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[Evaluation of antibiotic preparations for children from a standpoint of water-solubilities]
1Department of Pharmacy, Kumamoto University Hospital, Honjo 1-1-1, Kumamoto 860-8556, Japan.
Insights
Water-solubility varies significantly among pediatric antibiotic preparations. This study categorizes antibiotics like cefaclor (CCL) and faropenem sodium (FRPM) into three groups based on their solubility, suggesting dosage-form standardization.
Area of Science:
- Pharmaceutical Sciences
- Drug Formulation
- Pediatric Pharmacology
Context:
- Antibiotic preparations for pediatric use are widely prescribed.
- Variability in drug solubility can impact therapeutic efficacy and administration.
- Current dosage-form classifications may not fully reflect solubility characteristics.
Purpose:
- To evaluate the water-solubility of seven common pediatric antibiotic preparations.
- To assess solubility of both the final preparation and the active pharmaceutical ingredient.
- To propose a classification system for pediatric antibiotic dosage forms based on solubility.
Summary:
- Seven pediatric antibiotics (cefaclor, cefpodoxime proxetil, cefdinir, cefditoren pivoxil, cefcapene pivoxil, clarithromycin, faropenem sodium) were tested for water-solubility.
- Significant differences in solubility were observed, ranging from 40% to 100% for preparations and nearly 0% to 100% for component drugs.
- Antibiotics were categorized into three groups: suitable for solution/suspension, suitable for suspension, and fine granules unsuitable for suspension.
Impact:
- Highlights the need for standardized nomenclature for pediatric antibiotic dosage forms.
- Informs healthcare providers about potential formulation differences affecting drug delivery.
- Guides pharmaceutical development towards more predictable and administrable pediatric formulations.
Abstract:
The evaluation of seven widely-used antibiotic preparations [five cephem antibiotics; cefaclor (CCL), cefpodoxime proxetil (CPDX-PR), cefdinir (CFDN), cefditoren pivoxil (CDTR-PI), cefcapene pivoxil (CFPN-PI), one macrolide; clarithromycin (CAM) and one penem; faropenem sodium (FRPM)] for children were performed from a standpoint of water-solubilities, both as a preparation and as a component drug. As the results, these preparations showed great differences in the water-solubilities when added 10 ml water to 0.5 g of each preparation. That is, their solubilities differed from about 40% (CFPN-PI) to 100% (FRPM) as a preparation, and from nearly 0% (CAM) to 100% (FRPM, CCL) as a component drug. Additionally, about a half of the insoluble residues were found to be the component drug, in the cases of three preparations (CPDX-PX, CFDN, CDTR-PI) which were solubilized at 80-90%. From these results, it was suggested that the marketed antibiotic preparations for children might be classified into three categories; i.e., [A] preparation for solution and suspension (FRPM, CCL), [B] preparation suitable to suspension (CPDX-PR, CFDN, CDTR-PI), and [C] fine granule preparation for children unsuitable to suspension (CFPN-PI, CAM). Consequently, the names for dosage-forms of these preparations should be standardized.