کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2484878 | 1114339 | 2012 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Sufentanil-2âHydroxypropylâβâCyclodextrin Inclusion Complex for pain Treatment: Physicochemical, Cytotoxicity, and Pharmacological Evaluation
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
Sufentanil (SUF) is a synthetic analgesic opioid widely used for the management of acute and chronic pain. This drug was complexed with 2âhydroxypropylâβâcyclodextrin (HPâβâCD) and the physicochemical characterization, in vitro/ex vivo toxicity assays, and pharmacological evaluation were performed. Differential scanning calorimetry, Fourier transform infrared spectroscopy (FTIR) analysis, and Xâray powder diffraction showed the formation and the morphology of the complex. Nuclear magnetic resonance afforded data regarding inclusion complex stoichiometry (1:1) with an association binding constant (Ka) value of 515.2 ± 1.2âMâ1 between SUF and HPâβâCD. Complexation with HPâβâCD protected SUF from light exposure and increased its photostability. Release kinetics revealed a decrease in SUF release rate (Krel = 7.05 ± 0.52 and 5.61 ± 0.39âminâ1/2 for SUF-HPâβâCD and SUF, respectively) and reduced hemolytic or myotoxic effects after complexation. Time course of tailâflick test showed that the duration of analgesia induced by SUF (150.0 ± 34.6âmin) was significantly increased (p < 0.001) after complexation with HPâβâCD (355.7 ± 47.2âmin) when injected at the same dose (1âμg kgâ1), prolonging the duration of analgesia after intramuscular administration and representing an alternative on the development of effective and safe drugâdelivery system for opioid analgesics.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 101, Issue 10, October 2012, Pages 3698-3707
Journal: Journal of Pharmaceutical Sciences - Volume 101, Issue 10, October 2012, Pages 3698-3707
نویسندگان
Cristiane Volobuef, Carolina M. Moraes, Lázaro A. S. Nunes, CÃntia M. S. Cereda, Fabiano Yokaichiya, Margareth K. K. D. Franco, Angélica F.A. Braga, Eneida De Paula, Giovana Radomille Tófoli, Leonardo F. Fraceto, Daniele R. De Araujo,