edoc

An explorative analysis of process and formulation variables affecting comilling in a vibrational mill: the case of praziquantel

Perissutti, Beatrice and Passerini, Nadia and Trastullo, Ramona and Keiser, Jennifer and Zanolla, Debora and Zingone, Guglielmo and Voinovich, Dario and Albertini, Beatrice. (2017) An explorative analysis of process and formulation variables affecting comilling in a vibrational mill: the case of praziquantel. International journal of pharmaceutics, 533 (2). pp. 402-412.

Full text not available from this repository.

Official URL: http://edoc.unibas.ch/58034/

Downloads: Statistics Overview

Abstract

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 20Hz for 4h, using 3 spheres of 15mm 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.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Helminth Drug Development (Keiser)
UniBasel Contributors:Keiser, Jennifer
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Elsevier
ISSN:0378-5173
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:02 Feb 2018 09:13
Deposited On:02 Feb 2018 09:12

Repository Staff Only: item control page