Classification of orally administered drugs on the World Health Organization Model list of Essential Medicines according to the biopharmaceutics classification system

Lindenberg, Marc; Kopp, Sabine; Dressman, Jennifer B.

doi:10.1016/j.ejpb.2004.03.001

Cited by 728 publications

(503 citation statements)

References 219 publications

Supporting

Mentioning

453

Contrasting

Unclassified

Order By: Relevance

“…This results in decreased absorption and bioavailability of low permeability drugs that are sensitive to changes in gastrointestinal (GI) motility and transit time 10, 11. Lamivudine is a highly soluble and well‐absorbed drug with an absolute bioavailability of 86% in adults5; however, there are conflicting reports as to whether lamivudine is a low or high permeability drug,12 with the results of an in vitro Caco‐2 study characterizing its permeability as moderate 13. Although the lamivudine oral solution itself does not contain sorbitol, if the permeability of lamivudine is in the low‐to‐moderate range, it may be susceptible to an absorption‐based interaction with sorbitol present in coadministered antiretroviral drugs, such as abacavir oral solution and nevirapine suspension, as well as other chronically administered liquid formulations of prescription or over‐the‐counter medications used to treat comorbidities.…”

mentioning

confidence: 99%

Effect of Sorbitol on the Pharmacokinetic Profile of Lamivudine Oral Solution in Adults: An Open‐Label, Randomized Study

Adkison¹,

Wolstenholme

Lou

et al. 2017

Clin Pharma and Therapeutics

View full text Add to dashboard Cite

In children aged ≤4 years, the relative bioavailability of lamivudine oral solution was 37% lower than that of a tablet formulation. An open‐label, four‐way crossover study was conducted in healthy adults to evaluate the effect of sorbitol, a common liquid excipient, on the pharmacokinetics of lamivudine oral solution (ClinicalTrials.gov identifier, NCT02634073). Sixteen subjects were randomized to one of four sequences consisting of four doses of lamivudine 300 mg (10 mg/mL) alone or with sorbitol 3.2, 10.2, or 13.4 g. Sorbitol 3.2, 10.2, and 13.4 g decreased lamivudine maximum concentration (C max) by 28%, 52%, and 55% and area under the concentration–time curve from time 0 to 24 h (AUC0‐24) by 20%, 39%, and 44%, respectively. Three subjects (19%) reported five nonserious adverse events (one drug‐related). The dose‐dependent effects of sorbitol on lamivudine C max and AUC0‐24 reveal an absorption‐based interaction that may decrease lamivudine exposure in patients coadministered sorbitol‐containing medicines.

show abstract

mentioning

confidence: 99%

Effect of Sorbitol on the Pharmacokinetic Profile of Lamivudine Oral Solution in Adults: An Open‐Label, Randomized Study

Adkison¹,

Wolstenholme

Lou

et al. 2017

Clin Pharma and Therapeutics

View full text Add to dashboard Cite

show abstract

“…Moreover, their correlations are based on calculated partition coefficients, not on experimentally measured partition coefficients. Lindenberg et al [75] also classified prednisolone as BCS Class 1. The recently adopted revised WHO Guideline classifies prednisolone as BCS Class 1.…”

Section: Bcs Classificationmentioning

confidence: 99%

Biowaiver Monographs for Immediate Release Solid OralDosage Forms: Prednisolone

Vogt

Derendorf

Krämer³

et al. 2007

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

A project of the International Pharmaceutical Federation FIP, Groupe BCS, www.fip.org. This article reflects the scientific opinion of the authors and not the policies of regulating agencies. AbstractLiterature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing prednisolone are reviewed. Data on its solubility, oral absorption, and permeability are not totally conclusive, but strongly suggest a BCS Class 1 classification. Prednisolone's therapeutic indications and therapeutic index, pharmacokinetics, and the possibility of excipient interactions were also taken into consideration. Available evidence indicates that a biowaiver for IR solid oral dosage forms formulated with the excipients tabulated in this article would be unlikely to expose patients to undue risks.

show abstract

“…It should be noted that the clinical effectiveness of these dosage forms is determined by the solubility of the biologically active substances in vehicle, as well as their rheological parameters [3,5,6,9,13,18,22]. In ointments, the physicochemical properties of the vehicles, especially the relationship between solid and liquid phase, determine their viscosity (ŋ), and, therefore, modulate the magnitude of diffusion coefficient (D) as calculated by the Einstein-Smoluchowski equation (D = k·T/6π r ŋ) [4,10,15].…”

Section: Introductionmentioning

confidence: 99%

The influence of the viscosity of the ointment vehicles magisterial topical preparations, on the speed transfer of biologically active substances

Glogowski¹,

Kołodziejska

Kołodziejczyk

et al. 2015

Current Issues in Pharmacy and Medical Sciences

View full text Add to dashboard Cite

07located within Swietokrzyskie Province (Poland). As part of the study, viscosity, viscous elasticity and the rate of volatile component loss were marked, and the influence of these parameters on the diffusion rate of salicylic acid and boric acid to an in vitro external compartment was analyzed [7,23]. In this work, for the interpretation of the mass exchange process at the phase boundary, the method of agar plates containing the marker of diffusion was employed. The above study method was used to compare the ointment prepared by way of a conventional technique (in a mortar) and by way of the aid of an unguator [12]. EXPERIMENTAL Ointment vehiclesWhite petrolatum (Vaselinum album; PPF Hasco Lek S.A.), yellow petrolatum (Vaselinum flavum; PPF Hasco Lek S.A.), eucerin (Eucerini; PPF Eucerini Works, The aim of this study was to analyze the morphological parameters (viscosity, viscous elasticity and the rate of volatile component loss) of salicylic and boric acid-containing magisterial formulae (ointments). Moreover, the effects of these parameters on the diffusion rate of a therapeutic agent (salicylic acid) to an in vitro external compartment were analyzed. Finally, the applicatory properties of the ointments prepared by way of a conventional technique (in a mortar) and with the aid of an unguator, were compared. The rheological parameters of the analyzed ointments suggest that the preparations made with an aid of an unguator, irrespective of the physicochemical characteristics of their vehicles, are characterized by higher values of diffusion coefficient (D). In addition, conventionally-prepared formulae containing salicylic were shown to be characterized by better viscous elasticity. Surprisingly, irrespective of the preparation technique, the ointments based on an absorptive vehicle (containing lanolin) were characterized by similar viscous elasticity. The rate of volatile (water) component loss from ointments containing a 3% solution of boric acid suggests that such formulae lose no more than 2.3% of their mass when exposed at 37°C. Therefore, the viscosity of such ointments applied onto a patient's skin should remain relatively stable.

show abstract

Classification of orally administered drugs on the World Health Organization Model list of Essential Medicines according to the biopharmaceutics classification system

Cited by 728 publications

References 219 publications

Effect of Sorbitol on the Pharmacokinetic Profile of Lamivudine Oral Solution in Adults: An Open‐Label, Randomized Study

Effect of Sorbitol on the Pharmacokinetic Profile of Lamivudine Oral Solution in Adults: An Open‐Label, Randomized Study

Biowaiver Monographs for Immediate Release Solid OralDosage Forms: Prednisolone

The influence of the viscosity of the ointment vehicles magisterial topical preparations, on the speed transfer of biologically active substances

Contact Info

Product

Resources

About