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Pharmacokinetic Studies in Healthy Subjects for the Development of an Extended‐Release Tablet Formulation of Guaifenesin: A 505(b)(2) New Drug Application Approval
Author(s) -
Vilson Lineau,
Owen Joel S.
Publication year - 2013
Publication title -
clinical pharmacology in drug development
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.711
H-Index - 22
eISSN - 2160-7648
pISSN - 2160-763X
DOI - 10.1002/cpdd.8
Subject(s) - medicine , bioequivalence , dosing , pharmacokinetics , pharmacology , anesthesia
Guaifenesin is an expectorant used to improve mucociliary clearance (MCC) and relieve chest congestion from upper respiratory tract infections. Immediate‐release (IR) guaifenesin requires dosing every 4 hours to maintain efficacy because of the drug's short half‐life. Extended‐release (ER) guaifenesin has been developed to prolong efficacy and reduce dosing frequency. As part of the 505(b)(2) new drug application (NDA), the pharmacokinetics (PK) of an ER bi‐layer tablet formulation of guaifenesin (Mucinex®) and bioequivalence to an over‐the‐counter (OTC) monograph IR formulation were evaluated in healthy subjects. In one study, subjects received 1,200 mg ER guaifenesin every 12 hours or 400 mg IR guaifenesin every 4 hours for 6 days. Steady‐state exposures were equivalent between the two products, as demonstrated by AUC and C max . In another study, subjects received a single dose of 600 mg (fasted) or 1,200 mg (fasted or fed) ER bi‐layer tablet formulations. AUC and C max were equivalent between both states for the 1,200 mg ER dose. However, T max of 1,200 mg ER guaifenesin was later in the fed than the fasted state. ER guaifenesin is bioequivalent to corresponding OTC monograph doses of IR guaifenesin. ER guaifenesin offers a convenient 12‐hour dosing alternative to 4‐hour dosing of IR guaifenesin.