scholarly journals Inclusion Complex of Fexofenadine Hydrochloride with Cyclodextrins

2021 ◽  
Vol 11 (3) ◽  
pp. 282
Author(s):  
Melita Huremovic ◽  
Majda Srabovic ◽  
Mirsada Salihovic ◽  
Ekrem Pehlic
Keyword(s):  
Bathochromic Shift ◽  
Aqueous Solubility ◽  
Taste Masking ◽  
Solid Inclusion ◽  
Phase Solubility ◽  
Covalent Bonds ◽  
Molar Ratios ◽  
Solubility Study ◽  
Phase Solubility Study ◽  
Vis Spectroscopy

<p>Fexofenadine hydrochloride (FFN), (±)-4-[1-hydroxy-4[4-(hydroxydiphenylmethyl)-1-piperidinyl]-butyl] α,α-dimethylbenzeneacetic acid hydrochloride, is a second-generation antihistamine that is used to treat allergies. The drug is highly hydrophobic and slightly soluble in water. Cyclodextrins are widely used to improve the physicochemical and pharmaceutical properties such as solubility, stability, and bioavailability of poorly soluble drug molecules.Cyclodextrins can molecularly encapsulate various drugs into their hydrophobic cavity without forming any covalent bonds. Cyclodextrin (CDs), especially ß-Cyclodextrin (ß-CD), are widely used in the pharmaceutical field due to its ability to stabilize drug molecules and taste masking purposes.<strong> </strong></p><p>The phase solubility study was performed according to the method of Higuchi and Connors by adding the fexofenadine hydrochloride in excess to different concentrations of cyclodextrin solutions. Phase solubility study records show that the stability constant and complex stoichiometry of FFN-CD complexes increases linearly with CD concentration. Also, an increase in the concentration of β-cyclodextrin leads to an increase in the aqueous solubility of FFN. Complexes were analyzed by UV-VIS spectroscopy using the calibration curve of FFN. Also, UV-VIS spectra indicate a bathochromic shift which proves that complex formation has occurred.</p><p>Solid inclusion complexes of fexofenadine/β-cyclodextrin and its derivatives were prepared at the molar ratios of 1:1 by the physical mixing method. Characterization of the complexes was performed by using infrared spectroscopy. </p>

scholarly journals Dissolution Enhancement of Flurbiprofen by Solid Dispersion Adsorbate Technique

2021 ◽  
Vol 69 (2) ◽  
Author(s):  
Sohansinh S. Vaghela ◽  
Samkit M. Shah ◽  
Sanjesh G. Rathi ◽  
Shrenik K. Shah
Keyword(s):  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Dissolution Enhancement ◽  
Phase Solubility ◽  
Fusion Method ◽  
Poloxamer 188 ◽  
X Ray ◽  
Solubility Study ◽  
Phase Solubility Study

Flurbiprofen solid dispersion Adsorbate (SDA) has been prepared using PEG 4000 and Poloxamer 188 as carrier and Neusilin as adsorbent material. The SDA of Flurbiprofen was prepared by using Fusion method in various drugs to carrier ratios. The phase solubility study concludes that both polymers have ability to improve the aqueous solubility of flurbiprofen. Pure API Flurbiprofen and final formulation samples of SDA are characterized by FTIR, DSC and X-ray diffraction spectroscopy. X-ray powder diffraction and DSC study indicated that the drug was present in amorphous form. FTIR study revealed that the characteristic peaks in spectra of pure Flurbiprofen are also present in spectra of SDA’s. Drug found compatible with the excipients. The highest improvement in solubility and in-vitro drug release were observed in solid dispersion prepared with Poloxamer 188 (F14) by fusion method. The increased dissolution rate of drug from solid dispersion adsorbates may be due to surface tension lowering effect of polymer to the medium and increased wettability and dispersibility of drug. Hence, F14 Solid dispersion adsorbates with the Poloxamer carrier in 1:2 ratio considered as most satisfactory among all solid dispersion adsorbates.

scholarly journals Solubility Enhancement of Myricetin by Inclusion Complexation with Heptakis-O-(2-Hydroxypropyl)-β-Cyclodextrin: A Joint Experimental and Theoretical Study

