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Shah, Vinod P.; Tsong, Yi; Sathe, Pradeep; Liu, Jen‐pei

doi:10.1023/a:1011976615750

Cited by 551 publications

(125 citation statements)

References 5 publications

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“…Data were further evaluated using difference ( f 1 ) and similarity ( f 2 ) factors, broadly adopted by regulatory agencies as an indication of the similarity between dissolution profiles. 19,22,32) Values outside the specified range of f 1 =0 to 15 and f 2 =50 to 100 indicated differences between the dissolution profiles.…”

Section: Methodsmentioning

confidence: 99%

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Bezerra

Pinto

Cabral

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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Gliclazide (GLZ) is a second generation hypoglycemic drug used for the treatment of Type 2 diabetes mellitus. The low solubility of GLZ has been described as the rate limiting step for drug dissolution and absorption, thus a prediction of its in vivo behavior based on a discriminative dissolution test should lead to a relevant in vitro-in vivo correlation (IVIVC). The aim of this study was to develop a dissolution method for GLZ modified-release (MR) tablets using an United States Pharmacopeia (USP) apparatus 3 through its evaluation by an IVIVC analysis. Various dissolution parameters were evaluated to establish an in vitro method for GLZ tablets. The final dissolution conditions, referred to as method 3, utilized a 400 µm mesh and 30 dips per minute over a total period of 10 h that included 1h in HCl media (pH 1.2), 2h in acetate buffer solution (pH 4.5), 1 h in phosphate buffer solution (PBS; pH 5.8), 5h in PBS (pH 6.8) and finally 1h in PBS (pH 7.2). The calculated point-to-point IVIVC (R 2 0.9970) was significantly greater than other methods. The robustness of method 3 suggests it could be applied to pharmaceutical equivalence studies and for quality control analyses of GLZ.

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Section: Methodsmentioning

confidence: 99%

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Bezerra

Pinto

Cabral

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…In order to consider the two compared profiles as similar, the value of this factor needs to be greater than 50 (32). For the two optimal formulations, no significant differences in dissolution profiles were observed, the values registered for f 2 being 83.74 for the lactose formulation and 74.53 for the formulation developed with cellulose as diluent.…”

Section: Design Space and Formulation Optimizationmentioning

confidence: 99%

Formulation and pharmaceutical development of quetiapine fumarate sustained release matrix tablets using a QbD approach

et al. 2017

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The main objective of the present study was to apply QbD methodology in the development of once-a-day sustained release quetiapine tablets. The quality target product profile (QTPP) was defined after the pharmaceutical properties and kinetic release of the innovator product, Seroquel XR 200 mg. For the D-optimal experimental design, the level and ratio of matrix forming agents and the type of extragranular diluent were chosen as independent inputs, which represented critical formulation factors. The critical quality attributes (CQAs) studied were the cumulative percentages of quetiapine released after certain time intervals. After the analysis of the experimental design, optimal formulas and the design space were defined. Optimal formulas demonstrated zero-order release kinetics and a dissolution profile similar to the innovator product, with f 2 values of 74.53 and 83.74. It was concluded that the QbD approach allowed fast development of sustained release tablets with similar dissolution behavior as the innovator product.Keywords: quality by design, design of experiments, sustained release, hydrophilic matrix, quetiapineIn the past years, the main goal of antipsychotic drug development has been to develop molecules with higher efficacy and fewer side effects usually associated with the classic antipsychotic medications. The newly developed agents, called atypical antipsychotics, are successfully used in the treatment of both positive and negative symptoms of schizophrenia and are associated with fewer neurological and endocrine side effects compared to older medications (1). Quetiapine is a recently introduced atypical antipsychotic, which has an excellent risk/benefit ratio and is indicated as the first-line option for the treatment of psychotic disorder manifestations and schizophrenia (2). Quetiapine is available as fumarate salt in immediate as well as in sustained released formulations, the innovative product being Seroquel. The sustained release formulation was introduced several years ago and its primary objective is to release the drug slowly over an extended ALEXANDRU GAVAN

