Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Acetazolamide

Granero, Gladys E.; Longhi, Marcela R.; Becker, Corina; Junginger, Hans E.; Kopp, Sabine; Midha, K. K.; Shah, Vinod P.; Stavchansky, Salomon A; Dressman, Jennifer B.; Barends, D. M.

doi:10.1002/jps.21282

Cited by 51 publications

(49 citation statements)

References 36 publications

(38 reference statements)

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“…was given on days 2–5 (9 AM). On Day 5 when interactions between the two drugs were examined, ACZ was administered 1 h prior to oxycodone (9 AM and 10 AM respectively) in order to align their expected peak effects 14,16 . On study days, collected urine was combined over the following collection periods 7:00 AM–12PM, 12–3PM, 3–6PM, 6–9PM, 9PM–6:30AM.…”

Section: Methodsmentioning

confidence: 99%

“…The protocol for subjects 1–4 was designed based on previous studies 14,18 , that indicated most ACZ would be cleared within 24 h of dosing; the PK of ACZ alone was assessed on Day 4 and in combination with oxycodone on Day 5 with the final plasma sample drawn 24 h after dosing. An interim analysis of samples from these first four subjects revealed that the ACZ microdose was being eliminated more slowly than expected based on previously published studies 14,18 .…”

Section: Methodsmentioning

confidence: 99%

“…Acetazolamide is a sulfonamide, but it is structurally distinct from allergenic sulfa-antimicrobials and adverse reactions are rare 12,13 . Acetazolamide is not metabolized and is directly eliminated into urine 14 , providing some degree of promise for low inter-subject variability rates of urinary excretion.…”

Section: Introductionmentioning

confidence: 99%

“…This report describes the PK and rate of urinary excretion of a 15 mg ACZ microdose (equivalent to 6% of the recommended starting therapeutic dose 14 ). The data examining quinine using similar methods has been published elsewhere 15 .…”

Section: Introductionmentioning

confidence: 99%

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A Pharmacokinetic Study Examining Acetazolamide as a Novel Adherence Marker for Clinical Trials

Hampson

Babalonis

Lofwall³

et al. 2016

J Clin Psychopharmacol

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Rationale Accurate assessment of medication adherence is critical for determination of medication efficacy in clinical trials, but most current methods have significant limitations. This study tests a sub-therapeutic (microdose) of acetazolamide as a medication ingestion marker, because acetazolamide is rapidly absorbed and excreted without metabolism in urine and can be non-invasively sampled. Methods In a double-blind, placebo-controlled, residential study, ten volunteers received 15 mg oral acetazolamide for four consecutive days. Acetazolamide pharmacokinetics were assessed on Day 3, and its pharmacokinetic and pharmacodynamic interactions with a model medication (30 mg oxycodone) were examined on Day 4. The rate of acetazolamide elimination into urine was followed for several days after dosing cessation. Results Erythrocyte sequestration (half-life= 50.2±18.5h, mean±SD, n=6), resulted in the acetazolamide microdose exhibiting a substantially longer plasma half-life (24.5±5.6 h, n=10) than previously reported for therapeutic doses (3–6 h). Following cessation of dosing, the rate of urinary elimination decreased significantly (F(3,23)=247: p<0.05, n=6) in a predictable manner with low inter-subject variability and a half-life of 16.1±3.8h (n=10). For each of four consecutive mornings after dosing cessation, the rates of urinary acetazolamide elimination remained quantifiable. There was no overall effect of acetazolamide on the pharmacodynamics, Cmax, Tmax or elimination half-life of the model medication tested. Acetazolamide may have modestly increased overall oxycodone exposure (20%, p<0.05) compared with one of the two days when oxycodone was given alone, but there were no observed effects of acetazolamide on oxycodone pharmacodynamic responses. Conclusions Co-formulation of a once-daily trial medication with an acetazolamide microdose may allow estimation of the last time of medication consumption for up to 96h post-dose. Inclusion of acetazolamide may, therefore, provide an inexpensive new method to improve estimates of medication adherence in clinical trials.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

A Pharmacokinetic Study Examining Acetazolamide as a Novel Adherence Marker for Clinical Trials

Hampson

Babalonis

Lofwall³

et al. 2016

J Clin Psychopharmacol

View full text Add to dashboard Cite

show abstract

“…It presents two polymorphic forms, the solubility at 37 C of form I being 10% greater than form II. This small difference between solubilities does not seem to significantly affect its bioavailability [2][3][4] . It is administered in oral dosage forms, such as 125 or 250 mg tablets, depending on the country.…”

Section: Introductionmentioning

confidence: 99%

Formulation design of oral pediatric Acetazolamide suspension: dose uniformity and physico-chemical stability study

Santoveña

Suárez-González

Martín-Rodríguez

et al. 2016

Pharmaceutical Development and Technology

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Provisional BCS Classification of the Leading Oral Drugs on the Global Market

Dahan

Amidon

2010

Burger's Medicinal Chemistry and Drug Discovery

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In the early 1990s, a collaborative research effort between academia and the U.S. Food and Drug Administration (FDA) was initiated to establish a database of human jejunal permeabilities based on a Biopharmaceutics Classification System (BCS). The BCS broadly allowed the prediction of human absorption, Fraction absorbed ( F abs ) and the rate‐limiting step in the intestinal absorption process of drugs following oral administration. The BCS classified compounds into one of four biopharmaceutical classes according to water solubility and membrane permeability characteristics. Today, the BCS has generated remarkable impact on the global pharmaceutical sciences arena, in drug discovery, development and regulation, and an extensive validation/discussion of the BCS is continuously published in the literature. BCS has been effectively implanted by drug regulatory agencies around the world, and widely practiced by the pharmaceutical industry. The aim of this chapter is to present the BCS and its scientific basis, to describe its impact on regulatory practice of oral drug products, and to access the BCS classification of the top drugs on the global market. Finally, current and future directions in BCS related extensions, and their impact on the pharmaceutical industry, will be discussed.

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Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Acetazolamide

Cited by 51 publications

References 36 publications

A Pharmacokinetic Study Examining Acetazolamide as a Novel Adherence Marker for Clinical Trials

A Pharmacokinetic Study Examining Acetazolamide as a Novel Adherence Marker for Clinical Trials

Formulation design of oral pediatric Acetazolamide suspension: dose uniformity and physico-chemical stability study

Provisional BCS Classification of the Leading Oral Drugs on the Global Market

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