Influence of HPMC K100LV and Compritol® HD5 ATO on Drug Release and Rheological Behavior of HPMC K4M Matrix Tablets

Hamed, Rania; Al‐Samydai, Ali; Baraghthi, Tamadur Al; Tarawneh, Ola; Sunoqrot, Suhair

doi:10.1007/s12247-016-9269-2

Cited by 12 publications

(4 citation statements)

References 47 publications

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“…The positive values of Δ H for all studied formulations indicate that the dissolution of the studied glyceryl behenate matrix tablets is an endothermic process. Based on Equation (3), the value of Δ G is equal to Δ H − T Δ S , and if the relationship between Δ H and T Δ S is exactly linear with unit slope, there is no variation of Δ G value [ 44 ] and the value of Δ G does not depend on the amount of glyceryl behenate in a tablet. The dependence of T Δ S on Δ H for studied formulations based on glyceryl behenate is presented in Figure A.…”

Section: Resultsmentioning

confidence: 99%

A New Approach to the Dissolution Tests Management to Obtain Kinetic and Thermodynamic Data: Release of a Model Drug from Glyceryl Behenate Matrix Tablets

Slezáková

Matzick

Komersová

et al. 2021

Euro J Lipid Sci & Tech

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This study is focused on the use of glyceryl behenate as a lipophilic excipient of matrix tablets providing controlled drug release. The aim of this study is to evaluate activation energy (EA) and changes of the thermodynamic parameters (ΔH, ΔS, ΔG) of a dissolution process. These values, which have not yet been published, can lead to better understanding of a drug release mechanism and can extend the use options of glyceryl behenate in the pharmaceutical industry. Values of ΔH, ΔS, ΔG and EA, providing an overall thermodynamic view on the studied matrix tablets, are evaluated based on the temperature‐dependences of the release rate constant of a model drug (temperature range 25 ‐ 45 °C). The studied lipophilic matrix tablets contain 10% to 50% of glyceryl behenate. Dissolution testing is carried out in an aqueous solution of HCl with addition of NaCl (pH1.2). Positive values of ΔH in the range of 3.83 to 56.13 kJ mol‐1 and positive values of ΔG indicate that the dissolution of the studied glyceryl behenate matrix tablets is an endothermic process which does not proceed spontaneously (in a temperature range of 25 ‐ 45 °C). The negative slope of the linear curves of enthalpy‐entropy compensation confirms the entropy‐driven dissolution. Practical Applications: A better understanding of the dissolution process is an important aspect, e.g., in the field of drug formulation strategy. In this study, it is confirmed that the influence of temperature on the model drug release rate is negligible for tablets containing more than 40% of glyceryl behenate. It is an important result for drug design due to the reduction of risk of a possible dose dumping effect induced by temperature and the prevention of in vivo therapeutic failure.

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Section: Resultsmentioning

confidence: 99%

A New Approach to the Dissolution Tests Management to Obtain Kinetic and Thermodynamic Data: Release of a Model Drug from Glyceryl Behenate Matrix Tablets

Slezáková

Matzick

Komersová

et al. 2021

Euro J Lipid Sci & Tech

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“…For PHH-SLTs, the powerful inter-molecular interaction between swelling HPMC and CMC-Na ensured the strong continuity of the matrix. When the hydrated gel layer was fully formed, the erosion rate of polymers became slower, but the drug diffusion grew faster because of high content of water, and the drug release mechanism was mostly affected by drug diffusion [36]. During the last 2 h, PHH-SLTs and PHH-DLTs absorbed water rapidly again with a high polymer erosion rate, and thus the drug in the tablets showed a rapid and steady release.…”

Section: Resultsmentioning

confidence: 99%

Development of Paroxetine Hydrochloride Single Layer Controlled-Release Tablets Based on 32 Factorial Design

et al. 2018

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Major depressive disorder (MDD) is one of the main contributors to disability and suicide mortality globally. Paroxetine hydrochloride (PHH) is the most potent antidepressant used for MDD treatment. Due to its reduced side effects PAXIL® CR is a widely-used controlled-release formulation of PHH. However, the complicated double-layer production of PAXIL® CR faces the risk of layer separation. In this study, PHH enteric coating single layer controlled-release tablets (PHH-EC-SLTs) were designed as a simplified substitution of PAXIL® CR through a rational formulation screening. The optimized PHH-EC-SLTs showed similar release behaviors in vitro to PAXIL® CR and the release profiles corresponded to a zero-order release model (R2 = 0.9958). Polymer matrix erosion was the main release mechanism, according to the fitting exponents n > 1 in the Korsmeyer-Pappas model. Crucial pharmacokinetic parameters including peak-reaching time (Tmax), peak concentration (Cmax) and the area under the blood level-time curve (AUC0-48) of PHH-EC-SLTs and PAXIL® CR had no significant difference (p > 0.05) and the relative bioavailability (F = 97.97%) of PHH-EC-SLTs demonstrated their similar pharmacokinetic profiles in vivo. In view of avoiding layer separation risk and simplifying the preparation processing, the self-made PHH-EC-SLTs could be considered as a safe and economic alternative to PAXIL® CR.

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“…[28,35,36,37,38] Commercial derivatives of hydroxypropyl methylcellulose (HPMC) are frequently included in these oral controlled-release formulations and exist in various modifications and molecular sizes. [39] D-mannitol (MAN) is a common excipient for spray drying applications and can be used in formulations for diabetes mellitus treatment. MAN was added as a diluent to reduce the drug-load below 50 wt%.…”

Section: Introductionmentioning

confidence: 99%

Quantitative investigation of particle formation of a model pharmaceutical formulation using single droplet evaporation experiments and X-ray tomography

Doerr

Oswald

Florence

2018

Advanced Powder Technology

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The implementation of a particle design platform that can be applied to novel pharmaceutical systems using acoustic levitation (SAL) and X-ray tomography (XRT) is discussed. Acoustic levitation was employed to provide a container-less particle design environment for single droplet evaporation experiments. Dried particles were subject to further visual and quantitative structural analysis using X-ray tomography to assess the three-dimensional volume space. The workflow of the combined SAL-XRT platform

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Influence of HPMC K100LV and Compritol® HD5 ATO on Drug Release and Rheological Behavior of HPMC K4M Matrix Tablets

Cited by 12 publications

References 47 publications

A New Approach to the Dissolution Tests Management to Obtain Kinetic and Thermodynamic Data: Release of a Model Drug from Glyceryl Behenate Matrix Tablets

A New Approach to the Dissolution Tests Management to Obtain Kinetic and Thermodynamic Data: Release of a Model Drug from Glyceryl Behenate Matrix Tablets

Development of Paroxetine Hydrochloride Single Layer Controlled-Release Tablets Based on 32 Factorial Design

Quantitative investigation of particle formation of a model pharmaceutical formulation using single droplet evaporation experiments and X-ray tomography

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