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[Basic and clinical studies on clarithromycin in pediatrics]
Insights
Clarithromycin (TE-031) pediatric studies show it maintains high blood concentrations and is efficiently excreted. Bioavailability is slightly better when taken on an empty stomach, with granular and tablet forms showing equivalent absorption and excretion.
Area of Science:
- Pharmacology
- Pediatric Medicine
- Antibiotic Research
Background:
- Clarithromycin (TE-031) is a novel macrolide antibiotic developed for pediatric use.
- Studies evaluated pediatric pharmacokinetic profiles of granular and 50 mg tablet formulations.
Observation:
- Serum concentrations, urinary excretion, and half-life were assessed in children following oral administration.
- Administration timing (pre-meal vs. post-meal) and formulation type (granular vs. tablet) were investigated.
Findings:
- TE-031 demonstrated sustained high serum concentrations and efficient urinary excretion compared to conventional macrolides.
- Preprandial administration resulted in slightly superior bioavailability, with peak serum concentrations occurring earlier.
- Granular and 50 mg tablet formulations exhibited comparable absorption and excretion profiles.
Implications:
- TE-031 offers a promising pharmacokinetic profile for pediatric infections.
- Administration guidelines should consider preprandial dosing for potentially enhanced efficacy.
- The equivalence of different formulations simplifies pediatric dosing regimens.
Abstract:
Clarithromycin (TE-031, A-56268) is a new macrolide antibiotic developed by Taisho Pharmaceutical Co., Ltd. Basic and clinical studies in the field of pediatrics were carried out on a granular preparation and 50 mg tablets of TE-031 designed for use in children. The following results were obtained. 1. Concentrations of TE-031 in the serum and its excretion in the urine were investigated in children. Six children were orally administered with a TE-031 granular preparation at 10 mg/kg in a cross-over study 30 minutes before meal and 30 minutes after meal. When the drug was ingested before meal, the mean peak serum concentration occurred 1 hour later and was 5.32 +/- 1.20 micrograms/ml. The mean half-life of TE-031 in the serum was 3.6 +/- 1.0 hours, and drug levels decreased to 1.94 +/- 0.55 micrograms/ml at 6 hours after dosing. In cases of the postprandial administration, the mean peak serum level was 4.21 +/- 1.25 micrograms/ml, occurring 2 hours after ingestion. The mean serum half-life in these cases was 3.5 +/- 1.3 hours, and serum levels decreased to 1.66 +/- 0.47 micrograms/ml at 6 hours after dosing. Mean urinary recovery rates during the initial 6 hours after ingestion were 30.5 +/- 6.4% in the cases of preprandial administration and 34.7 +/- 7.3% with postprandial administration. In addition, 30 minutes before meal, 50 mg tablets of TE-031 were orally administered to 3 children in a dose level equivalent to approximately 10 mg/kg, followed by monitoring of serum and urinary levels. It was found that the mean serum concentration showed a peak value of 4.10 +/- 0.44 micrograms/ml at 2 hours after dosing, the mean serum half-life was 3.5 +/- 0.7 hours, and the mean level fell to 1.90 +/- 0.55 micrograms/ml by 6 hours after dosing. The mean 6-hour urinary recovery rate was 32.7 +/- 12.1%. On the basis of the above results, it has been surmised that, in comparison to conventional macrolide antibiotics. TE-031 is better maintained in the blood at a high concentration and is more efficiently excreted into the urine. In addition, the data show that the bioavailability of TE-031 is slightly superior when the drug is administered on an empty stomach compared with after a meal. And finally, it was found that the granular and 50 mg tablet preparations of TE-031 are almost equivalent in terms of the absorption and the excretion of the drug.(ABSTRACT TRUNCATED AT 400 WORDS)