2020 ◽  
Vol 21 (3) ◽  
pp. 766 ◽  
Author(s):  
Dongxu Han ◽  
Zhongbao Han ◽  
Liyan Liu ◽  
Ying Wang ◽  
Shigang Xin ◽  
...  
Keyword(s):  
Inclusion Complexation ◽  
Aqueous Solubility ◽  
Solubility Enhancement ◽  
Dynamics Simulation ◽  
Structural Deformation ◽  
Phase Solubility ◽  
Position Change ◽  
Oh Groups ◽  
Solubility Study ◽  
Phase Solubility Study

Four cyclodextrins (CD) including β-cyclodextrin (β-CD), γ-cyclodextrin (γ-CD), heptakis-O-(2-hydroxypropyl)-β-cyclodextrin (HP-β-CD), and heptakis-O-(2, 6-di-O-methyl)-β-cyclodextrin (DM-β-CD) were used as solubilizer to study the solubility enhancement of myricetin. The results of the phase solubility study showed that the presence of CDs could enhance the solubility of myricetin by forming 1:1 complexes. Among all CDs, HP-β-CD had the highest solubilization effect to myricetin. The concentration of myricetin could be 1.60 × 10−4 moL/L when the presence of HP-β-CD reached 1.00 × 10−2 moL/L, which was 31.45 times higher than myricetin’s aqueous solubility. Subsequently, the HP-β-CD:myricetin complex was characterized by Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), and thermogravimetric analysis (TGA). In order to get an insight of the plausible structure of the complex, molecular docking was used to study the complexation process of HP-β-CD and myricetin. In the complex, the A ring and C ring of myricetin were complexed into the hydrophobic cavity of HP-β-CD, while the ring B was located at the wide rim of HP-β-CD. Four hydrogen bonding interactions were found between HP-β-CD and -OH groups of the guest in the HP-β-CD: myricetin complex. The complexation energy (△E) for the host-guest interactions was calculated with a negative sign, indicating the formation of the complex was an exergonic process. A 30-ns molecular dynamics simulation was conducted to the HP-β-CD: myricetin complex. Calculation results showed that no large structural deformation or position change were observed during the whole simulation time span. The average root-mean-square deviation (RMSD) changes of the host and guest were 2.444 and 1.145 Å, respectively, indicating the complex had excellent stability.

scholarly journals The Preservation and Enantiomeric Selection of Linalool by Nanoencapsulation Using Cyclodextrins

2021 ◽  
Vol 89 (3) ◽  
pp. 42
Author(s):  
Tanaporn Poonphatanapricha ◽  
Sasimas Katanyutanon ◽  
Kulpavee Jitapunkul ◽  
Luckhana Lawtrakul ◽  
Pisanu Toochinda
Keyword(s):  
Inclusion Complexes ◽  
Computational Simulation ◽  
Aqueous Solubility ◽  
Free Form ◽  
Study Phase ◽  
Phase Solubility ◽  
Solubility Study ◽  
Beta Cyclodextrin ◽  
Phase Solubility Study ◽  
Enantiomeric Selectivity

Linalool, a volatile terpene alcohol, is responsible for a characteristic aroma in food, beverages, and cosmetics. However, linalool’s low aqueous solubility and high volatility limit the applications and shelf life of linalool-containing products. Nanoencapsulation using beta-cyclodextrin (BCD), methyl-beta-cyclodextrin (MBCD) and hydroxypropyl-beta-cyclodextrin (HPBCD) was studied to improve the aqueous solubility and stability of linalool. Linalool has two enantiomers with distinct flavors and odors which affect product quality. The enantiomeric selectivity of the cyclodextrins (CDs) toward racemic linalool standard was evaluated. A computational simulation was performed to predict the conformations and interactions of the inclusion complexes. The 1:1 host-guest ratio from the computer simulation was implemented in the experimental study. Phase solubility study shows an improvement in linalool aqueous solubility after being encapsulated by CDs. The encapsulation efficiencies of linalool/BCD, linalool/MBCD, and linalool/HPBCD inclusion complexes are 66.30%, 51.38% and 32.31%, respectively. Nanoencapsulation by CDs can preserve linalool in the form of inclusion complexes compared to its free form. The amount of remaining linalool in linalool/BCD, linalool/MBCD, and linalool/HPBCD inclusion complexes are 89.57%, 87.07%, and 74.86%, respectively which are considerably larger than that of pure linalool (42.30%). CDs also show the enantiomeric selectivity toward (R)-linalool as evident from (R)-linalool percentage of 54.53% in the inclusion complex.

