22 results match your criteria Brazilian Journal Of Pharmaceutical Sciences[Journal]

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Past, Present, and Future of Bioequivalence: Improving Assessment and Extrapolation of Therapeutic Equivalence for Oral Drug Products.

J Pharm Sci 2018 10 20;107(10):2519-2530. Epub 2018 Jun 20.

Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany. Electronic address:

The growth in the utilization of systems thinking principles has created a paradigm shift in the regulatory sciences and drug product development. Instead of relying extensively on end product testing and one-size-fits-all regulatory criteria, this new paradigm has focused on building quality into the product by design and fostering the development of product-specific, clinically relevant specifications. In this context, this commentary describes the evolution of bioequivalence regulations up to the current day and discusses the potential of applying a Bayesian-like approach, considering all relevant prior knowledge, to guide regulatory bioequivalence decisions in a patient-centric environment. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00223549183034
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http://dx.doi.org/10.1016/j.xphs.2018.06.013DOI Listing
October 2018
21 Reads

Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Proguanil Hydrochloride.

J Pharm Sci 2018 07 20;107(7):1761-1772. Epub 2018 Mar 20.

Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany. Electronic address:

Literature data relevant to the decision to waive in vivo bioequivalence testing for the approval of generic immediate release solid oral dosage forms of proguanil hydrochloride are reviewed. To elucidate the Biopharmaceutics Classification System (BCS) classification, experimental solubility and dissolution studies were also carried out. The antimalarial proguanil hydrochloride, effective via the parent compound proguanil and the metabolite cycloguanil, is not considered to be a narrow therapeutic index drug. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00223549183014
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http://dx.doi.org/10.1016/j.xphs.2018.03.009DOI Listing
July 2018
42 Reads

Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Folic Acid.

J Pharm Sci 2017 12 24;106(12):3421-3430. Epub 2017 Aug 24.

Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany. Electronic address:

This work presents a review of literature and experimental data relevant to the possibility of waiving pharmacokinetic bioequivalence studies in human volunteers for approval of immediate-release solid oral pharmaceutical forms containing folic acid as the single active pharmaceutical ingredient. For dosage forms containing 5 mg folic acid, the highest dose strength on the World Health Organization Essential Medicines List, the dose/solubility ratio calculated from solubility studies was higher than 250 mL, corresponding to a classification as "not highly soluble." Small, physiological doses of folic acid (≤320 μg) seem to be absorbed completely via active transport, but permeability data for higher doses of 1-5 mg are inconclusive. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00223549173057
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http://dx.doi.org/10.1016/j.xphs.2017.08.007DOI Listing
December 2017
21 Reads

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Amoxicillin Trihydrate.

J Pharm Sci 2017 10 5;106(10):2930-2945. Epub 2017 May 5.

Institute of Pharmaceutical Technology, Johann Wolfgang Goethe University, Frankfurt am Main, Germany. Electronic address:

Literature and experimental data relevant to waiver of in vivo bioequivalence (BE) testing for the approval of immediate-release solid oral dosage forms containing amoxicillin trihydrate are reviewed. Solubility and permeability characteristics according to the Biopharmaceutics Classification System (BCS), therapeutic uses, therapeutic index, excipient interactions, as well as dissolution and BE and bioavailability studies were taken into consideration. Solubility and permeability studies indicate that amoxicillin doses up to 875 mg belong to BCS class I, whereas 1000 mg belongs to BCS class II and doses of more than 1000 mg belong to BCS class IV. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00223549173033
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http://dx.doi.org/10.1016/j.xphs.2017.04.068DOI Listing
October 2017
40 Reads

Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Enalapril.

J Pharm Sci 2017 08 21;106(8):1933-1943. Epub 2017 Apr 21.

Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany. Electronic address:

Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhibitor enalaprilat. Enalapril as the maleate salt is shown to be highly soluble, but only 60%-70% of an orally administered dose of enalapril is absorbed from the gastrointestinal tract into the enterocytes. Read More

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http://dx.doi.org/10.1016/j.xphs.2017.04.019DOI Listing
August 2017
27 Reads

Assessment of Bioequivalence of Weak Base Formulations Under Various Dosing Conditions Using Physiologically Based Pharmacokinetic Simulations in Virtual Populations. Case Examples: Ketoconazole and Posaconazole.

J Pharm Sci 2017 02 16;106(2):560-569. Epub 2016 Nov 16.

