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Clin Transl Sci 2022 Jul 28. Epub 2022 Jul 28.

Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, Maryland, USA.

Metformin has been shown to repress transcription of the bile salt export pump (BSEP) in human primary hepatocytes. The primary objective of this study was to assess the effect of oral metformin on the human pharmacokinetics (PKs) of two BSEP probe substrates: pravastatin and chenodeoxycholic acid (CDCA; also known as chenodiol). Endogenous bile acid levels were assessed as a secondary measure of metformin impact. Read More

Pharmaceutics 2022 Jun 20;14(6). Epub 2022 Jun 20.

Clinical Pharmacology and Toxicology Institute, University Hospital Friuli Centrale ASU FC, 33100 Udine, Italy.

In the clinical practice management of heart transplant (HTx), the impact of calcineurin inhibitors co-administration on pharmacokinetics (PKs) of mycophenolic acid (MPA), mycophenolate mofetil (MMF) active drug, is not adequately considered. This retrospective study investigated full MPA-PK profiles by therapeutic drug monitoring (TDM) in 21 HTx recipients treated with MMF combined with cyclosporine (CsA) or tacrolimus (TAC) at a median time of 2.6 months post-transplant. Read More

Eur J Pharm Sci 2022 Jul 30;174:106198. Epub 2022 Apr 30.

Department of Pharmacy and Pharmaceutical Technology and Parasitology, University of Valencia, Av Vicent András Estellés, s/n. 46100, Valencia, Burjassot, Valencia, Spain; Interuniversity Research Institute for Molecular Recognition and Technological Development, Polytechnic University of Valencia-University of Valencia, Valencia, Spain.

Aims: The aims of this work are (i) to characterize the absorption properties of orally administered formulations at different dose levels, and (ii) to evaluate the impact of entero-hepatic circulation on the time-course of amiodarone (AM) in rats in order to optimize the development of new oral (OR) formulations.

Methods: Intravenous (IV) formulation consisted on a solution of a commercial injectable of AM chlorhydrate. OR formulations included the IV commercial formulation (Trangorex®) (Solution I), an aqueous supramicellar solution of AM chlorhydrate with Polysorbate at 5% (Solution II) and a suspension from Trangorex® tablets (Tablet). Read More

Transplant Cell Ther 2022 07 27;28(7):372.e1-372.e9. Epub 2022 Apr 27.

Experimental and Clinical Pharmacology, University of Minnesota College of Pharmacy, Minneapolis, MN. Electronic address:

Mycophenolate mofetil (MMF) is an important immunosuppressant used after allogeneic hematopoietic cell transplantation (HCT). MMF has a narrow therapeutic index, and blood concentrations of mycophenolic acid (MPA), the active component of MMF, are highly variable. Low MPA concentrations are associated with the risk of graft-versus-host disease (GVHD), whereas high concentrations are associated with toxicity. Read More

Clin Pharmacokinet 2022 05 11;61(5):619-635. Epub 2022 Apr 11.

Department of Pharmacy, Radboud University Medical Center, and Radboud Institute for Health Sciences, Geert Grooteplein-Zuid 10 (route 864), P.O. Box 9101, 6500 HB, Nijmegen (864), The Netherlands.

Bariatric surgery is increasingly applied among people living with HIV to reduce obesity and the associated morbidity and mortality. In people living with HIV, sufficient antiretroviral exposure and activity should always be maintained to prevent development of resistance and disease progression. However, bariatric surgery procedures bring various gastrointestinal modifications including changes in gastric volume, and acidity, gastrointestinal emptying time, enterohepatic circulation and delayed entry of bile acids. Read More