Design of experiment (DoE)-based formulation design of bepotastine sustained-release tablet and in vitro-in vivo pharmacokinetic correlation

Jeon, Sang-Won; Park, Jin‐Hyun; Kim, Joo-Eun; Park, Young-Joon

doi:10.1007/s40005-023-00611-4

Cited by 6 publications

(4 citation statements)

References 24 publications

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“…The therapeutic effectiveness of dosage forms is a critical aspect of pharmaceutical science and patient care. It depends on a combination of formulation design, pharmacokinetic properties, patient factors, and treatment adherence regimens [ 23 ]. Formulation scientists continuously strive to develop innovative dosage forms that maximize drug efficacy, safety, and patient convenience [ 8 , 24 , 25 ].…”

Section: Discussionmentioning

confidence: 99%

“…Formulation scientists continuously strive to develop innovative dosage forms that maximize drug efficacy, safety, and patient convenience [ 8 , 24 , 25 ]. Appropriate formulation design is an important parameter for pharmaceutical development that aims to ensure product quality by designing and controlling manufacturing processes [ 23 , 25 ]. It involves the application of scientific principles and risk-management strategies throughout the product lifecycle, from initial development to commercial production [ 26 ].…”

Section: Discussionmentioning

confidence: 99%

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In Vitro/In Vivo Correlation of Two Extended-Release Cilostazol Formulations

Min,

Kim,

Jin

et al. 2024

Pharmaceuticals

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This study aims to evaluate and determine the correlation between in vitro release and in vivo pharmacokinetics of two extended-release dosage forms of Cilostazol. In vitro release profiles for two dosage forms, tablet and capsule, were analyzed under physiologically mimicked medium conditions using the paddle and basket USP release apparatus. A single-dose, two-period crossover study design in beagle dogs was applied for the pharmacokinetic study. The fed and fast effects were considered for evaluation. Pseudo gastric release medium transfer setup study from pH 1.2 to pH 6.8 (+0.5% SLS) and pH 1.2 to pH 6.8 (+1.0% SLS) demonstrated that Pletaal® SR 200 mg capsules have higher drug release rates than Cilostan® CR 200 mg tablets. Similarly, in vivo study showed Cilostazol concentration in plasma and AUC was lower under the fast state than the fed state. The ratio of least squared geometric mean values, Cmax, AUC0-t, and AUC0-inf of Cilostazol were 2.53-fold, 2.89-fold, and 2.87-fold higher for Pletaal® SR 200 mg capsules compared with Cilostan® CR 200 mg tablets, respectively. Correlation of in vitro/in vivo data indicated that Pletal® SR 200 mg capsules have better release and pharmacodynamic effect than Cilostan® CR 200 mg tablets.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

In Vitro/In Vivo Correlation of Two Extended-Release Cilostazol Formulations

Min,

Kim,

Jin

et al. 2024

Pharmaceuticals

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“…Approximately 150 μL blood samples were collected from a cannula inserted into the femoral artery at 0, 2, 5, 10, 15, 30, 60, 120, 180, 240, 360, and 480 min post-administration. The blood was immediately centrifuged at 3000× g for 10 min at 4 °C to obtain the plasma [ 42 ], which was pretreated and analyzed using the UPLC-MS/MS method.…”

Section: Methodsmentioning

confidence: 99%

A High-Performance Liquid Chromatography with Photodiode Array Detection Method for Simultaneous Determination of Three Compounds Isolated from Wikstroemia ganpi: Assessment of the Effects on Cytochrome P450-Mediated Metabolism In Vitro and In Vivo

