Pharmaceutical Composition of Hydrochlorothiazide:β-Cyclo-dextrin: Preparation by Three Different Methods, Physico-Chemical Characterization and In Vivo Diuretic Activity Evaluation

Pires, Maria Arlete Silva; Santos, Robson A.S.; Sinisterra, Rubén D.

doi:10.3390/molecules16064482

Cited by 42 publications

(16 citation statements)

References 33 publications

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“…Some of these studies also found that the physicochemical properties depended on the method used for complex formation [20]. In further experiments, it would be interesting to investigate whether different complex morphologies lead to different bioavailabilities in vivo .…”

Section: Resultsmentioning

confidence: 99%

Analysis of the Enhanced Stability of R(+)-Alpha Lipoic Acid by the Complex Formation with Cyclodextrins

Ikuta

Sugiyama

Shimosegawa³

et al. 2013

IJMS

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R(+)-alpha lipoic acid (RALA) is one of the cofactors for mitochondrial enzymes and, therefore, plays a central role in energy metabolism. RALA is unstable when exposed to low pH or heat, and therefore, it is difficult to use enantiopure RALA as a pharma- and nutra-ceutical. In this study, we have aimed to stabilize RALA through complex formation with cyclodextrins (CDs). α-CD, β-CD and γ-CD were used for the formation of these RALA-CD complexes. We confirmed the complex formation using differential scanning calorimetry and showed by using HPLC analysis that complexed RALA is more stable than free RALA when subjected to humidity and high temperature or acidic pH conditions. Scanning electron microscopy studies showed that the particle size and shape differed depending on the cyclodextrin used for complexation. Further, the complexes of CD and RALA showed a different particle size distribution pattern compared with that of CD itself or that of the physical mixture of RALA and CD.

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Section: Resultsmentioning

confidence: 99%

Analysis of the Enhanced Stability of R(+)-Alpha Lipoic Acid by the Complex Formation with Cyclodextrins

Ikuta

Sugiyama

Shimosegawa³

et al. 2013

IJMS

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“…CDs are widely used to enhance the aqueous solubility of drugs [12–14] since the physicochemical properties of the guests (solubility, stability, bioavailability, antimicrobial activity, etc .) are altered upon complexation.…”

Section: Introductionmentioning

confidence: 99%

β-Cyclodextrin Inclusion Complex to Improve Physicochemical Properties of Pipemidic Acid: Characterization and Bioactivity Evaluation

Iacovino

Rapuano

Caso

et al. 2013

IJMS

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The aptitude of cyclodextrins (CDs) to form host-guest complexes has prompted an increase in the development of new drug formulations. In this study, the inclusion complexes of pipemidic acid (HPPA), a therapeutic agent for urinary tract infections, with native β-CD were prepared in solid state by kneading method and confirmed by FT-IR and 1H NMR. The inclusion complex formation was also characterized in aqueous solution at different pH via UV-Vis titration and phase solubility studies obtaining the stability constant. The 1:1 stoichiometry was established by a Job plot and the inclusion mechanism was clarified using docking experiments. Finally, the antibacterial activity of HPPA and its inclusion complex was tested on P. aeruginosa, E. coli and S. aureus to determine the respective EC50s and EC90s. The results showed that the antibacterial activity of HPPA:β-CD against E. coli and S. aureus is higher than that of HPPA. Furthermore, HPPA and HPPA:β-CD, tested on human hepatoblastoma HepG2 and MCF-7 cell lines by MTT assay, exhibited, for the first time, antitumor activities, and the complex revealed a higher activity than that of HPPA. The use of β-CD allows an increase in the aqueous solubility of the drug, its bioavailability and then its bioactivity.

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“…The ternary inclusion complex containing HPMC kneaded complex showed 97.99% drug release within 10 minutes. The enhancement of dissolution was due to formation of inclusion in solid state with reduction in crystallinity of HCT as confirmed by FTIR studies, leading to increased hydrophilicity higher effect and increase contact between drug and carrier [5,6,12].…”

Section: Dissolution Studiesmentioning

confidence: 99%

“…Host:guest interaction of HCT, βCD, and HPMC observed in spectra. It showed disappearance of OH deformation band of water molecule of CD cavity [5,6].…”

Section: Ftir Spectroscopymentioning

confidence: 99%

Spectroscopic Investigation for Photo stability of Hydrochlorothiazide Complexes with β-Cyclodextrin and HPMC.

Dhekale¹

2017

Asian J Pharm Clin Res

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Hydrochlorothiazide (HCT) is a poorly water-soluble drug. The aim of this study was to determine whether inclusion complexes between β-cyclodextrin and HCT are formed and also studied effect of auxiliary substance (HPMC) on HCT, photo-stability of HCT and to characterize these. Equimolar HCT/ βCD solid systems in the presence or absence of 0.2% (w/v) of HPMC were prepared by kneading method. The systems were characterized by phase solubility, Dissolution study, FTIR, DSC and the photo-stability test followed by u.v. spectroscopy. The results suggest that true binary and ternary inclusion complex. The test results have proved that the complexed HCT with hydroxypropyl β- cyclodextrin enhance the photo degradation rate and resolute the optimal molar ratio HCT to hydroxypropyl β- cyclodextrin as 1:1.

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Pharmaceutical Composition of Hydrochlorothiazide:β-Cyclo-dextrin: Preparation by Three Different Methods, Physico-Chemical Characterization and In Vivo Diuretic Activity Evaluation

Cited by 42 publications

References 33 publications

Analysis of the Enhanced Stability of R(+)-Alpha Lipoic Acid by the Complex Formation with Cyclodextrins

Analysis of the Enhanced Stability of R(+)-Alpha Lipoic Acid by the Complex Formation with Cyclodextrins

β-Cyclodextrin Inclusion Complex to Improve Physicochemical Properties of Pipemidic Acid: Characterization and Bioactivity Evaluation

Spectroscopic Investigation for Photo stability of Hydrochlorothiazide Complexes with β-Cyclodextrin and HPMC.

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