Solid State Properties of an Oral Iron Chelator, 1,2-Dimethyl-3-hydroxy-4-pyridone, and Its Acetic Acid Solvate. I: Physicochemical Characterization, Intrinsic Dissolution Rate, and Solution Thermodynamics

1991 ◽  
Vol 80 (7) ◽  
pp. 677-685 ◽  
Author(s):  
Hak-Kim Chan ◽  
Suresh Venkataram ◽  
David J.W. Grant ◽  
Yueh-Erh Rahman
Keyword(s):  
Acetic Acid ◽  
Solid State ◽  
Dissolution Rate ◽  
Physicochemical Characterization ◽  
Iron Chelator ◽  
Solution Thermodynamics ◽  
Oral Iron ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Oral Iron Chelator

Crystal Structures of a New Oral Iron Chelator, 1,2-Dimethyl-3-hydroxy-4- pyridone, and its Solvates with Acetic Acid and Formic Acid

1992 ◽  
Vol 81 (4) ◽  
pp. 353-358 ◽  
Author(s):  
Hak‐Kim Chan ◽  
Soumojeet Ghosh ◽  
Suresh Venkataram ◽  
Yueh‐Erh Rahman ◽  
David J.W. Grant
Keyword(s):  
Acetic Acid ◽  
Formic Acid ◽  
Crystal Structures ◽  
Iron Chelator ◽  
Oral Iron ◽  
Oral Iron Chelator

Deferiprone, an oral iron chelator, ameliorates experimental colitis and gastric ulceration in rats

2007 ◽  
Vol 5 (4) ◽  
pp. 253-261 ◽  
Author(s):  
Jacob Ablin ◽  
Oded Shalev ◽  
Elimelech Okon ◽  
Fanny Karmeli ◽  
Daniel Rachmilewitz
Keyword(s):  
Experimental Colitis ◽  
Iron Chelator ◽  
Gastric Ulceration ◽  
Oral Iron ◽  
Oral Iron Chelator

Critical Comparison of Novel and Existing Methods of Compliance Assessment During a Clinical Trial of an Oral Iron Chelator

1994 ◽  
Vol 34 (9) ◽  
pp. 944-949 ◽  
Author(s):  
Doreen Matsui ◽  
Christine Hermann ◽  
Julia Klein ◽  
Matitiahu Berkovitch ◽  
Nancy Olivieri ◽  
...  
Keyword(s):  
Clinical Trial ◽  
Iron Chelator ◽  
Oral Iron ◽  
Compliance Assessment ◽  
Critical Comparison ◽  
Oral Iron Chelator

scholarly journals Deferasirox, an oral iron chelator, with gemcitabine synergistically inhibits pancreatic cancer cell growth in vitro and in vivo

Oncotarget ◽  
2018 ◽  
Vol 9 (47) ◽  
pp. 28434-28444 ◽  
Author(s):  
Shuhei Shinoda ◽  
Seiji Kaino ◽  
Shogo Amano ◽  
Hirofumi Harima ◽  
Toshihiko Matsumoto ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Cell Growth ◽  
Cancer Cell ◽  
Pancreatic Cancer Cell ◽  
Iron Chelator ◽  
Oral Iron ◽  
Cancer Cell Growth ◽  
Oral Iron Chelator

scholarly journals Intrinsic Dissolution Rate Profiling of Poorly Water-Soluble Compounds in Biorelevant Dissolution Media

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 493
Author(s):  
Alexandra Teleki ◽  
Olivia Nylander ◽  
Christel A.S. Bergström
Keyword(s):  
Dissolution Rate ◽  
Water Soluble ◽  
Small Scale ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Fed State ◽  
Pharmaceutical Ingredients ◽  
Biorelevant Dissolution ◽  
Intestinal Fluids ◽  
Simulated Intestinal Fluids

The intrinsic dissolution rate (IDR) of active pharmaceutical ingredients (API) is a key property that aids in early drug development, especially selecting formulation strategies to improve dissolution and thereby drug absorption in the intestine. Here, we developed a robust method for rapid, medium throughput screening of IDR and established the largest IDR dataset in open literature to date that can be used for pharmaceutical computational modeling. Eighteen compounds with diverse physicochemical properties were studied in both fasted and fed state simulated intestinal fluids. Dissolution profiles were measured in small-scale experimental assays using compound suspensions or discs. IDR measurements were not solely linked to API solubility in either dissolution media. Multivariate data analysis revealed that IDR strongly depends on compound partitioning into bile salt and phospholipid micelles in the simulated intestinal fluids, a process that in turn is governed by API lipophilicity, hydrophobicity, and ionization.