Institute of Pharmaceutical Technology, Johann Wolfgang Goethe University, Frankfurt am Main, Germany. Electronic address:

Postabsorptive factors which can affect systemic drug exposure are assumed to be dependent on the active pharmaceutical ingredient (API), and thus independent of formulation. In contrast, preabsorptive factors, for example, hypochlorhydria, might affect systemic exposure in both an API and a formulation-dependent way. The aim of this study was to evaluate whether the oral absorption of 2 poorly soluble, weakly basic APIs, ketoconazole (KETO) and posaconazole (POSA), would be equally sensitive to changes in dissolution rate under the following dosing conditions-coadministration with water, with food, with carbonated drinks, and in drug-induced hypochlorhydria. Read More

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http://dx.doi.org/10.1016/j.xphs.2016.10.008DOI Listing
February 2017
11 Reads

Bridging the Gap Between In Vitro Dissolution and the Time Course of Ibuprofen-Mediating Pain Relief.

J Pharm Sci 2016 12 14;105(12):3658-3667. Epub 2016 Oct 14.

Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany. Electronic address:

In vitro-in vivo extrapolation techniques combined with physiologically based pharmacokinetic models represent a feasible approach to establishing links between critical quality attributes and the time course of drug concentrations in vivo. By further integrating the results with pharmacodynamic (PD) models, scientists can also explore the time course of drug effect. The aim of this study was to assess whether differences in dissolution rates would affect the onset, magnitude, and duration of the time course of ibuprofen-mediating pain relief. Read More

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http://dx.doi.org/10.1016/j.xphs.2016.08.024DOI Listing
December 2016
10 Reads

Dissolution Methods to Increasing Discriminatory Power of In Vitro Dissolution Testing for Ibuprofen Free Acid and Its Salts.

J Pharm Sci 2017 01 7;106(1):92-99. Epub 2016 Jul 7.

Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany. Electronic address:

The predictive capacity of in vitro dissolution tests using the Biopharmaceutics Classification System (BCS)-based experimental setup to anticipate in vivo bioequivalence outcomes for BCS class 2 weak acids has been questioned. In this work, the effect of buffer concentration media was investigated as a possible approach to ensuring the discriminative capacity of the in vitro dissolution methods. The case example used to test this approach was ibuprofen, formulated as either the free acid or in various salt forms. Read More

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http://dx.doi.org/10.1016/j.xphs.2016.06.001DOI Listing
January 2017
4 Reads

Exploratory Investigation of the Limiting Steps of Oral Absorption of Fluconazole and Ketoconazole in Children Using an In Silico Pediatric Absorption Model.

J Pharm Sci 2016 09 15;105(9):2794-2803. Epub 2016 Mar 15.

Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany. Electronic address:

Due to the higher total clearance of certain drugs in children than in adults, it is recommended that, in such cases, higher relative doses on a milligram/kilogram basis should be administered to children in order to achieve similar systemic exposure to adults. This is the case for fluconazole and ketoconazole. Even though the lower absorptive surface area and smaller volumes of intestinal fluids in children does not affect fluconazole absorption, cumulative fraction absorbed of ketoconazole seems to be dose dependent. Read More

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http://dx.doi.org/10.1016/j.xphs.2016.01.027DOI Listing
September 2016
14 Reads

Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Ribavirin.

J Pharm Sci 2016 Apr 5;105(4):1362-9. Epub 2016 Mar 5.

Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany. Electronic address:

Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release solid oral dosage forms containing ribavirin are reviewed. Ribavirin is highly soluble, but its permeability characteristics are not well defined. Therefore according to the Biopharmaceutical Classification System, and taking a "worst case" approach, ribavirin should be assigned to class III. Read More

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http://dx.doi.org/10.1016/j.xphs.2016.01.017DOI Listing
April 2016
39 Reads

Differences in Food Effects for 2 Weak Bases With Similar BCS Drug-Related Properties: What Is Happening in the Intestinal Lumen?

J Pharm Sci 2016 09 23;105(9):2712-2722. Epub 2016 Feb 23.

Institute of Pharmaceutical Technology, Johann Wolfgang Goethe University, Frankfurt am Main, Germany. Electronic address:

Ketoconazole and posaconazole are both Biopharmaceutics Classification System class 2 drugs (highly permeable, poorly soluble), are structurally similar, and are administered at the same doses. Nevertheless, the duodenal concentration profile and the magnitude of the positive food effect observed for these 2 drugs are markedly different. The aim of this study was to investigate, by means of in silico models, the likely mechanism(s) behind such differences. Read More

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http://dx.doi.org/10.1016/j.xphs.2015.11.033DOI Listing
September 2016
5 Reads

Formulation and Evaluation of a Mucoadhesive Thermoresponsive System Containing Brazilian Green Propolis for the Treatment of Lesions Caused by Herpes Simplex Type I.

J Pharm Sci 2016 Jan 13;105(1):113-21. Epub 2016 Jan 13.

