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Related Concept Videos

Pharmacokinetics in Pediatric Patients: Drug Excretion01:26

Pharmacokinetics in Pediatric Patients: Drug Excretion

In pediatric medicine, understanding the renal function and drug elimination nuances is crucial for administering safe and effective treatments. Newborns, in particular, display markedly slower renal functions than adults, profoundly affecting how drugs are cleared from their bodies. This slower drug clearance requires clinicians to extend the dosing intervals for many medications to prevent drug accumulation and toxicity while ensuring therapeutic efficacy.One key area where these adjustments...
Pharmacokinetics in Pediatric Patients: Overview and Drug Absorption01:23

Pharmacokinetics in Pediatric Patients: Overview and Drug Absorption

Understanding the physiological differences in the pediatric population is crucial for effective pharmacotherapy. Neonates, infants, and children exhibit significant variations in gastric pH, gastric emptying time, intestinal transit time, and biliary function. These variations profoundly affect oral drug absorption, necessitating a nuanced approach to pediatric dosing.Neonates present with a unique physiological profile, having a gastric pH greater than 4 and faster and more irregular gastric...
Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence01:27

Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence

Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
Pharmacokinetics in Pediatric Patients: Drug Metabolism01:24

Pharmacokinetics in Pediatric Patients: Drug Metabolism

In pediatric care, understanding the nuances of hepatic drug metabolism is crucial, as it significantly differs from that of adults. This divergence is primarily due to the developmental stage of drug-metabolizing enzymes, which affects how medications are processed in the body. In neonates, for instance, the activity of Phase I enzymes—critical for the initial breakdown of drugs—is markedly reduced, functioning at just 20–40% of the levels seen in adults. This reduction poses a challenge in...
Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...

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Updated: May 16, 2026

Methods Development for Blood Borne Macrophage Carriage of Nanoformulated Antiretroviral Drugs
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Published on: December 9, 2010

Pharmaceutical development and optimization of azithromycin suppository for paediatric use.

Tina Kauss1, Alexandra Gaubert, Chantal Boyer

  • 1Univ. Bordeaux, EA 4575 Analytical and Pharmaceutical Developments Applied to Neglected Diseases and Counterfeits, Bordeaux, France. tina.kauss@u-bordeaux2.fr

International Journal of Pharmaceutics
|December 11, 2012
PubMed
Summary

A new rectal azithromycin suppository offers a stable, easy-to-use alternative for pediatric patients, especially in tropical regions. This formulation demonstrates comparable bioavailability to oral forms, aiding antibiotic treatment in underserved areas.

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Published on: March 11, 2017

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Pediatric Formulations

Background:

  • Existing azithromycin formulations (oral, injectable) present challenges for pediatric use, particularly in resource-limited or tropical settings.
  • Need for a stable, user-friendly, and cost-effective pediatric formulation with reliable bioavailability is critical for effective antibiotic therapy.

Purpose of the Study:

  • To develop and optimize a novel pediatric rectal formulation of azithromycin.
  • To achieve a target product profile including ease of use, stability in tropical conditions, comparable bioavailability to oral forms, and rapid bactericidal concentrations.

Main Methods:

  • Characterization of polyethylene glycol (PEG) solid solution suppositories using in vitro analyses (visual, HPLC, DSC, FTIR, XRD).
  • Assessment of in vitro drug release and in vivo bioavailability in rabbits.
  • Comparative bioavailability study against rectal solution, intravenous product, and a previous non-optimized suppository formulation.

Main Results:

  • The optimized solid solution suppository demonstrated a relative bioavailability of 43% compared to intravenous administration, exceeding the target of 38% (human oral).
  • Preliminary 3-month stability and feasibility studies indicated suitability for industrial scale-up.
  • The formulation showed good in vitro drug release characteristics.

Conclusions:

  • The developed azithromycin solid solution suppository is a promising rectal formulation for pediatric use.
  • This formulation offers a viable alternative for treating infections, particularly in severely ill children in rural and tropical areas.
  • Further development with industrial partners is warranted to bring this product to market.