4-way crossover Butamirate Citrate PK & Dose study, healthy volunteers

• Research type

  Research Study

• Full title

  A Randomized, Open Label, Crossover Pharmacokinetic And Dose Proportionality Study Of Butamirate Citrate At Single Doses Of 22.5, 45, 67.5 and 90 mg In Healthy Adult Volunteers.

• IRAS ID

  26907

• Sponsor organisation

  Novartis Consumer Health S.A.

• Eudract number

  2009-013380-19

• ISRCTN Number

  N/A

• Clinicaltrials.gov Identifier

  N/A

• Research summary

  Butamirate citrate (butamirate) has been used in Europe for the treatment of acute cough of any etiology since 1965 under the name of Sinecod©. Sinecod© (1.5 mg butamirate citrate per mL) syrup is approved for the symptomatic treatment of cough of various origins. Butamirate citrate is a centrally acting cough suppressant which is neither chemically, nor pharmacologically related to opium alkaloids and does not induce habit forming effects or dependence. Butamirate citrate possesses non-specific anticholinergic and bronchospasmolytic effects which facilitate the respiratory function.Butamirate citrate has a broad therapeutic margin; it is thus well tolerated, even at high doses, and well suited for cough relief in adults and children.The available clinical pharmacology data indicate that butamirate citrate is rapidly absorbed and hydrolyzed 10 minutes after oral administration (Boehner 1997). Butamirate citrate is not detected in the plasma and the urine, whereas two metabolites have been identified: 2-phenylbutyric acid and diethylamino-ethoxyethanol (Jacquot and Mahuzier 1980, 1982). These metabolites present antitussive properties; they are, like butamirate citrate itself, extensively bound to plasma proteins (about 95%) possibly accounting for the long plasma elimination half life.. The purpose of this study is to evaluate the pharmacokinetic profile and the dose proportionality of 22.5 mg, 45 mg, 67.5 mg and 90 mg butamirate citrate single doses in healthy volunteers using modern analytical techniques."

• REC name

  Wales REC 2

• REC reference

  09/WSE02/36

• Date of REC Opinion

  15 Jul 2009

• REC opinion

  Favourable Opinion