Intranasal absorption of Δ9-tetrahydrocannabinol and WIN55,212-2 mesylate in rats

Valiveti, Satyanarayana; Agu, Remigius U.; Hammell, Dana C.; Paudel, Kalpana S.; Earles, D. Caroline; Wermeling, Daniel P.; Stinchcomb, Audra L.

doi:10.1016/j.ejpb.2006.08.009

Cited by 17 publications

(8 citation statements)

References 19 publications

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“…The maximum concentration of THC (Cmax) was observedin the first sample (10 min after rats were removed from the exposure chamber) and the concentration declined with a terminal half-life of 3.7 h; total AUC 0-t (h*μg/L) of THC after 50 min of continuous smoke exposure was 12.2 ± 3, AUC inf (h* μg/L) 13.9 ± 3.8. The clearance was calculated to 1.1 (L/h) which is consistent with previously reported clearance values in rats, which range from 1 to 5 (L/h) [12,18]. The maximum concentration (Cmax) of 88.6 (ng/ml) for rimonabant was seen 10–12 min after i.p administration and it declined with a terminal half-life of 5.4 h; total AUC 0-t (h* μg/L) of rimonabant after 3 mg/kg was 308.15; AUC inf (h* μg/L) 457.6.…”

Section: Resultssupporting

confidence: 88%

Simultaneous quantification of cannabinoids tetrahydrocannabinol, cannabidiol and CB1 receptor antagonist in rat plasma: An application to characterize pharmacokinetics after passive cannabis smoke inhalation and co-administration of rimonabant

Ravula

Chandasana

Setlow

et al. 2018

Journal of Pharmaceutical and Biomedical Analysis

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A highly sensitive and selective liquid chromatography-tandem mass spectrometry method for the determination of tetrahydrocannabinol (THC), cannabidiol, and rimonabant in rat plasma was developed. Analytes and the internal standard were extracted from plasma using a combination of protein precipitation followed by liquid-liquid extraction. Chromatographic separation was done using Waters Symmetry C18, 4.6 × 150 mm, 5 um column using 10 mm ammonium formate buffer and methanol. The total run time was 6 min, and separation was achieved using isocratic elution at a flow rate of 1 mL/min using a 10:90 (aqueous: organic) ratio. The ionization of the analytes was optimized using electrospray ionization in positive mode, and multiple reaction mode was used for this analysis. This method showed linearity from 0.1 to 100 ng/ml for all the analytes and was validated according to FDA Bioanalytical Method Validation Guidance in terms of accuracy, precession, linearity, stability, matrix effect, recovery, and stability. This method was successfully applied to characterize the pharmacokinetics of THC in rats after continuous passive smoke exposure for 50 min when rimonabant was co-administered with cannabis smoke. Maximum concentration (C) for THC was observed immediately after rats were removed from the exposure chamber (10 min post completion) which declined with a terminal half-life of 3.7 h and clearance was calculated to be 1.1 (L/h). Rimonabant (i.p) at a dose of 3 mg/kg was rapidly absorbed and maximum concentration (Cmax) was seen at 11 min which declined with a terminal half-life of 5.4 h and clearance was calculated to be 2.0 (L/h). Exposure AUC (h* μg/L) for THC and rimonabant were 13.9 and 457.6 respectively. As this method was highly sensitive and required only 50 μL of plasma, it is applicable in rodent models that assess the exposure-response relationships of these drugs.

