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Improving the Bioavailability of Medicines

1954 • 2012

In the 1950s, when Gattefossé discovered that Labrafil® could accelerate the bioavailability of antibiotics, the company then needed to convince pharmaceutical laboratories of the opportunities offered by this innovation. Fifty years later, the company continued to strengthen its expertise through scientific works.

1954

In 1954, Émile Mahler successfully transformed a type of plant oil into a hydrophilic substance. That is how Labrafil® came about, or rather the Labrafil®, because soon, Gattefossé had developed a dozen products using various plant oils. The Labrafil® may have been perfectly suited to a number of pharmaceutical formulations, however, they appeared to have particularly good properties for improving bioavailability and the therapeutic effectiveness of certain medicines such as drinkable vitamin solutes, preparations for ENT use, and antibiotic suppositories.

Henri-Marcel Gattefossé spoke to academics at the National Veterinary School in Lyon, asking them to carry out pharmacological studies on animals so the work could be scientifically proven. By comparing the physiological effects of tracers such as physostigmine and estradiol, researchers recorded more rapid transmucosal absorption when the tracers were carried in a Labrafil® rather than plant oil, which therefore enhanced and accelerated bioavailability. Gattefossé was then quick to make pharmaceutical laboratories aware of the benefits of using the Labrafil® as excipients for their active ingredients. Clin-Comar (Pfizer) was one of the first in line, choosing a Labrafil® to carry a derivative of thus boosting its absorption and stability.

Gattefossé stand at the 1957 French Pharmaceutical Days, Faculty of Pharmacy in Paris. Labrafil® is promoted.

This was a noteworthy innovation in the pharmaceutical world, giving Gattefossé a very important scientific edge, encouraging the company to further study bioavailability in relation to its other excipients, especially those for oral administration.

There would be a major step forward in this area when carrying out tests using Precirol® for a client in the Rhône-Poulenc group. The structure of Precirol®, a fatty acid ester, could be “arranged” to allow the controlled release of phenobarbital.

2012

At the start of the 2000s, when the pharmaceutical industry was producing molecules that were increasingly difficult to solubilize, Gattefossé was keen to show that its lipid excipients were particularly useful for carrying these new active ingredients and making them easy to absorb. Gattefossé would then go on to expend a lot of energy, conducting a large number of studies in partnership with academic laboratories, to convince the company’s industrial clients of its findings.

In 2012, the company overcame a significant hurdle with the issue of a patent for an “intestinal wall model”. This allowed Gattefossé to observe ex vivo the role of liquid excipients in the absorption of active ingredients.

To support its studies, the business worked in collaboration with universities and research centers, successfully demonstrating that the company’s excipients could protect peptides from gastric acidity but also keep them intact in the intestine. Around the same time, Gattefossé recorded another significant achievement when it successfully sold Labrasol® to an international laboratory for the development of a new medicine, effective in the treatment of prostate cancer.

Today, the study of Gattefossé excipients in orally administered therapeutic peptide formulations continues to be a major research subject for the business.

Poster promoting Gattefossé excipients, 2019 (LBDDS: Oral lipid based drug delivery system).

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Improving the Bioavailability of Medicines

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