Comparison of Dissolution Similarity Assessment Methods for Products with Large Variations: &lt;i&gt;f&lt;/i&gt;&lt;sub&gt;2&lt;/sub&gt; Statistics and Model-Independent Multivariate Confidence Region Procedure for Dissolution Profiles of Multiple Oral Products

Yoshida, Hiroyuki; Shibata, Hiroko; Izutsu, Ken‐ichi; Goda, Yukihiro

doi:10.1248/bpb.b16-00904

Cited by 13 publications

(8 citation statements)

References 8 publications

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“…Furthermore, there are 2 recent papers comparing different methods for the investigation of bioequivalence of dissolution profiles. For instance, Yoshida et al compared the f 2 , a model‐independent multivariate confidence region procedure and the f 2 bootstrapping method, showing that all these approaches could lead to different conclusions on the same datasets. Moreover, Paixão et al analysed the properties of the f 2 , the multivariate statistical distance, and f 2 bootstrapping methods in situations where the f 2 was not applicable because of high variability in the dissolution data.…”

Section: Introductionmentioning

confidence: 99%

“…4 Not more than 1 mean value of >85% dissolved for any of the formulations. 5 The relative standard deviation or coefficient of variation, that is, the ratio of the standard deviation to the sample mean, should be less than 20% for the first point and less than 10% from second to last time point for any product. It is computed across units at each time point independently in both groups.…”

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confidence: 99%

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Regulatory assessment of drug dissolution profiles comparability via maximum deviation

Moellenhoff

Dette

Kotzagiorgis³

et al. 2018

Statistics in Medicine

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In drug development, comparability of dissolution profiles of 2 different formulations is usually assessed using the similarity factor f . In practice, the drug dissolution profiles are deemed similar if the f exceeds 50, which occurs when a 10% maximum difference in the mean percentage of the dissolved drug at each time point between test and reference formulation is obtained. According to the Guideline on the Investigation of Bioequivalence (CPMP/EWP/QWP/1401/98 Rev. 1/ Corr **) use of the f is however restricted by a set of validity conditions. If some of these conditions are not satisfied, the f is not considered suitable, and alternative statistical methods are needed. In this article, we propose an inferential framework based on the maximum deviation between curves to test the comparability of drug dissolution profiles. The new methodology is applicable regardless whether the validity criteria of the f are met or not. Contrary to the f , this approach also integrates the variability of the measurements over time and not only their average. To benchmark our method, we performed simulations informed by 3 real case studies provided by the European Medicines Agency and extracted from dossiers submitted to the Centralised Procedure for Marketing Authorisation Application. In the scenarios of the simulation study, the new method controlled its type I error rate when the maximum deviation was greater than the similarity acceptance limit of 10%. The power exceeded 80% for small values of the maximum deviation, while the test was more conservative for intermediate ones. Our results were also very robust to sampling variations. Based on these positive findings, we encourage applicants to consider the new maximum deviation-based method as a valid alternative to the f , especially when the validity criteria of the latter are not met.

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Section: Introductionmentioning

confidence: 99%

mentioning

confidence: 99%

Regulatory assessment of drug dissolution profiles comparability via maximum deviation

Moellenhoff

Dette

Kotzagiorgis³

et al. 2018

Statistics in Medicine

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“…The average elution rate of each sample was compared to the sample formulated on day 0. The similarity of dissolution profiles was evaluated using the f2 statistic defined in the Ministry of Health, Labor, and Welfare guidelines [ 23 ].…”

Section: Methodsmentioning

confidence: 99%

Stability Study of Baclofen in an Oral Powder Form Compounded for Pediatric Patients in Japan

et al. 2022

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Baclofen is used as a skeletal muscle relaxant for multiple sclerosis patients and pediatric patients with cerebral palsy and is prescribed to pediatric patients at 0.3 to 1.0 mg/kg/dose. Baclofen tablets, an oral drug, are usually administered as a powder in pediatric wards after a formulation change by the pharmacist. However, there is no information about stability and assurance of quality for compounded products. The purpose of this study was to design a 10 mg/g oral powder of baclofen and to investigate the stability and changes in the physical properties of this compounded product. A 10 mg/g baclofen powder was prepared by adding extra-fine crystal lactose hydrate to crushed and filtrated baclofen tablets and was stored in a polycarbonate amber bottle with desiccant or in a coated paper laminated with cellophane and polyethylene. The stability of baclofen at 25 ± 2 °C/60 ± 5%RH was tested for 120 days in ‘bottle (closed)’, ‘bottle (in use)’, and ‘laminated’ storage conditions. Baclofen concentrations ranged from 90.0% to 110.0% of the initial concentration under all storage conditions. No crystallographic or dissolution changes were observed after storage. This information can help with the management of baclofen compounded powder in pharmacies.

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“…Also, this effect has been found in many works like that obtained by Mansouri and co-researchers, as in the preparation of ibuprofen formulation as nanoparticles using solvent: anti solvent method [25] . The difference factor of f1 and similarity factor of f2 have been widely used for dissolution profile comparison [26,27,28] . They were calculated to compare the dissolution profiles of pure, physical mixture, nano incorporated tablet in each media as shown in table (5).…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Preparation And Characterization Of Nimesulide Nanoparticles For Dissolution Improvement

Abd-AlRazaq

Rahi²,

Al-lami³

2018

AJPS

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Nimesulide is one of the types of non-steroidal anti-inflammatory drugs, widely used as analgesic and antipyretic. It is classified as class II drugs according to BCS guidance because of low solubility in water that leads to decrease in dissolution rate. So the objective of this study was to decrease particle size, increase solubility and dissolution rate of nimesulide by preparation of nimesulide nanoparticles using solvent/antisolvent precipitation method by addition of organic solution of drug onto the solution of stabilizer. The size of nimesulide nanoparticles were studied and considered by particle size analyzer, drug content and loading efficiency. The freeze dried nanoparticles were characterized by field emission electron microscope, X-Ray powder diffraction, differential scanning calorimetry and saturated solubility measurement. Tablet was manufactured by direct compression. The tablets were evaluated for drug release to measure the effect of nanoparticles on the dissolution improvement of drug.

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Comparison of Dissolution Similarity Assessment Methods for Products with Large Variations: <i>f</i><sub>2</sub> Statistics and Model-Independent Multivariate Confidence Region Procedure for Dissolution Profiles of Multiple Oral Products

Cited by 13 publications

References 8 publications

Regulatory assessment of drug dissolution profiles comparability via maximum deviation

Regulatory assessment of drug dissolution profiles comparability via maximum deviation

Stability Study of Baclofen in an Oral Powder Form Compounded for Pediatric Patients in Japan

Preparation And Characterization Of Nimesulide Nanoparticles For Dissolution Improvement

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