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“…11,12) The difference factor measures the percent error between two profiles as in the following equation. (4) where n is the sampling number, and R and T are the cumulative percentage dissolved amounts of the reference and test products at each time point j.…”

Section: Methodsmentioning

confidence: 99%

“…In general, f 1 values lower than 15 and f 2 values higher than 50 show the similarity of the dissolution profiles within 10% of the difference. 11) Pharmacokinetic Study in Beagle Dogs This was a single-dose, openlabel, randomized, two-period crossover study in dogs. The experiments for the evaluation of the pharmacokinetic study in dogs were approved by the Ethics Committee for Animal Experimentation of Haeeun Primate Research Center (Seongnam, Gyeonggi, Korea).…”

Section: Methodsmentioning

confidence: 99%

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Formulation Variation and in Vitro-in Vivo Correlation for a Rapidly Swellable Three-Layered Tablet of Tamsulosin HCl

Park

Shim

Park

et al. 2011

CHEMICAL & PHARMACEUTICAL BULLETIN

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Regular ArticleA novel three-layered tablet technology consisting of an inner immediate release layer and two extended release barrier layers with swellable polymers has been suggested and investigated as once-a-day tablet formulations. 1) In that formulation, dissolution medium quickly permeates to the inner layer of water-soluble excipients, and the two barrier layers swell to surround the inner layer rapidly, controlling drug release from the inner layer. After oral administration, the tablet might become fully hydrated quickly and reach the colon where little water is available. The hydrated state of the tablet might induce continuous drug release even in the colon.As an extended study on the technology and to investigate the feasibility as a once-a-day tablet formulation, a hydrophilic model drug (tamsulosin HCl) was selected and various three-layered tablet formulations were evaluated together with their properties. These formulations were also compared with a commercial product, tamsulosin OCAS ® , to achieve more consistent plasma drug concentrations. Additionally, a pharmacokinetic study of the three-layered tablets using beagle dogs was performed in comparison with the results of the reference tablet.Tamsulosin Fig. 1), is a third-generation a1-adrenoceptor (AR) antagonist and has been developed for the treatment of lower urinary tract symptoms suggestive of benign prostatic hyperplasia (LUTS/BPH). 2) Among the currently available a1-AR antagonists, tamsulosin is the most frequently prescribed pharmacological therapy due to its favorable selectivity for human prostatic tissue, which is probably related to the a1 A and a1 D -AR subtypes. 3,4) Tamsulosin HCl modified-release (MR) capsules are developed by Astellas Pharma Inc., and marketed under the trade names Harnal, Flomax, Flomaxtra, and Urimax. On the other hand, generic non-modified release capsules are still approved and marketed in many countries such as Canada and the U.S. The tamsulosin MR capsule formulations, however, have some limitations such as food dependent absorption.3) The labeling information recommends that the capsule needs to be taken after breakfast or after the first meal of the day. Lack of compliance with this dosing recommendation may cause increased exposure to the drug, leading to a higher risk of vasodilatation-related adverse effects like dizziness, headache, orthostatic hypotension, and syncope. 5) To reduce the occurrence of the adverse effects, new oral controlled absorption systems have been developed and used to overcome the low absorption properties even from the colon. 6) The OCAS ® formulation is a controlled release system of a gel matrix type, with gel-forming and gel-enhancing components. Polyethylene glycol (PEG), a gel-enhancing agent, is a hydrophilic agent that facilitates water uptake into the tablets. It may ensure very rapid and nearly complete gelation/hydration of a hydrophilic gel-forming agent (i.e., polyethylene oxide (PEO)) in the upper part of the gastrointestinal (GI) tract, stomach, and small int...

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Abstract: The similarity factor f2 is a simple measure for the comparison of two dissolution profiles. But the commonly used similarity factor estimate f2 is a biased and conservative estimate of f2. The bootstrap approach is a useful tool to simulate the confidence interval.

Cited by 551 publications

References 5 publications

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Formulation and pharmaceutical development of quetiapine fumarate sustained release matrix tablets using a QbD approach

Formulation Variation and in Vitro-in Vivo Correlation for a Rapidly Swellable Three-Layered Tablet of Tamsulosin HCl

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