Solubility behavior and biopharmaceutical classification of novel high-solubility ciprofloxacin and norfloxacin pharmaceutical derivatives

Breda, S.; Jiménez-Kairuz, Álvaro F.; Manzo, Rubén H.; Olivera, Marı́a Eugenia

doi:10.1016/j.ijpharm.2008.12.026

Cited by 121 publications

(85 citation statements)

References 41 publications

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“…According to González-Esquivel et al (2005), the apparent permeability coefficient of PZQ is 4.4 x 10 -5 cm/s. For this reason, PZQ has been classified as a Class II drug in the Biopharmaceutics Classification System (BCS) (Passerini et al, 2006;Breda et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterisation of Dextran-70 hydrogel for controlled release of praziquantel

Campos

Cassimiro

Crespi

et al. 2013

Braz. J. Pharm. Sci.

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A hydrogel was developed from 70 kDa dextran (DEX-70) and praziquantel (PZQ) incorporated as a model drug. Biopharmaceutical properties, such as solubility and dissolution rate, were analysed in the design of the hydrogel. Furthermore, the hydrogel was also characterized by IR spectroscopy and DSC. Tests of the swelling rate showed that the hydrogel swelled slowly, albeit faster than the rate for the free polymer. In dissolution tests, the hydrogel released the drug slowly and continuously. This slow release was similar to that observed in the swelling tests and resulted in controlled release of the drug. Thus, this dextran is a suitable polymer for the development of hydrogels as vehicles for the controlled release of drugs.Uniterms: Hydrogel/development. Hydrogel/biopharmaceutical properties. Dextran/hydrogel development. Praziquantel/controlled release. Hydrogel/swelling test.Um hidrogel foi desenvolvido a partir de dextrano 70 kDa (DEX-70) e praziquantel incorporado (PZQ) como fármaco modelo. Propriedades biofarmacêuticas, como solubilidade e velocidade de dissolução, foram analisadas no desenvolvimento do hidrogel. Além disso, o hidrogel também foi caracterizado por espectroscopia na região do infravermelho e calorimetria diferencial exploratória (DSC). Testes da taxa de intumescimento mostraram que o hidrogel intumesce lentamente, embora tenha sido mais rápido do que a taxa do polímero livre. Nos testes de dissolução, o hidrogel liberou o fármaco lenta e continuamente. Esta liberação lenta foi semelhante a observada nos testes de intumescimento e resultou em uma liberação controlada do fármaco. Assim, o dextrano 70 kDa é um polímero adequado para o desenvolvimento de hidrogéis como veículos para a liberação controlada de fármacos.Unitermos: Hidrogel/desenvolvimento. Hidrogel/propriedades biofarmacêuticas. Dextrano/ desenvolvimento de hidrogel. Praziquantel/liberação controlada. Hidrogel/teste de intumescimento.

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Section: Introductionmentioning

confidence: 99%

Preparation and characterisation of Dextran-70 hydrogel for controlled release of praziquantel

Campos

Cassimiro

Crespi

et al. 2013

Braz. J. Pharm. Sci.

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“…In vitro drug release study from nanofiber mats We deduced that although aqueous 50% acetic acid can provide a homogenous solution of PVAc and CipHCl, the incompatibility between hydrophobic PVAc and hydrophilic CipHCl 45 would increase the migration of the drug molecules toward the nanofibers surface during the rapid elongation and quick solvent evaporation during electrospinning. These superficial drug molecules can easily diffuse into the aqueous medium and cause an initial quick burst release.…”

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confidence: 99%

Composite poly(vinyl alcohol)/poly(vinyl acetate) electrospun nanofibrous mats as a novel wound dressing matrix for controlled release of drugs

Jannesari¹,

Varshosaz²,

Morshed³

et al. 2011

IJN

141

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The aim of this study was to develop novel biomedicated nanofiber electrospun mats for controlled drug release, especially drug release directly to an injury site to accelerate wound healing. Nanofibers of poly(vinyl alcohol) (PVA), poly(vinyl acetate) (PVAc), and a 50:50 composite blend, loaded with ciprofloxacin HCl (CipHCl), were successfully prepared by an electrospinning technique for the first time. The morphology and average diameter of the electrospun nanofibers were investigated by scanning electron microscopy. X-ray diffraction studies indicated an amorphous distribution of the drug inside the nanofiber blend. Introducing the drug into polymeric solutions significantly decreased solution viscosities as well as nanofiber diameter. In vitro drug release evaluations showed that both the kind of polymer and the amount of drug loaded greatly affected the degree of swelling, weight loss, and initial burst and rate of drug release. Blending PVA and PVAc exhibited a useful and convenient method for electrospinning in order to control the rate and period of drug release in wound healing applications. Also, the thickness of the blend nanofiber mats strongly influenced the initial release and rate of drug release.

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“…Stock standard solution of 1000 μg mL −1 NF was prepared by dissolving an appropriate amount in 1.0 mL of 1.0 mol L −1 HCl [36] and then diluted with water. Stock standard solution of 1000 μg mL −1 CF was prepared by dissolving an appropriate amount directly in water.…”

Section: Preparation Of Reagents and Samplesmentioning

confidence: 99%

Facile assay method for norfloxacin and ciprofloxacin by sequential injection chromatography

Elgorashe

Idris

Abdelrahman

et al. 2014

Acta Chromatographica

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Summary. Sequential injection chromatography (SIC) is a simple, inexpensive, portable, reagent-saving, and environmentally benign separation technique. This paper reports the development of a facile assay method for norfloxacin (NF) and ciprofloxacin (CF) in their formulations (tablets and eye drops) using SIC. The analytes were rapidly chromatographed on a short C18 monolithic column (4.6 × 50 mm) at a flow rate of 30 μL s −1 . An isocratic mode was adopted. The optimum mobile phase composition was 90% water, 10% acetonitrile, and 0.3% triethylamine at pH 3.0. Miniaturized fiber optic spectrometric devices were coupled to the SIC system for UV detection at 280 nm. Sufficient separation with a resolution of 1.6 and numbers of theoretical plates of more than 1500 was achieved. Additionally, acceptable peak shapes with peak symmetries of 0.89 and 0.92 for NF and CF, respectively, were obtained. The method was validated and found to be reliable (the recovery was 98.0-100.6%) and precise (the RSDs of intra-/inter-day precision were less than 2.0%). The method is also sensitive. The limits of detection were less than 0.27 μg mL −1 . The provided method could be considered an industrial scale since the sample frequency was seven samples h −1 and the total volume of consumed reagents was 11.5 mL.

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Solubility behavior and biopharmaceutical classification of novel high-solubility ciprofloxacin and norfloxacin pharmaceutical derivatives

Cited by 121 publications

References 41 publications

Preparation and characterisation of Dextran-70 hydrogel for controlled release of praziquantel

Preparation and characterisation of Dextran-70 hydrogel for controlled release of praziquantel

Composite poly(vinyl alcohol)/poly(vinyl acetate) electrospun nanofibrous mats as a novel wound dressing matrix for controlled release of drugs

Facile assay method for norfloxacin and ciprofloxacin by sequential injection chromatography

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