Lipid excipients from Stéarinerie Dubois for oral dosage forms
There has always been a continual quest for improvement in pharmaceutical formulations, and this applies to all galenic forms we have today: tablets, capsules, liquids, emulsions, dispersions, and semi-solids. The market diversity of esters, in particular those available in the range of Stéarinerie Dubois for standard and innovative formulations, offers developers a wide range of possibilities.
In this article, Dr. Samer Joudeh, Head of the Pharmaceutical Division at Stéarinerie Dubois, provides an overview of various lipid-based pharmaceutical excipients, such as fatty acids or fatty acid esters, and their use in oral lipid-based formulations (OLBF).
Lipid excipients from Stéarinerie Dubois: Innovation & diversity
Esters are derivatives of carbonic acid, in which the hydrogen of the carbonic acid (-COOH) has been replaced by an alkyl group (-R). The functional group of the ester can thus be represented as -COOR. The number of possible combinations in the molecular structure is practically infinite since, depending on the fatty acid, there are countless differences in chain length, degree of saturation, presence of branches, and type and number of bound molecules (e.g. glycerin, other fatty acids, propylene glycol, polyglycerin, saccharose, etc.). This makes for a broad range in terms of the following parameters:
- Application areas for these excipients
- Range of the hydrophilic/lipophilic balance (HLB)
- Wetting behaviours & polarities
- Gel-forming properties
- Melting points, crystallinities, and porosities
Oral lipid-based formulations (OLBF) are the most commonly used drug delivery system (DDS) because they improve the oral bioavailability of poorly water-soluble pharmaceuticals by improving the dissolution of drugs in the gastrointestinal tract (GI tract) or the dwelling time in the stomach.
Lipid formulations are therefore highly attractive, but present a number of challenges in terms of their development. Often, developers are faced with problems like masking tastes, improving shelf life and API stability, or controlling release, in particular when processing many APIs, such as chloroquine, acetaminophen, metoprolol tartrate, ibuprofen, herbal extracts, diltiazem, diclofenac, bromhexine, antibiotics, n-acetylcysteine or mesalazine.
In order to meet this challenge, Stéarinerie Dubois offers a wide and diverse range of effective excipients that help to combine the chemistry, functionality, and behaviour of the excipient with those of your active ingredient (hydrophobicity, hydrophilicity, acidity, hygroscopy, polymorphism, instability, taste, ...). They have a multitude of lipid excipients with different melting points (27–85 °C) available, which allows the integration of many different technologies and methods that have been developed specifically for lipid formulations on an industrial scale:
Lipid-based excipients from Dubois
|Example products||Product segment||Example applications|
|StellipressTM, Stearic acid, Myristic acid, Palmitic acid||Fatty acids||Lubricants, Tabletting excipients, Coating excipients|
|Carnauba wax, beeswax alternatives||Waxes||Coating excipients, Matrixes, API protection|
|DUB PP, hard fats||Fully or partially hydrogenated vegetable oils and fats, Hydrogenated coco-glycerides||Matrixes|
|PEG 6 or 8 stearates||PEG fatty acid esters||Taste masking, controlled API release|
|StelliestersTM, oleic acid macroglycerides, caprylocaprate macroglycerides||Polyoxylglycerides||Solubilizers, Bioavailability enhancers|
|DUBCARETM, Glyceryl monostearate, Glycerol monooleate||Monoacylglycerides||Taste masking, controlled API release|
|Stelliesters, Glyceryl dibehenate, Glyceryl palmitostearate||Diacylglyceride||Taste masking, controlled API release|
|Stelliesters MCTs||Triglycerides of fatty acids||Solubilizers, vehicles, Bioavailability enhancers|
|Stelliesters SE||Fatty acid esters of saccharose||Surfactants, bioavailability enhancers, tabletting excipients|
Clever chemistry that promotes an environmentally friendly future
All GMP excipients from Stéarinerie Dubois are developed and produced under strict quality control and under careful selection of the raw materials and supply chain. This “Quality by Design” approach reflects Dubois’ efforts to enter into the era of “green chemistry”: chemistry that respects the environment and is conscious of its practices and its impact on the planet.
With its words, “Our ingredients for a responsible future are the reflection of our sincere, pragmatic and long-term approach to sustainability,” Stéarinerie Dubois states its aim to make a positive influence for people and the environment throughout the entire value added chain from the selection of raw materials, to the first production steps, to the marketing of the products.
Quality by Design approach