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199,816 Newest Publications
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Modifying the Diffusion Layer of Soluble Salts of Poorly Soluble Basic Drugs To Improve Dissolution Performance
04-10-2010 | Michael Hawley; Walter Morozowich, Molecular Pharmaceutics, 2010
The dissolution mechanism of soluble salts of poorly soluble bases can be complex because both the dissolution of the salt and precipitation of the free base can occur depending on the experimental conditions and properties of the molecule. The dissolution of three soluble salts of poorly ...
Sodium N-(Methylsulfonyl)-N-(4-nitro-2-phenoxyphenyl)sulfamate: A Water-Soluble Nimesulide Prodrug for Parenteral Use
04-10-2010 | Simona Rapposelli; Maria Digiacomo; Silvia Franchi; Sara Moretti; Mario Pinza; Paola Sacerdote; Aldo Balsamo, Molecular Pharmaceutics, 2010
Several nimesulide preparations (i.e., tablet form, gels) have been marketed, but no parenteral solution has achieved the market because of their low wettability and unsatisfactory chemical−physical properties required for parenteral use. In this paper we describe the synthesis of the ...
Study of the Amorphous Glibenclamide Drug: Analysis of the Molecular Dynamics of Quenched and Cryomilled Material
04-10-2010 | Z. Wojnarowska; K. Grzybowska; K. Adrjanowicz; K. Kaminski; M. Paluch; L. Hawelek; R. Wrzalik; M. Dulski; W. Sawicki ..., Molecular Pharmaceutics, 2010
Glibenclamide (GCM) is an oral hypoglycemic agent of the sulfonylurea group used in the treatment of non-insulin-dependent diabetes. Crystalline GCM is characterized by low bioavailability, which is attributed to its poor dissolution properties. It prompted us to prepare this drug in its ...
Use of Artificial Stomach−Duodenum Model for Investigation of Dosing Fluid Effect on Clinical Trial Variability
04-10-2010 | Christopher S. Polster; Faraj Atassi; Sy-Juen Wu; David C. Sperry, Molecular Pharmaceutics, 2010
Lilly Compound X (LCX) is an oncology drug that was tested in a phase I clinical study using starch blend capsules. The drug was given to a small patient population (4 patients) and showed large inter- and intra-patient variability. In order to evaluate the possible effect of stomach pH on ...
MEK Inhibition Potentiates the Activity of Hsp90 Inhibitor 17-AAG against Pancreatic Cancer Cells
04-10-2010 | Tao Zhang; Yanyan Li; Zhenkun Zhu; Mancang Gu; Bryan Newman; Duxin Sun, Molecular Pharmaceutics, 2010
The Ras/Raf/MEK/ERK signaling has been implicated in uncontrolled cell proliferation and tumor progression in pancreatic cancer. The purpose of this study is to evaluate the antitumor activity of MEK inhibitor U0126 in combination with Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin ...
XIAP Gene Expression Protects β-Cells and Human Islets from Apoptotic Cell Death
04-10-2010 | Hao Wu; Ravikiran Panakanti; Feng Li; Ram I. Mahato, Molecular Pharmaceutics, 2010
Islet transplantation has the potential to treat type I diabetes, however, its clinical application is limited due to the massive apoptotic cell death and other post-transplantation challenges to islet grafts. Therefore, the objective of this study was to determine whether ex vivo ...
Simultaneous Release and ADME Processes of Poorly Water-Soluble Drugs: Mathematical Modeling
04-10-2010 | Gabriele Grassi; Dritan Hasa; Dario Voinovich; Beatrice Perissutti; Barbara Dapas; Rossella Farra; Erica Franceschin ..., Molecular Pharmaceutics, 2010
The importance of studying oral drug absorption is well recognized by both research facilities/institutions and the pharmaceutical industry. The use of mathematical models can represent a very profitable and indispensable tool to understand oral drug absorption. Indeed, mathematical models ...
Analysis of Amorphous Solid Dispersions Using 2D Solid-State NMR and 1H T1 Relaxation Measurements
04-10-2010 | Tran N. Pham; Simon A. Watson; Andrew J. Edwards; Manisha Chavda; Jacalyn S. Clawson; Mark Strohmeier; Frederick G. Vogt, Molecular Pharmaceutics, 2010
Solid-state NMR (SSNMR) can provide detailed structural information about amorphous solid dispersions of pharmaceutical small molecules. In this study, the ability of SSNMR experiments based on dipolar correlation, spin diffusion, and relaxation measurements to characterize the structure of ...
Effect of Variations in the Amounts of P-Glycoprotein (ABCB1), BCRP (ABCG2) and CYP3A4 along the Human Small Intestine on PBPK Models for Predicting Intestinal First Pass
04-10-2010 | Arnaud Bruyère; Xavier Declèves; Francois Bouzom; Kathryn Ball; Catie Marques; Xavier Treton; Marc Pocar ..., Molecular Pharmaceutics, 2010
It is difficult to predict the first-pass effect in the human intestine due to a lack of scaling factors for correlating in vitro and in vivo data. We have quantified cytochrome P450/3A4 (CYP3A4) and two ABC transporters, P-glycoprotein (P-gp, ABCB1) and the breast cancer resistant protein ...
Aqueous Boundary Layers Related to Oral Absorption of a Drug: From Dissolution of a Drug to Carrier Mediated Transport and Intestinal Wall Metabolism
04-10-2010 | Kiyohiko Sugano, Molecular Pharmaceutics, 2010
The aqueous boundary layer (ABL) affects various aspects of oral absorption of a drug, from dissolution of the drug to the apparent Km value of intestinal wall metabolism and carrier mediated transport. However, the importance of ABL has often been entirely ignored in oral absorption ...
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