In vitro and in vivo evaluation of novel immediate release carbamazepine tablets: Complexation with hydroxypropyl-β-cyclodextrin in the presence of HPMC

Kou, Wen; Cai, Cuifang; Xu, Song; Wang, Huan; Liu, Jing; Yang, Dan; Zhang, Tianhong

doi:10.1016/j.ijpharm.2011.02.042

Cited by 37 publications

(21 citation statements)

References 20 publications

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“…Kou et al developed a solid dispersion of carbamazepine by complexation with hydroxypropyl-β-cyclodextrin with 95 times increase in the solubility of Carbamazepine. The SD when formulated as an ODT showed 1.5-fold increased bioavailability (P b 0.05) as compared to commercial tablets [15]. Similarly, Rao et al prepared SD of Nimodipine which were compressed into fast dissolving tablets and demonstrated enhanced dissolution (99.63% drug release within 9 min) [16].…”

Section: Introductionmentioning

confidence: 99%

Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability

Desai

Poddar

Sawant

2016

Materials Science and Engineering: C

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Section: Introductionmentioning

confidence: 99%

Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability

Desai

Poddar

Sawant

2016

Materials Science and Engineering: C

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“…While a number of papers on CD complexation have been published over the past 20+ years, many of the manuscripts are descriptive studies that characterize the solubility and/or dissolution increase of various poorly soluble compounds (25)(26)(27)(28). Several papers have demonstrated CD complexation potential to enhance drug permeability and bioavailability (29,30).…”

Section: Introductionmentioning

confidence: 99%

Experimental and Computational Studies of Physicochemical Properties Influence NSAID-Cyclodextrin Complexation

Felton

Popescu²,

Wiley

et al. 2014

AAPS PharmSciTech

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Abstract. The objective of this research was to investigate physicochemical properties of an active pharmaceutical ingredient (API) that influence cyclodextrin complexation through experimental and computational studies. Native β-cyclodextrin (B-CD) and two hydroxypropyl derivatives were first evaluated by conventional phase solubility experiments for their ability to complex four poorly watersoluble nonsteroidal anti-inflammatory drugs (NSAIDs). Differential scanning calorimetry was used to confirm complexation. Secondly, molecular modeling was used to estimate Log P and aqueous solubility (S o ) of the NSAIDs. Molecular dynamics simulations (MDS) were used to investigate the thermodynamics and geometry of drug-CD cavity docking. NSAID solubility increased linearly with increasing CD concentration for the two CD derivatives (displaying an A L profile), whereas increases in drug solubility were low and plateaued in the B-CD solutions (type B profile). The calculated Log P and S o of the NSAIDs were in good concordance with experimental values reported in the literature. Side chain substitutions on the B-CD moiety did not significantly influence complexation. Explicitly, complexation and the associated solubility increase were mainly dependent on the chemical structure of the NSAID. MDS indicated that each NSAID-CD complex had a distinct geometry. Moreover, complexing energy had a large, stabilizing, and fairly constant hydrophobic component for a given CD across the NSAIDs, while electrostatic and solvation interaction complex energies were quite variable but smaller in magnitude.

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“…This study found that the PK and F abs of form I, form III, and the dihydrate of CBZ in rats differed Kahela et al (1983), Elqidra et al (2004), andCotter et al (1977), respectively; d,e data for dogs from Kobayashi et al (2000) and Kou et al (2011), respectively; n.c., not calculated, because the parameter was calculated from pooled data; n.a., not available depending on the doses administered. The absorption and elimination of the three forms were not significantly different at the low dose for the investigated species.…”

Section: Comparison Of Pk and Bioavailabilities Among The Speciesmentioning

confidence: 72%

“…Data for humans were adapted from those reported in the literature (Cotter et al, 1977;Kahela et al, 1983;Gérardin et al, 1990;Winnicka et al, 2002;Elqidra et al, 2004), while the data for dogs were obtained mainly from Kobayashi et al (2000) and Kou et al (2011). The main PK parameters of CBZ in species are compared in Table II.…”

Section: Comparison Of Pk and Bioavailabilities Among The Speciesmentioning

confidence: 99%

Pharmacokinetics of carbamazepine polymorphs and dihydrate in rats, related to dogs and humans

Zou

Liu

et al. 2011

Arch. Pharm. Res.

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Species differences in the oral pharmacokinetics and absolute bioavailability (F ( abs )) of carbamazepine polymorphs (form I and form III) and dihydrate were studied. The pharmacokinetics of each form was investigated in rats following a single oral/intravenous administration of 10 mg/kg and an oral dose of 80 mg/kg, which were compared with the published data obtained from dogs and humans. No significant differences were found in their C (max), T (max), AUC(0-∞) and F ( abs ) among the forms at the low dose. However, significant differences were observed at the high dose. The Fabs of each form was markedly reduced with increasing of doses in species (e.g. F ( abs ) in rats ranged from > 82% to 38.4%-56.0%). At a comparable dose, the C (max), and AUC(0-∞) of rats and humans were about 3-10 times higher than in dogs. The absorption rate of form III in rats exhibited a similar trend to that in humans, and was far higher in dogs. A multi-peak phenomenon in plasma curves was observed in rats and humans, but not in dogs. In conclusion, rats appear to be a better predictor of carbamazepine polymorphs absorbed in humans, and form III may be more suitable as a pharmaceutical crystal.

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In vitro and in vivo evaluation of novel immediate release carbamazepine tablets: Complexation with hydroxypropyl-β-cyclodextrin in the presence of HPMC

Cited by 37 publications

References 20 publications

Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability

Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability

Experimental and Computational Studies of Physicochemical Properties Influence NSAID-Cyclodextrin Complexation

Pharmacokinetics of carbamazepine polymorphs and dihydrate in rats, related to dogs and humans

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