Phase Solubility Studies of Poorly Soluble Drug Molecules by Using O-Phosphorylated Calixarenes as Drug-Solubilizing Agents

2011 ◽  
Vol 57 (1) ◽  
pp. 233-239 ◽  
Author(s):  
Mevlüt Bayrakcı ◽  
Şeref Ertul ◽  
Mustafa Yilmaz
Keyword(s):  
Phase Solubility ◽  
Drug Molecules ◽  
Phase Solubility Studies ◽  
Poorly Soluble ◽  
Solubility Studies ◽  
Poorly Soluble Drug

PHASE SOLUBILITY STUDIES OF ONDANSETRON -2- HYDROXYPROPYL BETACYCLODEXTRIN FOR DEVELOPMENT OF ONDANSETRON ORODISPERSIBLE FILMS

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (08) ◽  
pp. 53-56
Author(s):  
H Kanekar ◽  
◽  
A. Khale ◽  
S Maurya ◽  
B. Dey
Keyword(s):  
Inclusion Complex ◽  
Research Work ◽  
Microscopy Study ◽  
Electron Microscopy Study ◽  
Phase Solubility ◽  
Orodispersible Films ◽  
Phase Solubility Studies ◽  
Poorly Soluble ◽  
Solubility Studies ◽  
Apparent Stability

The present research work was aimed to formulate transparent mouth dissolving films of ondansetron. Ondansetron is poorly soluble in aqueous solvents (less than 5 mg/mL) and thus improvisation in solubility was crucial. The phase solubility studies were carried in order to study the formation of inclusion complex with Hydroxy Propyl Beta cyclodextrin. The phase solubility diagrams revealed the formation of stable inclusion complex and apparent stability constants were evaluated. The calculated apparent stability constant, Kc was found to be 288.5 mol-1. The shape of solubility graph indicated that there is probability of the formation of 1:1complex with respect to HP-b-CD concentration (Slope of less than 1). The Scanning Electron Microscopy study of plain ondansetron and ondansetron orodispersible film revealed the formation of stable inclusion complex, which renders the complete solubilisation of ondansetron, yielding the formation of transparent mouth dissolving films.

Studies on the Preparation, Characterization and Solubility of -Cyclodextrin-Roxythromycin Inclusion Complexes

2009 ◽  
Vol 2 (2) ◽  
pp. 523-530
Author(s):  
D. Nagasamy Venkatesh ◽  
S. Karthick ◽  
M. Umesh ◽  
G. Vivek ◽  
R.M. Valliappan ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Phase Solubility ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Ir Studies ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

Roxythromycin/ β-cyclodextrin (Roxy/ β-CD) dispersions were prepared with a view to study the influence of β-CD on the solubility and dissolution rate of this poorly soluble drug. Phase-solubility profile indicated that the solubility of roxythromycin was significantly increased in the presence of β-cyclodextrin and was classified as AL-type, indicating the 1:1 stoichiometric inclusion complexes. Physical characterization of the prepared systems was carried out by differential scanning calorimetry (DSC), X-ray diffraction studies (XRD) and IR studies. Solid state characterization of the drug β-CD binary system using XRD, FTIR and DSC revealed distinct loss of drug crystallinity in the formulation, ostensibly accounting for enhancement of dissolution rate.

scholarly journals Co-solvation effect on the binding mode of the α-mangostin/β-cyclodextrin inclusion complex

2015 ◽  
Vol 11 ◽  
pp. 2306-2317 ◽  
Author(s):  
Chompoonut Rungnim ◽  
Sarunya Phunpee ◽  
Manaschai Kunaseth ◽  
Supawadee Namuangruk ◽  
Kanin Rungsardthong ◽  
...  
Keyword(s):  
Complex Formation ◽  
Inclusion Complex ◽  
Binding Mode ◽  
Phase Solubility ◽  
Binary Complex ◽  
Experimental Phase ◽  
Drug Molecules ◽  
Poorly Soluble ◽  
Experimental And Theoretical Studies ◽  
Solvent Complex

