Preparation and In Vitro/In Vivo Evaluation of Orally Disintegrating/Modified-Release Praziquantel Tablets
| Autor: | Yangfeng Xu, Fang Fang, Meiling Yu, Xin Deng, Guoqing Yan, Zhaoyou Deng, Xuemei Wen, Jiakang He, Xin Feng, Liqin Wu, Qiuling Liang |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Thermogravimetric analysis
Chromatography hot-melt extrusion praziquantel Pharmaceutical Science Hydrochloric acid orally integrating tablets Article Bioavailability Praziquantel RS1-441 chemistry.chemical_compound Differential scanning calorimetry Pharmacy and materia medica chemistry Pharmacokinetics parasitic diseases medicine Extrusion modified-release Phosphoric acid pharmacokinetics medicine.drug |
| Zdroj: | Pharmaceutics, Vol 13, Iss 1567, p 1567 (2021) Pharmaceutics Volume 13 Issue 10 |
| ISSN: | 1999-4923 |
| Popis: | This study was designed to develop orally disintegrating/sustained-release praziquantel (PZQ) tablets using the hot-melt extrusion (HME) technique and direct compression, and subsequently evaluate their release in in vitro and in vivo pharmacokinetics. For the extrusion process, hypromellose acetate succinate (HPMCAS)-LG was the carrier of pure PZQ, with a standard screw configuration used at an extrusion temperature of 140 °C and a screw rotation speed of 100 rpm. Differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), powder X-ray diffraction (PXRD) and Fourier-transform infrared spectroscopy (FTIR) were performed to characterize the extrudate. Orally disintegrating/sustained-release praziquantel tablets (PZQ ODSRTs) were prepared by direct compression after appropriate excipients were blended with the extrudate. The release amount was 5.10% in pH 1.0 hydrochloric acid at 2 h and over 90% in phosphoric acid buffer at 45 min, indicating the enteric-coating character of PZQ ODSRTs. Compared with the pharmacokinetics of marketed PZQ tablets (Aipuruike®) in dogs, the times to peak (Tmax), elimination half-life (t1/2λ) and mean residence time (MRT) were extended in PZQ ODSRTs, and the relative bioavailability of PZQ ODSRTs was up to 184.48% of that of Aipuruike®. This study suggested that PZQ ODSRTs may have potential for the clinical treatment of parasitosis. |
| Databáze: | OpenAIRE |
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