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Section: Resultssupporting

confidence: 88%

Simultaneous quantification of cannabinoids tetrahydrocannabinol, cannabidiol and CB1 receptor antagonist in rat plasma: An application to characterize pharmacokinetics after passive cannabis smoke inhalation and co-administration of rimonabant

Ravula

Chandasana

Setlow

et al. 2018

Journal of Pharmaceutical and Biomedical Analysis

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“…Indeed, the t 1/2 obtained in our study is comparable to the t 1/2 values more recently reported by Deiana et al [34] who used LC-MS/MS method for the detection of CBD. Similarly, the pharmacokinetic parameters obtained for THC in the current study are more comparable with the recent pharmacokinetic study by Valiveti et al [53], who used LC-MS technique to detect THC. Further studies will be required to accurately assess the pharmacokinetic parameters for CBD and THC after intravenous as well as oral administrations.…”

Section: Pharmacokinetic Studysupporting

confidence: 89%

Development of a simple and sensitive HPLC–UV method for the simultaneous determination of cannabidiol and Δ9-tetrahydrocannabinol in rat plasma

Zgair

Wong

Sabri

et al. 2015

Journal of Pharmaceutical and Biomedical Analysis

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“…Nasal and transdermal delivery systems have been examined as alternative dosage forms. [6][7][8] Among these, intranasal sildenafil citrate formulated as a microemulsion (ME) composed of oleic acid (OA)/Labrasol/Transcutol/H 2 O (8.33%:33.33%:16.67%:41.67%) represents a safe and viable approach to achieving rapid-onset systemic drug levels and higher bioavailability by bypassing liver metabolism for the management of ED. 3 Furthermore, transdermal permeation of a sildenafil citrate-loaded self-nanoemulsifying drug delivery system and nanoemulsions was proven to improve the therapeutic performance of sildenafil citrate via the oral route.…”

Section: Introductionmentioning

confidence: 99%

Rapid-Onset Sildenafil Sublingual Drug Delivery Systems: In Vitro Evaluation and In Vivo Pharmacokinetic Studies in Rabbits

Sheu

Hsieh

Chen

et al. 2016

Journal of Pharmaceutical Sciences

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The aim of the present study was to prepare sublingual delivery systems for sildenafil and evaluate its relative bioavailability after sublingual administration in rabbits to attain a rapid onset of action with good efficacy at lower doses. For sublingual application, sildenafil and its citrate were formulated in 2 different dosage forms: the first was a sublingual spray consisting of sildenafil in 2 microemulsion systems, oleic acid or propylene glycol (PG), and the second was sublingual tablets prepared with various granulated sublingual sprays adsorbed onto a silicate adsorbant (Florite(®) R), binders (Cyclocel(®) or EMDEX(®)), and disintegrants (Ac-Di-Sol(®) or Kollidon(®) CL). Results showed that sublingual absorption of sildenafil spray prepared with PG was fairly rapid. At a 0.5-mg dose, the mean onset of action was 1.3 ± 0.6 min and lasted for about 1.5 h according to the pharmacokinetic studies. In vivo studies also showed that for sublingual tablets formulated with sildenafil in PG adsorbed onto Florite(®) R at a 1:1 weight ratio then mixed with Cycloel(®) and Ac-Di-Sol(®), the onset action was fast at 1.9 ± 0.4 min and lasted for about 1 h at 0.5 mg. These findings suggest the potential for the sublingual delivery of sildenafil instead of the conventional oral administration.

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Intranasal absorption of Δ9-tetrahydrocannabinol and WIN55,212-2 mesylate in rats

Cited by 17 publications

References 19 publications

Simultaneous quantification of cannabinoids tetrahydrocannabinol, cannabidiol and CB1 receptor antagonist in rat plasma: An application to characterize pharmacokinetics after passive cannabis smoke inhalation and co-administration of rimonabant

Simultaneous quantification of cannabinoids tetrahydrocannabinol, cannabidiol and CB1 receptor antagonist in rat plasma: An application to characterize pharmacokinetics after passive cannabis smoke inhalation and co-administration of rimonabant

Development of a simple and sensitive HPLC–UV method for the simultaneous determination of cannabidiol and Δ9-tetrahydrocannabinol in rat plasma

Rapid-Onset Sildenafil Sublingual Drug Delivery Systems: In Vitro Evaluation and In Vivo Pharmacokinetic Studies in Rabbits

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