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Esters are derivatives of carbonic acid, in which the hydrogen of the carbonic acid (-COOH) has been replaced by an alkyl group (-R).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