In vivo pharmacokinetics in human volunteers: oral administered guar gum-based colon-targeted 5-fluorouracil tablets

Krishnaiah, Y. S. R.; Satyanarayana, V.; Kumar, Bimlesh; Karthikeyan, Ramadoss; Bhaskar, P.

doi:10.1016/s0928-0987(03)00139-8

Cited by 91 publications

(34 citation statements)

References 21 publications

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“…On oral administration of F6 tablets, FLB reached peak concentration (C max =12,374.67 ±16.72 ng/ml) at 12 h T max, which revealed that the compression coating was able to retard the drug release in the upper GIT. The shift in the T max to a higher value is typical for the colonic systems (22). But after reaching the colonic environment, drug release from colon-targeted tablet by disintegration of swollen cellulose tablets was progressive.…”

Section: Discussionmentioning

confidence: 98%

A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets

Vemula

2015

AAPS PharmSciTech

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Abstract. A significant plan is executed in the present study to study the effect of double-compression coating on flurbiprofen core mini-tablets to achieve the pulsatile colonic delivery to deliver the drug at a specific time as per the patho-physiological need of the disease that results in improved therapeutic efficacy. In this study, pulsatile double-compression-coated tablets were prepared based on timecontrolled hydroxypropyl methylcellulose K100M inner compression coat and pH-sensitive Eudragit S100 outer compression coat. Then, the tablets were evaluated for both physical evaluation and drugrelease studies, and to prove these results, in vivo pharmacokinetic studies in human volunteers were conducted. From the in vitro drug-release studies, F6 tablets were considered as the best formulation, which retarded the drug release in the stomach and small intestine (3.42±0.12% in 5 h) and progressively released to the colon (99.78±0.74% in 24 h). The release process followed zero-order release kinetics, and from the stability studies, similarity factor between dissolution data before and after storage was found to be 88.86. From the pharmacokinetic evaluation, core mini-tablets producing peak plasma concentration (C max ) was 14,677.51±12.16 ng/ml at 3 h T max and pulsatile colonic tablets showed C max =12,374.67± 16.72 ng/ml at 12 h T max . The area under the curve for the mini and pulsatile tablets was 41,238.52 and 72,369.24 ng-h/ml, and the mean resident time was 3.43 and 10.61 h, respectively. In conclusion, development of double-compression-coated tablets is a promising way to achieve the pulsatile colonic release of flurbiprofen.

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Section: Discussionmentioning

confidence: 98%

A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets

Vemula

2015

AAPS PharmSciTech

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“…Concentration of 5-FU in the samples was determined using HPLC method reported by Krishnaiah et al (2003) with slight modification as per system requirement. The system used was Shimadzu LC-10AT VP having a UV detector (Shimadzu, Kyoto, Japan) and the software used was Class VP, version 5.032.…”

Section: Hplc Determination Of 5-fumentioning

confidence: 99%

Novel microbially triggered colon specific delivery system of 5-Fluorouracil: Statistical optimization, in vitro, in vivo, cytotoxic and stability assessment

Dev

Bali

Pathak

2011

International Journal of Pharmaceutics

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“…The detection wavelength was 266.5 nm, and the mobile phase consisted of HPLC-grade water. The flow rate was maintained at 0.8 ml/min, and the analytical column used was a reverse phase C18 column (4.6 × 250 mm, 5 μm) (Krishnaiah et al, 2003).…”

Section: Estimation Of 5-fu In Blood and Various Tissues/ Biodistribumentioning

confidence: 99%

Targeted delivery of an anti-cancer agent via steroid coupled liposomes

Mishra¹,

Gulbake²,

Jain³

et al. 2009

Drug Delivery

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In vivo pharmacokinetics in human volunteers: oral administered guar gum-based colon-targeted 5-fluorouracil tablets

Cited by 91 publications

References 21 publications

A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets

A Novel Approach to Flurbiprofen Pulsatile Colonic Release: Formulation and Pharmacokinetics of Double-Compression-Coated Mini-Tablets

Novel microbially triggered colon specific delivery system of 5-Fluorouracil: Statistical optimization, in vitro, in vivo, cytotoxic and stability assessment

Targeted delivery of an anti-cancer agent via steroid coupled liposomes

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