DYNASAN® 118 – Your Formulation Challenges – Our Solutions

21. October 2021

In 1843 the Englishman William Brockedon (1787 – 1854) applied for a patent for the tablet and caused “one of the most tremendous upheavals that the pharmacists have ever experienced”1. Thereby active ingredients can be precisely dosed and are very stable, the taking is convenient, the production cheap and they are easy to transport. As a result, tablets occupy a special position today with a share of almost 50% among the drug forms.

However, pressing tablets regularly poses various challenges for galenical experts. For the compression of powders and granulates into tablets, auxiliaries are required that give the tablet mechanical and chemical stability and simplify the production process. In addition to bulking agents, binders and disintegrants, tabletting lubricants are of great importance. Typically, this category of functional adjuvant is of oleochemical origin. The materials support the powder flow and the compacting process of the tablet body, enable defect-free ejection from the tablet matrix and, depending on the dosage, can also modulate release profiles.

The Pharma business unit of IOI Oleo GmbH offers a variety of plant-based mono-, di- and triglycerides for a wide variety of dosage forms. Our DYNASAN® portfolio is particularly suitable for producing tablets. The products are lipid-based and can not only help to overcome the formulation hurdles, but also to simplify the production of the tablets.

The chemical origin, the raw materials and the production under GMP conditions give the DYNASAN® product range advantageous properties and an optimized purity profile. The high degree of esterification leads to negligible free OH functionality and results in an extremely inert auxiliary. DYNASAN® products are to be distinguished from the metal soaps, that are typically used as lubricants. The following difficulties occur regularly with metal salts from fatty acids 2:

  • Metal salt contaminants interacting with APIs
  • API interaction with lubricants due to their ionic properties

  • pH shift of the micro-environment into an alkaline medium, which can result in the risk of active ingredient hydrolysis
  • Breakdown of APIs through redox cascades and metal ions
  • Ionic auxiliaries and corresponding counterions show reactivity towards amines, which often occur as functional groups in APIs
Incompatibilties limiting the usability of metallic soaps in tablet formulations have been reported for the following active pharmaceutical ingredients:

Ibuprofen, acetylsalicylic acid, norfloxacin, glimepiride, cephalexin, indomethacin, ketoprofen, temazepam, glibenclamide, penicillin G, oxacillin, clopidogrelbesylate, erythromycin, captopril.

In our DYNASAN® product family, DYNASAN® 118 is the highlight, thanks to the USP-NF monograph „Glyceryl Tristearate“ . For galenic experts this is official proof that this product is suitable for the production of pharmaceuticals. Supplied as a microfine powder, it offers a number of benefits for the formulator 3,4.

  • Effective lubricant for tablet production in low concentrations (appr. 0,5%) without the risks of fatty acid soaps

  • No influence on drug release up to a concentration of 1%, model drug Acetylsalicylic Acid

  • Improved dissolution properties

  • Higher concentrations from 2% to 5% increase the hydrophobic characteristics of tablet matrix and introduce retardation effects into oral dosage forms for sustained release characteristics (also read the article “US Market Insights“)

  • Enhances the tablet fracture stability due to an increased lubricity factor resulting from particle morphology and particle surface

We have put together further details for you in our brochure “Lipids for solid dosage forms”. We are at your disposal for further information or product samples.

[1. Wolf-Dieter Müller-Jahncke, Christoph Friedrich, Ulrich Meyer: Arzneimittelgeschichte. 2., überarb. und erw. Auflage. Wiss. Verl.-Ges, Stuttgart 2005, S. 31 ff]
[2. Lubricants in Pharmaceutical Solid Dosage Forms, Jinjiang Li and Yongmei Wu, Lubri- cants 2014, 2, 21-43 ]
[3. Lubricating properties of triacylgycerols related to the release of medicaments: M. Vitko- va; M. Chalabala; J. Rak, Faculty of Pharmacy, 832-32, Bratislava, Czecho-Slovakia]
[4. A. Stamm, Sci. Techn. Pharm. 9 (1), 471 – 478 (1980)]

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Robert Radsziwill

Robert Radsziwill joined IOI Oleo GmbH in 2019 as Sales Manager Europe in the Pharma division. Prior to joining IOI Oleo Pharma, Robert held technical and commercial roles in sales and product management for nine years at a supplier of raw materials to the Pharmaceutical and Medical Device industry. Through his experience with materials for pharmaceutical use and medical devices, Robert has contributed to the successful initiation and completion of new product development projects with industrial and academic partners in the Healthcare sector. Understanding, ranking and navigating technical, functional and regulatory concerns are paramount for him during early project ideation and material selection to ensure success for all project participants. Robert earned his diploma degree in Business Chemistry at the Westfälische-Wilhelms-University of Münster and has focused ever since on those disciplinary interfaces where technical and commercial minds join forces to innovate and improve the status quo.