Abstract
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.
Highlights
Parasitic diseases, especially schistosomiasis, cysticercosis and echinococcosis, are common diseases in dogs and cats, some of which are seriously harmful to animal growth and health and even play a crucial role in transmission between humans and domestic livestock [1]
AquaSolveTM hypromellose acetate succinate (HPMCAS)LG was purchased from Ashland Specialty Ingredients (Wilmington, DE, USA)
The results demonstrated that the physical mixture and PZQ hot-melt extrudate had similar characteristic peaks at 2933.1, 1623.7~1646.9 and 1000~1350 cm−1, and their Fourier-transform infrared spectroscopy (FTIR) spectra were a simple superposition of the spectra for HPMCAS and pure
Summary
Especially schistosomiasis, cysticercosis and echinococcosis, are common diseases in dogs and cats, some of which are seriously harmful to animal growth and health and even play a crucial role in transmission between humans and domestic livestock [1]. Parts of the Congo River and some developing countries in Asia and Brazil [3], where thousands of people have experienced impacts on their health and wellbeing because of helminth infections with blood flukes [4]. Cerebral cysticercosis and multiheaded mites parasitizing the host brain could cause neurological symptoms. This parasite may bring potential danger to the development of the breeding industry, and it could damage the health of people by parasitizing meat products or pets of human beings [6]. For the above-mentioned diseases, maintaining a clean and comfortable dwelling environment and expelling parasites via drug treatment is a preferable way to control the prevalence of parasitosis in animals
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