Lipid Excipients from Stéarinerie DUBOIS * in Oral Sustainable & Green formulations
This is an article created by our Pharmaceuticals partner, Stéarinerie DUBOIS and written by Dr. Samer JOUDIEH, Head of the pharmaceutical Division.
Nowadays ongoing quest for improvement in pharmaceutical formulation encompasses all galenic forms: tablets, capsules, liquids, emulsions, dispersions, and semisolids. The variety of esters available on the market and specifically inside Stérainerie dubois’s range and their unique properties offer a wide range of possibilities for formulators seeking to develop standard and innovative formulations.
This short paper is an overview of our pharmaceutical lipid based excipients (Fatty Acids and fatty esters) and their use in Oral Lipid-based formulations (OLBF)
Lipid excipients from Stearinerie DUBOIS is world of innovation and possibilities.
Esters are the derivatives of carboxylic acids in which the hydrogen of carboxylic acid (-COOH) has been replaced by an alkyl group (-R) . The ester functional group may be represented as -COOR.
Nevertheless, the number of possible combinations of the molecular structure is virtually infinite, depending on the fatty acid (e.g., chain length, the grade of saturation, the presence of branches, and nature and number of the linked molecule (e.g., glycerol, additional fatty acids, propylene glycol, polyglycerol, sucrose etc.). This leads to a wide :
A. Field of application of these excipients
B. Range of hydrophilic-lipophilic balance (HLB)
C. Values of contact angle and, consequently, the wetting behavior
D. Polarities, and gel-formation properties
E. Melting points, crystallinity and porosity
Including now in the equation the nature of the drug (e.g., solubility, melting point) itself and the way the drug is integrated into the formulation, to evaluate the formulation environment and the main role in drug release and its bioavailability.
Table I: Lipid Based Excipients from DUBOIS, example:
| Example of our Excipients | Excipient class | Example of Functionalities |
|---|---|---|
| StellipressTM, stearic acid, Myristic acid, palmitic acid | Fatty acids | Lubricants, tableting aid, Coating Film ingredients |
| Carnauba wax , Bees wax alternatives | Waxes | Coating film, Matrix, API protection |
| DUB PP, Hard Fats | Fully or partially hydrogenated vegetable oils and fats Hydrogenated coco-glycerides | Matrix |
| PEG 6 or 8 Stearates | PEG fatty acid esters | Taste masking, Control release |
| StelliestersTM, Oleic Macrogolglycerides, Caprylocaprate macrogolglycerides | Polyoxylglycerides | Solubilizers, Bioavailability enhancers |
| DUBCARETM, Glyceryl monostearate, Glycerol monooleate | Monoacylglycerides | Taste masking, Control release |
| Stelliesters , Glyceryl Dibehenate , Glyceryl palmitostearate | Diacylglycerides | Taste masking, Control release |
| Stelliesters MCTs, | Triglycerides of fatty acids | Solubilizers, Vehicles, Bioavailability enhancers |
| Stelliesters SE | Sucrose fatty acid esters | Surfactants, Bioavailability enhancers, Tablet aid |
Oral Lipid-based formulations (OLBF) are one of the most widely used Drug Delivery Systems ( DDS) to improve oral bioavailability of poorly water-soluble drugs by enhancing the dissolution of drugs in the gastrointestinal (GI) tract or prolonging the gastric retention time.
The lipid formulation strategy using is growing where formulators over the world try to fix Taste masking, immediate release, storage stability, API stability and control release challenges faced with a wide range of APIS like: Chloroquine, Acetaminophen, Metoprolol tartrate, Ibuprofen, Herbal extract, Diltiazem, Diclofenac, Bromhexin, Antibiotics, N-acetylcysteine or Mesalazine.
We supply the pharmaceutical market with adequate and diverse galenic “Tools” where our expert could support to link our excipients chemistry, functionality, and behavior to your API’s specificity (hydrophobic, hydrophilic, Acid, hygroscopic, polymorph, instable, taste …) and the formulation and process challenges.
The wide range of melting points of our lipid excipients (27-85°C) allows them to integrate diverse technologies and process designed more specifically to achieve lipid formulation at the industrial scale:
Clever chemistry, dedicated to an eco-responsible future,
ll our GMPs excipients are designed and produced under a strict quality control process and perfect mastery and selection of raw materials and supply chain. This quality by design approach is based on Dubois' efforts to enter the era of "Green Chemistry": a chemistry respectful of its environment, conscious of itself and its impact on our planet. Throughout our value chain, from the selection of our raw materials, from the first steps of production to the marketing of products, our ambition is to be a producer with a positive impact on environment and people.
Our ingredients for a responsible future are the reflection of our sincere, pragmatic and long-term approach to sustainability.