scholarly journals Investigating the phase-solubility and compatibility study of anticancer drug complexed with β-cyclodextrin and HP–β-cyclodextrin

2018 ◽  
Vol 9 (3) ◽  
Author(s):  
Preeti Dhurve ◽  
Atul Tripathi ◽  
Bina Gidwani ◽  
Amber Vyas
Keyword(s):  
Aqueous Solubility ◽  
Phase Solubility ◽  
Compatibility Study ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Solubility Study ◽  
Kneading Method ◽  
Phase Solubility Study ◽  
Critical Problems ◽  
Ft Ir

Poor  aqueous  solubility  and  dissolution  rates  are  critical  problems  that  hinders  the  formulation, development  and  delivery  of  most  of  BCS  class  II  and  class  IV  drugs.  Gefitinib  is  a  cytotoxic chemotherapeutic  drug  used  in  treatment  of  cancer.    The  objective  of  the  present  study  was  to investigate  the  drug-cyclodextrin  compatibility  study  by  FTIR  and  DSC  study.  The  phase solubility  study  revealed  formation  of  1:1  stoichiometry  binary  inclusion  complex.  The  complex was  prepared  by  kneading  method.  FT-IR  spectra  provided  the  data  indicating  that  the  HP-β-CD was  more  effective  than  β-CD.  Differential  scanning  calorimetry  thermograms  indicated  stronger amorphization and entrapment of  gefitinib with HP-β-CD.

scholarly journals Characterization, in Vitro and in Vivo Evaluation of Naringenin-Hydroxypropyl-β-Cyclodextrin Inclusion for Pulmonary Delivery

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 554 ◽  
Author(s):  
Minyi Guan ◽  
Rui Shi ◽  
Yuying Zheng ◽  
Xuan Zeng ◽  
Weiyang Fan ◽  
...  
Keyword(s):  
Pulmonary Delivery ◽  
Pharmacokinetic Profile ◽  
Proton Nuclear Magnetic Resonance ◽  
Flavonoid Compound ◽  
Phase Solubility ◽  
Local Concentration ◽  
Nmr Studies ◽  
Solubility Study ◽  
Phase Solubility Study

Naringenin, a flavonoid compound which exists abundantly in Citrus fruits, is proven to possess excellent antitussive and expectorant effects. However, the clinical applications of naringenin are restricted by its poor solubility and low local concentration by oral administration. The aim of the present study is to prepare a naringenin-hydroxypropyl-β-cyclodextrin (naringenin-HPβCD) inclusion as an inhalation solution for pulmonary delivery. The naringenin-HPβCD inclusion was characterized by phase solubility study, XRD, differential scanning calorimetry (DSC), proton nuclear magnetic resonance (1HNMR), and two-dimensional rotating frame Overhauser effect spectroscopy (2D ROESY). The in vitro permeability of the inclusion was evaluated on Calu-3 cells and the pharmacokinetic profile of pulmonary delivery was investigated in Sprague-Dawley (SD) rats. Based on the linear model of phase solubility study, the relationship between naringenin and HPβCD was identified as AL type with a 1:1 stoichiometry. XRD, DSC, and NMR studies indicated that the entire naringenin molecule is encapsulated into the cavity of HPβCD. HPβCD could increase the concentration of naringenin in the epithelium-lining fluid (ELF) of Calu-3 cells and act as a sustained release system for naringenin. The pharmacokinetic profile of naringenin-HPβCD inclusion showed rapid response and higher local concentration by pulmonary delivery. In conclusion, pulmonary delivery of naringenin-HPβCD inclusion is a promising formulation strategy, which could provide a new possibility for the clinical application of naringenin.

