Polymorphism of glyceryl behenates: From the individual compounds to the pharmaceutical excipient

Pivette, Perrine; Faivre, Vincent; Brubach, Jean‐Blaise; Daste, Georges; Ollivon, Michel; Lesieur, Sylviane

doi:10.1016/j.chemphyslip.2014.07.005

Cited by 24 publications

(34 citation statements)

References 51 publications

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“…The polymorphic behavior of Compritol 888 ATO, which mainly consists of glyceryl dibehenate, has been studied extensively with DSC, time-resolved synchrotron x-ray diffraction and infrared spectroscopy at different conditions ( e.g., cooling rate, addition of pure acyl glycerides etc. ) ( 135 , 226 ). These studies revealed that the ratio of mono-, di- and tribehenin and especially the monobehenin amount is important for the formation of a pseudohexagonal sub-α and hexagonal α-phase ( 226 ).…”

Section: Characterization Methods Challenges and Controlling Strategmentioning

confidence: 99%

“…( 135 , 226 ). These studies revealed that the ratio of mono-, di- and tribehenin and especially the monobehenin amount is important for the formation of a pseudohexagonal sub-α and hexagonal α-phase ( 226 ). In particular the less stable and compact sub-α-form shows a higher drug incorporation, which is desired in the preparation of solid lipid microparticles ( 226 , 227 ).…”

Section: Characterization Methods Challenges and Controlling Strategmentioning

confidence: 99%

“…These studies revealed that the ratio of mono-, di- and tribehenin and especially the monobehenin amount is important for the formation of a pseudohexagonal sub-α and hexagonal α-phase ( 226 ). In particular the less stable and compact sub-α-form shows a higher drug incorporation, which is desired in the preparation of solid lipid microparticles ( 226 , 227 ). Therefore a variation in the batch composition of the supplier as well as the mixture with excipients containing monoacylglycerides themselves can lead to changes in the equilibrium and different polymorphic behavior ( 226 ).…”

Section: Characterization Methods Challenges and Controlling Strategmentioning

confidence: 99%

“…In particular the less stable and compact sub-α-form shows a higher drug incorporation, which is desired in the preparation of solid lipid microparticles ( 226 , 227 ). Therefore a variation in the batch composition of the supplier as well as the mixture with excipients containing monoacylglycerides themselves can lead to changes in the equilibrium and different polymorphic behavior ( 226 ). Nevertheless, Compritol 888 ATO has been widely used in controlled release formulations and seems to be able to provide a stable release profile during storage ( 43 , 228 ).…”

Section: Characterization Methods Challenges and Controlling Strategmentioning

confidence: 99%

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Solvent-Free Melting Techniques for the Preparation of Lipid-Based Solid Oral Formulations

2015

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Lipid excipients are applied for numerous purposes such as taste masking, controlled release, improvement of swallowability and moisture protection. Several melting techniques have evolved in the last decades. Common examples are melt coating, melt granulation and melt extrusion. The required equipment ranges from ordinary glass beakers for lab scale up to large machines such as fluid bed coaters, spray dryers or extruders. This allows for upscaling to pilot or production scale. Solvent free melt processing provides a cost-effective, time-saving and eco-friendly method for the food and pharmaceutical industries. This review intends to give a critical overview of the published literature on experiences, formulations and challenges and to show possibilities for future developments in this promising field. Moreover, it should serve as a guide for selecting the best excipients and manufacturing techniques for the development of a product with specific properties using solvent free melt processing.

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Section: Characterization Methods Challenges and Controlling Strategmentioning

confidence: 99%

Section: Characterization Methods Challenges and Controlling Strategmentioning

confidence: 99%

Section: Characterization Methods Challenges and Controlling Strategmentioning

confidence: 99%

Section: Characterization Methods Challenges and Controlling Strategmentioning

confidence: 99%

See 2 more Smart Citations

Solvent-Free Melting Techniques for the Preparation of Lipid-Based Solid Oral Formulations

2015

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“…Due to their chemical and physical complexity, meltable lipid binders may exhibit a complex behaviour (i.e. melting and crystallization, physical modifications on storage) [14,15] which has not been thoroughly investigated before.…”

Section: Introductionmentioning

confidence: 99%

Influence of Different Meltable Binders on the Solid-State Behaviour and Dissolution Profiles of Solid Lipid Extrudates Processed Via Continuous Hot Melt Granulation

Gejage¹,

Pawar²,

Amin³

et al. 2018

Preprint

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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.

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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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Polymorphism of glyceryl behenates: From the individual compounds to the pharmaceutical excipient

Cited by 24 publications

References 51 publications

Solvent-Free Melting Techniques for the Preparation of Lipid-Based Solid Oral Formulations

Solvent-Free Melting Techniques for the Preparation of Lipid-Based Solid Oral Formulations

Influence of Different Meltable Binders on the Solid-State Behaviour and Dissolution Profiles of Solid Lipid Extrudates Processed Via Continuous Hot Melt Granulation

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

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