Comparative study of itraconazole-cyclodextrin inclusion complex and its commercial product

Alsarra, Ibrahim A.; Alanazi, Fars K.; Ahmed, Sayed M.; Bosela, Ahmed A.; Alhamed, Suliman S.; Mowafy, Hammam A.; Neau, Steven H.

doi:10.1007/s12272-010-0706-3

Cited by 14 publications

(6 citation statements)

References 43 publications

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“…Various techniques have been used to improve the solubility of poorly water-soluble drugs, including using surfactants, 5 inclusion complexation, 6 , 7 and solid dispersion (SD) techniques. 8 For example, the SD technique has been well used to enhance the dissolution rate of ITZ, 4 , 8 – 10 and one of the commercial products of ITZ (Sporanox ® ) is a hard capsule form containing ITZ coated on sugar spheres.…”

Section: Introductionmentioning

confidence: 99%

Itraconazole solid dispersion prepared by a supercritical fluid technique: preparation, in vitro characterization, and bioavailability in beagle dogs

Yin

Daintree²,

Ding³

et al. 2015

DDDT

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This research aimed to develop a supercritical fluid (SCF) technique for preparing a particulate form of itraconazole (ITZ) with good dissolution and bioavailability characteristics. The ITZ particulate solid dispersion was formulated with hydroxypropyl methylcellulose, Pluronic F-127, and L-ascorbic acid. Aggregated particles showed porous structure when examined by scanning electron microscopy. Powder X-ray diffraction and Fourier transform infrared spectra indicated an interaction between ITZ and excipients and showed that ITZ existed in an amorphous state in the composite solid dispersion particles. The solid dispersion obtained by the SCF process improved the dissolution of ITZ in media of pH 1.0, pH 4.5, and pH 6.8, compared with a commercial product (Sporanox®), which could be ascribed to the porous aggregated particle shape and amorphous solid state of ITZ. While the solid dispersion did not show a statistical improvement (P=0.50) in terms of oral bioavailability of ITZ compared with Sporanox®, the Cmax (the maximum plasma concentration of ITZ in a pharmacokinetic curve) of ITZ was raised significantly (P=0.03) after oral administration. Thus, the SCF process has been shown to be an efficient, single step process to form ITZ-containing solid dispersion particles with good dissolution and oral bioavailability characteristics.

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Section: Introductionmentioning

confidence: 99%

Itraconazole solid dispersion prepared by a supercritical fluid technique: preparation, in vitro characterization, and bioavailability in beagle dogs

Yin

Daintree²,

Ding³

et al. 2015

DDDT

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show abstract

“…The same results were detected in IBU 3 physical mixture and IBU 3 free drug compared to IBU 45 physical mixture and IBU 45 free drug. Furthermore, the two PMs showed faster dissolution rate than corresponding free drug of IBU3 and IBU 45, which was attributed to the wettability of β-CD and partly forming inclusion complex [32] ( fig. 8, Table 1).…”

Section: Resultsmentioning

confidence: 97%

Effect of Drug Particle Size on Complexation, Physicochemical Properties and Dissolution of Cyclodextrin Inclusion Complexes

Ai¹,

Ma²,

Li³

et al. 2017

ijps

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Ai, et al.: Effect of Drug Particle Size on Cyclodextrin Inclusion ComplexesThe main purpose of this study was to investigate the role of drug particle size on the complexation, physicochemical properties and dissolution of β-cyclodextrin inclusion complexes. In this work, ibuprofen in size of 3 μm and 45 μm (ibuprofen 3 and ibuprofen 45) were employed as the poorly water-soluble drug model. Complexation kinetics and complexation efficiency studies were conducted to investigate the complexation of ibuprofen with β-cyclodextrin in water. The solid cyclodextrins inclusion complexes were prepared with kneading method and characterized by Fourier transform-infrared spectroscopy, differential scanning calorimetry, X-ray powder difractometry, optical microscopy analyses and dissolution test. Ibuprofen with smaller particle size showed higher complexation rate with β-cyclodextrin in complexation kinetics study. By comparing the apparent stability constant, K c and complexation efficiency of complexes, it also indicated that smaller drug particles are more efficient to interact with β-cyclodextrin than larger particles. The phase solubility diagram could be classified as Bs type, which denotes complexes with limited solubility. The Fourier transform-infrared spectroscopy, differential scanning calorimetry, X-ray powder difractometry and optical microscopy analyses confirmed the formation of β-cyclodextrin inclusion complexes with ibuprofen 3 or ibuprofen 45. In the dissolution study, the inclusion complexes presented faster dissolution rate on contrast with the physical mixtures and pure drugs. What is more, the inclusion complexes prepared with ibuprofen in small particle size showed improving dissolution rate than in large particle size.

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“…0.0453 mg/ml 4 however, few studies on the water solubility enhancement of TPZ have been reported in the literature. To improve solubility of water insoluble drugs, micelles, 5 inclusion complexation, 6,7 self‐microemulsifying drug delivery systems, and solid dispersion (SD) techniques have been applied in the pharmaceutical industry 8 . Among these technologies, SD has been considered a potential technology to improve the bioavailability (BA) of low‐water soluble drugs by enhancing water solubility and dissolution rate 9 .…”

Section: Introductionmentioning

confidence: 99%

Polymeric solid dispersion enhances the equilibrium solubility and oral bioavailability of tegoprazan

Won

Yang²,

Hong

et al. 2023

Bulletin Korean Chem Soc

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The recently developed water‐insoluble tegoprazan (TPZ) belongs to the biopharmaceutical classification system (BCS) class II group was formulated through solid dispersion (SD) technology. SD formulations of TPZ were prepared using hydroxymethylcellulose (HPMC) and polyvinylpyrrolidone (PVP) polymers via the solvent evaporation method. SDs were characterized by scanning electron microscopy (SEM), powder x‐ray diffraction (PXRD), and differential scanning calorimetry (DSC). In addition, the equilibrium solubility of SDs, in vitro dissolution, and in vivo bioavailability (BA) study in rats were performed. PXRD and DSC revealed that TPZ was successfully transformed to amorphous forms in SDs. The equilibrium solubility was enhanced by 15–18‐fold, and in vitro dissolution was improved by approximately 2.2‐fold. Consequently, the BA of TPZ was increased up to 2.1‐fold. In conclusion, the use of SDs of TPZ using HPMC and PVP are considered a potential strategy to improve the therapeutic effect of TPZ via enhanced dissolution and BA.

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Comparative study of itraconazole-cyclodextrin inclusion complex and its commercial product

Cited by 14 publications

References 43 publications

Itraconazole solid dispersion prepared by a supercritical fluid technique: preparation, in vitro characterization, and bioavailability in beagle dogs

Itraconazole solid dispersion prepared by a supercritical fluid technique: preparation, in vitro characterization, and bioavailability in beagle dogs

Effect of Drug Particle Size on Complexation, Physicochemical Properties and Dissolution of Cyclodextrin Inclusion Complexes

Polymeric solid dispersion enhances the equilibrium solubility and oral bioavailability of tegoprazan

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