Effect of gastrointestinal transit on micro-environmental pH inside HPMC matrix tablets – in vitro study

Vrbanac, Helena; Trontelj, Jurij; Osojnik, Ajda; Berginc, Katja; Janković, Biljana

doi:10.1016/j.ijpharm.2021.120718

Cited by 3 publications

(1 citation statement)

References 29 publications

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“…A linear relationship between percentage drug release and orifice diameter and weight gain after coating was also reported by Gundu et al, 2020). An extensive literature survey was performed to select process and formulation factors (Li N. et al, 2019;Cheng et al, 2020;Gioumouxouzis et al, 2020;Vrbanac et al, 2021). Vrbanac et al also used Methocel ™ K4M as rate controlling agent in sustained and controlled release oral dosage forms prepared by the direct compression method because of its good compressibility (Vrbanac and Krese, 2019).…”

Section: Design Of Experiments (Doe) For Elementary Osmotic Tabletsmentioning

confidence: 94%

SeDeM tool-driven full factorial design for osmotic drug delivery of tramadol HCl: Formulation development, physicochemical evaluation, and in-silico PBPK modeling for predictive pharmacokinetic evaluation using GastroPlus™

Saleem

Shoaib²,

Yousuf³

et al. 2022

Front. Pharmacol.

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The study is based on using SeDeM expert system in developing controlled-release tramadol HCl osmotic tablets and its in-silico physiologically based pharmacokinetic (PBPK) modeling for in-vivo pharmacokinetic evaluation. A Quality by Design (QbD) based approach in developing SeDEM-driven full factorial osmotic drug delivery was applied. A 24 Full-factorial design was used to make the trial formulations of tramadol HCl osmotic tablets using NaCl as osmogen, Methocel K4M as rate controlling polymer, and avicel pH 101 as diluent. The preformulation characteristics of formulations (F1-F16) were determined by applying SeDeM Expert Tool. The formulation was optimized followed by in-vivo predictive pharmacokinetic assessment using PBPK “ACAT” model of GastroPlus™. The FTIR results showed no interaction among the ingredients. The index of good compressibility (ICG) values of all trial formulation blends were ≥5, suggesting direct compression is the best-suited method. Formulation F3 and F4 were optimized based on drug release at 2, 10, and 16 h with a zero-order kinetic release (r2 = 0.992 and 0.994). The SEM images confirmed micropores formation on the surface of the osmotic tablet after complete drug release. F3 and F4 were also stable (shelf life 29.41 and 23.46 months). The in vivo simulation of the pharmacokinetics of the PBPK in-silico model revealed excellent relative bioavailability of F3 and F4 with reference to tramadol HCl 50 mg IR formulations. The SeDeM expert tool was best utilized to evaluate the compression characteristics of selected formulation excipients and their blends for direct compression method in designing once-daily osmotically controlled-release tramadol HCl tablets. The in-silico GastroPlus™ PBPK modeling provided a thorough pharmacokinetic assessment of the optimized formulation as an alternative to tramadol HCl in vivo studies.

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Section: Design Of Experiments (Doe) For Elementary Osmotic Tabletsmentioning

confidence: 94%

SeDeM tool-driven full factorial design for osmotic drug delivery of tramadol HCl: Formulation development, physicochemical evaluation, and in-silico PBPK modeling for predictive pharmacokinetic evaluation using GastroPlus™

Saleem

Shoaib²,

Yousuf³

et al. 2022

Front. Pharmacol.

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Propranolol Hydrochloride Film Coated Tablets Using Natural Rubber Latex Blends as Film Former

et al. 2021

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Towards a better understanding of thermally treated polycarbophil matrix tablets for controlled release

Baldassari

Cirrincione

Ailuno

et al. 2021

International Journal of Pharmaceutics: X

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Effect of gastrointestinal transit on micro-environmental pH inside HPMC matrix tablets – in vitro study

Cited by 3 publications

References 29 publications

SeDeM tool-driven full factorial design for osmotic drug delivery of tramadol HCl: Formulation development, physicochemical evaluation, and in-silico PBPK modeling for predictive pharmacokinetic evaluation using GastroPlus™

SeDeM tool-driven full factorial design for osmotic drug delivery of tramadol HCl: Formulation development, physicochemical evaluation, and in-silico PBPK modeling for predictive pharmacokinetic evaluation using GastroPlus™

Propranolol Hydrochloride Film Coated Tablets Using Natural Rubber Latex Blends as Film Former

Towards a better understanding of thermally treated polycarbophil matrix tablets for controlled release

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