In vitro dissolution of sparingly water-soluble drug dosage forms

Shah, Vinod P.; Noory, Assad; Noory, Carol; McCullough, B. D.; Clarke, S. G.; Everett, Richard L.; Naviasky, Helen; Srinivasan, B. N.; Fortman, Don; Skelly, Jerome P.

doi:10.1016/0378-5173(95)00123-z

Cited by 88 publications

(73 citation statements)

References 9 publications

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“…The Food and Drug Administration discourages the use of only water as a dissolution medium for highly lipophilic agents, and recommends the use of a slight quantity of a surfactant in the dissolution medium to improve the dissolution efficiency of such chemical entities. 34 Therefore, 900 mL of 2% (w/v) polysorbate 80 was used as a dissolution medium in our study. 33 The reduction in the degree of crystallinity might be caused by improvements in the aqueous solubility and dissolution rate of the drug.…”

Section: P0mentioning

confidence: 99%

“…The dissolution medium consisted of 900 mL of 2% (w/v) Tween 80. 33,34 The dissolution test was accomplished at 37°C±0.5°C using a paddle rotation of 100 rpm. The dissolution medium-containing vessel was surrounded by an International Journal of Nanomedicine 2015:10 submit your manuscript | www.dovepress.com Dovepress outer water bath in order to maintain a specific temperature.…”

Section: Dissolutionmentioning

confidence: 99%

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Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation

Yousaf¹,

Kim²,

Oh³

et al. 2015

IJN

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Background The intention of this research was to prepare and compare various solubility-enhancing nanoparticulated systems in order to select a nanoparticulated formulation with the most improved oral bioavailability of poorly water-soluble fenofibrate. Methods The most appropriate excipients for different nanoparticulated preparations were selected by determining the drug solubility in 1% (w/v) aqueous solutions of each carrier. The polyvinylpyrrolidone (PVP) nanospheres, hydroxypropyl-β-cyclodextrin (HP-β-CD) nanocorpuscles, and gelatin nanocapsules were formulated as fenofibrate/PVP/sodium lauryl sulfate (SLS), fenofibrate/HP-β-CD, and fenofibrate/gelatin at the optimized weight ratios of 2.5:4.5:1, 1:4, and 1:8, respectively. The three solid-state products were achieved using the solvent-evaporation method through the spray-drying technique. The physicochemical characterization of these nanoparticles was accomplished by powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and Fourier-transform infrared spectroscopy. Their physicochemical properties, aqueous solubility, dissolution rate, and pharmacokinetics in rats were investigated in comparison with the drug powder. Results Among the tested carriers, PVP, HP-β-CD, gelatin, and SLS showed better solubility and were selected as the most appropriate constituents for various nanoparticulated systems. All of the formulations significantly improved the aqueous solubility, dissolution rate, and oral bioavailability of fenofibrate compared to the drug powder. The drug was present in the amorphous form in HP-β-CD nanocorpuscles; however, in other formulations, it existed in the crystalline state with a reduced intensity. The aqueous solubility and dissolution rates of the nanoparticles (after 30 minutes) were not significantly different from one another. Among the nanoparticulated systems tested in this study, the initial dissolution rates (up to 10 minutes) were higher with the PVP nanospheres and HP-β-CD nanocorpuscles; however, neither of them resulted in the highest oral bioavailability. Irrespective of relatively retarded dissolution rate, gelatin nanocapsules showed the highest apparent aqueous solubility and furnished the most improved oral bioavailability of the drug (~5.5-fold), owing to better wetting and diminution in crystallinity. Conclusion Fenofibrate-loaded gelatin nanocapsules prepared using the solvent-evaporation method through the spray-drying technique could be a potential oral pharmaceutical product for administering the poorly water-soluble fenofibrate with an enhanced bioavailability.

