Understanding the solid-state behaviour of triglyceride solid lipid extrudates and its influence on dissolution

2009 ◽  
Vol 71 (1) ◽  
pp. 80-87 ◽  
Author(s):  
M WINDBERGS ◽  
C STRACHAN ◽  
P KLEINEBUDDE
Author(s):  
Santosh Gejage ◽  
Jaywant Pawar ◽  
Purnima Amin ◽  
Mohammed Maniruzzaman

Mere similar grades of same excipients manufactured by two different manufacturers often differ significantly that they even have an impact on the variations in final product or dosage form. Solid lipids are one of the most available options as matrix former in sustained drug delivery. Due to their chemical and physical complexity, lipids may exhibit a complex behaviour (i.e. melting crystallization and polymorphism). The aim of this study was to evaluate the physical and chemical properties of two Glyceryl Monostearate (GMS) lipids (Geleol from Gattefosse and Capmul GMS 50K from Abitec Corp. USA) and how these properties may affect during melt granulation process for sustained release applications. Thermal processing was applied on GMS samples to understand the polymorphic nature and suitability as meltable binders. Niacin was used as model drug. A thorough evaluation of GMS samples and sustained release tablets was undertaken using analytical techniques such as differential scanning calorimetry (DSC), X-ray diffraction (XRD). Moreover, melt viscosity study assisted to apprehend the behaviour of GMS samples in hot melt extrusion processing. Surface morphology of the drug and extruded granules examined via SEM and AFM revealed high level of surface interaction and dense structure of drug inside lipid matrix. The DSC and XRD study confirmed that Geleol could not withstand the heat treatment applied during thecontinuous melt granulation processing. The shifting of stable β form to an unstable α form in Geleol was detected. In the contrary case, Capmul GMS 50K was able to withstand the heat treatment supported by the applied analytical techniques. Nonetheless,both GMS samples perform differently in final dosage form. This change in stable β form to an unstable α form affected dissolution profiles at 3 months storage in accelerated condition. This study helped to interpret the complex solid-state behaviour of solid lipid extrudates with different compositions, in order to the simply and outline a suitable formulation strategy for the development of lipid-based oral dosage forms.


Heterocycles ◽  
1987 ◽  
Vol 26 (2) ◽  
pp. 333 ◽  
Author(s):  
Jos� Elguero ◽  
Robert Faure ◽  
Emile-Jean Vincent ◽  
Andr� Rousseau

Author(s):  
Renata Battini ◽  
Giovanna Gavioli Battistuzzi ◽  
Giulia Grandi ◽  
Ledi Menabue ◽  
Gian Carlo Pellacani ◽  
...  

2016 ◽  
Vol 45 (36) ◽  
pp. 14243-14251 ◽  
Author(s):  
E. E. Hardy ◽  
M. A. Eddy ◽  
B. A. Maynard ◽  
A. E. V. Gorden

Here, we describe and compare the synthesis, solution characterization, and solid-state behaviour of the salphenazine ligand and metal complexes.


RSC Advances ◽  
2015 ◽  
Vol 5 (29) ◽  
pp. 22665-22673 ◽  
Author(s):  
Ana Raquel Madureira ◽  
Débora A. Campos ◽  
Pedro Fonte ◽  
Sara Nunes ◽  
Flávio Reis ◽  
...  

Illustration of the final product of solid carnauba nanoparticles loaded with rosmarinic acid in the dried solid state suitable for food incorporation.


1991 ◽  
Vol 187 (2) ◽  
pp. 197-200 ◽  
Author(s):  
Luca Forti ◽  
Monica Saladini ◽  
Marco Sola
Keyword(s):  

2014 ◽  
Vol 70 (a1) ◽  
pp. C919-C919
Author(s):  
Marietjie Schutte-Smith ◽  
Hendrik Visser ◽  
Andreas Roodt

In the last few years the coordination chemistry of rhenium and technetium has gained major interest for the possible use in radiopharmacy, due to its compact size, its low positive charge, coordination properties, d6 low-spin configuration and significant stability. This interest was further fuelled when Alberto remarkably synthesized fac-[99mTc-(CO)3(H2O)3] from [99mTcO4]- in aqueous medium and under mild conditions. Several fac-[M(CO)3]+ (M = Re, 99mTc) type complexes have been synthesized to date with a large number of ligand systems.[1,2] The three labile aqua ligands on the starting synthon fac-[Re(CO)3(H2O)3]+ can easily be substituted by a variety and/or combinations of ligands producing stable compounds and potential radiopharmaceuticals with many different characteristics. Our interest focuses on the fac-[Re(CO)3]+ moiety and related compounds by adopting the [2+1] approach.[3] The solid state behaviour of the complexes are explored as well as different effects such as the charge of the complexes as well as the effect of different types of donor atoms and electron donating or withdrawing systems. The influence of coordinated bidentate ligands on the rate of substitution in solution, by a variety of entering ligands, is also investigated. Crystal structures of Re(I) tricarbonyl tropolonato complexes with various monodentate incoming ligands were obtained in the study and will form part of this presentation.


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