Biopharmaceutical characterization of oral controlled/modified-release drug products. In vitro/in vivo correlation of roxatidine

Frick, Annke; Möller, H.; Wirbitzki, Ehrenfried

doi:10.1016/s0939-6411(98)00046-0

Cited by 8 publications

(4 citation statements)

References 3 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The classical methods of deconvolution of plasma profiles include modeldependent methods, such as Wagner-Nelson (Turner et al, 2004) and LooRiegelman (Langenbucher, 2002) and model independent method, such as the numerical deconvolution method (Frick et al, 1998;Mahayni et al, 2000).…”

Section: Deconvolution and Convolutionmentioning

confidence: 99%

In Vitro–In Vivo Correlation in Dosage Form Development: Case Studies

Li¹,

Royce²,

Serajuddin³

2008

Biopharmaceutics Applications in Drug Development

View full text Add to dashboard Cite

Section: Deconvolution and Convolutionmentioning

confidence: 99%

In Vitro–In Vivo Correlation in Dosage Form Development: Case Studies

Li¹,

Royce²,

Serajuddin³

2008

Biopharmaceutics Applications in Drug Development

View full text Add to dashboard Cite

“…(1 -y) 2 y > 0 for y > 0 (H7) G′(y) ) (y -1 -ln y)(1 + y) -(1 -y) 2 (1 -y) 3 (H8) h(y) ) (y -1 -ln y)(1 + y) -(1 -y) 2 (H9) h′(y) ) 1 -ln y -y -1 (H10) ln y ) y -1 y (H11) h′′(y ) 1) ) 0 (H17) h′(y) < 0 (H18) h(y ) 1) ) 0 (H19) h(y < 1) > 0 (H20) h(y > 1) < 0 (H21)…”

Section: G(y) )unclassified

“…), linear Level A IVIVC are anticipated (assuming that drug release is the rate-limiting step in the process of in vivo drug absorption). 3 In these cases the procedure is applicable, even in the absence of in vivo data. If the reference product in vivo data are available, the dissolution specifications can be widened.…”

Section: Introductionmentioning

confidence: 99%

Dissolution specifications based on release rates

Elkoshi

1999

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

A procedure based on release rates is proposed for the establishment of dissolution specifications that ensure the bioequivalence of a test and a reference product. This procedure, which confines Cmax (the maximum concentration of the drug in vivo) and AUCinfinity (the area under the time-concentration curve, extrapolated to infinity) values within any desired range (relative to a reference product), can be used as an alternative to the methods presented in the FDA guidance1 or the USP.2 The method is appropriate for zero-order or first-order release products with linear Level A in vitro/in vivo correlations (IVIVC). Based on the result that the relative difference in Cmax must always be smaller than the relative difference in the absorption rate constants (for any test and reference products of a given drug), the "minimum range" specifications are set. These specifications, which are identical for both zero-order and first-order release products, are of general validity. They depend only on the relative extents of release, but are otherwise drug or formulation independent. For certain extended release products demonstrating a constant release rate that is unaffected by dissolution conditions (thus allowing the assumption of Level A IVIVC), the "minimum range" dissolution limits are applicable even when in vivo data is not available. If the reference product in vivo data is available, wider limits (which are product specific) may be set. If the drug disposition is monoexponential, the specifications generated are the widest possible. They are termed the "ideal" specifications. In the case of a multiexponential disposition, the limits set by the procedure will (generally) not be the widest possible. Although the method is based on one-compartment models, it is essentially model independent in the sense that microscopic modeling is redundant for its application.

show abstract

“…9 Various IVIVC studies have been published for a number of formulations, including Busprion, propranolol, nevirapine, metoprolol and other drugs. [6][7][8][9][10][11][12][13][14][15][16][17] The concepts and methods used in establishing the IVIVC are reviewed elsewhere. 4,5 According to BCS classification naproxen sodium comes under class 2 drug and in addition naproxen is relatively having a short life suggest suitable applicant for modified release formulation.…”

Section: Introductionmentioning

confidence: 99%

Development, Internal and External Validation of Naproxen Sodium Sustained Release Formulation: an Level A <i>In Vitro-In Vivo</i> Correlation

