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Dose escalation pharmacokinetics of intranasal scopolamine gel formulation

2014; Wiley; Volume: 55; Issue: 2 Linguagem: Inglês

10.1002/jcph.391

1552-4604

Lei Wu, Jason Boyd, Vernie Daniels, Zuwei Wang, Diana S.‐L. Chow, Lakshmi Putcha,

Cholinesterase and Neurodegenerative Diseases

The Journal of Clinical PharmacologyVolume 55, Issue 2 p. 195-203 Pharmacokinetics Dose escalation pharmacokinetics of intranasal scopolamine gel formulation Lei Wu BS, Lei Wu BS University of Houston Houston, College of Pharmacy, Houston, TX, USASearch for more papers by this authorJason L. Boyd PhD, Jason L. Boyd PhD Universities Space Research Association, Houston, TX, USASearch for more papers by this authorVernie Daniels MS, RPh, Vernie Daniels MS, RPh Wyle Laboratories, Houston, TX, USASearch for more papers by this authorZuwei Wang PhD, Zuwei Wang PhD Wyle Laboratories, Houston, TX, USASearch for more papers by this authorDiana S-L. Chow PhD, Diana S-L. Chow PhD University of Houston Houston, College of Pharmacy, Houston, TX, USASearch for more papers by this authorLakshmi Putcha PhD, Corresponding Author Lakshmi Putcha PhD NASA Johnson Space Center, Houston, TX, USA Corresponding Author: Lakshmi Putcha, PhD, FCP, NASA Johnson Space Center, 2101 NASA Parkway, MC: SK3, Houston, TX, USA Email: [email protected]Search for more papers by this author Lei Wu BS, Lei Wu BS University of Houston Houston, College of Pharmacy, Houston, TX, USASearch for more papers by this authorJason L. Boyd PhD, Jason L. Boyd PhD Universities Space Research Association, Houston, TX, USASearch for more papers by this authorVernie Daniels MS, RPh, Vernie Daniels MS, RPh Wyle Laboratories, Houston, TX, USASearch for more papers by this authorZuwei Wang PhD, Zuwei Wang PhD Wyle Laboratories, Houston, TX, USASearch for more papers by this authorDiana S-L. Chow PhD, Diana S-L. Chow PhD University of Houston Houston, College of Pharmacy, Houston, TX, USASearch for more papers by this authorLakshmi Putcha PhD, Corresponding Author Lakshmi Putcha PhD NASA Johnson Space Center, Houston, TX, USA Corresponding Author: Lakshmi Putcha, PhD, FCP, NASA Johnson Space Center, 2101 NASA Parkway, MC: SK3, Houston, TX, USA Email: [email protected]Search for more papers by this author First published: 04 September 2014 https://doi.org/10.1002/jcph.391Citations: 4Read the full textAboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinkedInRedditWechat Abstract Astronauts experience Space Motion Sickness requiring treatment with an anti-motion sickness medication, scopolamine during space missions. Bioavailability after oral administration of scopolamine is low and variable, and absorption form transdermal patch is slow and prolonged. Intranasal administration achieves faster absorption and higher bioavailability of drugs that are subject to extrahepatic, first pass metabolism after oral dosing. We examined pharmacokinetics of 0.1, 0.2, and 0.4 mg doses of the Investigational New Drug formulation of intranasal scopolamine gel (INSCOP) in 12 healthy subjects using a randomized, double-blind cross-over study design. Subjects received one squirt of 0.1 g of gel containing either 0.1 mg or 0.2 mg/0.1 mL scopolamine or placebo in each nostril. Serial blood samples and total urine voids were collected after dosing and drug concentrations were determined using a modified LC-MS-MS method. Results indicate dose-linear pharmacokinetics of scopolamine with linear increases in Cmax and AUC within the dose range tested. Plasma drug concentrations were significantly lower in females than in males after administration of 0.4 dose. All three doses were well tolerated with no unexpected or serious adverse side effects reported. These results suggest that intranasal scopolamine gel formulation (INSCOP) offers a fast, reliable, and safe alternative for the treatment of motion sickness. Citing Literature Volume55, Issue2February 2015Pages 195-203 RelatedInformation