Keem,

Seo,

Kim

et al. 2023

Nutrients

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In natural products, the content and quality of the marker components differ depending on the part, production area, collection period, and extraction method; therefore, a standardized analysis method is required to obtain consistent results. This study developed a simultaneous analysis method for three marker components (7-methoxylutolin-5-O-glucoseide, pilloin 5-O-β-d-glucopyranoside, rutarensin) isolated and purified from Wikstroemia ganpi (W. ganpi). Simultaneous analysis was performed using high-performance liquid chromatography with photodiode array detection (HPLC-PDA) method that was validated according to the International Council for Harmonisation (ICH) guidelines. The developed analytical method exhibited linearity (r2 > 0.999), detection limits (0.72–3.34 μg/mL), and quantification limits (2.19–10.22 μg/mL). The relative standard deviation (RSD) value of intra- and inter-day precisions was less than 1.68%, and analyte recoveries (93.42–117.55%; RSD < 1.86%) were validated according to the analytical procedures, and all parameters were within the allowable range. Quantitative analysis of the three marker components from W. ganpi MeOH extract (WGM) showed 7-methoxylutolin-5-O-glucoseide with the highest content (51.81 mg/g). The inhibitory effects of WGM on cytochrome P450 (CYP) substrate drugs were further investigated. The in vitro study revealed that WGM inhibited the CYP3A-mediated metabolism of buspirone and that 7-methoxylutolin-5-O-glucoseide and pilloin 5-O-β-d-glucopyranoside inhibited the metabolism of buspirone with IC50 values of 2.73 and 18.7 μM, respectively. However, a single oral dose of WGM did not have significant effects on the pharmacokinetics of buspirone in rats, suggesting that WGM cannot function as an inhibitor of CYP3A-mediated metabolism in vivo.

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“…The direct compression (DC) method is the first choice for preparing tablets [ 14 ]. The production process includes blending the active substances with pharmaceutical excipients and lubricants, followed by tabletization, with no additional processing steps.…”

Section: Introductionmentioning

confidence: 99%

Novel Bioequivalent Tablet of Solifenacin Succinate Prepared Using Direct Compression Technique for Improved Chemical Stability

Kim

Jeong

et al. 2023

Pharmaceutics

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We designed a bioequivalent tablet form of solifenacin succinate (SOL) with an improved storage stability using a direct compression (DC) technique. An optimal direct compressed tablet (DCT) containing an active substance (10 mg), lactose monohydrate, and silicified microcrystalline cellulose as diluents, crospovidone as a disintegrant, and hydrophilic fumed silica as an anti-coning agent was constructed by evaluating the drug content uniformity, mechanical properties, and in vitro dissolution. The physicochemical and mechanical properties of the DCT were as follows: drug content 100.1 ± 0.7%, disintegration time of 6.7 min, over 95% release within 30 min in dissolution media (pH 1.2, 4.0, 6.8, and distilled water), hardness > 107.8 N, and friability ~0.11%. The SOL-loaded tablet fabricated via DC showed an improved stability at 40 °C and RH 75%, exhibiting markedly reduced degradation products compared to those fabricated using ethanol or water-based wet granulation or a marketed product (Vesicare®, Astellas Pharma). Moreover, in a bioequivalence study in healthy subjects (n = 24), the optimized DCT offered a pharmacokinetic profile comparable to that of the marketed product, with no statistical differences in the pharmacokinetic parameters. The 90% CIs for the geometric mean ratios of the test to the reference formulation for the area under the curve and the maximum drug concentration in plasma were 0.98–1.05 and 0.98–1.07, respectively, and satisfied the FDA regulatory criteria for bioequivalence. Thus, we conclude that DCT is a beneficial oral dosage form of SOL with an improved chemical stability.

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Design of experiment (DoE)-based formulation design of bepotastine sustained-release tablet and in vitro-in vivo pharmacokinetic correlation

Cited by 6 publications

References 24 publications

In Vitro/In Vivo Correlation of Two Extended-Release Cilostazol Formulations

In Vitro/In Vivo Correlation of Two Extended-Release Cilostazol Formulations

A High-Performance Liquid Chromatography with Photodiode Array Detection Method for Simultaneous Determination of Three Compounds Isolated from Wikstroemia ganpi: Assessment of the Effects on Cytochrome P450-Mediated Metabolism In Vitro and In Vivo

Novel Bioequivalent Tablet of Solifenacin Succinate Prepared Using Direct Compression Technique for Improved Chemical Stability

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