Drug release from extruded solid lipid matrices: Theoretical predictions and independent experiments

Güres, Sinan; Siepmann, Florence; Siepmann, Juergen; Kleinebudde, Peter

doi:10.1016/j.ejpb.2011.10.002

Cited by 20 publications

(5 citation statements)

References 28 publications

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“…In a first step, we investigated lipid-based extrudates, a solid oral dosage form exhibiting a cylindrical morphology. These drug delivery systems were obtained after extrusion of physical powder mixtures and have already been thoroughly characterized in the past (19)(20)(21). However, analysis of component distribution with confocal Raman microscopy has thus far been limited to cross sections as the curvature of the cylindrical form impaired analysis of the exterior surface.…”

Section: Resultsmentioning

confidence: 99%

Chemical Imaging of Drug Delivery Systems with Structured Surfaces–a Combined Analytical Approach of Confocal Raman Microscopy and Optical Profilometry

Kann

Windbergs

2013

AAPS J

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Confocal Raman microscopy is an analytical technique with a steadily increasing impact in the field of pharmaceutics as the instrumental setup allows for nondestructive visualization of component distribution within drug delivery systems. Here, the attention is mainly focused on classic solid carrier systems like tablets, pellets, or extrudates. Due to the opacity of these systems, Raman analysis is restricted either to exterior surfaces or cross sections. As Raman spectra are only recorded from one focal plane at a time, the sample is usually altered to create a smooth and even surface. However, this manipulation can lead to misinterpretation of the analytical results. Here, we present a trendsetting approach to overcome these analytical pitfalls with a combination of confocal Raman microscopy and optical profilometry. By acquiring a topography profile of the sample area of interest prior to Raman spectroscopy, the profile height information allowed to level the focal plane to the sample surface for each spectrum acquisition. We first demonstrated the basic principle of this complementary approach in a case study using a tilted silica wafer. In a second step, we successfully adapted the two techniques to investigate an extrudate and a lyophilisate as two exemplary solid drug carrier systems. Component distribution analysis with the novel analytical approach was neither hampered by the curvature of the cylindrical extrudate nor the highly structured surface of the lyophilisate. Therefore, the combined analytical approach bears a great potential to be implemented in diversified fields of pharmaceutical sciences.

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Section: Resultsmentioning

confidence: 99%

Chemical Imaging of Drug Delivery Systems with Structured Surfaces–a Combined Analytical Approach of Confocal Raman Microscopy and Optical Profilometry

Kann

Windbergs

2013

AAPS J

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“…The dataset contains results of dissolution tests carried out for 5 various formulations of lipid extrudates. Extrudates consisting of diprophylline (Diprophylline Base, BASF, Ludwigshafen, Germany), tristearin (Dynasan 118, Sasol, Witten, Germany), and polyethylene glycol of a mean molecular weight of 20000 (Polyglykol 20000, Clariant, Sulzbach, Germany) in a 50 : 45 : 5%-ratio (w/w/w) were produced by solid lipid extrusion [ 26 ]. Extrudates were varied by their length ( L ) and diameter ( d ), where L was in the range from 5 mm to 18 mm and d between 0.6 mm and 3.5 mm ( Table 1 ).…”

Section: Methodsmentioning

confidence: 99%

From Heuristic to Mathematical Modeling of Drugs Dissolution Profiles: Application of Artificial Neural Networks and Genetic Programming

Mendyk

Güres

Jachowicz

et al. 2015

Computational and Mathematical Methods in Medicine

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The purpose of this work was to develop a mathematical model of the drug dissolution (Q) from the solid lipid extrudates based on the empirical approach. Artificial neural networks (ANNs) and genetic programming (GP) tools were used. Sensitivity analysis of ANNs provided reduction of the original input vector. GP allowed creation of the mathematical equation in two major approaches: (1) direct modeling of Q versus extrudate diameter (d) and the time variable (t) and (2) indirect modeling through Weibull equation. ANNs provided also information about minimum achievable generalization error and the way to enhance the original dataset used for adjustment of the equations' parameters. Two inputs were found important for the drug dissolution: d and t. The extrudates length (L) was found not important. Both GP modeling approaches allowed creation of relatively simple equations with their predictive performance comparable to the ANNs (root mean squared error (RMSE) from 2.19 to 2.33). The direct mode of GP modeling of Q versus d and t resulted in the most robust model. The idea of how to combine ANNs and GP in order to escape ANNs' black-box drawback without losing their superior predictive performance was demonstrated. Open Source software was used to deliver the state-of-the-art models and modeling strategies.

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“…The molding and spray congealing of insoluble lipids create a very incomprehensible system that releases extremely slow drugs so a very long period of time, but the compression of a physical powder mixture makes it easy for water to spread into the device. The inclusion of other components may be used to control and optimize the drug released from the lipid matrix 45,46 . This modulation is caused by facilitation or inhibition of water input to the matrix.…”

Section: Drug Release Adjustmentmentioning

confidence: 99%

A Concise review on application of solid lipids and various techniques in the formulation development

Ahire¹,

Kamble²

2023

J. Drug Delivery Ther.

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Lipids have wide range of applications in food and pharmaceuticals. The pharmaceuticals application of lipid is to improve solubility of drug also helps to improve the bioavailability. The dissolution/dissolving phase, which is probably the rate-limiting component for oral absorption of poorly water-soluble drugs, is eliminated by pre-dissolving pharmaceuticals in lipids, surfactants, or combinations of lipid excipients and surfactants. The most widely used co-solvents, together with lipid excipients, are propylene glycol, glycerol, and polyethylene glycols-400, poloxamer etc. various technologies are used such as melt extrusion, melt granulation for preparation of lipid based oral modified released dosage forms. This review summaries the overview of the lipid excipients in terms of their classification, methods of absorption, and lipid-based product development. The manufacture of solid and semi-solid lipid formulations using various methodologies, applications, phase behaviour, and the regulatory outlook of lipid excipients are covered. Keywords: Solid lipids, lipid classification, solidification techniques, modified released.

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Drug release from extruded solid lipid matrices: Theoretical predictions and independent experiments

Cited by 20 publications

References 28 publications

Chemical Imaging of Drug Delivery Systems with Structured Surfaces–a Combined Analytical Approach of Confocal Raman Microscopy and Optical Profilometry

Chemical Imaging of Drug Delivery Systems with Structured Surfaces–a Combined Analytical Approach of Confocal Raman Microscopy and Optical Profilometry

From Heuristic to Mathematical Modeling of Drugs Dissolution Profiles: Application of Artificial Neural Networks and Genetic Programming

A Concise review on application of solid lipids and various techniques in the formulation development

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