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Your reliable supplier for drug development
As a leading provider of functional lipid excipients and formulation solutions to healthcare industries worldwide, Gattefossé is committed to delivering high-quality excipients, technical support and inspiring formulations for drug delivery.
Oral drug delivery
Lipid excipients for oral drug delivery include solubility and bioavailability enhancers, lubricants, modified release, taste-masking, API protection and suspending agents. Excipients are used in a variety of processes enabling the formulation of different dosage forms, mainly tablets, granules, hard and soft capsules.
Many active pharmaceutical ingredients have poor water solubility and/or poor permeability, which affect their bioavailability. Lipidbased formulations are widely used to overcome these issues and can be developed in using a stepwise approach, which is described in Gattefossé’s brochure.
Gelucire 44/14 and Labrasol ALF are self-emulsifying excipients that can be used as single excipient to increase drug solubility, permeability and/or bioavailability of drugs. Multiple excipient combinations using oils (e.g. Maisine CC, Peceol), surfactants (e.g. Gelucire, Labrafil) and solvents (e.g. Transcutol HP) form self-emulsifying lipid-based formulations. Click on the link for more information: https://bit.ly/3wJtlmQ.
Tablets and capsules are the most preferred dosage forms. However, a lubricant is required to reduce the friction between particles and equipment when manufacturing tablets and capsules.
Compritol 888 ATO is a lubricant of choice for challenging pharmaceutical tablets when used at 1% to 3%. Its inertness eliminates drug-excipient incompatibility issues. As mixing time and speed do not affect its efficiency or tablet hardness, it offers flexibility in formulation development and production. It is the ‘trouble-shooting’ lubricant for tabletting. Click on the link for more information: https://bit.ly/3fXyce8.
Many APIs have an unpleasant taste or odour which need to be masked to facilitate their absorption. Coating the drug particle with a lipid film is a common practice to positively change the drug organoleptic properties.
Precirol ATO 5 can be used in a high shear or fluid bed coating process and enables the formation of a film coating around the drug particle to mask its taste. Click on the link for more information: https://bit.ly/32dIP4N.
Ideal drug candidates for sustained-release delivery are often BCS class 1 (high water solubility, high permeability) with a short half-life. Formulating a modified release dosage form is also a strategy frequently pursued by pharmaceutical laboratories to extend their market exclusivity after patent expiry. For patients, sustained release formulations enable reduced dosing frequency, reduced drug blood level fluctuations, improved patient compliance and less side effects.
Compritol 888 ATO is a smart solution for sustained drug release when used at 10% to 25%. It forms an inert matrix from which the drug diffuses slowly over time. Used alone or in combination with HPMC it enables the production of sustained-release tablets using a direct compression process and with higher drug load achievable. Click on the link for more information: https://bit.ly/3fYdOtE.
Popularity of soft gels is booming. They can be filled with a carrier containing the drug in a solubilised or dispersed manner. Geloil SC is an ideal ready-touse suspending agent, specially designed for easy soft gelatin capsule production.
If drug solubility and bioavailability are a limiting factor, then a liquid lipid-based formulation can be developed and filled into a soft gel. Click on the link for more information: https://bit.ly/320PYW0.
Topical drug delivery
Lipid excipients for topical drug delivery include solubilisers, emulsifiers and viscosity modifying agents. Emulsifiers are designed for challenging formulations and deliver excellent texture and sensorial properties. Solubilisers provide skin penetration enhancement and viscosity agents that stabilise formulations. These excipients are used in creams, emulgels, lotions, foams, microemulsions and gels.
The texture of the topical dosage form is important as it impacts patient compliance. Gattefossé has a full range of emulsifiers and texture modifiers enabling the formulation of light or rich creams, all types of gels, balms, ointments and more.
Tefose 63 is a multifunctional emulsifier, enabling a one-pot process and offering excellent mucosal and skin tolerance. It is used worldwide with a broad range of APIs, including the ‘azole’ antifungals to treat vaginal infections and mycosis. In combination with Labrafil M 1944 CS, it delivers exceptional heat stability to topical emulsions. Click on the link for more information: https://bit.ly/3t3TV8d.
Skin delivery is successfully achieved when the drug is properly formulated in a vehicle, enabling its solubilisation and diffusion in the skin layers. Depending on the target (topical or transdermal), the vehicle contains a solubiliser and/or permeation enhancer to assist in drug solubilisation and diffusion in the skin.
Transcutol P is a safe and effective hydrophilic solvent widely used to deliver a drug to the skin. In combination with Capryol or Lauroglycol, it offers interesting synergies for transdermal drug delivery. Click on the link for more information: https://bit.ly/3t6xijd.
Rectal and vaginal drug delivery
Lipid excipients for suppository and pessary formulation include hard fat and hard fat with additives. These bases provide excellent physico-chemical stability and optimise drug delivery for a wide range of active pharmaceutical ingredients and manufacturing equipment.
Suppocire NAI 25 A is a versatile suppository base used with numerous APIs, including paracetamol, guaranteeing excellent drug release properties for a fast-acting antipyretic effect.
Ovucire 3460 is a hard fat pessary base delivering enhanced spreadability within the vaginal cavity and good mechanical resistance. As it is non-irritant and provides excellent mucosal tolerance, it is widely used in antifungal treatments. Click on the link for more information: https://bit.ly/2PFSFK1.
International technical support
With an international network of technical representatives and technical centres of excellence in USA, France, India and China, Gattefossé provides bespoke technical and regulatory support to accelerate drug development.
For local support do not hesitate to contact Carst & Walker in South Africa. For more information on Gattefossé’s excipients and to download up-to-date technical and regulatory documentation, brochures and case studies, please visit the company’s website. •
Gattefossé – www.gattefosse.com Carst & Walker – www.carst.co.za