scholarly journals Enhanced Bioavailability of Itraconazole in Hydroxypropylβ-Cyclodextrin Solution versus Capsules in Healthy Volunteers

1998 ◽  
Vol 42 (7) ◽  
pp. 1862-1865 ◽  
Author(s):  
Joseph A. Barone ◽  
Bruce L. Moskovitz ◽  
Joseph Guarnieri ◽  
Alan E. Hassell ◽  
John L. Colaizzi ◽  
...  
Keyword(s):  
Crossover Study ◽  
Healthy Volunteers ◽  
Oral Solution ◽  
Solution Versus ◽  
Male Volunteers ◽  
The Times

ABSTRACT The bioavailabilities and bioequivalences of single 200-mg doses of itraconazole solution and two capsule formulations were evaluated in a crossover study of 30 male volunteers. The two capsule formulations were bioequivalent. The bioavailabilities of the solutions itraconazole and hydroxyitraconazole were 30 to 33% and 35 to 37% greater, respectively, than those of either capsule. However, the maximum concentrations of the drug in plasma (C max), the times to C max, and the terminal half-lives were comparable for all three formulations. These data indicate that the bioavailabilities of itraconazole and hydroxyitraconazole are enhanced when administered as an oral solution instead of capsules.

Effect of food on the pharmacokinetics of dronabinol oral solution versus dronabinol capsules in healthy volunteers.

2016 ◽  
Vol 34 (26_suppl) ◽  
pp. 199-199
Author(s):  
Christina Cognata Smith ◽  
D. Alexander Oh ◽  
Neha Parikh ◽  
Varun Khurana ◽  
Santosh Vetticaden
Keyword(s):  
Healthy Volunteers ◽  
Therapeutic Benefit ◽  
Oral Solution ◽  
Individual Variability ◽  
Pharmacokinetic Data ◽  
Inadequate Response ◽  
Open Label ◽  
Post Dose ◽  
Solution Versus ◽  
Fed State

199 Background: Dronabinol, a pharmaceutical tetrahydrocannabinol (THC), capsule is approved for anorexia associated with weight loss in patients with AIDS and for cancer chemotherapy-induced nausea/vomiting in patients with inadequate response to conventional antiemetic therapy. Food effects on absorption and bioavailability of a new dronabinol oral solution was compared with marketed capsules. Methods: In an open-label, single-dose, 3-period crossover study, healthy volunteers were randomized to receive dronabinol oral solution 4.25 mg (fed) or dronabinol capsule 5 mg (fed or fasted), after a 7-day washout period. Doses were administered under a fasted (overnight) or fed state (high-fat/calorie meal 30 minutes pre-dose). Plasma pharmacokinetics was evaluated for dronabinol and the major metabolite, 11-OH-Δ9-THC. Results: Pharmacokinetic data of 54 volunteers were analyzed. In the fed state, initial dronabinol absorption was rapid with oral solution versus capsules (mean Tlag, 0.15 vs 2.02 h), and 100% and 15% of volunteers receiving oral solution and capsules, respectively, had detectable plasma dronabinol levels 30 minutes post-dose. Inter-individual variability in plasma dronabinol concentrations during early absorption was less with oral dronabinol solution (%CV: 82.79%, 83.94%, and 90.68%) versus capsules (%CV: 318.54%, 250.33%, and 182.01%) observed at 0.5, 1, and 2 h, respectively, after dosing. Food increased mean AUC0-t similarly for dronabinol oral solution and capsules, versus capsules with fasting, increasing exposure to oral solution and capsules 2.1- to 2.4-fold. Mean Tmax was similarly delayed for dronabinol oral solution (7.7 h) and capsules (5.6 h) with food relative to fasting (1.7 h). On the basis of 11-OH-Δ9-THC plasma levels, AUC0-t up to 48 h postdose and AUC0-inf were found to be similar for the oral solution and capsules under fed conditions. Conclusions: An appreciable food effect was observed for dronabinol oral solution and capsules. Dronabinol oral solution may offer therapeutic benefit to patients given its rapid absorption and lower inter-individual variability compared with dronabinol capsules. Clinical trial information: NCT01448772.

scholarly journals Bioavailability study of dronabinol oral solution versus dronabinol capsules in healthy volunteers

2016 ◽  
Vol Volume 8 ◽  
pp. 155-162
Author(s):  
Neha Parikh ◽  
William Kramer ◽  
Varun Khurana ◽  
Christina Cognata Smith ◽  
Santosh Vetticaden
Keyword(s):  
Healthy Volunteers ◽  
Oral Solution ◽  
Solution Versus ◽  
Bioavailability Study

scholarly journals Pharmacokinetics of DFN-15, a Novel Oral Solution of Celecoxib, Versus Celecoxib 400-mg Capsules: A Randomized Crossover Study in Fasting Healthy Volunteers

2017 ◽  
Vol 37 (10) ◽  
pp. 937-946 ◽  
Author(s):  
Arindam Pal ◽  
Srinivas Shenoy ◽  
Anirudh Gautam ◽  
Sagar Munjal ◽  
Jing Niu ◽  
...  
Keyword(s):  
Crossover Study ◽  
Healthy Volunteers ◽  
Oral Solution ◽  
Randomized Crossover Study

A single-dose comparative bioavailability study of dronabinol oral solution versus dronabinol capsules in healthy volunteers.