Systematic Development of Bicalutamide Immediate Release Pellets using Aeroperl and Non-MCC Extruder aid

2020 ◽  
Vol 15 ◽  
Author(s):  
Hardik Rana ◽  
Hussain Hasan ◽  
Mukesh Gohel ◽  
Vaishali Thakkar ◽  
Tejal Gandhi
Keyword(s):  
Drug Release ◽  
Propylene Glycol ◽  
Microcrystalline Cellulose ◽  
Immediate Release ◽  
Phase Solubility ◽  
Disintegration Time ◽  
Solubility Study ◽  
Short Period ◽  
Phase Solubility Study ◽  
Pellet Formulation

Background: The Microcrystalline Cellulose is called as a gold standard for the manufacture of pellets. The poor disintegration leads to incomplete drug release restricts the use of MCC in the immediate-release formulation. Objective: The present work aims to explore non-MCC extruder aid for pellet formulation and solubility modulation potential of Aeroperl® 300 Pharma. Methods: Bicalutamide (BCL) was selected as a model BCS class-II drug. The solubility of BCL was assessed in different vehicles like polyethylene glycol, propylene glycol, and Tween by carrying out phase solubility study. The suitable vehicle was selected based on the higher solubility of BCL. The vehicle was further adsorbed on newer adsorbent Aeroperl® 300 Pharma to formulate liquisolid granules. The liquisolid granules were further incorporated into the pellet using mannitol and microcrystalline cellulose as an extruder aid. Box-Behnken design was adopted for optimization of formulation considering MCC: mannitol ratio, concentration of HPMC and spheronizer speed as independent factors whereas drug release at 30 min, disintegration time and aspect ratio were selected as dependent variables. The pellets were evaluated for different evaluation parameters. Results: Propylene glycol was selected for the formulation of liquisolid technique based on the results of the phase solubility study. Propylene glycol containing BCL was adsorbed on Aeroperl 300 Pharma. The optimized batch was selected exploring the Design-Expert software by considering limits of different responses. Pellet had excellent flowability. Friability was found to be within the range (<1%). Pellets were found to be spherical and had pores on the surfaces. Conclusion: Liquisolid granules containing newer solubilizer Aeroperl was found to be a promising approach for the improvement in the solubility of the drug. The use of mannitol with MCC has a profound effect on disintegration time, without altering flow property and other parameters. No patents were reported on the combination of Bicalutamide, mannitol and Aeroperl. The critical finding of the present work is to use mannitol as an extruder aid to fasten the disintegration leads to complete drug release within a short period of time. Aeroperl and Mannitol, MCC: mannitol ratio, concentration of HPMC and spheronizer speed was found to be significant and had the potential effect in pellet formulation.

A Phase Solubility Study on the Chiral Discrimination of Ibuprofen by β-Cyclodextrin Complexes

2011 ◽  
Vol 6 (2) ◽  
pp. 267-273 ◽  
Author(s):  
Vincenza Crupi ◽  
Graziano Guella ◽  
Domenico Majolino ◽  
Ines Mancini ◽  
Barbara Rossi ◽  
...  
Keyword(s):  
Chiral Discrimination ◽  
Phase Solubility ◽  
Cyclodextrin Complexes ◽  
Solubility Study ◽  
Phase Solubility Study

β-Cyclodextrin as water-solubility enhancer for butylated hydroxytoluene

2015 ◽  
Vol 69 (5) ◽  
Author(s):  
Marcin Lukasiewicz ◽  
Stanislaw Kowalski ◽  
Anna Ptaszek ◽  
Pawel Ptaszek
Keyword(s):  
Water Solubility ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Ternary Systems ◽  
Butylated Hydroxytoluene ◽  
Phase Solubility ◽  
Solubility Study ◽  
Phase Solubility Study ◽  
Endothermic Process

AbstractThe phenomenon of the increase in solubility of the non-polar phenolic antioxidant - butylated hydroxytoluene (BHT) - in aqueous solutions containing β-cyclodextrin (CD) was studied. The complexation of BHT by CD was investigated using a phase solubility study. This method makes it possible to calculate the apparent formation constant for the host-guest complex. In addition, the thermodynamic properties were evaluated, revealing a spontaneous endothermic process of complex formation. Two solubility models were also used to verify their applicability to predicting the BHT concentration in solution. Those models included the modified Apelblat and Buchowski-Ksiazczak equations. In order to investigate the antioxidant properties of the BHT/CD/water ternary systems, a radical scavenging activity using a DPPH stable radical was performed. The experiments indicated that the antioxidant activity is temperature- and CD concentration-dependent. It was shown that complexation may inhibit the radical scavenging by BHT or change the scavenging stoichiometry.

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