Amoxicillin 250 mg, Carbocisteine 150 mg Hard-gelatin capsules

Amoxicillin is an antibacterial drug [see Microbiology ( 12.4)].

Absorption:Amoxicillin is stable in the presence of gastric acid and is rapidly absorbed after oral administration. The effect of food on the absorption of amoxicillin from the tablets and suspension of amoxicillin has been partially investigated; 400 mg and 875 mg formulations have been studied only when administered at the start of a light meal.

Orally administered doses of 250 mg and 500 mg amoxicillin capsules result in average peak blood levels 1 to 2 hours after administration in the range of 3.5 mcg/mL to 5.0 mcg/mL and 5.5 mcg/mL to 7.5 mcg/mL, respectively.

Mean amoxicillin pharmacokinetic parameters from an open, two‑part, single‑dose crossover bioequivalencestudy in 27 adults comparing 875 mg of AMOXICILLIN with 875 mg of AUGMENTIN ®(amoxicillin and clavulanate potassium) showed that the 875 mg tablet of Amoxicillin produces an AUC 0-∞of 35.4 ± 8.1 mcg•hr/mL and a C maxof 13.8 ± 4.1 mcg/mL. Dosing was at the start of a light meal following an overnight fast.

Orally administered doses of amoxicillin suspension, 125 mg/5 mL and 250 mg/5 mL, result in average peak blood levels 1 to 2 hours after administration in the range of 1.5 mcg/mL to 3.0 mcg/mL and 3.5 mcg/mL to 5.0 mcg/mL, respectively.

Oral administration of single doses of 400 mg chewable tablets and 400 mg/5 mL suspension of amoxicillin to 24 adult volunteers yielded comparable pharmacokinetic data:

†Mean values of 24 normal volunteers. Peak concentrations occurred approximately 1 hour after the dose.

Distribution: Amoxicillin diffuses readily into most body tissues and fluids, with the exception of brain and spinal fluid, except when meninges are inflamed. In blood serum, amoxicillin is approximately 20% protein‑bound. Following a 1 gram dose and utilizing a special skin window technique to determine levels of the antibiotic, it was noted that therapeutic levels were found in the interstitial fluid.

Metabolism and Excretion: The half-life of amoxicillin is 61.3 minutes. Approximately 60% of an orally administered dose of amoxicillin is excreted in the urine within 6 to 8 hours. Detectable serum levels are observed up to 8 hours after an orally administered dose of amoxicillin. Since most of the amoxicillin is excreted unchanged in the urine, its excretion can be delayed by concurrent administration of probenecid [see Drug Interactions ( 7.1) ].

Carbocisteine modifies the nature and amount of respiratory mucus glycoproteins. The reference distinguishes animal mucus-secretion findings from human observations of reduced goblet-cell hyperplasia.

Carbocisteine is rapidly absorbed from the gastrointestinal tract. In the cited healthy-volunteer study, two 375 mg capsules three times daily for seven days produced a mean peak time of 2 hours and an elimination half-life of 1.87 hours, with ranges of 1–3 and 1.4–2.5 hours respectively. These values describe that capsule study and are not a dosing recommendation or a measured profile for a different combination.