by weight and 12% α-pinene by weight), so that β-CD: eucalyptus limonene oil mass ratio is 1:1.08, 1:1: 2. 1:5, 1:8, 1:10, 1:15 (g / g, the specific weight is shown in Table 1 below), sonicate at 20°C for 1 hour, cool overnight, filter with suction, and filter the residue at 40°C dry conditions. Calculate the clathrate yield according to the following formula.

[0049]

[0050] Wherein, in this formula, the actual yield is...

Embodiment 3

[0055] Example 3 The cyclodextrin inclusion compound was prepared by ultrasonic method, and the effect of the inclusion compound at different temperatures on the yield of the cyclodextrin inclusion compound was studied.

[0056] 0.74 g of β-cyclodextrin was weighed and added into purified water to prepare a supersaturated aqueous solution, which was filtered to obtain a saturated aqueous solution. Then add the eucalyptus limonene oil of 2 times amount (eucalyptus limonene oil comprises that weight percent is 50% eucalyptol, weight percent is 38% limonene and weight percent is 12% α-pinene, actual eucalyptus limonene oil The weighing amount is shown in Table 2 below), and the cyclodextrin inclusion compound was prepared by ultrasonic at different inclusion temperatures of 20°C, 30°C, 40°C, 50°C, and 60°C. The ultrasonic time was 1h, and the ultrasonic frequency was 40KHz. After sonication, cool overnight, filter with suction, and dry the filter residue at 40°C to obtain a cyclo...

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Abstract

The invention relates to a cyclodextrin inclusion compound and a preparation method thereof. The cyclodextrin inclusion compound provided by the invention comprises a pharmaceutical composition and cyclodextrin or a derivative thereof, The pharmaceutical composition is prepared from the following components in parts by weight: 35 to 65 parts of eucalyptol, 15 to 50 parts of limonene and 10 to 30 parts of alpha-pinene. The cyclodextrin inclusion compound provided by the invention can be prepared by an ultrasonic method. The cyclodextrin inclusion compound provided by the invention is high in stability, the solubility is obviously increased, and the cyclodextrin inclusion compound can be used for preparing different dosage forms.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a cyclodextrin inclusion compound and a preparation method thereof, in particular to a cyclodextrin inclusion compound containing eucalyptol, limonene and α-pinene and a preparation method thereof. Background technique [0002] The pharmaceutical composition containing eucalyptol, limonene and α-pinene is a mucolytic expectorant with clear curative effect, but the pharmaceutical composition is volatile and irritating, and it is easily lost when directly added to the preparation, thus causing It affects the curative effect of the preparation, and may affect the stability of the preparation using the pharmaceutical composition as the raw material drug, and has certain irritation to the gastrointestinal tract after direct administration. [0003] The application number is 201910036486.7, and the Chinese patent application with publication number CN109528649A discloses a se...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K31/35A61K31/015A61P11/10
CPCA61K47/6951A61K31/35A61K31/015A61P11/10A61K2300/00
Inventor 沈芳玲聂红梅胡昱
Owner BEIJING GRAND JOHAUM PHARMA CO LTD
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