Inclusion complexes of hydrochlorothiazide and β-cyclodextrin: Physicochemical characteristics, in vitro and in vivo studies

Mendes, Cassiana; Buttchevitz, Aline; Kruger, Jéssica Henriques; Kratz, Jadel M.; Simões, Cláudia Maria Oliveira; Benedet, Patricia de Oliveira; Oliveira, Paulo Renato de; Silva, Marcos Antônio Segatto

doi:10.1016/j.ejps.2015.12.015

Cited by 30 publications

(14 citation statements)

References 25 publications

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“…Figure depicted the thermograms of the BCL, β‐CD, the physical mixture and the inclusion complex β‐CD/BCL. Natural β‐CD (Figure a) exhibited a broad endothermic peak at about 87 °C, corresponding to water removal from the β‐CD cavity . In addition, β‐CD revealed a peak of glass transition temperature at 218 °C.…”

Section: Resultsmentioning

confidence: 99%

“…In addition, the peaks of phenolic –OH group of BCL at 3491 and 3552 cm −1 were completely diminished in the inclusion complex, which suggests that there may be a formation of intermolecular hydrogen bond between the phenolic ‐OH group of BCL and the ‐OH group of β‐CD. Such changes were distinctive signatures of the inclusion of the BCL molecule in the hydrophobic cavity of β‐CD as well as the hydrogen bonds formation between BCL and β‐CD …”

Section: Resultsmentioning

confidence: 99%

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The formation of a host-guest inclusion complex system between β-cyclodextrin and baicalin and its dissolution characteristics

Jiang

Deng

et al. 2017

Journal of Pharmacy and Pharmacology

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

The formation of a host-guest inclusion complex system between β-cyclodextrin and baicalin and its dissolution characteristics

Jiang

Deng

et al. 2017

Journal of Pharmacy and Pharmacology

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“…According to the results of the above phase solubility studies, DMbCD was found to be the optimal complexing excipient for solubilizing simvastatin among all the investigated CDs. Thus, the drug complex with DMbCD at a 1:1 stoichiometric ratio was prepared by the co-evaporation method (22). Accurately weighed simvastatin was dissolved in a minimum volume of acetone, while DMbCD was dissolved in a suitable volume of water.…”

Section: Preparation Of Simvastatin/dmbcd Complexmentioning

confidence: 99%

Preparation and characterization of simvastatin/DMβCD complex and its pharmacokinetics in rats

Ning

Fan

et al. 2018

Acta Pharmaceutica

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Simvastatin is poorly bioavailable because it is practically insoluble in water and shows dissolution rate-limited absorption. Solubilizing effects of several β-cyclodextrin (βCD) derivatives such as HPβCD, SBEβCD and DMβCD on simvastatin in aqueous solution were investigated using the phase solubility technique. The solubility diagram of simvastatin with each βCD derivative could be classified as AL-type, indicating soluble complex formation of 1:1 stoichiometry. Among the above βCD derivatives DMβCD was found to be the ideal complexing agent for improving drug solubility. The simvastatin complex with DMβCD was prepared using the co-evaporation method and was then characterized by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR) and in vitro dissolution. Dissolution and pharmacokinetic studies indicated that the simvastatin/DMβCD complex exhibited an increased dissolution rate, rapid absorption, and improved bioavailability in rats compared to free drug. Maximum plasma concentration (cmax) and the time to reach it (tmax) were 21.86 μg mL-1 and 1.4 h for the drug complex, 8.25 μg mL-1 and 3.0 h for free drug, respectively. Main pharmacokinetic parameters such as tmax, cmax were significantly different (p < 0.01) between the simvastatin complex and free drug. Bioavailability of the simvastatin complex relative to free drug was up to 167.0 %.

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“…Despite the potential medical benefits of ABAM, its low aqueous solubility limits its use as a drug. Thus, strategies such as salt formation [ 11 ], particle size reduction [ 12 , 13 , 14 ], formation of solid dispersion [ 15 ] and complexation with cyclodextrins [ 16 ] have been used to enhance the solubility of ABAM and increase its dissolution rate.…”

Section: Introductionmentioning

confidence: 99%

Development, Physicochemical Characterization and In Vitro Anti-Inflammatory Activity of Solid Dispersions of α,β Amyrin Isolated from Protium Oilresin

et al. 2017

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α,β Amyrin (ABAM) is a natural mixture of pentacyclic triterpenes that has shown a variety of pharmacological properties, including anti-inflammatory effect. ABAM is isolated from Burseraceae oilresins, especially from the Protium species, which is commonly found in the Brazilian Amazon. This work aimed to develop solid dispersions (SD) of ABAM with the following hydrophilic polymers: polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG-6000) and hydroxypropylmethylcellulose (HPMC). The SDs were prepared by physical mixture (PM), kneading (KND) and rotary evaporation (RE) methods. In order to verify any interaction between ABAM and the hydrophilic polymers, physicochemical characterization was performed by Fourier transform infrared (FTIR), scanning electron microscopy (SEM), powder X-ray diffraction (XRD), thermogravimetry (TG) and differential scanning calorimetry (DSC) analysis. Furthermore, an in vitro anti-inflammatory assay was performed with ABAM alone and as SDs with the hydrophilic polymers. The results from the characterization analysis show that the SDs were able to induce changes in the physicochemical properties of ABAM, which suggests interaction with the polymer matrix. In vitro anti-inflammatory assay showed that the SDs improved the anti-inflammatory activity of ABAM and showed no cytotoxicity. In conclusion, this study showed the potential use of SDs as an efficient tool for improving the stability and anti-inflammatory activity of ABAM without cytotoxicity.

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Inclusion complexes of hydrochlorothiazide and β-cyclodextrin: Physicochemical characteristics, in vitro and in vivo studies

Cited by 30 publications

References 25 publications

The formation of a host-guest inclusion complex system between β-cyclodextrin and baicalin and its dissolution characteristics

The formation of a host-guest inclusion complex system between β-cyclodextrin and baicalin and its dissolution characteristics

Preparation and characterization of simvastatin/DMβCD complex and its pharmacokinetics in rats

Development, Physicochemical Characterization and In Vitro Anti-Inflammatory Activity of Solid Dispersions of α,β Amyrin Isolated from Protium Oilresin

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