Simultaneous assay of four stereoisomers of diltiazem hydrochloride. Application to in vitro chiral inversion studies

1995 ◽  
Vol 41 (5-6) ◽  
pp. 450-454 ◽  
Author(s):  
K. Ishii ◽  
K. Minato ◽  
H. Nakai ◽  
T. Sato
Keyword(s):  
Diltiazem Hydrochloride ◽  
Chiral Inversion

Simultaneous assay of four stereoisomers of diltiazem hydrochloride. Application to in vitro chiral inversion studies

1995 ◽  
Vol 41 (7-8) ◽  
pp. 450-454 ◽  
Author(s):  
K. Ishii ◽  
K. Minato ◽  
H. Nakai ◽  
T. Sato
Keyword(s):  
Diltiazem Hydrochloride ◽  
Chiral Inversion

Metabolic chiral inversion of flurbiprofen-CoA In vitro

1991 ◽  
Vol 42 (1) ◽  
pp. R1-R4 ◽  
Author(s):  
David J. Porubek ◽  
Susan M. Sanins ◽  
Jeffrey R. Stephens ◽  
Mark P. Grillo ◽  
David G. Kaiser ◽  
...  
Keyword(s):  
Chiral Inversion

scholarly journals In vitro and in vivo evaluation of guar gum matrix tablets for oral controlled release of water-soluble diltiazem hydrochloride

2005 ◽  
Vol 6 (1) ◽  
pp. E14-E21 ◽  
Author(s):  
Saleh M. Al-Saidan ◽  
Yellela S. R. Krishnaiah ◽  
S. Patro ◽  
Vemulapalli Satyanaryana
Keyword(s):  
Controlled Release ◽  
Guar Gum ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Diltiazem Hydrochloride ◽  
In Vivo Evaluation

Pharmacokinetics of Darolutamide in Mouse – Assessment of the Disposition of the Diastereomers, Key Active Metabolite and Interconversion Phenomenon: Implications to Cancer Patients

2020 ◽  
Vol 14 ◽  
Author(s):  
Neeraj Kumar Saini ◽  
Bhavesh Babulal Gabani ◽  
Umesh Todmal ◽  
Suresh P Sulochana ◽  
Vinay Kiran ◽  
...  
Keyword(s):  
Protein Binding ◽  
Liver Microsomes ◽  
Stability Study ◽  
Pharmacokinetic Data ◽  
Chiral Inversion ◽  
Tissue Samples ◽  
Clinical Pharmacokinetics ◽  
Oral And Intravenous Dosing

Background: Darolutamide is recently approved for the treatment of non-metastatic castrate resistance prostate cancer. Hitherto, no stereoselective pharmacokinetic data has been published pertaining to darolutamide and its diastereomers in animals or humans. The key aims of the experiment were to examine darolutamide, S,S-darolutamide and S,R-darolutamide with respect to (a) assessment of in vitro stability and protein binding (b) characterization of in vivo oral and intravenous pharmacokinetics in mice. Method: In vitro (liver microsomes stability and protein binding) and in vivo experiments (oral/intravenous dosing to mice) were carried out using darolutamide, S,S-darolutamide and S,R-darolutamide. Besides, tissue levels of darolutamide, S,S-darolutamide and S,R-darolutamide were measured following oral and intravenous dosing. Appropriate plasma/tissue samples served to determine the pharmacokinetics of various analytes in mice. Liquid chromatography in tandem with mass spectrometry procedures enabled the delineation of the plasma pharmacokinetics, in vitro and tissue uptake data of the various analytes. Results: Chiral inversion was absent in the metabolic stability study. However, darolutamide showed profound stereoselectivity (S,Sdarolutamide greater than S,R-darolutamide) after either intravenous or oral dosing. S,R-darolutamide but not S,S-darolutamide showed conversion to its antipode post oral and intravenous dosing to mice. Regardless of oral or intravenous dosing, active keto darolutamide formation was evident after administration of darolutamide, S,S-darolutamide or S,R- darolutamide. Tissue data supported the observations in plasma; however, tissue exposure of the various darolutamide, S,S-darolutamide and S,R-darolutamide were much lower as compared to plasma. Conclusion: In lieu of the human pharmacokinetic data, although the administration of diastereomeric darolutamide was justified, it is proposed to delineate the clinical pharmacokinetics of S,R-darolutamide and S,S-darolutamide relative to darolutamide in future clinical pharmacology studies.

Thin-layer chromatographic and polarimetric investigation of the oscillatory in-vitro chiral inversion ofS-(+)-ketoprofen

2008 ◽  
Vol 21 (5) ◽  
pp. 349-353 ◽  
Author(s):  
Mieczysław Sajewicz ◽  
Monika Gontarska ◽  
Dorota Kronenbach ◽  
Teresa Kowalska
Keyword(s):  
Thin Layer ◽  
Chiral Inversion

Preparation and in vitro characterization of diltiazem hydrochloride loaded alginate microspheres

2009 ◽  
Vol 14 (3) ◽  
pp. 321-331 ◽  
Author(s):  
Y. Sultana ◽  
Shalini Mall ◽  
D. P. Maurya ◽  
D. Kumar ◽  
M. Das
Keyword(s):  
Diltiazem Hydrochloride ◽  
In Vitro Characterization
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