Programa de Pós-graduação em Ciências Farmacêuticas, Universidade Estadual de Maringá, Maringá, Paraná, Brazil; Departamento de Ciências Básicas da Saúde, Universidade Estadual de Maringá, Maringá, Paraná, Brazil. Electronic address:

The aim of the present work was to develop a topical delivery system that contains Brazilian green propolis extract (PE-8) to increase efficiency and convenience when applied to herpetic lesions. The cytotoxicity and antiherpetic activity was determined in vitro and in vivo. The PE-8 was added to a system that contained poloxamer 407 and carbopol 934P. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00223549150013
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http://dx.doi.org/10.1016/j.xphs.2015.11.016DOI Listing
January 2016
5 Reads

Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Nifedipine.

J Pharm Sci 2015 Oct 6;104(10):3289-98. Epub 2015 Jul 6.

Institute of Pharmaceutical Technology, J.W. Goethe University, Frankfurt am Main, Germany.

Literature data relevant to the biopharmaceutical properties of the active pharmaceutical ingredient (API) nifedipine are reviewed to evaluate whether a waiver of in vivo bioequivalence (BE) testing of immediate-release (IR) dosage forms formulated as tablets and soft gelatin capsules is warranted. Nifedipine's solubility and permeability, its therapeutic use and index, pharmacokinetics, food drug interactions, and any reported BE/bioavailability problems were all taken into consideration. Solubility and BA data indicate conclusively that nifedipine is a class II substance of biopharmaceutics classification system (BCS) and that the formulation of drug product plays a key role on the dissolution characteristics of the API. Read More

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http://dx.doi.org/10.1002/jps.24560DOI Listing
October 2015
21 Reads

Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Levetiracetam.

J Pharm Sci 2015 Sep 6;104(9):2676-87. Epub 2015 Feb 6.

Institute of Pharmaceutical Technology, Johann Wolfgang Goethe University, Frankfurt am Main, Germany.

Literature and experimental data relevant for the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing levetiracetam are reviewed. Data on solubility and permeability suggest that levetiracetam belongs to class I of the biopharmaceutical classification system (BCS). Levetiracetam's therapeutic use, its wide therapeutic index, and its favorable pharmacokinetic properties make levetiracetam a valid candidate for the BCS-based biowaiver approach. Read More

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https://fip.org/files/fip/BPS/BCS/Monographs/Isoniazid.pdf
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https://www.fip.org/files/fip/BPS/BCS/Monographs/Ibuprofen.p
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http://deepblue.lib.umich.edu/bitstream/handle/2027.42/50637
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http://linkinghub.elsevier.com/retrieve/pii/S002235491630052
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http://dx.doi.org/10.1002/jps.24350DOI Listing
September 2015
70 Reads

Biowaiver monograph for immediate-release solid oral dosage forms: fluconazole.

J Pharm Sci 2014 Dec 13;103(12):3843-3858. Epub 2014 Oct 13.

Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany. Electronic address:

Literature data pertaining to the decision to allow a waiver of in vivo bioequivalence (BE) testing requirements for the approval of immediate release (IR) solid oral dosage forms containing fluconazole as the only active pharmaceutical ingredient (API) are reviewed. The decision is based on solubility, dissolution, permeability, therapeutic index, pharmacokinetic parameters, pharmacodynamic properties, and other relevant data. BE/bioavailability (BA) problems and drug-excipients interaction data were also reviewed and taken into consideration. Read More

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http://dx.doi.org/10.1002/jps.24181DOI Listing
December 2014
53 Reads

Use of physiologically based pharmacokinetic models coupled with pharmacodynamic models to assess the clinical relevance of current bioequivalence criteria for generic drug products containing Ibuprofen.

J Pharm Sci 2014 Oct 16;103(10):3263-75. Epub 2014 Jul 16.

Division of Bioequivalence, Brazilian Health Surveillance Agency (ANVISA), Brasília, Brazil; Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany.

Physiologically based pharmacokinetic models coupled with pharmacodynamic (PBPK/PD) models can be useful to identify whether current bioequivalence criteria is overly conservative or venturesome for different drugs. A PBPK model constructed with Simcyp Simulator(®) using reported biopharmaceutics parameters for ibuprofen was coupled with two published PD models: one for antipyresis and one for dental pain relief. Using products with doses of 400 mg and 10 mg/kg as "reference (R)" drug products, virtual products with doses of 280 mg and 7 mg/kg, respectively, could be interpreted as representing bioinequivalent test (T) drug products, as the point estimate for the ratios T/R are well below the bioequivalence limits. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00223549153039
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http://dx.doi.org/10.1002/jps.24076DOI Listing
October 2014
5 Reads

Biowaiver monographs for immediate-release solid oral dosage forms: Zidovudine (azidothymidine).

J Pharm Sci 2013 Aug 10;102(8):2409-23. Epub 2013 Jun 10.

Brazilian Health Surveillance Agency (Anvisa), Division of Bioequivalence, Brasília, Brazil.

