Formation of Mefenamic Acid Nanocrystals with Improved Dissolution Characteristics

Konnerth, Christoph; Braig, Veronika; Ito, Atsutoshi; Schmidt, Jochen; Lee, Geoffrey; Peukert, Wolfgang

doi:10.1002/cite.201600190

Cited by 20 publications

(8 citation statements)

References 69 publications

(85 reference statements)

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“…Obtained drug particles are only composed of the most stable polymorph. Direct compressed tablets containing MA nanocrystals exhibit a significant improvement of in vitro dissolution kinetics as compared to tablets with micronized drug particles [74]. The modeling of process chains with or without recirculation requires approaches that are known in chemical engineering as flowsheet simulations.…”

Section: Post-processing and Modeling Of Process Chainsmentioning

confidence: 99%

Modeling and Simulation of Process Technology for Nanoparticulate Drug Formulations—A Particle Technology Perspective

Uhlemann

Diedam

Hoheisel³

et al. 2020

Pharmaceutics

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Crystalline organic nanoparticles and their amorphous equivalents (ONP) have the potential to become a next-generation formulation technology for dissolution-rate limited biopharmaceutical classification system (BCS) class IIa molecules if the following requisites are met: (i) a quantitative understanding of the bioavailability enhancement benefit versus established formulation technologies and a reliable track record of successful case studies are available; (ii) efficient experimentation workflows with a minimum amount of active ingredient and a high degree of digitalization via, e.g., automation and computer-based experimentation planning are implemented; (iii) the scalability of the nanoparticle-based oral delivery formulation technology from the lab to manufacturing is ensured. Modeling and simulation approaches informed by the pharmaceutical material science paradigm can help to meet these requisites, especially if the entire value chain from formulation to oral delivery is covered. Any comprehensive digitalization of drug formulation requires combining pharmaceutical materials science with the adequate formulation and process technologies on the one hand and quantitative pharmacokinetics and drug administration dynamics in the human body on the other hand. Models for the technical realization of the drug production and the distribution of the pharmaceutical compound in the human body are coupled via the central objective, namely bioavailability. The underlying challenges can only be addressed by hierarchical approaches for property and process design. The tools for multiscale modeling of the here-considered particle processes (e.g., by coupled computational fluid dynamics, population balance models, Noyes–Whitney dissolution kinetics) and physiologically based absorption modeling are available. Significant advances are being made in enhancing the bioavailability of hydrophobic compounds by applying innovative solutions. As examples, the predictive modeling of anti-solvent precipitation is presented, and options for the model development of comminution processes are discussed.

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Section: Post-processing and Modeling Of Process Chainsmentioning

confidence: 99%

Modeling and Simulation of Process Technology for Nanoparticulate Drug Formulations—A Particle Technology Perspective

Uhlemann

Diedam

Hoheisel³

et al. 2020

Pharmaceutics

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“…DOI: 10.13040/IJPSR.0975-8232.11 (8). This article can be accessed online on www.ijpsr.com DOI link: http://dx.doi.org/10.13040/IJPSR.0975-8232.11 (8).3960-67…”

Section: Quick Response Codementioning

confidence: 99%

Untitled

2020

IJPSR

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In the present work, the aim was to prepare a selfemulsifying drug delivery system of poorly soluble analgesic, mefenamic acid to improve its solubility with a view to enhance its oral bioavailability. From the solubility studies the selected oil, surfactant and co-surfactant was soyabean oil; tween 80, span 20; glycerol. Blends of surfactant mixtures containing tween 80, span 20, and glycerol were prepared. Three ratios of S mix containing tween 80: span 20: glycerol viz. 1:0.25:1, 1:1:1, 2:2:1; were used to construct pseudo ternary phase diagram to select nine formulation composition. Nine self-emulsifying formulations of mefenamic were prepared and evaluated for optical transparency, low refractive index, uniformity index, low viscosity, and drug release. The best formulations in all aspects of the evaluation were subjected to stability testing. The optimized formulation has been found to have good physical stability and longest shelf life of 13.45 months under accelerated storage conditions with degradation rate constant 1.38 × 10-3 months.

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“…Ten years later Osawa et al, [5] and Sarode et al, [6], gave the same explanation for the better solubility and permeability results of sulindac [5] and felodipine [6], in HPC-SSL containing solid dispersions. A short time ago, some of us published the effi cient performance of the ultra-low molecular weight HPC-UL as best milling aid and solubilizer for Izraconazole in aqueous nano-suspensions [7].…”

Section: Introductionmentioning

confidence: 99%

Differential Analysis of O-(2- hydroxypropyl) cellulose by Using Two-Dimensional 1H-NMR Spectroscopy

Sakamoto¹,

Stoyanov²

2020

Biomed Sci Eng

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Two-dimensional 1 H-NMR is used to determine the intra-molecular interactions of O-(2-hydroxypropyl) cellulose (HPC) in aqueous (D 2 O), DMF and DMSO solutions. Four grades HPC with different molecular weights are analyzed by using NOESY (Nuclear Overhauser Effect Spectroscopy) for proton-proton cross-interactions. A strong dependence of the polymer chain structure on the HPC Molecular Weight (MW) is overserved. The lower MW HPCs exist in solutions as a more linear chain showing less proton-proton interactions whereas the higher MW HPCs are more twisted and bended and form a tangled molecule mess with very intensive interactions between the -CH 3 , -CH 2 -and -C-H protons. From all the grades, the ultra-low molecular weight HPC-UL (MW 20,000) revealed the weakest proton-proton cross-relaxations and exists in solutions probably only as an almost linear chain polymer.

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Formation of Mefenamic Acid Nanocrystals with Improved Dissolution Characteristics

Cited by 20 publications

References 69 publications

Modeling and Simulation of Process Technology for Nanoparticulate Drug Formulations—A Particle Technology Perspective

Modeling and Simulation of Process Technology for Nanoparticulate Drug Formulations—A Particle Technology Perspective

Untitled

Differential Analysis of O-(2- hydroxypropyl) cellulose by Using Two-Dimensional 1H-NMR Spectroscopy

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