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Related Concept Videos

Pharmaceutical Alternatives: Stability-Related Therapeutic Nonequivalence01:22

Pharmaceutical Alternatives: Stability-Related Therapeutic Nonequivalence

Generic intravenous (IV) drugs are considered bioequivalent to their branded counterparts due to their 100% bioavailability upon administration. However, variations in stability among different drug products can significantly influence their therapeutic performance, even if they are pharmaceutically equivalent.Cefuroxime, a prophylactic antimicrobial, is often used as a single-dose IV injection for patients undergoing coronary artery bypass grafting surgery. A 3 g dose typically provides...
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...
Drug Distribution: Plasma Protein Binding01:29

Drug Distribution: Plasma Protein Binding

Drugs predominantly attach to plasma proteins, with only a small percentage remaining unbound. The unbound portion can be calculated as one minus the bound fraction. Acidic drugs form large, inactive complexes by reversibly binding to plasma albumin, which prevents them from diffusing across biological barriers. These drug-protein complexes act as reservoirs for the drugs. As the concentration of unbound drugs decreases, these complexes quickly dissociate to release the free drug, maintaining...
Drug Distribution: Tissue Binding01:21

Drug Distribution: Tissue Binding

Upon entering the systemic circulation, drugs can distribute into the interstitial and intracellular fluid of various tissue cells. This distribution is facilitated by the binding of drugs to different cellular components within tissues, which may lead to drug accumulation in specific areas. Drugs bound to tissue components serve as reservoirs that release free drugs back into the system, prolonging the drug's overall action. However, this accumulation can also result in local toxicity.
For...
Modified-Release Drug Delivery Systems: Bioavailability01:30

Modified-Release Drug Delivery Systems: Bioavailability

Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
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Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics

All neuromuscular blocking agents are injected intravenously because they are poorly absorbed from the GI tract. Rapid onset is achieved with intravenous administration, although absorption is also adequate from an intramuscular injection. Since these agents are highly ionized, they do not readily penetrate cell membranes or cross the blood-brain barrier.
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Related Experiment Video

Updated: May 12, 2026

A Reference Broth Microdilution Method for Dalbavancin In Vitro Susceptibility Testing of Bacteria that Grow Aerobically
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A Reference Broth Microdilution Method for Dalbavancin In Vitro Susceptibility Testing of Bacteria that Grow Aerobically

Published on: September 9, 2015

Oral availability of bilastine.

B Sádaba1, A Gómez-Guiu, J R Azanza

  • 1Clinical Research Unit, Servicio de Farmacología Clínica, Clínica Universidad de Navarra, c/Pío XII, n° 36, 31008, Pamplona, Navarra, Spain. bsadaba@unav.es

Clinical Drug Investigation
|March 27, 2013
PubMed
Summary
This summary is machine-generated.

Bilastine, a non-sedating antihistamine, demonstrated moderate oral bioavailability of 60.67% in healthy adults. This study assessed the absorption of bilastine following oral administration.

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Multiplex Therapeutic Drug Monitoring by Isotope-dilution HPLC-MS/MS of Antibiotics in Critical Illnesses
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Multiplex Therapeutic Drug Monitoring by Isotope-dilution HPLC-MS/MS of Antibiotics in Critical Illnesses

Published on: August 30, 2018

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Last Updated: May 12, 2026

A Reference Broth Microdilution Method for Dalbavancin In Vitro Susceptibility Testing of Bacteria that Grow Aerobically
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Multiplex Therapeutic Drug Monitoring by Isotope-dilution HPLC-MS/MS of Antibiotics in Critical Illnesses
11:17

Multiplex Therapeutic Drug Monitoring by Isotope-dilution HPLC-MS/MS of Antibiotics in Critical Illnesses

Published on: August 30, 2018

Area of Science:

  • Pharmacology
  • Clinical Pharmacology

Background:

  • Bilastine is a novel, non-sedating H1 receptor antagonist for allergic rhinitis and urticaria.
  • Clinical trials have established the efficacy and safety of bilastine.

Purpose of the Study:

  • To determine the absolute oral bioavailability of bilastine in humans.
  • To characterize the pharmacokinetic profile of bilastine after oral administration.

Main Methods:

  • A randomized, single-dose, open-label, two-arm crossover study.
  • Twelve healthy adults received either a 20-mg oral tablet or a 10-mg intravenous formulation of bilastine.
  • Blood and urine samples were collected for pharmacokinetic analysis.

Main Results:

  • The absolute oral bioavailability of bilastine was determined to be 60.67%.
  • The maximum concentration of bilastine occurred at 1.31 hours post-oral administration.
  • Pharmacokinetic parameters were consistent with previous findings, and the drug was well-tolerated.

Conclusions:

  • Bilastine is rapidly absorbed after oral administration in healthy subjects.
  • The absolute oral bioavailability of bilastine is moderate.