Literature data on the properties of zidovudine relevant to waiver of in vivo bioequivalence (BE) testing requirements for the approval of immediate-release (IR) solid oral dosage forms containing zidovudine alone or in combination with other active pharmaceutical ingredients (APIs) are reviewed. Solubility, dissolution, and permeability data for zidovudine, along with its dosing schedule, therapeutic index and pharmacokinetic properties, and reports related to BE/bioavailability were all taken into consideration. Data for solubility and permeability suggest that zidovudine belongs to Class I according to the Biopharmaceutics Classification System. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00223549153097
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http://dx.doi.org/10.1002/jps.23624DOI Listing
August 2013
13 Reads

A comparative analysis of biopharmaceutics classification system and biopharmaceutics drug disposition classification system: a cross-sectional survey with 500 bioequivalence studies.

J Pharm Sci 2013 Sep 11;102(9):3136-44. Epub 2013 Apr 11.

Division of Bioequivalence, Brazilian Health Surveillance Agency (ANVISA), Brasília, Brazil.

Although policies of waiving bioequivalence studies are part of the legal framework of various regulatory agencies, there is no harmonization with regard to extension of the biowaiver to drugs other than those with high solubility and high permeability, nor is there any consensus or official endorsement of the biopharmaceutics drug disposition classification system (BDDCS). To better understand the applicability of the biowaiver, we carried out a cross-sectional survey to estimate the relative risk of obtaining nonbioequivalent (non-BE) or bioinequivalent (BIE) results for drug products containing drugs belonging to each of the biopharmaceutics classification system (BCS) and BDDCS classes. Five hundred bioequivalence studies were randomly sampled from a database of the Brazilian Health Surveillance Agency (ANVISA). Read More

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http://dx.doi.org/10.1002/jps.23515DOI Listing
September 2013
15 Reads

Biowaiver monographs for immediate release solid oral dosage forms: efavirenz.

J Pharm Sci 2013 Feb 22;102(2):318-29. Epub 2012 Nov 22.

Brazilian Health Surveillance Agency (Anvisa), Division of Bioequivalence, Londrina State University, Londrina, Brazil.

Literature data pertaining to the decision to allow a waiver of in vivo bioequivalence testing for the approval of immediate-release (IR) solid oral dosage forms containing efavirenz as the only active pharmaceutical ingredient (API) are reviewed. Because of lack of conclusive data about efavirenz's permeability and its failure to comply with the "high solubility" criteria according to the Biopharmaceutics Classification System (BCS), the API can be classified as BCS Class II/IV. In line with the solubility characteristics, the innovator product does not meet the dissolution criteria for a "rapidly dissolving product. Read More

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http://dx.doi.org/10.1002/jps.23380DOI Listing
February 2013
13 Reads

Biowaiver monographs for immediate-release solid oral dosage forms: stavudine.

J Pharm Sci 2012 Jan 15;101(1):10-6. Epub 2011 Sep 15.

Brazilian Health Surveillance Agency, Anvisa, Division of Bioequivalence, Brasilia, Brazil.

Literature 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 stavudine (d4T) are reviewed. According to Biopharmaceutics Classification System (BCS), d4T can be assigned to BCS class I. No problems with BE of IR d4T formulations containing different excipients and produced by different manufacturing methods have been reported and, hence, the risk of bioinequivalence caused by these factors appears to be low. Read More

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http://dx.doi.org/10.1002/jps.22756DOI Listing
January 2012
40 Reads

Biowaiver monographs for immediate release solid oral dosage forms: levofloxacin.

J Pharm Sci 2011 May 21;100(5):1628-36. Epub 2011 Jan 21.

Brazilian Health Surveillance Agency (Anvisa), Division of Bioequivalence, Brazil.

Literature 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 levofloxacin as the only active pharmaceutical ingredient (API) are reviewed. According to the current Biopharmaceutics Classification System, levofloxacin can be assigned to Class I. No problems with BE of IR levofloxacin formulations containing different excipients and produced by different manufacturing methods have been reported and hence the risk of bioinequivalence caused by these factors appears to be low. Read More

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http://dx.doi.org/10.1002/jps.22413DOI Listing
May 2011
9 Reads

Biowaiver monographs for immediate release solid oral dosage forms: metronidazole.

J Pharm Sci 2011 May 19;100(5):1618-27. Epub 2011 Jan 19.

Brazilian Health Surveillance Agency (Anvisa), Division of Bioequivalence, Brasilia, Brazil.

Literature 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 metronidazole are reviewed. Metronidazole can be assigned to Biopharmaceutics Classification System Class I. Most BE studies that were identified reported the investigated formulations to be bioequivalent, indicating the risk of bioinequivalence to be low. Read More

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http://linkinghub.elsevier.com/retrieve/pii/S002235491532160
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http://dx.doi.org/10.1002/jps.22409DOI Listing
May 2011
22 Reads
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