Nos publications
Amélioration de la biodisponibilité des substances actives via la formulation [Bioavailability enhancement of active pharmaceutical ingredients through formulation strategies] galénique
STP Pharma Pratiques, Mai-Juin 2017, n°1 - 2017
The SFSTP commission on Bioavailability published an article reviewing the formulation strategies to enhance the bioavailability of APIs.
Interestingly this article is both in French and English languages.
Table of content:
I Introduction
II Prerequisites
1 Initial identification and characterization of the active ingredient
1.1 Physico-chemical characteristics
1.2 Impact of physicochemical characteristics on absorption
1.3 Passive diffusion prediction tools
1.4 In silico prediction
2 Biopharmaceutical classifications
III Formulation strategies
1 Prerequisites
2 Techniques for increasing the dissolution rate
3 Solubility enhancement technologies
4 Improving the permeability, oral route
IV Control, assessment, prediction of the bioavailability
1 Physicochemical control methods for the manufacturing intermediates and finished products
2 Assessing and predicting the bioavailability of the formulations
V Alternative strategy: changing the route of administration
VI Conclusion: decision tree
Inclusion of digestible surfactants in solid SMEDDS formulation removes lag time and influences the formation of structured particles during digestion
The AAPS Journal, Vol. 19, No. 3 - mai 2017
The objective of this study is to evaluate how solid self-microemulsifying drug delivery systems (SMEDDS) behave during digestion. SMEDDS containing Gelucire® 44/14 and surfactants were prepared and their dispersion and digestion behaviors were studied using an in vitro lipolysis model, coupled with small-angle X-ray scattering (SAXS) to determine the formed colloidal structures during digestion in real time.
The study shows that the lipid to surfactant ratio has a significant effect on the kinetics of digestion and an optimum ratio is prerequisite to develop rapidly digestible solid SMEDDS system.
Comparison of the protective effect of self-emulsifying peptide drug delivery systems towards intestinal proteases and glutathione
International Journal of Pharmaceutics, Volume 523, Issue 1, Pages 357–365 https://doi.org/10.1016/j.ijpharm.2017.03.027 - mai 2017
This study shows that independent from the type of peptide all the SEDDS showed a prolonged release and can provide a 100% protective effect towards protease degradation and deactivation by reduced glutathione.
Hydrophobic ion pairing: Key to highly payloaded self-emulsifying peptide drug delivery systems
International Journal of Pharmaceutics, Volume 520, Issues 1–2, 30 March 2017, Pages 267–274 - mar 2017
In this study, hydrophobic ion pairing is used to form complexes between different anionic surfactants and leuprorelin, insulin and desmopression as model peptides. These complexes were formulated in SEDDS and evaluated for payload and stability.
Comparative evaluation of Compritol® HD5 ATO with Sodium Stearyl Fumarate and PEG 6000 as amphiphilic, hydrodispersible pharmaceutical lubricants
Journal of Excipients and Food Chemicals, Vol. 8, Issue 1, pages 5-17 - mar 2017
In the present study the lubricant capacity of Compritol® HD5 ATO was compared with commonly used amphiphilic lubricants. The
effect of the concentration and mixing time on flow properties, tablet ejection force, hardness, disintegration time and rate of dissolution of paracetamol tablets was evaluated.
The physical properties of the lubricants such as crystallinity, wettability, thermal behaviour and surface area were also measured.
Compritol® HD5 ATO was found to be an as effective a lubricant for a fast disintegrating paracetamol formulation containing microcrystalline cellulose, lactose and PVP prepared by wet granulation in comparison with sodium stearyl fumarate and PEG 6000.