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[Experimental study of an ampicillin suppository (KS-R1) in adults and children]
Insights
This study compared rectal ampicillin (KS-R1) with oral and IV forms in adults and children. Rectal KS-R1 showed faster absorption and comparable peak levels to oral ampicillin, with good bioavailability.
Area of Science:
- Pharmacology and Pharmaceutics
- Drug Delivery Systems
Context:
- Ampicillin sodium (ABPC) is a widely used antibiotic.
- Rectal drug administration offers an alternative route, particularly for pediatric patients.
- Evaluating novel rectal formulations like KS-R1 is crucial for optimizing antibiotic delivery.
Purpose:
- To compare the pharmacokinetic profile and bioavailability of KS-R1 (rectal ampicillin suppository) against oral and parenteral ampicillin.
- To assess the rectal absorption, excretion, and irritation potential of KS-R1.
- To evaluate the safety and efficacy of KS-R1 in both adult volunteers and pediatric patients.
Summary:
- Rectal administration of KS-R1 in adults resulted in a mean peak plasma concentration (Cmax) of 2.6 mcg/ml at 30 minutes, with a half-life of 0.55 hours. Peak time was faster than oral and equal to intramuscular administration.
- In pediatric patients, KS-R1 achieved higher Cmax (4.8-7.1 mcg/ml) and AUC compared to oral ampicillin, with peak plasma levels reached significantly faster.
- The relative bioavailability of KS-R1 was approximately 40% in adults, while in children, it demonstrated significantly improved absorption compared to oral ampicillin. No remarkable irritation was noted.
Impact:
- KS-R1 represents a viable alternative for ampicillin administration, potentially improving patient compliance and therapeutic outcomes, especially in pediatric populations.
- The study provides valuable pharmacokinetic data for rectal ampicillin, aiding in the development of optimized dosing strategies.
- Findings support the use of KS-R1 as an effective rectal delivery system for ampicillin, offering advantages in absorption kinetics over oral administration.
Abstract:
KS-R1, a new rectal suppository of ampicillin (ABPC) sodium, was compared with oral and parenteral ABPC in terms of absorption and excretion in childish patients and healthy adult male volunteers. In addition, the irritation of KS-R1 to the rectum was studied. 1. Eight healthy adult male volunteers received 250 mg (potency) of KS-R1 rectally and 125 mg of ABPC intravenously in a cross-over study. Then, 4 of them were given intramuscularly 250 mg of ABPC, and 3 of the remaining 4 volunteers were given 250 mg of ABPC orally. The rectal administration of 250 mg of KS-R1 resulted in a mean peak ABPC plasma level (Cmax) of 2.6 mcg/ml at 30 minutes, and then ABPC levels declined with biological half-life (T2/1) of 0.55 hour. The peak time (Tmax) of occurrence after rectal dose of KS-R1 was earlier than that after oral dose of ABPC, and was equal to that after intramuscular dose of ABPC. Cmax after rectal dose of KS-R1 was equal to that after the oral dose, and was about 40% of the value attained with the intramuscular dose. Urinary recovery of ABPC during 6 hours after rectal dose of KS-R1 was 24.0%, compared with 34.0% for the oral dose, 59.6% for the intramuscular dose and 61.4% for the intravenous dose. The relative bioavailability of KS-R1, calculated on the basis of urinary recovery after intravenous administration of ABPC, was about 40%. 2. When KS-R1 (250 mg) was given to 2 adult volunteers 3 times daily for 5 days, no remarkable difference was found in plasma concentration and urinary recovery of ABPC. The pharmacokinetic parameters following the last administration were similar to those following a single administration of KS-R1. 3. KS-R1, oral ABPC and intravenous ABPC were administered at the dose of 125 mg (potency) to 5, 4 and 3 children and at the dose of 250 mg (potency) to 5, 3 and 3 children, respectively. Peak plasma level (Cmax) of ABPC after rectal administration of 125 mg and 250 mg of KS-R1 was reached in 15 minutes, indicating 4.8 and 7.1 mcg/ml, respectively. Peak time (Tmax) of ABPC after the rectal doses of KS-R1 was about 2 hours earlier than that after oral doses of ABPC. Cmax after KS-R1 was 3-4 times as high as that after the oral doses. Area under the curve (AUC) with KS-R1 was 1.38-1.55 times greater than that of oral ABPC, and about 24% of the values obtained with intravenous doses of ABPC. Urinary recoveries of ABPC rectal doses of KS-R1 were 30.4 to 45.6%, compared with 29.2 to 30.8% for the oral doses and 61.1 to 76.1% for the intravenous doses.(ABSTRACT TRUNCATED AT 400 WORDS)