Solutions for Poorly Soluble Drugs*

  • 23.03.2020
According to BCS (Biopharmaceutical Classification System), the bioavailability of Class II (low solubility-high permeability) and Class IV (low solubility- low permeability) drugs could be enhanced through eutectic mixtures, SEDDS (Self emulsifying drug delivery systems), SMEDDS (Self-microemulsifying drug delivery systems), SNEDDS ( Self nano-emulsifying drug delivery systems), hot melt coating, hot melt extrusion, SLN (Solid Lipid Nano Particles), super saturated solutions systems by using various excipients of IOI OleoChemical Pharma such as DYNASAN®, IMWITOR®, SOFTIGEN®. We have the pleasure to introduce these excipients ‘Made in Germany’, under the highest quality standards with EU-GMP certification and US-FDA approval. We would like to share the related application areas and the literature information in the below table. DYNASAN® series are monoacid triglycerides with specific physico- chemical properties that makes them very suitable for certain applications. As given in the table, DYNASAN® series are trimyristin, tripalmitin and glyceryl tristearate by monograph or chemical names. IMWITOR® series are glycerides that are partially esterified with glycerine. This product family provides functionalized lipids for drug delivery systems. The short chain partial glycerides are more hydrophilic, and they have excellent solvent properties for many poorly soluble drugs. SOFTIGEN® 767, compendial name as per Ph. Eur. Is Macrogol 6 Glycerol Caprylocaprate, is designed for special pharmaceutical formulations. It is suitable for use in the preparation of SEDDS. It is a solubilizer for drugs, wetting and refatting agent. SOFTIGEN ® 767 is soluble in water and hydrophilic oils (such as MCT).

* Compiled and translated from IOI Oleo Chemicals ‘Solutions for Poorly Soluble Drugs’ brochure.

  • Literature 1) Lubricating properties of triacylgycerols related to the release of medicaments: M. Vitkova; M.Chalabala; J. Rak, Faculty of Pharmacy, 832-32, Bratislava, Czecho-Slovakia. 2) Taste masked lipid pellets with enhanced release of hydrophobic active ingredient: Vaassen, Jonathan; Bartscher, Kathrin; Breitkreutz, Joerg, International Journal of Pharmaceutics (Amsterdam, Netherlands) (2012), 429(1-2), 99-103. 3) Paclitaxels-containing nanometer liposome for injection and the preparation method thereof: Li, Shubin; Liu, Dan; Song, Jian; Bao, Jie; Ning, Hong; Li, Minghui; Guo, Zhifu; Wang, Hong; Yu, Na; Li, Lei; Faming Zhuanli Shenqing Gongkai Shuomingshu (2009), CN 101366697 A 20090218. 4) Active ingredient matrix dosage forms: Francas, Gernot; Przyklenk, Karl-Heinz, Ger. Offen. (2012), DE 102011051304 A1 20121227. 5) Optimization of 5-Fluorouracil solid lipid nano-particles: a preliminary study to treat colon cancer: Yassin, Alaa Eldeen B.; Khalid Anwer, Md.; Mowafy, Hammam A.; ElBagory, Ibrahim M.; Bayomi, Mohsen A.; Alsarra, Ibrahim A., International Journal of Medical Sciences (2010), 7(6), 398–408. 6) Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo: G. Connaire, J. Woodley, P. Herman, A. Cloarec, C. Arellano, G. Houin, International Journal of Pharmaceutics 278 (2004), 119–131. 7) Self Microemulsifying Drug Delivery System: A Novel Approach For Hydrophobic Drugs: Shinde Ganesh; Kuchekar Shantanu; Kamble Pravin; Kuchekar Ashwin; Kshirsagar Rajesh; Kuchekar Bhanudas, International Journal of Pharmaceutical Sciences, (2011), 3(1), 988–1005. 8) Self Emulsifying Drug Delivery System: An Approach To Enhance Bioavailability: Himani Bajaj; Seema Bisht; Mayank Yadav; Vinod Singh; Mamta Singh, International Journal of Pharma. Research and Development – Online (IJPRD). 9) New approaches in nanoparticulate drug delivery system - a review: Rakesh Bagul; Vjay Mahajan; Avinash Dhake, International Journal of Current Pharmaceutical Research, Vol 4, Issue 3 (2012). 10) Novel Self Micro-emulsifying Drug Delivery Systems (SMEDDS) of Efavirenz: Ashish Deshmukh and Shirishkumar Kulakrni, Journal of Chemical and Pharmaceutical Research, (2012), 4(8), 3914–3919. 11) Spheronization of solid lipid extrudates: Reitz, Claudia;

Yazıyı Paylaş