Cefzil

[Cefprozil]

Clinical Pharmacology
CLINICAL PHARMACOLOGY

The pharmacokinetic data were derived from the capsule formulation; however, bio-equivalence has been demonstrated for the oral solution, capsule, tablet, and suspen-sion formulations under (C max ) of cefprozil. However, there was an increase of 0.25 to 0.75 hours in the time to maximum plasma concentra-tion of cefprozil (T max ). The bioavailability of the capsule formulation of cefprozil was not affected when administered 5 minutes following an antacid. Plasma protein binding is approximately 36% and is infasting conditions.

Following oral administration of cefprozil to fasting subjects, approximately 95% of the dose was absorbed. The average plasma half-life in normal subjects was 1.3 hours, while the steady-state volume of distribution was estimated to be 0.23 L/ kg. The total body clearance and renal clearance rates were approximately 3 mL/ min/ kg and 2.3 mL/ min/ kg, respectively.

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Average peak plasma concentrations after administration of 250 mg, 500 mg, or 1 g doses of cefprozil to fasting subjects were approximately 6.1, 10.5, and 18.3 µg/ mL, respectively, and were obtained within 1.5 hours after dosing. Urinary recovery account-ed for approximately 60% of the administered dose. (See Table.)
Dosage Mean Plasma Cefprozil 8-hour Urinary (mg) Concentrations (µg / mL)* Excretion (%)

Peak appx. 1.5 h 4 h 8 h

250 mg 6.1 1.7 0.2 60% 500 mg 10.5 3.2 0.4 62%
1000 mg 18.3 8.4 1.0 54%
*Data represent mean values of 12 healthy volunteers.

During the first 4-hour period after drug administration, the average urine con-centrations following 250 mg, 500 mg, and 1 g doses were approximately 700 µg/ mL, 1000 µg/ mL, and 2900 µg/ mL, respectively. Administration of CEFZIL tablet or suspension formulation with food did not affect the extent of absorption (AUC) or the peak plasma concentration dependent of concentration in the range of 2 µg/ mL to 20 µg/ mL. There was no evidence of accumulation of cefprozil in the plasma in individuals with normal renal function following multiple oral doses of up to 1000 mg every 8 hours for 10 days.

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