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Section: P0mentioning

confidence: 99%

Section: Dissolutionmentioning

confidence: 99%

Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation

Yousaf¹,

Kim²,

Oh³

et al. 2015

IJN

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show abstract

“…Each nanospherule formulation, equivalent to 15 mg of fenofibrate, was properly enclosed in a dialysis bag (Spectra/Por ® dialysis membrane, molecular weight cutoff: 3,500 Da; Spectrum Laboratories, Rancho Dominguez, CA, USA) and the loaded bag was placed in the basket. The basket was immersed in 500 mL of 2% (w/v) aqueous Tween 80 27,28 at 37°C±0.5°C. The rotation speed of the basket was set to 100 rpm.…”

Section: Dissolution Testmentioning

confidence: 99%

Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate

Yousaf

Mustapha

Kim

et al. 2016

IJN

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Purpose The purpose of the present research was to develop a novel electrosprayed nanospherule providing the most optimized aqueous solubility and oral bioavailability for poorly water-soluble fenofibrate. Methods Numerous fenofibrate-loaded electrosprayed nanospherules were prepared with polyvinylpyrrolidone (PVP) and Labrafil ® M 2125 as carriers using the electrospray technique, and the effect of the carriers on drug solubility and solvation was assessed. The solid state characterization of an optimized formulation was conducted by scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopic analyses. Oral bioavailability in rats was also evaluated for the formulation of an optimized nanospherule in comparison with free drug and a conventional fenofibrate-loaded solid dispersion. Results All of the electrosprayed nanospherule formulations had remarkably enhanced aqueous solubility and dissolution compared with free drug. Moreover, Labrafil M 2125, a surfactant, had a positive influence on the solubility and dissolution of the drug in the electrosprayed nanospherule. Increases were observed as the PVP/drug ratio increased to 4:1, but higher ratios gave no significant increases. In particular, an electrosprayed nanospherule composed of fenofibrate, PVP, and Labrafil M 2125 at the weight ratio of 1:4:0.5 resulted in a particle size of <200 nm with the drug present in the amorphous state. It demonstrated the highest solubility (32.51±2.41 μg/mL), an excellent dissolution (~85% in 10 minutes), and an oral bioavailability ~2.5-fold better than that of the free drug. It showed similar oral bioavailability compared to the conventional solid dispersion. Conclusion Electrosprayed nanospherules, which provide improved solubility and bioavailability, are promising drug delivery tools for oral administration of poorly water-soluble fenofibrate.

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“…In addition, dissolution is a requirement for regulatory approval for product marketing. [9][10][11][12] At the moment, no dissolution test has been described in literature for BCZ. The present work has two main objectives.…”

Section: Buclizine Hydrochloride (Bcz) (Rs)-1-(4-tert-butylbenzyl)-4mentioning

confidence: 99%

Development and validation of a stability-indicating HPLC method for the determination of buclizine hydrochloride in tablets and oral suspension and its application to dissolution studies

et al. 2012

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Recebido em 10/3/11; aceito em 24/5/11; publicado na web em 22/7/11 A method using liquid chromatography has been developed and validated for determination of buclizine in pharmaceutical formulations and in release studies. Isocratic chromatography was performed on a C18 column with methanol:water (80:20 v/v, pH 2.6) as mobile phase, at a flow rate of 1.0 mL/min, and UV detection at 230 nm. The method was linear, accurate, precise, sensible and robust. The dissolution test was optimized and validated in terms of dissolution medium, apparatus agitation and rotation speed. The presented analytical and dissolution procedures can be conveniently adopted in the quality and stability control of buclizine in tablets and oral suspension.

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In vitro dissolution of sparingly water-soluble drug dosage forms

Cited by 88 publications

References 9 publications

Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation

Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation

Novel electrosprayed nanospherules for enhanced aqueous solubility and oral bioavailability of poorly water-soluble fenofibrate

Development and validation of a stability-indicating HPLC method for the determination of buclizine hydrochloride in tablets and oral suspension and its application to dissolution studies

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