Pharmaceutical Research
1573-904X
Cơ quản chủ quản: N/A
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Các bài báo tiêu biểu
The Stability of Insulin in Crystalline and Amorphous Solids: Observation of Greater Stability for the Amorphous Form
Tập 14 Số 10 - Trang 1379-1387 - 1997
Purpose. Generalizations based upon behavior of small molecules have established that a crystalline solid is generally much more stable toward chemical degradation than is the amorphous solid. This study examines the validity of this generalization for proteins using biosynthetic human insulin as the model protein. Methods. Amorphous insulin was prepared by freeze drying the supernate from a suspe......
The Oral Absorption of Micro- and Nanoparticulates: Neither Exceptional Nor Unusual
Tập 14 Số 3 - Trang 259-266 - 1997
This mini-review covers some of the historical and recent arguments over the experimental evidence on the uptake by and translocation from the intestinal mucosa of microparticulates after oral administration. It is concluded that there is now no dispute over the fact that this is a normal occurrence. Particulate uptake does take place, not only via the M-cells in the Peyer's patches and the isolat......
Improvement of the Pulmonary Absorption of (Asu1,7)-Eel Calcitonin by Various Protease Inhibitors in Rats
Tập 11 Số 6 - Trang 909-913 - 1994
The effects of protease inhibitors, Na-glycocholate, bacitracin, bestatin, nafamostat mesilate and soybean trypsin inhibitor (STI) on the pulmonary absorption of (Asu1,7)-eel calcitonin (ECT, molecular weight 3363) were investigated in rats. The pulmonary absorption of ECT was estimated by measuring its hypocalcemic effect. When ECT alone was administered into the lung, the pharmacological availab......
Proteolysis of Human Calcitonin in Excised Bovine Nasal Mucosa: Elucidation of the Metabolic Pathway by Liquid Secondary lonization Mass Spectrometry (LSIMS) and Matrix Assisted Laser Desorption lonization Mass Spectrometry (MALDI)
Tập 13 Số 11 - Trang 1679-1685 - 1996
Purpose. Two calcitonins, i.e. human calcitonin (hCT) and, for comparison, salmon calcitonin (sCT), were chosen as peptide models to investigate nasal mucosal metabolism. Methods. The susceptibility of hCT and sCT to nasal mucosal enzymes was assessed by in-and-out reflection kinetics experiments in an in vitro model based on the use of freshly excised bovine nasal mucosa, with the mucosal surface......
Photo-Oxidation Mechanisms in Liquid Pharmaceutical Formulations: The Overlooked Role of Singlet Oxygen Presented as a Case Study
- 2022
Oxidation is one of the most common degradation pathways for active pharmaceutical ingredients (APIs) in pharmaceutical formulations, mostly involving 1-electron processes via peroxy radicals and 2-electron processes by peroxides. In liquid pharmaceutical formulations, several factors can impact oxidative instabilities including pH, excipient impurities, headspace oxygen, and the potential for pho......
Hydrophilic Matrices for Controlled Drug Delivery: An Improved Mathematical Model to Predict the Resulting Drug Release Kinetics (the “sequential Layer” Model)
Tập 17 Số 10 - Trang 1290-1298 - 2000
Purpose. The aims of this study were (i) to elucidate the transport mechanisms involved in drug release from hydrophilic matrices; and (ii) to develop an improved mathematical model allowing quantitative predictions of the resulting release kinetics. Methods. Our previously presented model has been substantially modified, by adding: (i) inhomogeneous swelling; (ii) poorly water-soluble drugs; and ......
Comparison of the Anticancer Effect of Free and HPMA Copolymer-Bound Adriamycin in Human Ovarian Carcinoma Cells
Tập 16 Số 7 - Trang 986-996 - 1999
Purpose. To study peculiarities and the mechanism of the anticancer effect of free and HPMA copolymer-bound ADR in sensitive and resistant human ovarian carcinoma cells. Methods. Sensitive A2780 and ADR resistant A2780/AD cells were exposed to different doses of drugs during 12, 24, 36, 48, 60, and 72 hours. Cell viability, drug accumulation, apoptosis, cellular metabolism, lipid peroxidation, DNA......
In Vivo Evaluation of a Colon-Specific Drug Delivery System: An Absorption Study of Theophylline from Capsules Coated with Azo Polymers in Rats
Tập 12 Số 2 - Trang 244-247 - 1995
Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N′-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coatings for colon-specific drug delivery. The gastrointestinal absorption of theophylline from capsules coated with the azo polymers was examined in the proximal part of the smal......
Intestinal Drug Absorption and Metabolism in Cell Cultures: Caco-2 and Beyond
Tập 14 Số 12 - Trang 1655-1658 - 1997
Development of New Lipophilic Derivatives of Tetragastrin: Physicochemical Characteristics and Intestinal Absorption of Acyl-tetragastrin Derivatives in Rats
Tập 10 Số 10 - Trang 1488-1492 - 1993
In order to improve the intestinal absorption of tetragastrin (TG), we synthesized lipophilic derivatives of TG by acylation of its N-terminal amino group with acetic acid, caproic acid, and lauric acid. The purified TG derivatives, acetyl-tetragastrin (Ac-TG), caproyl-tetragastrin (Cap-TG), and lauroyl-tetragastrin (Lau-TG), were confirmed to be more lipophilic than the parent TG by high-performa......