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A new soluble and bioactive polymorph of praziquantel.
Zanolla D, Perissutti B, Passerini N, Chierotti MR, Hasa D, Voinovich D, Gigli L, Demitri N, Geremia S, Keiser J, Cerreia Vioglio P, Albertini B. Zanolla D, et al. Eur J Pharm Biopharm. 2018 Jun;127:19-28. doi: 10.1016/j.ejpb.2018.01.018. Epub 2018 Jan 31. Eur J Pharm Biopharm. 2018. PMID: 29409939 Free article.
The preparation of the crystalline polymorph was realized via a neat grinding process in a vibrational mill. The new phase (Form B) was chemically identical to the starting material (as proved by HPLC, (1)H NMR, and polarimetry), but showed different physical properties (a …
The preparation of the crystalline polymorph was realized via a neat grinding process in a vibrational mill. The new phase (Form B) w …
Activity and pharmacokinetics of a praziquantel crystalline polymorph in the Schistosoma mansoni mouse model.
Lombardo FC, Perissutti B, Keiser J. Lombardo FC, et al. Eur J Pharm Biopharm. 2019 Sep;142:240-246. doi: 10.1016/j.ejpb.2019.06.029. Epub 2019 Jun 29. Eur J Pharm Biopharm. 2019. PMID: 31265895
Pharmacokinetic (PK) profiles of R- and S-praziquantel and R- and S- polymorph B following oral administration with both formulations were generated by sampling mice at 30, 60, 240 min and 24 h post-treatment, followed by LC-MS/MS analysis. ...Praziquantel showed higher in …
Pharmacokinetic (PK) profiles of R- and S-praziquantel and R- and S- polymorph B following oral administration with both formulations …
Synthesis and hydrolysis by cathepsin B of fluorogenic substrates with the general structure benzoyl-X-ARG-MCA containing non-natural basic amino acids at position X.
Melo RL, Barbosa Pozzo RC, Alves LC, Perissutti E, Caliendo G, Santagada V, Juliano L, Juliano MA. Melo RL, et al. Biochim Biophys Acta. 2001 May 5;1547(1):82-94. doi: 10.1016/s0167-4838(01)00171-6. Biochim Biophys Acta. 2001. PMID: 11343794
Bz-F-R-MCA was the best substrate for cathepsin B but also hydrolyzed Bz-R-R-MCA with lower efficiency, since the protease accepts Arg at S(2) due to the presence of Glu(245) at the bottom of this subsite. ...In addition, the substrate with 4-aminocyclohexyl-alanine presen …
Bz-F-R-MCA was the best substrate for cathepsin B but also hydrolyzed Bz-R-R-MCA with lower efficiency, since the protease accepts Ar …
Combining Mechanochemistry and Spray Congealing for New Praziquantel Pediatric Formulations in Schistosomiasis Treatment.
Albertini B, Perissutti B, Bertoni S, Zanolla D, Franceschinis E, Voinovich D, Lombardo F, Keiser J, Passerini N. Albertini B, et al. Int J Mol Sci. 2019 Mar 12;20(5):1233. doi: 10.3390/ijms20051233. Int J Mol Sci. 2019. PMID: 30870971 Free PMC article.
A 1:1 by wt PZQ-Povidone coground-was prepared in a vibrational mill under cryogenic conditions, for favoring amorphization. PZQ was neat ground to obtain its polymorphic form (Form B), which has an improved solubility and bioactivity. Then, activated PZQ powders were load …
A 1:1 by wt PZQ-Povidone coground-was prepared in a vibrational mill under cryogenic conditions, for favoring amorphization. PZQ was neat gr …
Hybrids between H2S-donors and betamethasone 17-valerate or triamcinolone acetonide inhibit mast cell degranulation and promote hyperpolarization of bronchial smooth muscle cells.
Giordano F, Corvino A, Scognamiglio A, Citi V, Gorica E, Fattorusso C, Persico M, Caliendo G, Fiorino F, Magli E, Perissutti E, Santagada V, Severino B, Pavese RC, Petti F, Martelli A, Calderone V, Frecentese F. Giordano F, et al. Eur J Med Chem. 2021 Oct 5;221:113517. doi: 10.1016/j.ejmech.2021.113517. Epub 2021 May 5. Eur J Med Chem. 2021. PMID: 33984803
Exploring mechanochemical parameters using a DoE approach: Crystal structure solution from synchrotron XRPD and characterization of a new praziquantel polymorph.
Zanolla D, Perissutti B, Vioglio PC, Chierotti MR, Gigli L, Demitri N, Passerini N, Albertini B, Franceschinis E, Keiser J, Voinovich D. Zanolla D, et al. Eur J Pharm Sci. 2019 Dec 1;140:105084. doi: 10.1016/j.ejps.2019.105084. Epub 2019 Oct 15. Eur J Pharm Sci. 2019. PMID: 31626966 Free article.
A rotated Doehlert matrix was utilized to explore the experimental design space around the milling parameters of Praziquantel (PZQ) polymorph B formation in terms of frequency and milling time. Three experimental responses were evaluated on the resulting ground samples: tw …
A rotated Doehlert matrix was utilized to explore the experimental design space around the milling parameters of Praziquantel (PZQ) polymorp …
Solid state mechanochemical simultaneous activation of the constituents of the Silybum marianum phytocomplex with crosslinked polymers.
Voinovich D, Perissutti B, Magarotto L, Ceschia D, Guiotto P, Bilia AR. Voinovich D, et al. J Pharm Sci. 2009 Jan;98(1):215-28. doi: 10.1002/jps.21417. J Pharm Sci. 2009. PMID: 18428992
When the 1/3 coground systems with PVP-CL(R) and Ac-Di-Sol(R) were dissolved in saturated conditions they gave a concentration improvement compared to the native product of 8 and 31 times of silybin A, 7 and 27 times of silybin B, whereas in the case of silychristin a doub …
When the 1/3 coground systems with PVP-CL(R) and Ac-Di-Sol(R) were dissolved in saturated conditions they gave a concentration improvement c …
Effect of cytokines on the secretion of the fifth and eighth complement components by HepG2 cells.
Perissutti S, Tedesco F. Perissutti S, et al. Int J Clin Lab Res. 1994;24(1):45-8. doi: 10.1007/BF02592409. Int J Clin Lab Res. 1994. PMID: 8180423
Information, so far available only for the early components, indicates that these cytokines exhibit different effects on various complement proteins. For instance, they promote the biosynthesis of C3 and B but have no effect on that of C4 and C2. These observations led us …
Information, so far available only for the early components, indicates that these cytokines exhibit different effects on various complement …
Quantification of dapaconazole in human plasma using high-performance liquid chromatography coupled to tandem mass spectrometry: application to a phase I study.
de Moraes FC, Bittencourt SF, Perissutti E, Frencentese F, Arruda AM, Chen LS, Babadópulos T, De Nucci G. de Moraes FC, et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 May 1;958:102-7. doi: 10.1016/j.jchromb.2014.01.053. Epub 2014 Mar 12. J Chromatogr B Analyt Technol Biomed Life Sci. 2014. PMID: 24705538
13 results