Prednisone/Cyclodextrin Inclusion Complexation: Phase Solubility, Thermodynamic, Physicochemical and Computational Analysis

2008 ◽  
Vol 38 (1) ◽  
pp. 83-94 ◽  
Author(s):  
Ameer Ghuzlaan ◽  
Mahmoud M. Al Omari ◽  
Khaldoun A. Al-Sou’od
INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (11) ◽  
pp. 19-23
Author(s):  
J Shaikh ◽  
◽  
S. V. Deshmane ◽  
R. N Purohit ◽  
K. R. Biyani

The main objective of the present study was to enhance the solubility and dissolution rate of poorly water soluble aceclofenac using its solid dispersion with β-cyclodextrin. FTIR and DSC study was carried out to find out any incompatibility. The phase solubility of drug was carried out in 1, 2, 5, and 10% of β-cyclodextrin in distilled water. Kneading method and solvent evaporation method was use to prepared solid dispersion of aceclofenac and β-cyclodextrin. Different evaluation tests like solubility study in different solvents, PXRD and in vitro dissolution study of aceclofenac- β-cyclodextrin inclusion complex were carried out. The overall finding indicated that β-cyclodextrin is a desirable water soluble carrier, that helps in increasing solubility of drug. Due to its structural feature, β-cyclodextrin forms a good inclusion complex that decreases contact angle of drug with water molecules by increasing wetting properties. Hence, it can be concluded that, β-cyclodextrin is better water soluble carrier molecule in terms of its compatibility and increasing solubility behavior of poorly water soluble drug aceclofenac.


2005 ◽  
Vol 73 (3) ◽  
pp. 147-161 ◽  
Author(s):  
Charumanee S. ◽  
Weiss-Greiler P. ◽  
Wolschann P. ◽  
Viernstein H. ◽  
Titwan A. ◽  
...  

Thermodynamic studies of piroxicam in aqueous solution complexed with β-cyclodextrin (β-CD), γ-cyclodextrin (γ-CD) and two β-cyclodextrin derivatives, hydroxypropyl-β-cyclodextrin (HP-P-CD) and methyl-β-cyclodextrin (Me-β-CD) were performed at different temperatures and pH values using the phase solubility method. The phase solubility diagrams of β-CD, γ-CD and HP-β-CD is of AL-type behavior, indicating the formation of 1:l complexes. The related stability constants range from β-CD > γ-CD > Me-β-CD > HP-β-CD, respectively. An Ap-type solubility diagram is observed for Me-β-CD, indicating the formation of 1:2 complexes at higher CD concentrations. From the temperature dependence of the equilibrium constants the reaction enthalpies and entropies have been determined. The contributions of the reaction entropies are small and no enthalpy-entropy-compensation is observed, except for γ-CD, where a very small negative reaction entropy could be estimated. Moreover, the influence of the pH value is rather high because the differently charged forms of piroxicam show different solubility behavior in water.


2021 ◽  
pp. 27-32
Author(s):  
Olga Mikhailovna Balakhonova ◽  
Viktoriya Sergeevna Tyukova ◽  
Stanislav Anatolievich Kedik

The paper presents the results of a study of the stability of aqueous solutions of inclusion complexes of hydroxypropyl-β-cyclodextrin with diisopropylphenol in various systems by the Higuchi-Connors phase solubility method. The phase solubility profiles for each system corresponding to the AN type are determined graphically, and the stability constants of the resulting inclusion complexes are calculated. An aqueous solution containing 0.2 % Tween 80 and 0.2 % mannitol was selected as the optimal condition for obtaining the hydroxypropyl-β-cyclodextrin inclusion complex with diisopropylphenol.


1970 ◽  
Vol 6 (1) ◽  
pp. 25-36 ◽  
Author(s):  
RP Patel ◽  
MM Patel

Several attempts have been made to improve the solubility of water insoluble drugs. Over the years, inclusion complexation of drugs with ?-cyclodextrin has emerged as a viable attempt to improve the dissolution of water insoluble drugs. The aim of the present work was to improve the dissolution rate of lovastatin, a water insoluble drug, by inclusion complexation with ?-cyclodextrin. The stoichiometric ratio determined by phase solubility analysis for inclusion complexation of lovastatin with ?-cyclodextrin was 1:1. The solubility of lovastatin increased with increasing amount of ?-cyclodextrin in water. Gibbs free energy (?Gtr°) values were all negative, indicating the spontaneous nature of lovastatin solubilization. Complexes of lovastatin were prepared with ?-cyclodextrin by various methods such as kneading, coevaporation and physical mixing. The complexes were characterized by Fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD) patterns. These studies indicated the inclusion of lovastatin in the cavity of ?-cyclodextrin. The complexation resulted in a marked improvement in the solubility of lovastatin. The complex prepared by kneading method showed fastest and highest in vitro dissolution rate compared to the tablets of pure of lovastatin. Physical mixture of ?-cyclodextrin/lovastatin also showed significant improvement in the dissolution rate compared to pure lovastatin. Mean dissolution time (MDT) of lovastatin decreased significantly after preparation of complexes and physical mixture of lovastatin with ?-cyclodextrin. Similarity factor (f2) indicated significant difference between the release profiles of lovastatin from complexes and from pure lovastatin. Key words: Lovastatin, ?-cyclodextrin, inclusion complexation, in vitro dissolution studies. Dhaka Univ. J. Pharm. Sci. 6(1): 25-36, 2007 (June) The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website


2013 ◽  
Vol 579 (1) ◽  
pp. 22-29 ◽  
Author(s):  
Shigeaki Abe ◽  
Takashi Hirota ◽  
Takayuki Kiba ◽  
Naoyuki Miyakawa ◽  
Fumio Watari ◽  
...  

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