Biowaiver Monographs for Immediate Release Solid OralDosage Forms: Prednisolone

Abstract

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.

Biowaiver monographs for immediate release solid oral dosage forms: Rifampicin

“…This systematic approach to recommend or advise against a biowaiver decision is referred to in the recently published World Health Organization (WHO) Guideline 2. Biowaiver monographs have already been published for acetaminophen (INN: paracetamol),3 acetazolamide,4 aciclovir,5 amitriptyline,6 atenolol,1 chloroquine,7 cimetidine,8 diclofenac sodium and diclofenac potassium,9 ethambutol dihydrochloride,10 ibuprofen,11 isoniazid,12 metoclopramide,13 prednisolone,14 prednisone,15 propranolol,1 pyrazinamide,16 ranitidine,17 and verapamil 1. They are also available online at http://www.fip.org/bcs 18…”

Biowaiver monographs for immediate release solid oral dosage forms: Quinidine sulfate

“…It is to be understood that these monographs do not simply apply the WHO,2 FDA,3 and EMEA Guidances,4 but also aim to serve as a critical validation of these regulatory documents. Biowaiver monographs have already been published for acetaminophen (INN: paracetamol),5 acetazolamide,6 aciclovir,7 amitriptyline,8 atenolol,1 chloroquine,9 cimetidine,10 diclofenac,11 ethambutol,12 ibuprofen,13 isoniazid,14 metoclopramide,15 prednisolone,16 prednisone,17 pyrazinamide,18 propranolol,1 ranitidine,19 and verapamil 1. They are also available on‐line at http://www.fip.org/bcs.…”

A Minireview: Usefulness of Transporter-Targeted Prodrugs in Enhancing Membrane Permeability

“…This compound is a substrate for P-gp but classified as a BCS class I drug. 102 The usefulness of amino acid and peptide prodrugs of prednisolone was examined by determining the solubility, permeability, and the avoidance of P-gp-mediated efflux transport. 103 Prodrugs exhibited significantly higher solubility and stability under acidic condition.…”