scholarly journals CHARACTERIZATION AND INTRINSIC DISSOLUTION RATE STUDY OF MICROWAVE ASSISTED CYCLODEXTRIN INCLUSION COMPLEXES OF GEMFIBROZIL

2016 ◽  
Vol 8 (10) ◽  
pp. 160
Author(s):  
S. Ain ◽  
R. Singh ◽  
Q. Ain
Keyword(s):  
Inclusion Complex ◽  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Microwave Drying ◽  
Phase Solubility ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Solubility Study ◽  
Microwave Assisted ◽  
Rate Study

<p><strong>Objective: </strong>The aim of the present study was to carry out characterization and intrinsic dissolution rate study of microwave assisted inclusion complex of poorly water soluble, lipid lowering agent gemfibrozil [5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid]<strong> </strong>with naturally occurring β-cyclodextrins (CDs) or cycloheptaamylase.</p><p><strong>Methods: </strong>In this work, the phase solubility study was performed to find the ratio of drug and cyclodextrin complexes. Inclusion complexes were prepared by kneading and the prepared complex was subjected to microwave drying and conventional drying techniques. The prepared complexes were evaluated by intrinsic dissolution rate studies and equilibrium solubility study. Further characterization was done by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray powder diffractometry (DSC).</p><p><strong>Results: </strong>The phase solubility studies showed a linear A<sub>L</sub>-type diagram indicating the formation of inclusion complexes in 1:1 molar ratio β-CD-gemfibrozil complex with maximum stability constant of 148.88 M<sup>-1</sup>was selected for preparation of inclusion complex. The microwave dried product was identified as the inclusion complex with maximum IDR when compared to the conventional dried product.</p><p><strong>Conclusion: </strong>This study was concluded that the microwave drying is the most suitable of the previously occurring drying techniques. Since it showed the highest solubility and IDR value.</p>

scholarly journals Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals

Crystals ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 996
Author(s):  
Zhengxuan Liang ◽  
Hongbo Chen ◽  
Chenguang Wang ◽  
Changquan Calvin Sun
Keyword(s):  
Oxalic Acid ◽  
Dissolution Rate ◽  
Physical Stability ◽  
Formulation Development ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
Conjugate Acid ◽  
Enhanced Solubility ◽  
Antihistamine Drug ◽  
Low Solubility

Loratadine (Lor) is an antihistamine drug commonly used to relieve the symptoms of allergy. It has high permeability but low solubility under physiological conditions. To overcome the problem of low solubility, we synthesized and characterized two Loratadine multi-component crystalline phases with oxalic acid (Oxa), i.e., a 1:1 Lor-Oxa conjugate acid-base (CAB) cocrystal (Lor-Oxa CAB) and a 2:1 Lor-Oxa cocrystal monohydrate (Lor-Oxa hydrate). Both cocrystals exhibited an enhanced solubility and intrinsic dissolution rate (IDR) compared to Lor and adequate physical stability. The intrinsic dissolution rate of Lor-Oxa CAB is 95 times that of Lor, which makes it a promising candidate for tablet formulation development.

Relationship between the pharmacokinetics and iron excretion pharmacodynamics of the new oral iron chelator 1,2-dimethyl-3-hydroxypyrid-4-one in patients with thalassemia

1991 ◽  
Vol 50 (3) ◽  
pp. 294-298 ◽  
Author(s):  
Doreen Matsui ◽  
Julia Klein ◽  
Christine Hermann ◽  
Victor Grunau ◽  
Robert Mcclelland ◽  
...  
Keyword(s):  
Iron Chelator ◽  
Oral Iron ◽  
Iron Excretion ◽  
Oral Iron Chelator

The Oral Iron Chelator Deferasirox Induces Apoptosis in Myeloid Leukemia Cells by Targeting Caspase

2011 ◽  
Vol 126 (4) ◽  
pp. 241-245 ◽  
Author(s):  
Jung-Lim Kim ◽  
Han-Na Kang ◽  
Myoung Hee Kang ◽  
Young A. Yoo ◽  
Jun Suk Kim ◽  
...  
Keyword(s):  
Myeloid Leukemia ◽  
Iron Chelator ◽  
Oral Iron ◽  
Leukemia Cells ◽  
Oral Iron Chelator
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