Narayanasamy¹,

Shabaraya²

2017

tjps

View full text Add to dashboard Cite

Amaç: Bu çalışmanın amacı, naproksen sodyumun sürekli salım tableti için in vitro-in vivo korelasyon (IVIVC) geliştirmek, doğrulamak ve zamana bağlı plazma konsantrasyonlarını derhal salınan tabletle karşılaştırmaktır. Gereç ve Yöntemler: İn vitro salım hızı verileri, pH 7.4 fosfat tampon içinde 50 dev/dakikada, USP Apparatus II, palet karıştırıcısı kullanılarak her bir tablet için elde edilmiştir. Naproksen sodium 375 mg sürekli salım ve 500 mg derhal salım tabletleri 6 sağlıklı kişiye uygulanarak dört yönlü bir çaprazlama çalışması gerçekleştirilmiştir. Yirmi dört saat boyunca toplanan kan örnekleri valide edilmiş sıvı kromatografisi tandem-kütle spektrometresi yöntemi kullanılarak tayin edilmiştir. Bulgular: Hesaplanan ve 50-100 arasında bulunan değerler benzerlik faktörlerini göstermektedir. C max ve AUC ortalama değerlerine yakın bulunmuştur. Tahmin edilen ve gözlemlenen biyoyararlanım değerlendirmesi yapıldı ve Gıda İlaç İdaresi yönetmeliklerine göre % tahmin hataları (PE) hesaplandı; iç tahmin ile IVIVC'nin oluşturulması için C max 'ın ortalama mutlak %PE'si ve formülasyonun bireysel formülasyonun AUC'si %15'in altında bulundu, naproksen sodyumun IVIVC modelleri geçerlidir. Dış validasyon sırasında, naproksen sodyumun sürekli salım tableti için öngörülen eğri, derhal salım tableti ile aynı bulunması geçerli olduğunu göstermektedir. Sonuç: Bu IVIVC, in vivo biyoyararlanım araştırması için vekil olarak hizmet edebilir ve biyolojik yönlendiricileri destekler, çözünme yöntemlerini ve spesifikasyon ayarlarını destekler ve onaylar, ölçek büyütme ve onay sonrası değişiklikler sırasında kalite kontrolünde yardımcı olur. Yer değişikliği, proses değişiklikleri ve farklı emisyon oranlarına sahip naproksen sodyum ürünlerinin emme performansını tahmin etmek için kullanılabilir. Anahtar kelimeler: IVIVC, naproksen sodyum, sürekli salım, çözünme, in vivo biyoyararlanım çalışması, iç ve dış öngörülebilirlik Objectives:The aim of the present study was to develop and validate an in vitro-in vivo correlation (IVIVC) for naproxen sodium-sustained release tablets and to compare their plasma concentrations over time with the immediate-release tablets. Materials and Methods:In vitro release rate data were obtained for each tablet by using the USP Apparatus II, paddle stirrer at 50 rpm in pH 7.4 phosphate buffer. A four-way crossover study was conducted in 6 healthy subjects by administering naproxen sodium sustained release 375 mg and 500 mg of immediate release tablets. Series of blood samples were collected over 24 hours and estimated by using the validated liquid chromatography tandem-mass spectrometry method. Results: The similarity factor was calculated and it was found that values between, 50 and 100 indicates similarity of the profiles. Assessment of predicted and observed bioavailability was performed and prediction errors (PE) % calculated, as per the Food Drug Administration guidelines, the average absolute PE% of C max and AUC of individual formulation was found below 15% for establishment of IVIVC, based on ...

show abstract

Biopharmaceutical characterization of oral controlled/modified-release drug products. In vitro/in vivo correlation of roxatidine

Cited by 8 publications

References 3 publications

In Vitro–In Vivo Correlation in Dosage Form Development: Case Studies

In Vitro–In Vivo Correlation in Dosage Form Development: Case Studies

Dissolution specifications based on release rates

Development, Internal and External Validation of Naproxen Sodium Sustained Release Formulation: an Level A <i>In Vitro-In Vivo</i> Correlation

Contact Info

Product

Resources

About