A method for improving the inclusion performance of pharmaceutical excipients β-cyclodextrin

An auxiliary material package and cyclodextrin technology, which is applied in the directions of pharmaceutical formulations, organic active ingredients, and non-active ingredients medical preparations, etc., can solve the problem of low inclusion rate, insufficient stability of inclusion compounds, and low inclusion rate of cyclodextrin. and other problems, to achieve the effect of improving the inclusion rate and facilitating the inclusion performance

Active Publication Date: 2020-12-01
广东省药品检验所 +1
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, there are many manufacturers of pharmaceutical excipient β-CD, and the production process is different. During the production process of β-CD, it mainly contains a small amount of α, γ-cyclodextrin impurities, which will affect the inclusion rate. , and the current methods for preparing inclusion compounds mainly include grinding method and saturated solution method. The inclusion compound prepared by grinding method is not stable enough and the inclusion rate is low, while the saturated solution method usually uses a more polar substance as a solvent , generally water is used as the solvent, and the prepared inclusion compound is not high. There are two reasons, ① the raw material β-cyclodextrin has a small amount of impurities; ② the process of combining cyclodextrin with the drug, due to the , the solvent occupies the inner cavity of the β-cyclodextrin. During the stirring process, the drug molecules cannot quickly enter the inner cavity of the β-cyclodextrin, which lacks a driving force, resulting in a low inclusion rate of the cyclodextrin.

Method used

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  • A method for improving the inclusion performance of pharmaceutical excipients β-cyclodextrin

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Effect test

Embodiment 1

[0016] (1) Recrystallize β-cyclodextrin with purified water, dry at 60°C for 12 hours, and set aside; (2) Use saturated solution method, use mixed solvent (water:[EMIM]Cl=9.5:0.5 (weight ratio)) After preparing 27 mL of the saturated solution of purified β-cyclodextrin, add the drug naproxen, wherein the drug naproxen and the purified β-cyclodextrin are in a solid-to-solid molar ratio of 1:3, and stirred at 70°C for 2 hours (3) Measure the inclusion rate of the inclusion compound by ultraviolet spectrophotometry, and compare the inclusion effect of the inclusion compound before and after purification.

Embodiment 2

[0018] (1) Purify β-cyclodextrin with ethanol, dry it at 60°C for 12 hours, and set aside; (2) Use a saturated solution method, use 27 mL of a mixed solvent (water:[EMIM]Cl=9:1 (weight ratio)) After preparing a saturated solution of the purified β-cyclodextrin, add the drug naproxen, wherein the drug naproxen and the purified β-cyclodextrin are stirred at 70° C. for 2 hours at a solid-to-solid molar ratio of 1:3 3) Measure the inclusion rate of the inclusion compound by ultraviolet spectrophotometry, and compare the inclusion effect of the inclusion compound before and after purification.

Embodiment 3

[0020] (1) Purify β-cyclodextrin with acetone, dry it at 60°C for 12 hours, and set aside; (2) Use saturated solution method, use 27 mL of mixed solvent (water:[EMIM]Cl=8:2 (weight ratio)) After preparing a saturated solution of the purified β-cyclodextrin, add the drug naproxen, wherein the drug naproxen and the purified β-cyclodextrin are stirred at 70° C. for 2 hours at a solid-to-solid molar ratio of 1:3 (3) Measure the inclusion rate of the inclusion compound by ultraviolet spectrophotometry, and compare the inclusion effect of the inclusion compound before and after purification.

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Abstract

A method for improving inclusion performance of an adjuvant is disclosed. The method includes (1) purifying and drying the adjuvant; and (2) adding the adjuvant into a mixed solvent to prepare a saturated solution, adding a medicine with the mole ratio of the medicine to the adjuvant being 1:(3-5), and performing inclusion under stirring at 50-70 DEG C. The method allows the inclusion rate of an inclusion compound prepared by beta-cyclodextrin to be greatly increased and facilitates inclusion performance of the pharmaceutical adjuvant beta-cyclodextrin. Through infrared, ultraviolet and microscopic analysis identification, the structure and performance of the inclusion compound formed by the medicine molecule and the beta-cyclodextrin are not changed. An effective technical guidance for a pharmacy enterprise is provided.

Description

technical field [0001] The invention belongs to the field of pharmaceutical auxiliary materials, and in particular relates to a method for improving the inclusion performance of auxiliary materials β-cyclodextrin. Background technique [0002] β-cyclodextrin (β-CD) is a ring composed of 7 glucose residues combined with β-1,4-glucosidic bonds, which is extracted from starch by microbial enzymes, and has a cone-shaped cylinder. Shaped three-dimensional structure, is a new type of pharmaceutical excipients. Since the outer ring of β-CD is hydrophilic and the inner ring is hydrophobic, it can form inclusion complexes with various compounds through weak van der Waals force, making it stable, solubilizing, slow-release, emulsifying, anti-oxidation, anti-decomposition, and heat preservation , Moisture-proof, and has the function of masking peculiar smell. It is a new type of molecular wrapping material, which can be widely used in the fields of food, chemistry, medicine, agricultu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/61A61K31/192A61K31/216
CPCA61K31/192A61K31/216
Inventor 罗卓雅帅放文林生文王向锋章家伟王淼靳贵英
Owner 广东省药品检验所
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