Guaifenesin - CAS 93-14-1
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Guaifenesin is thought to act as an expectorant.
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1.Ethylcellulose film coating of guaifenesin-loaded pellets: A comprehensive evaluation of the manufacturing process to prevent drug migration.
Melegari C1, Bertoni S1, Genovesi A2, Hughes K2, Rajabi-Siahboomi AR3, Passerini N1, Albertini B4. Eur J Pharm Biopharm. 2016 Mar;100:15-26. doi: 10.1016/j.ejpb.2015.12.001. Epub 2015 Dec 11.
The aim of the research was to investigate the complete process of pellet production in a Wurster fluidized bed coater in order to determine the main factors affecting the migration phenomenon of a soluble API through the ethycellulose film coating (Surelease®) and hence the long-term stability of the controlled release pellets. Guaifenesin (GFN), as BCS class I model drug, was layered on sugar spheres using a binder-polymer solution containing the dissolved GFN. The drug loaded pellets were then coated with Surelease®. The influence of drug loading (4.5-20.0% w/w), curing conditions (40-60°C and dynamic-static equipment), coating level (12-20% theoretical weight gain) and composition of the binder-layering solution (hypromellose versus Na alginate) on process efficiency (RSDW%), GFN content uniformity (RSDC%), GFN solid state (DSC and XRD) and pellet release profiles was evaluated. The effectiveness of the Surelease film was strongly affected by the ability of GFN to cross the coating layer and to recrystallize on the pellet surface.
2.Pharmacokinetics of guaifenesin following administration of multiple doses to exercised Thoroughbred horses.
Knych HK1,2, Stanley SD1,2, Benson D3, Arthur RM4. J Vet Pharmacol Ther. 2016 Jan 14. doi: 10.1111/jvp.12287. [Epub ahead of print]
Guaifenesin is an expectorant commonly used in performance horses to aid in the clearance of mucus from the airways. Guaifenesin is also a centrally acting skeletal muscle relaxant and as such is a prohibited drug with withdrawal necessary prior to competition. To the authors' knowledge, there are no reports in the literature describing single or multiple oral administrations of guaifenesin in the horse to determine a regulatory threshold and related withdrawal time. Therefore, the objective of the current study was to describe the pharmacokinetics of guaifenesin following oral administration in order to provide data upon which appropriate regulatory recommendations can be established. Nine exercised Thoroughbred horses were administered 2 g of guaifenesin orally BID for a total of five doses. Blood samples were collected immediately prior to drug administration and at various times postadministration. Serum guaifenesin concentrations were determined and pharmacokinetic parameters calculated.
3.Guaifenesin Pharmacokinetics Following Single-Dose Oral Administration in Children Aged 2 to 17 Years.
Thompson GA1, Solomon G2, Albrecht HH3, Reitberg DP4, Guenin E2. J Clin Pharmacol. 2015 Dec 3. doi: 10.1002/jcph.682. [Epub ahead of print]
This study characterized guaifenesin pharmacokinetics in children aged 2-17 years (N = 40) who received a single oral dose of guaifenesin (age-based doses of 100-400 mg) 2 hours after breakfast. Plasma samples were obtained before and for 8 hours after dosing and analyzed for guaifenesin using liquid chromatography-tandem mass spectrometry. Pharmacokinetic parameters were estimated using non-compartmental methods, relationships with age were assessed using linear regression and dose proportionality was assessed on 95% confidence intervals. Based on the upper dose recommended in the monograph (for both children and adolescents), area under the curve from time zero to infinity and maximum plasma concentration increased with age. However, when comparing the upper dose for children aged 2-11 years with the lower dose for adolescents aged 12-17 years, similar systemic exposure was observed. As expected due to increasing body size, oral clearance (CLo ) and terminal volume of distribution (Vz /F) increased with age.
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CAS 93-14-1 Guaifenesin

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