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[Experimental and clinical evaluation of an ampicillin suppository (KS-R1) in children]
Insights
Rectal ampicillin (ABPC) via KS-R1 suppository showed rapid absorption in children, with peak plasma levels achieved within 20 minutes. Clinical trials demonstrated high effectiveness and pathogen eradication in pediatric infections.
Area of Science:
- Pharmacology
- Pediatrics
- Infectious Diseases
Context:
- Pediatric infections require effective and safe antimicrobial delivery methods.
- Rectal administration of medications can be a viable alternative for children, especially when oral intake is difficult.
- Ampicillin is a widely used antibiotic for various bacterial infections.
Purpose:
- To evaluate the pharmacokinetic profile of ampicillin (ABPC) delivered via a novel rectal suppository formulation (KS-R1) in pediatric patients.
- To assess the clinical effectiveness and tolerability of KS-R1 in treating infections in children.
- To determine the dose-response relationship and absorption characteristics of rectal ampicillin.
Summary:
- Rectal administration of KS-R1 (125 and 250 mg) in 154 children resulted in peak ampicillin plasma levels within 15-20 minutes, varying by age group.
- Dose-dependent increases in plasma ampicillin levels were observed with doses ranging from <10.9 mg/kg to >21.0 mg/kg.
- KS-R1 demonstrated excellent clinical effectiveness in 51 pediatric patients with various infections, achieving pathogen eradication in all cases studied. Adverse events like insertion pain and discharge were minimal and comparable to other suppositories.
Impact:
- The study establishes KS-R1 as a potentially effective rectal formulation for ampicillin delivery in pediatric populations.
- Findings support the use of rectal ampicillin for treating pediatric infections, offering an alternative route of administration.
- The pharmacokinetic and efficacy data provide a basis for further clinical development and application of KS-R1 in pediatric care.
Abstract:
Plasma levels of ampicillin (ABPC) after the single rectal insertion of KS-R1 at doses of 125 and 250 mg in 154 children reached a peak at 11 approximately 15 minutes in children of age less than 1 year old, at 16 approximately 20 minutes in children of 1 approximately 3 years, 4 approximately 6 years and more than 7 years old with the highest levels of 11.50, 8.69, 10.33 and 8.30 micrograms/ml, respectively. Highest plasma levels of ABPC were 6.48, 8.00, 12.32 and 17.83 micrograms/ml by the administration of KS-R1 at doses of less than 10.9 mg/kg, 11.0 approximately 15.9, 16.0 approximately 20.9 mg/kg and more than 21.0 mg/kg, respectively, with dose-dependent response which were observed at 11 approximately 15 minutes or 16 approximately 20 minutes. There was no difference of plasma levels between the administration of 125 and 250 mg of KS-R1. The pain of insertion was observed in 0.6% of total 167 cases, the feeling of defecation in 2.4% and the discharge of suppository or its dissolved material or defecation within 30 minutes after insertion in 12.6%, without the influence of patients ages and dosage level. These figures were almost the same as those after the insertion of other suppositories such as erythromycin suppository or antipyretic suppository. Clinical effectiveness of KS-R1 was examined in 51 childish patients with various infections. KS-R1 was rectally given to them at doses of average 41.6 mg/kg/day divided into 3 to 4 times for 7 days. All cases showed excellent and good effects. Bacteriologically, all pathogens which were isolated from 12 patients were eradicated.