Chloroquine absorption in children from polyethylene glycol base suppositories

Area of Science:

• Pharmacology
• Pharmaceutical Sciences
• Pediatric Medicine

Background:

• Chloroquine phosphate (CP) is a vital antimalarial and antirheumatic drug.
• Effective drug delivery systems are crucial for pediatric patient populations.
• Rectal administration offers an alternative route for drug delivery in children.

Purpose of the Study:

• To formulate and evaluate chloroquine phosphate (CP) suppositories for pediatric rectal administration.
• To assess the pharmacokinetic profile of CP following rectal administration in children.
• To determine the therapeutic potential of CP suppositories for malaria and rheumatoid disease.

Main Methods:

• Chloroquine phosphate (CP) was formulated into suppositories using a polyethylene glycol (PEG) base (PEG 1000 and PEG 6000 in a 7:3 ratio) with 0.5% polysorbate 80 as an absorption enhancer.
• Pharmacokinetic parameters, including peak blood levels and elimination half-lives, were determined in pediatric subjects (mean weight 10 kg, age 21 months) after rectal administration of 200 mg and 300 mg CP suppositories.
• Blood samples were analyzed to measure CP concentrations over time.

Main Results:

• Peak chloroquine blood levels in children were 0.67 ± 0.08 µg/mL (200 mg CP) and 1.06 ± 0.23 µg/mL (300 mg CP), with a baseline of 0.30 ± 0.02 µg/mL.
• Elimination half-lives were calculated as 3.3 hours (200 mg CP) and 2.7 hours (300 mg CP).
• The 300 mg CP suppository achieved blood levels considered therapeutic for malaria and rheumatoid disease.

Conclusions:

• Rectal administration of chloroquine phosphate (CP) suppositories in children yields potentially therapeutic blood concentrations.
• The developed suppository formulation, incorporating PEG and polysorbate 80, demonstrates feasibility for pediatric drug delivery.
• Further clinical studies are warranted to confirm the efficacy and safety of CP suppositories in treating pediatric malaria and rheumatoid disease.