Ondansetron Absorption in Adults: Effect of Dosage Form, Food, and Antacids

Bozigian, Haig; Pritchard, J. Frederick; Gooding, Ann E.; Pakes, Gary E.

doi:10.1002/jps.2600830717

Cited by 28 publications

(17 citation statements)

References 10 publications

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“…However, the flux obtained with 60% v/v ethanol-water vehicle (8.91 ± 0.27 μg/cm 2. h) is not sufficient to provide the required flux (84 μg/cm 2. h) for formulating the drug reservoir system. The required flux (J) was calculated based on the mean pharmacokinetic parameters of ondansetron hydrochloride (Clearance, CL= 21,240 ml/h) so as to obtain a mean steady-state plasma drug concentration (C ss ) of 26.2 ng/ml in humans (Markham and Sorkin 1993;Bozigian et al 1994) using the equation: J = [(C ss X CL)/ Area of the membrane]. The area of membrane exposed to drug permeation during in vitro permeation study was 6.6 cm 2 .…”

Section: Optimization Of Ethanol-water Solvent Systemmentioning

confidence: 99%

Penetration-Enhancing Effect of Ethanolic Solution of Menthol on Transdermal Permeation of Ondansetron Hydrochloride Across Rat Epidermis

et al. 2008

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The aim of this investigation was to study the effect of an ethanolwater solvent system and ehtanolic solution of menthol on the permeation of ondansetron hydrochloride across the rat epidermis in order to select a suitable ethanol-water vehicle and optimal concentration of menthol for the development of a transdermal therapeutic system. The solubility of ondansetron hydrochloride in ethanol, water and selected concenetrtaion of ethanol-water vehicles (20:80 v/v, 40:60 v/v and 60:40 v/v) was determined. The effect of these solvent vehicles, containing 1.5% w/v of ondansetron hydrochloride, on the in vitro permeation of the drug was studied across the rat epidermis. The highest permeation was observed from 60% v/v of ethanol-water vehicle that showed highest solubilty. Hence, the hydroxypropyl cellulose (HPC) (2% w/w) gel formulations containing 1.5% w/w of ondansetron hydrochloride and selected concentrations of menthol (0, 2, 4, 8 and 10% w/w) were prepared using 60% v/v of ethanol-water vehicle, and subjected to in vitro permeation of the drug across rat epidermis. The transdermal permeation of ondansetron hydrochloride was enhanced markedly by the addition of menthol to HPC gel drug reservoir formulations. A maximum flux of ondansetron hydrochloride (77.85 ± 2.85 μg/cm 2. h) was observed with a mean enhancement ratio of 13.06 when menthol was incorporated at a concentration of 8% w/w in HPC gels. However, there was no significant increase in the drug flux with 10% w/w menthol when compared to that obtained with 8% w/w of menthol in HPC gel formulations. The results suggest that 2% w/w HPC gel drug reservoir formulation, prepared with 60% v/v ethanol-water, containing 8% w/w of menthol provides an optimal transdermal permeation of ondansetron hydrochloride.

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Section: Optimization Of Ethanol-water Solvent Systemmentioning

confidence: 99%

Penetration-Enhancing Effect of Ethanolic Solution of Menthol on Transdermal Permeation of Ondansetron Hydrochloride Across Rat Epidermis

et al. 2008

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“…Ondansetron is a serotonin subtype 3 (5-HT3) receptor antagonist used in CINV management. Orally administered OND undergoes extensive hepatic first-pass metabolism, which accounts for its low bioavailability and short half-life [1]. It tends to be vomited before being absorbed and has limited use in patients with difficulty swallowing after chemotherapy [2,3].…”

Section: Introductionmentioning

confidence: 99%

Development and In vitro Evaluation of Self-Adhesive Matrix-Type Transdermal Delivery System of Ondansetron Hydrochloride

David¹,

Rajabalaya²,

Zhia³

2015

Trop. J. Pharm Res

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“…[1] Due to its short half-life and low bioavailability, it is administered orally 3 to 4 times a day, wherein the patient compliance is low. [2] Rectal and nasal administration of ondansetron are also considered to have low patient compliance. [3,4] Even with oral controlled-release dosage forms, fluctuation in plasma concentration of drug is high, which in turn results in low patient compliance.…”

Section: Introductionmentioning

confidence: 99%

“…The desired flux (J) was calculated based on the mean pharmacokinetic parameters of ondansetron hydrochloride (clearance, CL = 21,240 ml/h) to obtain a mean steady-state plasma drug concentration (C ss ) of 26.2 ng/ml in humans using the equation: J = [(C ss × CL)/ area of the membrane]. [1,2] The area of membrane exposed to drug permeation during in vitro permeation study was 6.6 cm 2 . Taking the difference in the permeability of rat epidermis and human skin, and that of the possible resistance of the TTS components, it warrants for formulating the drug reservoir with other terpene penetration enhancers such as nerodilol, carvone, and limonene.…”

Section: Introductionmentioning

confidence: 99%

Studies on Optimizing In Vitro Transdermal Permeation of Ondansetron Hydrochloride Using Nerodilol, Carvone, and Limonene as Penetration Enhancers

Krishnaiah

Raju

Kumar

et al. 2008

Pharmaceutical Development and Technology

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The present investigation was carried out to formulate a terpene-based hydroxypropyl cellulose (HPC) gel drug reservoir system for its optimal transdermal permeation of ondansetron hydrochloride. The HPC gel formulations containing ondansetron hydrochloride (3% w/w) and selected concentrations of either nerodilol (0% w/w, 1% w/w, 2% w/w, 3% w/w, and 4% w/w), carvone (0% w/w, 2% w/w, 4% w/w, 8% w/w, and 10% w/w), or limonene (0% w/w, 2% w/w, 3% w/w, and 4% w/w) were prepared and subjected to in vitro permeation of the drug across rat epidermis. All the 3 terpene enhancers increased the transdermal permeation of ondansetron hydrochloride. The optimal transdermal permeation was observed with 3% w/w of nerodilol (175.3 ± 3.1 μg/ cm 2. h), 8% w/w of carvone (87.4 ± 1.6 μg/cm 2. h), or 3% w/w of limonene (181.9 ± 0.9 μg/cm 2. h). The enhancement ratio (ER) in drug permeability with 3% w/w nerodilol, 8% w/w carvone, and 3% w/w limonene were 21.6, 10.8, and 22.5, respectively, when compared with that obtained without a terpene enhancer (control). However, there was 1.04-, 2.09-, and 2.17-fold increase in the optimal drug flux obtained with carvone, nerodilol, and limonene, respectively, when compared with the desired drug flux (84 μg/cm 2. h). It was concluded that the HPC gel drug reservoir systems containing either 3% w/w nerodilol or 3% w/w limonene act as optimal formulations for use in the design of membrane-controlled transdermal therapeutic system (TTS) of ondansetron hydrochloride.

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Ondansetron Absorption in Adults: Effect of Dosage Form, Food, and Antacids

Cited by 28 publications

References 10 publications

Penetration-Enhancing Effect of Ethanolic Solution of Menthol on Transdermal Permeation of Ondansetron Hydrochloride Across Rat Epidermis

Penetration-Enhancing Effect of Ethanolic Solution of Menthol on Transdermal Permeation of Ondansetron Hydrochloride Across Rat Epidermis

Development and In vitro Evaluation of Self-Adhesive Matrix-Type Transdermal Delivery System of Ondansetron Hydrochloride

Studies on Optimizing In Vitro Transdermal Permeation of Ondansetron Hydrochloride Using Nerodilol, Carvone, and Limonene as Penetration Enhancers

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