Drug and cyclodextrin interaction and its pharmaceutical property Raman spectrum analysis method

A technology of Raman spectroscopy and analysis method, which is applied in the field of Raman spectroscopy analysis of interactions and pharmaceutical performance parameters, which can solve the problem of inability to accurately identify changes in the inclusion degree of the system, poor accuracy, and difficulty in judging drugs and cyclodextrins Effects and other issues

Inactive Publication Date: 2006-08-09
NANJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, conventional analysis methods such as powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), infrared spectrum (IR), NHR and other methods can only judge whether the drug and cyclodextrin in the inclusion compound are effective or not, especially in the system When the drug content is low or the drug exists in a multi-component complex system, the accuracy of the results provided by the above analysis methods is poor, and generally it is impossible to accurately identify the change of the inclusion degree of the system, and it is impossible to quantitatively analyze the inclusion degree of the inclusion compound. The characterization of the binding mode in the system is also very limited
Especi

Method used

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  • Drug and cyclodextrin interaction and its pharmaceutical property Raman spectrum analysis method
  • Drug and cyclodextrin interaction and its pharmaceutical property Raman spectrum analysis method
  • Drug and cyclodextrin interaction and its pharmaceutical property Raman spectrum analysis method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1, Raman spectrum characterization of the interaction between nimodipine and hydroxypropyl-β-cyclodextrin and its pharmaceutical properties

[0048] Nimodipine (NM) is a second-generation 1,4-dihydropyridine calcium antagonist. It is a commonly used cardiovascular and cerebrovascular drug widely used in clinical practice. In this study, nimodipine was clathrated with hydroxypropyl cyclodextrin (HP-β-CD) to form a supramolecular system, and tablets were prepared after adding corresponding excipients. Dissolution parameters, dissolution parameters, penetration parameters, pharmacokinetic parameters were analyzed and predicted and compared with the experimental results.

[0049]

[0050] Sample preparation: Nimodipine / HP-β-CD supramolecular inclusion complex was prepared by spray drying method, and the molar ratio of nimodipine / HP-β-CD was 1:3. The sample was added with lactose, microcrystalline cellulose, micropowder silica gel, and magnesium stearate, and wa...

Embodiment 2

[0090] Example 2, Raman spectrum characterization of the interaction between ibuprofen and hydroxypropyl-β-cyclodextrin and its pharmaceutical properties

[0091] Ibuprofen (bf) is currently an alkyl propionate antipyretic, analgesic, and anti-inflammatory drug with definite clinical curative effect, few adverse reactions and high safety, which has been widely used in clinic. However, due to the poor water solubility, which affects the bioavailability, there have been many literature reports at home and abroad to use water-soluble cyclodextrin derivatives to prepare supramolecular bodies to improve bioavailability.

[0092]

[0093] Good water solubility and bioavailability. In this study, the inclusion of ibuprofen with hydroxypropyl-β-cyclodextrin (HP-β-CD) and sulfobutyl ether cyclodextrin SBE-β-CD was used to form a supramolecular system, and capsules were prepared after adding corresponding excipients , Raman spectroscopy was used to analyze and predict the inclusion ...

Embodiment 3

[0123] Example 3, Raman spectrum characterization of the interaction between cefditoren pivoxil and sulfobutyl ether-β-cyclodextrin and its pharmaceutical properties

[0124] Cefditoren Pivoxil (Cefditoren Pivoxil) is a fourth-generation cephalosporin antibiotic, which has a broad antibacterial spectrum against Gram-positive and negative bacteria, especially Staphylococcus, Streptococcus including Streptococcus pneumoniae, etc. Positive bacteria, Gram-negative bacteria such as Escherichia coli, Branhamella catarrhalis, Klebsiella, Proteus, Haemophilus influenzae, and Peptostreptococcus, Propionibacterium acnes, Bacteroides, etc. Anaerobic bacteria show strong antibacterial power. In this study, cefditoren pivoxil and sulfobutyl ether-β-cyclodextrin

[0125]

[0126] After (SBE-β-CD) inclusion, a supramolecular system was formed, and granules were prepared after adding corresponding excipients. Raman spectroscopy was used to analyze and predict the inclusion degree and diss...

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Abstract

Present invention refers to medicine and schardinger dextrin interaction and pharmacy performance Raman spectra analytical procedure.It contains adopts Raman spectrometer or Fourier Raman spectrometer to proceed atlas determination to medicine, classifying and selecting Chinese traditional medicine absorption band or absorption peak in atlas, selecting specifical vibrational band used as featuring reference band, collecting or calculating band wave number, spectral bandwidth, band intensity, band shape coefficient etc parameter, using standard control or working curve qualitative and quantify identifying and analysing medicine clathration state and level in different system or preparation, predicting pharmic dissolve out performance, penetrating quality and medicine dynamics parameter.Said invention has non - contacting, nondestructive, short time, and high detection sensitivity.

Description

technical field [0001] The invention relates to a pharmaceutical analysis method of cyclodextrin inclusion compound, in particular to a Raman spectrum analysis method of the interaction between medicine and cyclodextrin and its pharmaceutical performance parameters. Background technique [0002] Cyclodextrin has a cage structure that is hydrophilic on the outside and hydrophobic on the inside. The whole molecule or lipophilic structure of the lipophilic guest can form so-called inclusion complexes with it by displacing the water molecules in the CD cavity, that is, the guest drug and the host Supramolecular body formed by CD. Also known as "molecular microcapsules" at the molecular level. The purpose of drug / cyclodextrin supramolecular body application is mainly to: increase the water solubility of the drug; improve the stability of the drug; promote the absorption of the drug and improve the bioavailability of the drug; reduce the stimulation and side effects of the drug o...

Claims

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Application Information

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IPC IPC(8): G01N21/31G01N21/25
Inventor 杨星昊
Owner NANJING NORMAL UNIVERSITY
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