Cyclodextrins (CDs) have been extensively utilized as host molecules to enhance the solubility, stability and bioavailability of hydrophobic drug molecules through the formation of inclusion complexes. It was previously reported that the use of co-solvents in such studies may result in ternary (host:guest:co-solvent) complex formation. The objective of this work was to investigate the effect of ethanol as a co-solvent on the inclusion complex formation between α-mangostin (α-MGS) and β-CD, using both experimental and theoretical studies. Experimental phase-solubility studies were carried out in order to assess complex formation, with the mechanism of association being probed using a mathematical model. It was found that α-MGS was poorly soluble at low ethanol concentrations (0–10% v/v), but higher concentrations (10–40% v/v) resulted in better α-MGS solubility at all β-CD concentrations studied (0–10 mM). From the equilibrium constant calculation, the inclusion complex is still a binary complex (1:1), even in the presence of ethanol. The results from our theoretical study confirm that the binding mode is binary complex and the presence of ethanol as co-solvent enhances the solubility of α-MGS with some effects on the binding affinity with β-CD, depending on the concentration employed.

scholarly journals Characterization and Antiproliferative Activity of a Novel 2-Aminothiophene Derivative-β-Cyclodextrin Binary System

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3130 ◽  
Author(s):  
Elayne Ferreira ◽  
Walter da Silva Júnior ◽  
Jonas de Oliveira Pinheiro ◽  
Aldilane da Fonseca ◽  
Telma Moura Lemos ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Binary Systems ◽  
Human Cancer ◽  
Aqueous Solubility ◽  
Phase Solubility ◽  
Human Cancer Cell Lines ◽  
Rotary Evaporation ◽  
Phase Solubility Studies ◽  
Physical Mixing ◽  
Solubility Studies

The novel 2-aminothiophene derivative 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile (6CN) has shown potential anti-proliferative activity in human cancer cell lines. However, the poor aqueous solubility of 6CN impairs its clinical use. This work aimed to develop binary 6CN-β-cyclodextrin (βCD) systems with the purpose of increasing 6CN solubility in water and therefore, to improve its pharmacological activity. The 6CN-βCD binary systems were prepared by physical mixing, kneading and rotary evaporation methods and further characterized by FTIR, XRD, DSC, TG and SEM. In addition, molecular modeling and phase solubility studies were performed. Finally, MTT assays were performed to investigate the cytostatic and anti-proliferative effects of 6CN-βCD binary systems. The characterization results show evident changes in the physicochemical properties of 6CN after the formation of the binary systems with βCD. In addition, 6CN was associated with βCD in aqueous solution and the solid state, which was confirmed by molecular modeling and the aforementioned characterization techniques. Phase solubility studies indicated that βCD forms stable 1:1 complexes with 6CN. The MTT assay demonstrated the cytostatic and anti-proliferative activities of 6CN-βCD binary systems and therefore, these might be considered as promising candidates for new anticancer drugs.

scholarly journals Preparation and Cyclodextrin Solubilization of the Antibacterial Agent Benzoyl Metronidazole

2013 ◽  
Vol 2013 ◽  
pp. 1-3 ◽  
Author(s):  
Qing Huang ◽  
Benpeng Li ◽  
Shuo Yang ◽  
Peipei Ma ◽  
Zhizhong Wang
Keyword(s):  
Oral Bioavailability ◽  
Antibacterial Agent ◽  
Association Constant ◽  
Phase Solubility ◽  
Cyclodextrin Complexes ◽  
One Pot ◽  
Solubility Method ◽  
Phase Solubility Studies ◽  
Coupling Reagent ◽  
Solubility Studies

A one-pot method for the preparation of benzoyl metronidazole was achieved by usingN,N′-carbonyldiimidazole as a coupling reagent. Moreover, it was found that the byproduct imidazole as the catalyst promoted the reaction. In addition, theβ-cyclodextrin solubilization of benzoyl metronidazole was investigated by phase-solubility method. The phase-solubility studies indicated that the solubility of benzoyl metronidazole (S=0.1435 g/L) was substantially increased 9.7-fold (S′=1.3881 g/L) by formation of 1 : 1 benzoyl metronidazole/β-cyclodextrin complexes in water, and the association constantKavalue was determined to be 251 (±23) dm3/mol. Therefore,β-cyclodextrin can work as a pharmaceutical solubilizer for benzoyl metronidazole and may improve its oral bioavailability.

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