Preparation, characterization and in vitro dissolution study of Nitrazepam: Cyclodextrin inclusion complex
The objectives of this research were to prepare and characterize inclusion complexes of Nitrazepam with Hydroxypropyl-β-cyclodextrin (HPβCD) and Sulfobutyl ether β-cyclodextrin (SBEβCD) to study the effect of complexation on the dissolution rate of Nitrazepam, a water-insoluble drug. The phase solub...
Main Authors: | , |
---|---|
Format: | Article |
Language: | English |
Published: |
Wolters Kluwer Medknow Publications
2012-01-01
|
Series: | Journal of Pharmacy and Bioallied Sciences |
Subjects: | |
Online Access: | http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2012;volume=4;issue=5;spage=106;epage=107;aulast=Patel |
id |
doaj-113611e7bfc944e7a35847e332cdd616 |
---|---|
record_format |
Article |
spelling |
doaj-113611e7bfc944e7a35847e332cdd6162020-11-24T21:27:57ZengWolters Kluwer Medknow PublicationsJournal of Pharmacy and Bioallied Sciences0975-74060976-48792012-01-014510610710.4103/0975-7406.94158Preparation, characterization and in vitro dissolution study of Nitrazepam: Cyclodextrin inclusion complexJ S PatelR P PatelThe objectives of this research were to prepare and characterize inclusion complexes of Nitrazepam with Hydroxypropyl-β-cyclodextrin (HPβCD) and Sulfobutyl ether β-cyclodextrin (SBEβCD) to study the effect of complexation on the dissolution rate of Nitrazepam, a water-insoluble drug. The phase solubility profile of Nitrazepam with Hydroxypropyl- β-cyclodextrin and Sulfobutyl ether β-cyclodextrin was an AP-type, indicating the formation of 2:1 stoichiometric inclusion complexes. Gibbs free energy values were all negative, indicating the spontaneous nature Nitrazepam solubilization and their value decreased with increase in the cyclodextrin concentration, demonstrating that the reaction conditions became more favorable as the concentration of cyclodextrins increased. Complexes of Nitrazepam were prepared with cyclodextrin using various methods such as physical mixing, kneading, spray-drying and lyophilization. The complexes were characterized by Differential scanning calorimetry, Fourier-transform infrared, scanning electron microscopy and powder X-ray diffraction studies. These studies indicated that a complex prepared by lyophilization had successful inclusion of the Nitrazepam molecule into the cyclodextrin cavity. Complexation resulted in a marked improvement in the solubility and wettability of Nitrazepam. Among all the samples, a complex prepared with Sulfobutyl ether β-cyclodextrin by lyophilization had the greatest improvement in the in vitro rate of Nitrazepam dissolution. The mean dissolution time for Nitrazepam decreased significantly after preparing complexes. The similarity factor indicated a significant difference between the release profiles of Nitrazepam from complexes, physical mixtures and plain Nitrazepam. To conclude that, the tablets containing complexes prepared with Cyclodextrins had significant improvement in the release profile of Nitrazepam as compared to tablets containing Nitrazepam without cyclodextrin.http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2012;volume=4;issue=5;spage=106;epage=107;aulast=PatelInclusion complexeshydroxypropyl-β-cyclodextrinsulfobutyl ether β-cyclodextrinnizatriptam |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
J S Patel R P Patel |
spellingShingle |
J S Patel R P Patel Preparation, characterization and in vitro dissolution study of Nitrazepam: Cyclodextrin inclusion complex Journal of Pharmacy and Bioallied Sciences Inclusion complexes hydroxypropyl-β-cyclodextrin sulfobutyl ether β-cyclodextrin nizatriptam |
author_facet |
J S Patel R P Patel |
author_sort |
J S Patel |
title |
Preparation, characterization and in vitro dissolution study of Nitrazepam: Cyclodextrin inclusion complex |
title_short |
Preparation, characterization and in vitro dissolution study of Nitrazepam: Cyclodextrin inclusion complex |
title_full |
Preparation, characterization and in vitro dissolution study of Nitrazepam: Cyclodextrin inclusion complex |
title_fullStr |
Preparation, characterization and in vitro dissolution study of Nitrazepam: Cyclodextrin inclusion complex |
title_full_unstemmed |
Preparation, characterization and in vitro dissolution study of Nitrazepam: Cyclodextrin inclusion complex |
title_sort |
preparation, characterization and in vitro dissolution study of nitrazepam: cyclodextrin inclusion complex |
publisher |
Wolters Kluwer Medknow Publications |
series |
Journal of Pharmacy and Bioallied Sciences |
issn |
0975-7406 0976-4879 |
publishDate |
2012-01-01 |
description |
The objectives of this research were to prepare and characterize inclusion complexes of Nitrazepam with Hydroxypropyl-β-cyclodextrin (HPβCD) and Sulfobutyl ether β-cyclodextrin (SBEβCD) to study the effect of complexation on the dissolution rate of Nitrazepam, a water-insoluble drug. The phase solubility profile of Nitrazepam with Hydroxypropyl- β-cyclodextrin and Sulfobutyl ether β-cyclodextrin was an AP-type, indicating the formation of 2:1 stoichiometric inclusion complexes. Gibbs free energy values were all negative, indicating the spontaneous nature Nitrazepam solubilization and their value decreased with increase in the cyclodextrin concentration, demonstrating that the reaction conditions became more favorable as the concentration of cyclodextrins increased. Complexes of Nitrazepam were prepared with cyclodextrin using various methods such as physical mixing, kneading, spray-drying and lyophilization. The complexes were characterized by Differential scanning calorimetry, Fourier-transform infrared, scanning electron microscopy and powder X-ray diffraction studies. These studies indicated that a complex prepared by lyophilization had successful inclusion of the Nitrazepam molecule into the cyclodextrin cavity. Complexation resulted in a marked improvement in the solubility and wettability of Nitrazepam. Among all the samples, a complex prepared with Sulfobutyl ether β-cyclodextrin by lyophilization had the greatest improvement in the in vitro rate of Nitrazepam dissolution. The mean dissolution time for Nitrazepam decreased significantly after preparing complexes. The similarity factor indicated a significant difference between the release profiles of Nitrazepam from complexes, physical mixtures and plain Nitrazepam. To conclude that, the tablets containing complexes prepared with Cyclodextrins had significant improvement in the release profile of Nitrazepam as compared to tablets containing Nitrazepam without cyclodextrin. |
topic |
Inclusion complexes hydroxypropyl-β-cyclodextrin sulfobutyl ether β-cyclodextrin nizatriptam |
url |
http://www.jpbsonline.org/article.asp?issn=0975-7406;year=2012;volume=4;issue=5;spage=106;epage=107;aulast=Patel |
work_keys_str_mv |
AT jspatel preparationcharacterizationandinvitrodissolutionstudyofnitrazepamcyclodextrininclusioncomplex AT rppatel preparationcharacterizationandinvitrodissolutionstudyofnitrazepamcyclodextrininclusioncomplex |
_version_ |
1725972423388430336 |