2016 ◽  
Vol 34 (15_suppl) ◽  
pp. e21595-e21595
Author(s):  
Neha Parikh ◽  
William G. Kramer ◽  
Varun Khurana ◽  
Christina Cognata Smith ◽  
Santosh Vetticaden
Keyword(s):  
Single Dose ◽  
Healthy Volunteers ◽  
Oral Solution ◽  
Solution Versus ◽  
Bioavailability Study ◽  
Comparative Bioavailability ◽  
Comparative Bioavailability Study

scholarly journals Effect of food on the pharmacokinetics of dronabinol oral solution versus dronabinol capsules in healthy volunteers

2017 ◽  
Vol Volume 9 ◽  
pp. 9-17 ◽  
Author(s):  
D. Alexander Oh ◽  
Neha Parikh ◽  
Varun Khurana ◽  
Christina Cognata Smith ◽  
Santosh Vetticaden
Keyword(s):  
Healthy Volunteers ◽  
Oral Solution ◽  
Solution Versus ◽  
Effect Of Food

A single-dose comparative bioavailability study of dronabinol oral solution versus dronabinol capsules in healthy volunteers.

2016 ◽  
Vol 34 (26_suppl) ◽  
pp. 198-198
Author(s):  
Christina Cognata Smith ◽  
Neha Parikh ◽  
William G. Kramer ◽  
Varun Khurana ◽  
Santosh Vetticaden
Keyword(s):  
Single Dose ◽  
Plasma Concentration ◽  
Healthy Volunteers ◽  
Oral Solution ◽  
Individual Variability ◽  
Pharmacokinetic Data ◽  
Maximum Plasma ◽  
Inadequate Response ◽  
Solution Versus ◽  
Time Zero

198 Background: The capsule formulation of dronabinol, a pharmaceutical tetrahydrocannabinol (THC), is approved for anorexia associated with weight loss in patients with AIDS and for cancer chemotherapy-associated nausea/vomiting in patients with inadequate response to conventional antiemetics. A new oral formulation (i.e., dronabinol solution) was evaluated in a bioequivalence study versus currently marketed dronabinol capsules. Methods: In an open-label, 2-treatment, 2-sequence, 4-period, single-dose crossover study, healthy volunteers were randomized to receive 1 of 2 treatment sequences (T-R-T-R or R-T-R-T; T = dronabinol 4.25 mg oral solution and R = dronabinol 5 mg capsules). Dosing occurred after an overnight fast, with a minimum 7-day washout period between treatment periods. A validated liquid chromatography-tandem mass spectrometry method was used to determine plasma concentrations of dronabinol and the primary metabolite 11-OH-Δ9-THC. Results: Fifty-one of 52 enrollees had pharmacokinetic data for analysis. Mean pharmacokinetics were (oral solution vs capsule): Cmax (2.0 vs 2.4 ng/mL), median Tmax (1.0 vs 1.5 h), AUC0-∞ (3.8 vs 4.1 h∙ng/mL), and t1/2 (5.6 vs 3.1 h). The 2 formulations were bioequivalent with respect to maximum plasma concentration (Cmax; reference-scaled criteria) and area under the plasma concentration-time curve (from time zero to last measurable concentration and from time zero to infinity [AUC0-∞]; average bioequivalence) of dronabinol. The data for the 11-OH-Δ9-THC metabolite provide further support for the bioequivalence of the 2 products. Post hoc analysis demonstrated that all volunteers (100%) had detectable plasma dronabinol concentrations at 15 min with the oral solution compared with < 25% of volunteers for the capsules. Intra-individual variability was lower with oral solution versus capsules (for AUC0-∞, 13.5% vs 36.8%, respectively). Conclusions: Dronabinol oral solution 4.25 mg was bioequivalent to dronabinol capsules 5 mg, and exhibited quicker onset of detectable levels and lower intra-individual variability in comparison with dronabinol capsules 5 mg. Clinical trial information: NCT01448772.

scholarly journals Comparative Bioavailability of Metformin Hydrochloride Oral Solution Versus Metformin Hydrochloride Tablets in Fasting Mexican Healthy Volunteers

2018 ◽  
Vol 36 (2) ◽  
pp. 407-415
Author(s):  
Lourdes Garza-Ocañas ◽  
Jorge González-Canudas ◽  
Eduardo Tamez-de la O ◽  
Christian Badillo-Castañeda ◽  
Marco Vinicio Gómez-Meza ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Oral Solution ◽  
Metformin Hydrochloride ◽  
Solution Versus ◽  
Comparative Bioavailability
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