The influence of different mechanical stress on the release properties of HPMC matrix tablets in sucrose-NaCl media

Vrbanac, Helena; Krese, Ana

doi:10.1016/j.jddst.2019.101246

Cited by 9 publications

(5 citation statements)

References 38 publications

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“…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). Sodium chloride was used as an osmogen, and it has been reported that even when used in smaller concentrations it produces high osmotic pressure, than any other osmogens (Liu et al, 2020;Nie et al, 2020).…”

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

confidence: 99%

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: 99%

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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“…Hydroxypropyl methyl cellulose is a semisynthetic cellulose ether polymer that can be dissolved in water and a solution of alcohol, propanol, and dichloroethane (Vrbanac & Krese, 2019). The properties of HPMC are relatively stable, and its colloidal solution has a certain viscoelasticity (Tam, Oguz, Aydogdu, Sumnu, & Sahin, 2017).…”

Section: Physicochemical Properties Of Hydroxypropyl Methyl Cellulosementioning

confidence: 99%

Soil infiltration and conservative solute transport characteristics with different viscosity of hydroxypropyl methyl cellulose

Ren

Shao

et al. 2020

Soil Science Soc of Amer J

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Hydroxypropyl methyl cellulose (HPMC), a potential soil improver with the ability to hold water, has practical applicability in alleviating soil and water nutrient loss. By using Cl− as tracer ions, we evaluated the effects of different HPMC viscosities on soil water infiltration characteristics and conservative solute migration characteristics. Hydroxypropyl methyl cellulose with viscosities of 2 × 104, 6 × 104, 10 × 104, and 20 × 104 mPa s−1 was selected. Experimental results revealed that the cumulative infiltration amount, wetting front migration distance, and infiltration rate decreased significantly with increased HPMC viscosity. The addition of HPMC delayed the soil solute transport process, and HPMC with a higher viscosity caused greater soil solute transport delay. Both the convection‐dispersion equation (CDE) and the two‐region model (TRM) accurately simulated solute transport, but the simulation accuracy of the TRM was higher. Results of parametric fitting based on the TRM indicated that the average pore water velocity, hydrodynamic dispersion coefficient, and dispersion degree decrease with increased HPMC viscosity. The average pore water velocity decreased by 13.6–28.2% relative to the control group (CG). Compared with the CG, the water content ratio in movable water of HPMC groups changed irregularly with an increase in viscosity. The mass exchange coefficient increased significantly compared with the CG, with an irregular trend. These data will be useful in the application and promotion of HPMC as a soil improver.

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“…The influence of this osmotically active and viscous medium on the release properties of HPMC tablets is more expressed compared to the highcalorie Ensure Plus®. The observed effects have been already studied [35,38,39,61,62], however, in contrast to these experiments with extremely high contents of solutes, a more realistic dissolution medium with lower sugar content was used in our study. Despite the lower concentrations, we observed a drastic effect on the model drug release kinetics, which could potentially be manifested as a lower plasma concentration in vivo in a similar situation.…”

Section: Effect Of Dietary Sugarsmentioning

confidence: 99%

“…The effects of food, food components or alcoholic beverages on the in vitro model drug release kinetics have been already investigated in many studies. However, in most of these studies, static dissolution apparatuses were used where only hydrodynamic stress was present [33][34][35][36], or devices that exert relatively low mechanical stresses [37][38][39]. In the present study, we employ a biorelevant in vitro dissolution model, the advanced gastric simulator (AGS) [31,40] to study the effect of fed conditions combined with strong mechanical stresses on the BCS class I model drug (paracetamol) release form the HPMC matrix tablets.…”

Section: Introductionmentioning

confidence: 99%

Mechanistic study of model drug release from HPMC matrices in fed gastric media

Vrbanac

Trontelj

Kalčič³

et al. 2020

Journal of Drug Delivery Science and Technology

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The influence of different mechanical stress on the release properties of HPMC matrix tablets in sucrose-NaCl media

Cited by 9 publications

References 38 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™

Soil infiltration and conservative solute transport characteristics with different viscosity of hydroxypropyl methyl cellulose

Mechanistic study of model drug release from HPMC matrices in fed gastric media

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