کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9918701 | 1557554 | 2005 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Self-association properties of 4-[1-hydroxy-1-methylethyl]-2-propyl-1-[4-[2-[tetrazole-5-yl]phenyl]phenyl] methylimidazole-5-carboxylic acid monohydrate (CS-088), an antiglaucoma ophthalmic agent
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
علوم دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Self-association properties of 4-[1-hydroxy-1-methylethyl]-2-propyl-1-[4-[2-[tetrazole-5-yl]phenyl]phenyl] methylimidazole-5-carboxylic acid monohydrate (CS-088), an antiglaucoma ophthalmic agent Self-association properties of 4-[1-hydroxy-1-methylethyl]-2-propyl-1-[4-[2-[tetrazole-5-yl]phenyl]phenyl] methylimidazole-5-carboxylic acid monohydrate (CS-088), an antiglaucoma ophthalmic agent](/preview/png/9918701.png)
چکیده انگلیسی
Self-association properties of CS-088, an antiglaucoma ophthalmic agent, were investigated. Various analytical methods, such as surface tension measurement, demonstrated that CS-088 is a self-associating compound with critical micellar concentration (CMC) of approximately 10Â mg/mL. Light scattering analysis revealed that the micellar molecular weight (MMW) of CS-088 aggregates well above the CMC was approximately 2260, corresponding to a pentamer. In addition, the MMW corresponding to a dimer was detected by NMR spectroscopy, indicating that self-association of monomers to pentamers is via the formation of dimers. According to the Stokes-Einstein equation, hydrodynamic radii of the dimer and pentamer were calculated to be 0.87 and 1.16Â nm, respectively. The concentration-dependent change in the NMR chemical shift indicated that hydrophobic interaction between biphenyl groups is an important factor in the self-association of CS-088 molecules. Furthermore, measurement of particle size distribution using a Nicomp Submicron Particle-Sizer revealed that the addition of either n-propanol or urea to CS-088 solution led to monomerization of the dimers and pentamers, suggesting that not only hydrophobic interaction but also hydrogen bonding is involved in stabilizing CS-088 aggregates. No bigger aggregate than a pentamer was formed in the absence of NaCl, whereas further aggregation was observed with increasing concentrations of NaCl.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 299, Issues 1â2, 11 August 2005, Pages 100-106
Journal: International Journal of Pharmaceutics - Volume 299, Issues 1â2, 11 August 2005, Pages 100-106
نویسندگان
Takayuki Kikuchi, Nobuya Ito, Masahiko Suzuki, Akira Kusai, Ken Iseki, Hitoshi Sasaki,