Limitations of Presently Available<i>In Vitro</i>Release Data for the Prediction of<i>In Vivo</i>Performance

Kottke, M. K.; Rhodes, C. T.

doi:10.3109/03639049109043851

Cited by 9 publications

(3 citation statements)

References 12 publications

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“…To assess the viability and validity of the sustaining nature of IPN microparticles, IVIVC study is essential, since prolonged-release products may be specially suited for this kind of study (Kottke & Rhodes, 1991). When the fraction of drug released in pH 6.8 was plotted against the fraction of drug absorbed, a linear correlation was obtained (Figure 12).…”

Section: In Vitro In Vivo Correlation (Ivivc)mentioning

confidence: 96%

Novel interpenetrating network microspheres of xanthan gum–poly(vinyl alcohol) for the delivery of diclofenac sodium to the intestine—in vitro and in vivo evaluation

Ray¹,

Banerjee²,

Maiti³

et al. 2010

Drug Delivery

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Section: In Vitro In Vivo Correlation (Ivivc)mentioning

confidence: 96%

Novel interpenetrating network microspheres of xanthan gum–poly(vinyl alcohol) for the delivery of diclofenac sodium to the intestine—in vitro and in vivo evaluation

Ray¹,

Banerjee²,

Maiti³

et al. 2010

Drug Delivery

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“…To assess the viability and validity of the sustaining nature of RCMX-PEI bead, IVIVC study is essential since prolonged-release products may be specially suited for this kind of study (Kottke et al, 1991). When the fraction of drug released in pH 6.8 was plotted against the fraction of drug absorbed, a linear correlation was obtained (Fig.…”

Section: In Vitro In Vivo Correlation (Ivivc)mentioning

confidence: 99%

Polyethyleneimine-treated xanthan beads for prolonged release of diltiazem: in vitro and in vivo evaluation

Ray¹,

Maiti

2010

Arch. Pharm. Res.

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The purpose of the study was to develop a multiunit sustained release dosage form of diltiazem hydrochloride using a natural polymer, sodium carboxymethyl xanthan gum and polyethyleneimine (PEI) from a completely aqueous environment. PEI treated diltiazem resin complex loaded beads were characterized by morphology, drug entrapment efficiency, in vitro and in vivo release behaviour. 40% and 80% drug was released in 2 hour in pH 1.2 and in 5 to 6 h in pH 6.8 respectively depending on the formulation variables. The prolonged release was attributed to decreased swelling of the beads due to PEI treatment. Maintaining the shape throughout the dissolution process, PEI treated diltiazem resin complex beads released the drug following non-Fickian transport phenomena. In vivo pharmacokinetic evaluation in rabbits shows slow and prolonged drug release when compared with diltiazem solution. The designed beads are suitable for prolonged release of a water soluble drug under a complete aqueous environment using natural gum.

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“…To assess the viability and the validity of the controlling nature of polystyrene microparticles in comparison to Fenlong-SR, an IVIVC study is essential since prolonged-release products may be especially suited for this kind of study. 28 Furthermore, the low aqueous solubility and the poor wettability of ibuprofen 29 may lead to bioavailability problems; bioavailability is likely to be rate-limited by the product's dissolution. By developing and evaluating an IVIVC study, one may be able to establish the dissolution test as a surrogate for human bioequivalence studies.…”

Section: Ivivcmentioning

confidence: 99%

In vitro and in vivo evaluation of single-unit commercial conventional tablet and sustained-release capsules compared with multiple-unit polystyrene microparticle dosage forms of ibuprofen

Shunmugaperumal

2006

AAPS PharmSciTech

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The major aims of the present study were (1) to select a multiple-unit formulation that matched the in vitro dissolution profile of single-unit sustained-release commercial capsules, (2) to compare the sustaining/controlling efficacy of the selected multiple-unit formulation with that of the single-unit commercial conventional tablet and sustainedrelease capsules, and (3) to determine whether an in vitroin vivo correlation exists for single-and multiple-unit formulations. Ibuprofen (20%-60% wt/wt)-loaded multipleunit polystyrene microparticles were prepared by an emulsionsolvent evaporation method from an aqueous system. The in vitro release profiles obtained in phosphate buffer of pH 6.8 for drug-loaded polystyrene microparticles and for commercial sustained-release capsules (Fenlong-SR, 400 mg) were compared. Since the microparticles with 30% ibuprofen load showed a release profile comparable to that of the Fenlong-SR release profile, the microparticles with this drug load were considered to be the optimized/selected formulation and, therefore, were subjected to stability study and in vivo study in human volunteers. A single-dose oral bioavailability study revealed significant differences in C max , T max , t 1/2a , t 1/2e , K a , K e , and AUC between the conventional tablet and optimized or Fenlong-SR capsule dosage forms. However, all the parameters, with the exception of K a along with relative bioavailability (F) and retard quotient (R Δ ), obtained from the optimized ibuprofenloaded microparticles were lower than that obtained from the commercial Fenlong-SR formulation. Furthermore, linear relationship obtained between the percentages dissolved and absorbed suggests a means to predict in vivo absorption by measuring in vitro dissolution.

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Limitations of Presently AvailableIn VitroRelease Data for the Prediction ofIn VivoPerformance

Cited by 9 publications

References 12 publications

Novel interpenetrating network microspheres of xanthan gum–poly(vinyl alcohol) for the delivery of diclofenac sodium to the intestine—in vitro and in vivo evaluation

Novel interpenetrating network microspheres of xanthan gum–poly(vinyl alcohol) for the delivery of diclofenac sodium to the intestine—in vitro and in vivo evaluation

Polyethyleneimine-treated xanthan beads for prolonged release of diltiazem: in vitro and in vivo evaluation

In vitro and in vivo evaluation of single-unit commercial conventional tablet and sustained-release capsules compared with multiple-unit polystyrene microparticle dosage forms of ibuprofen

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