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Drug Formulation in Pediatrics: If it tastes bad it must be good for you

Drug Formulation in Pediatrics: If it tastes bad it must be good for you. Jeffrey Blumer, Ph.D., M.D. Professor of Pediatrics and Pharmacology Case Western Reserve University Chief, Pediatric Pharmacology and Critical Care Rainbow Babies and Children’s Hospital Cleveland, Ohio.

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Drug Formulation in Pediatrics: If it tastes bad it must be good for you

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  1. Drug Formulationin Pediatrics:If it tastes bad it must be good for you Jeffrey Blumer, Ph.D., M.D.Professor of Pediatrics and PharmacologyCase Western Reserve University Chief, Pediatric Pharmacology and Critical CareRainbow Babies and Children’s HospitalCleveland, Ohio

  2. Drug Treatmentfor Infants and Children– The Challenge – • Pediatric Patients are dynamic with respect to drug disposition • Developmental changes in body composition • Developmental changes in drug metabolism • Developmental changes in organ function

  3. Drug Treatmentfor Infants and Children– The Challenge – • Pediatric patients are different with respect to drug action • Ontogeny of receptor expression and function • Greater regenerative and recuperative potential • Unique disease processes • Patients with chronic diseases will undergo growth and developmental changes during therapy

  4. Practical Issuesin Pediatric Drug Dosing • Traditionally pediatric dosing is weight based (mg/kg) • Drug dose will often require change as the child grows • Parenteral dosage forms often require significant dilution prior to administration • Children are often unable to swallow pills or capsules until they are 6 (or 7 or 12 or never) years of age

  5. Practical Issuesin Pediatric Drug Dosing • Complex solid dosage forms (e.g. sustained release preparations) are not engineered with consideration of pediatric GI physiology • Palatability is the major determinant of compliance with treatment with oral liquids and chewable/dissolving dosage forms • Dosing of young children generally depends on parent/guardian

  6. Intravenous Solutions Emulsions Oral Solutions Suspensions Elixirs Syrups Granules Tablets Effervescent tablets Chewable tablets Drops Rectal Solutions Foams Cutaneous Creams Ointments Percutaneous Patches Formulations Availablefor Treating Infants and Children

  7. Pediatric Formulation Methods • Bona fide pediatric formulations (e.g., drops, suspensions, chewable tablets or syrups) • Extemporaneous pediatric formulations made with “standardized” extemporaneous vehicles (e.g., NF, USP, or marketed vehicles) • Extemporaneous pediatric formulations made with food (e.g., sprinkles on applesauce or yogurt)

  8. Determinants of the Typeof Formulation for Children • Age • Ability to handle solid dosage forms • Disease / Disorder being treated

  9. Recommended Drug Formulations for Infantsand Children • Oral solutions • Oral suspensions • Rapidly dissolving tablets • Sprinkles/sachets • Transcutaneous delivery systems • Implantable reservoirs

  10. The Pediatric Holy Grail AnOralLiquidPreparation

  11. Statement of thePediatric Pharmacy Advocacy Grouphttp://www.ppag.org/ For every new chemical entity and currently marketed drug still under patent, with or without safety and effectiveness data in children, where no oral liquid dosage form is available, the manufacturer should be required to provide a formulation that effectively converts an oral solid or intravenous dosage form to an oral solution or suspension dosage form.

  12. Is This What We ReallyWant / Need?

  13. Pediatric Formulation Approaches • Proprietary – Liquids, suspensions, chewable tablets • Extemporaneous preparations • Compounded with known vehicles • Crushed solid dosage forms

  14. Oral Formulations for Children– The Down Side – • Solutions often contain potentially toxic excipients • Suspensions often result in unequal drug delivery over time due to nonuniform dispersal • Suspensions often have palatability problems due to both taste and texture • Sprinkles/sachets often have erratic absorption • Transcutaneous delivery systems depend on uniform nature of integument

  15. Issues Affecting Extemporaneous Preparations • Stability • Bioavailability • Nonuniform composition • Variable effect of food

  16. The Food Myth • Generally accepted that food may affect bioavailability • “Not all applesauce is created equal”S. Hirschfeld M.D., Ph.D. • Generally little impact • No studies dealing with foods children actually eat

  17. Results to Date Bona fide • Many antivirals • Atovaquone/proguanil • Ibuprofen/ pseudoephedrine • Gabapentin • Midazolam Extemporaneous “standardized” • Enalapril • Sotalol Sprinkles • Topiramate • Montelukast

  18. “Bona Fide” Applications – Pediatric Antivirals Zidovudine Oral Solution Didanosine Powder (reconstitute with antacid) Lamivudine Oral Solution Abacavir Oral Solution Nevirapine Suspension Efavirenz Capsules (50 mg for 7 kg patient) Ritonavir Solution Nelfinavir mesylate Oral Powder (mix with foods) Amprenavir Oral Solution (propylene glycol) Lopinavir/Ritonavir Oral Solution Acyclovir Oral Suspension Ribavirin Powder for Inhalation Solution Oseltamavir phosphate Suspension

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