Distribution of Active Ingredients in Pharmaceutical Products
Many issues from the field of pharmaceutical and medical technology research and development require the use of surface analytical techniques. Examples from our practice deal with residues and contamination in ampoules, particles in and discoloration of blister packaging, residues from cleaning agents in syringes and needles, the distribution of active pharmaceutical ingredients (API) on stents, implants or patches, delamination of coatings and many more.
The drug form (galenic form) itself can also be the subject of surface analysis. We use ToF-SIMS in our test laboratory to analyze the layer structure or the distribution of the API in the tablet cross-section. It offers the possibility of identifying different molecules of API and excipients using mass spectrometry. The layer structure can be examined in organic depth profiles. With ToF-SIMS Imaging, the dosage form and the API distribution can be shown in detail in the distribution image.
Nanoparticles are also used as carriers for active ingredients. The distribution of the active substance also plays a role here.
In addition to ToF-SIMS, Tascon uses other techniques such as SEM-EDX (scanning electron microscopy) and XPS (photoelectron spectroscopy) in the surface analysis laboratory. Depending on the specific analytical question, they are used to examine the drug form, the active ingredient, the metabolites or the excipients and provide additional information.
We support development processes in our surface analysis laboratory, carry out failure diagnostics and help with the analysis of competing products in reverse engineering. With our analysis reports and accompanying advice, we provide reliable data to as evidence for the formulation. The results can be used by experts and patent attorneys in patent disputes. In the event of patent disputes, Tascon is at your side with many years of experience.
The following example describes analyzes for the localization of an (API) in a tablet cross-section.
Imaging of the lateral distribution of the active pharmaceutical ingredient
In addition to the active pharmaceutical ingredients (APIs), tablets often also contain a number of excipients. The distribution of the API and additives in the tablet is critical to its effectiveness. The analysis of tablet cross-sections using ToF-SIMS imaging is an excellent way of investigating this distribution.
In the present case, an Ibuprofen-containing tablet was embedded in epoxy resin and cut with a microtome. The cross-section was then analyzed with regard to its chemical composition. The results show that, in addition to the distribution of the API, various other ingredients could also be detected and localized. The sugar component 1 forms a matrix for these components. The Ibuprofen is present in agglomerates with sizes between 50 and 100 µm. The second sugar component agglomerates to grain sizes between 50 and 75 µm. The fatty acid conjugates that are also detected are distributed relatively homogeneously over the cross-sectional area. The fine distribution of Si-containing material indicates the use of an excipient to improve the flow properties.
Tascon - your partner for the analysis of the distribution of active pharmaceutical ingredients
You are interested in the distribution of active pharmaceutical ingredients in pharmaceutical products? Tascon is your competent partner laboratory for all questions on this field of analysis. Please do not hesitate to contact us. Our friendly and competent team looks forward to your inquiry and will be happy to advise you personally and without obligation.