Pediatric drug formulations

Use of protease inhibitors other than LPV/r and NFV is problematic in children due to lack of suitable pediatric drug formulations for IDV and SQV (Table 10(a) and (b)). 

Because many medications are not available as liquid preparations, there are times when powder papers or suspensions must be prepared. An excellent information source about the preparation of liquid dosage forms for pediatric patients has been published by Nahata and Hippie (Nahata, M. C., Hippie, T. F. Pediatric Drug Formulations, 4th Ed. Harvey Whitney Books Cincinnati, 2000). 

Nahata, M.C. Pediatric drug formulations challenges and potential solutions. Ann. Pharmacother. 1999, dd, 247-249. 

Nahata, M.C. Hippie, T.F. Pediatric Drug Formulations, 4th Ed. Harvey Whitney Books Cincinnati, 2000. 

Nahata, M.C. Lack of pediatric drug formulations. Pediatrics 1999, 104 (3 Supplement Part 2), 607 -609. 

Nahata MC, Pai V, Hippie TF. Pediatric Drug Formulations, 5 th ed. Cincinnati, Harvey Whitney Books, 2003 1—307. 

Nahata M C, Hippie T F (2003). Pediatric Drug Formulations, 5th edn. Cincinnati, OH Harvey Whitney Books Co. 

Effective and safe drug therapy for newborns, infants, and children depends on knowledge of pediatric pharmacokinetics and pharmacodynamics and knowledge of the drug formulation and delivery issues specific to this population. 

The critical void in pediatric drug therapy now lies in effective drug-delivery systems. Some inroads have been made in the manufacturing of pediatric dosing systems, particularly OTC preparations. There needs to be a redirection of the focus in nonparenteral drug formulations towards pediatric dosage forms with proven stability and bioavailability that can be easily and accurately administered to infants and children. 

Kayumba, P. C., Huyghebaert, N., Cordelia, C., Ntawukuliryayo, J. D., Vervaet, C., and Remon, J. P. (2007). Quinine sulphate pellets for flexible pediatric drug dosing Formulation development and evaluation of taste-masking efficiency using the electronic tongue. Eur. J. Pharm. Biophurm. 66,460-465. 

Many drugs can now be delivered rectally instead of by parenteral injection (intravenous route) or oral administration. Generally, the rectal delivery route is particularly suitable for pediatric and elderly patients who experience difficulty ingesting medication or who are unconscious. However, rectal bioavailabilities tend to be lower than the corresponding values of oral administration. The nature of the drug formulation has been shown to be an essential determinant of the rectal absorption profiles. The development of novel absorption enhancers with potential efficacy without mucosal irritation (low toxicity) is very important. The delivery of peptide and protein drugs by the rectal route is currently being explored and seems to be feasible. 

Most therapeutic categories of medications used for ophthalmic purposes contain such drug formulations, and these are easily administered by mouth using a teaspoon or various modifications designed for pediatric use. 

Different consumer needs, whether for infant, child, or adult, varies the concentrations of the active ingredients in a nasal drug formulation. Fig. 4 shows a typical nasal spray system fitted with a snap-on closure. The dispensing system can be adapted to the anatomy of the patient. The actuators for pediatric application are slimmer in their geometry and the dosage volume is reduced (Fig. 5). 

Stricldey RG, Iwata Q, Wu S, et al. Pediatric drugs—a review of commercially available oral formulations. J Pharm Sci 2008 97 1731-1774. 

Pawar S, Kumar A (2002) Issues in the formulation of drugs for oral use in children role of excipients. Pediatr Drugs 4(6) 371-379... 

Formulate appropriate patient counseling information for patients undergoing drug therapy for urinary incontinence or pediatric enuresis. 

Hepatic metabolism of ethanol involves a nonlinear saturable pathway. Young children have a limited ability to metabolize and thereby detoxify ethanol. Ethanol intoxication has been recorded in children with blood levels as low as 25 mg/dL. Alcohol has a volume of distribution of approximately 0.65 L/kg. Ingestion of 20 mL of a 10% alcohol solution will produce a blood level of 25 mg/dL in a 30 pound child. The American Academy of Pediatrics (AAP) Committee on Drugs recommends that pharmaceutical formulations intended for use in children should not produce ethanol blood levels of >25 mg/dL after a single dose. 

The dosage forms most commonly employed for pediatric formulations are liquids and chewable tablets. A perceived unpleasant taste is much more evident with these dosage forms than when a drug is administered as a conventional solid oral dosage form. Second, it is widely believed that children younger than the age of 6 years have more acute taste perception than older children and adults. Taste buds and olfactory receptors are fully developed in early infancy. Loss of taste perception accompanies the aging process. 

Suspensions are two-phase systems consisting of a finely divided solid dispersed in a liquid, solid, or a gas (Table 6). They are appropriate when the drug to be incorporated is not sufficiently soluble in an ordinary solvent or cosolvent system. They are used orally and topically. Examples of compounded suspensions include pediatric oral liquids where a commercial pediatric dosage form is not available. Commercial tablets and capsules are formulated into a vehicle and can be individually flavored to the patient s preference. 

Even if a medication is available in multiple formulations and dosage forms, the prescriber must consider the absorption and distribution differences between adult and pediatric patients. Blood supply at injection or infusion site, available blood supply for unit muscle mass, and skeletal muscle mass relative to body mass vary with patient age and size, causing drug absorption to vary, as well. A rapid intravenous bolus in a pediatric patient might result in acute toxicity a slow intravenous infusion, often required in neonates, can cause erratic, unreliable drug delivery in an older child. In addition, the volume of fluid tolerated for intravenous delivery varies significantly with the age and size of the patient. The blood supply and blood flow to and from the injection site are of prime importance since a gradual decrease in blood supply per unit muscle mass is seen with maturation. In addition, the skeletal muscle mass relative to... 

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