An explorative analysis of process and formulation variables affecting comilling in a vibrational mill: The case of praziquantel
| Autor: | Beatrice Albertini, Nadia Passerini, Beatrice Perissutti, Ramona Trastullo, Dario Voinovich, Guglielmo Zingone, Debora Zanolla, Jennifer Keiser |
|---|---|
| Přispěvatelé: | Perissutti, Beatrice, Passerini, Nadia, Trastullo, Ramona, Keiserc, Jennifer, Zanolla, Debora, Zingone, Guglielmo, Voinovich, Dario, Albertini, Beatrice, Beatrice Perissutti, Null, Keiser, Jennifer |
| Rok vydání: | 2016 |
| Předmět: |
Stereochemistry
Chemistry Pharmaceutical Drug Compounding Pharmaceutical Science 02 engineering and technology 030226 pharmacology & pharmacy Vibration Praziquantel law.invention 03 medical and health sciences Crystallinity Mice 0302 clinical medicine Drug Stability law medicine Vibrational mill Animals Crystallization Solubility chemistry.chemical_classification Residual crystallinity Anthelmintics Aqueous solution Experimental design for screening Chemistry Polymer Drug recovery Schistosoma mansoni 021001 nanoscience & nanotechnology Schistosomiasis mansoni Grinding Chemical engineering Scientific method Female 0210 nano-technology medicine.drug |
| Zdroj: | International journal of pharmaceutics. 533(2) |
| ISSN: | 1873-3476 |
| Popis: | Praziquantel, a BCS II class anthelmintic drug used for the treatment of schistosome infections, was coground in a vibrational mill with different polymers (linear and crosslinked povidone, copovidone and sodium starch glycolate). An explorative analysis of formulation variables (drug-polymer wt ratio and polymer type) and process parameters (type of grinding media, grinding time and frequency) was carried out with the help of an experimental screening design. The influence of the above mentioned factors on three PZQ characteristics (residual crystallinity, water solubility enhancement and drug recovery) was studied. The variation of carrier amount proved to be by far the most important variable affecting all the experimental responses. A lower impact and, in some cases, rather null effect, had the variation of the process variables. All coground systems were characterized by a high amorphous degree and a solubility significantly higher than the API. A very promising product was obtained by processing at 20 Hz for 4 h, using 3 spheres of 15 mm as grinding media, i.e. a coground having a 50% API content, showing a 4.6-fold greater solubility at 20 C than pure praziquantel. This product maintained the same antischistosomal activity of pure API and was both physically and chemically stable for at least 6 months. © 2017 Elsevier B.V. All rights reserved. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect