Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Stavudine

Silva, Arthur L.L.; Cristofoletti, Rodrigo; Storpirtis, Sílvia; Sousa, Varley D.; Junginger, Hans E.; Shah, Vinod P.; Stavchansky, Salomon A; Dressman, Jennifer B.; Barends, D. M.

doi:10.1002/jps.22756

Cited by 8 publications

(4 citation statements)

References 38 publications

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“…paraoxon is an organophosphorous ester and the lactones are cyclic esters) that are hydrolyzed by this enzyme. However in plasma there are other esterases such as albumin, cholinesterases (acetyl and/or butyril) or carboxylesterase that can carry out ester hydrolysis [73,49]. Also carbonic anhydrase, alpha-chymotrypsin [74] and lipase [56] can hydrolyse ester substrates.…”

Section: Technical Aspects Of the Assaysmentioning

confidence: 99%

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Serum paraoxonase 1 (PON1) measurement: an update

2014

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Paraoxonase 1 (PON1) is a widely studied enzyme based on its protective role against poisoning by organophosphate (OP) metabolites of specific OP insecticides and in vascular disease, as well as its use as biomarker of diseases involving oxidative stress, inflammation and liver diseases.This review provides an update about the current knowledge in the field of the analytical procedures that are used for PON1 measurements. It will be specially focused on: (a) characteristics of the different substrates used for measuring PON1, with emphasis in four aspects: toxicity, polymorphism influence, rate of hydrolysis and diagnostic performance. And (b) the technical aspects of PON1 assays, in which the reagents and reaction conditions, sources of variation, quality control systems, equipment and interferences with other esterases will be discussed.The information provided in this review can contribute to a more accurate and safe measurements of PON1 in laboratories and encourage researchers to explore the wide areas of PON1 in veterinary medicine that are still unknown.

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Section: Technical Aspects Of the Assaysmentioning

confidence: 99%

“…– Human, monkey, dog or minipig plasmas do not contain any carboxylesterase, however this esterase should be taken in consideration in other species such as rabbit, mouse and rat in which it is the major component of the plasma [49]. …”

Section: Technical Aspects Of the Assaysmentioning

confidence: 99%

Serum paraoxonase 1 (PON1) measurement: an update

2014

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“…Physiologic parameters of the PBPK model for rats (weight of 250 g), such as organ volumes, both total and vascular fraction, plasma flows and apparent permeability were the mean values found in the literature (Table 1) [22][23][24][25]. The Cl and Vd values used were obtained from a model-independent analysis of in vivo study results.…”

Section: • Model Parametersmentioning

confidence: 99%

Physiologically Based Pharmacokinetic (PBPK) Model of Gold Nanoparticle-Based Drug Delivery System for Stavudine Biodistribution

et al. 2022

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Computational modelling has gained attention for evaluating nanoparticle-based drug delivery systems. Physiologically based pharmacokinetic (PBPK) modelling provides a mechanistic approach for evaluating drug biodistribution. The aim of this work is to develop a specific PBPK model to simulate stavudine biodistribution after the administration of a 40 nm gold nanoparticle-based drug delivery system in rats. The model parameters used have been obtained from literature, in vitro and in vivo studies, and computer optimization. Based on these, the PBPK model was built, and the compartments included were considered as permeability rate-limited tissues. In comparison with stavudine solution, a higher biodistribution of stavudine into HIV reservoirs and the modification of pharmacokinetic parameters such as the mean residence time (MRT) have been observed. These changes are particularly noteworthy in the liver, which presents a higher partition coefficient (from 0.27 to 0.55) and higher MRT (from 1.28 to 5.67 h). Simulated stavudine concentrations successfully describe these changes in the in vivo study results. The average fold error of predicted concentrations after the administration of stavudine-gold nanoparticles was within the 0.5–2-fold error in all of the tissues. Thus, this PBPK model approach may help with the pre-clinical extrapolation to other administration routes or the species of stavudine gold nanoparticles.

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“…In the same year, a meeting, with representatives from organizations such as FDA, EMA and WHO, was held in Brazil. Moreover, during this period representatives of the Coordination of Bioequivalence team up with scientists from the International Pharmaceutical Federation in order to write biowaiver monographs, resulting in 3 published articles [1,18,31], and consequently, internal knowledge in this area has been expanded, preparing the team for receiving biowaiver based on BCS submissions. Differently from other regulatory authorities, ANVISA listed all drugs for which BCS-based biowaiver decisions could be granted.…”

Section: Brazilmentioning

confidence: 99%

Generic and similar products in Latin American countries: Current aspects and perspectives on bioequivalence and biowaivers

Storpirtis

Gai

Cristofoletti³

2014

Pharmaceuticals, Policy and Law

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In the XIX and XX centuries, Latin American countries have experienced several changes on politics and economics, facing problems related to progress and growth, technological development, demographic transition, and the environment. In the 2010s this region presents a high level of health demands, which causes financial difficulties, especially in expenditures with medicines. In this scenario have emerged policies to regulate and harmonize the register of generic and similar products based on in vitro and in vivo assays that support therapeutical equivalence and interchangeability, but heterogeneity is still observed, especially in terms of the assessment criteria and time from application until marketing authorization. Data obtained from the pharmaceutical market predict that this segment could reach USD 1,200 billion by 2016, mainly from market expansion in the leading emerging countries and from generics. The aim of this article is to present and discuss relevant aspects on bioequivalence, and biowaivers criteria, highlighting the different approaches adopted by the regional regulatory authorities in Latin America.

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Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Stavudine

Cited by 8 publications

References 38 publications

Serum paraoxonase 1 (PON1) measurement: an update

Serum paraoxonase 1 (PON1) measurement: an update

Physiologically Based Pharmacokinetic (PBPK) Model of Gold Nanoparticle-Based Drug Delivery System for Stavudine Biodistribution

Generic and similar products in Latin American countries: Current aspects and perspectives on bioequivalence and biowaivers

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