10.05.2013 | Miyoshi Morimoto, Kazuo Samizo, Shin Ohta, Takashi Mizuma, Journal of Pharmaceutical Sciences, 2013

Abstract Drug toxicity impedes drug development and its clinical use. In the present study, a toxicity risk index (TRI), which is an index for warning idiosyncratic drug toxicity (IDT), was proposed. The TRI of drugs was defined as a function of dose, pharmacokinetic parameters, and ...

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10.05.2013 | Noritaka Nakamichi, Hiroyo Shima, Satoshi Asano, Takahiro Ishimoto, Tomoko Sugiura, Kazuki Matsubara, Hiroyuki Kusuh ..., Journal of Pharmaceutical Sciences, 2013

Abstract Metformin is a widely used oral anti‐diabetic, but the molecular mechanism(s) of its gastrointestinal membrane permeation remains unclear. Here, we examined the role of carnitine/organic cation transporter OCTN1/SLC22A4, which is localized on apical membranes of small intestine ...

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10.05.2013 | Lasse Murtomäki, Tuomas Vainikka, Silvia Pescina, Sara Nicoli, Journal of Pharmaceutical Sciences, 2013

Abstract The affinity of a drug to a biological membrane can affect the distribution and the availability of the active compound to its target. Adsorption is usually determined with in vitro distribution studies based on partitioning of the drug between buffer and tissue, which have ...

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10.05.2013 | Hsin‐Te Hsu, Wen‐Hung Wang, Cheng‐Ying Han, Chun‐Nan Chen, Chi‐Ming Chen, Wun‐Chang Ko, Journal of Pharmaceutical Sciences, 2013

Abstract The phosphodiesterase (PDE)4 molecule exists as two distinct conformers, PDE4H and PDE4L, which have high and low affinities, respectively, for the selective PDE4 inhibitor, rolipram. The inhibition of PDE4H and PDE4L is associated with adverse responses, such as nausea, ...

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10.05.2013 | Damir E. Zecevic, Karl G. Wagner, Journal of Pharmaceutical Sciences, 2013

Abstract Effective and predictive small‐scale selection tools are inevitable during the development of a solubility enhanced drug product. For hot‐melt extrusion, this selection process can start with a microscale performance evaluation on a hot‐stage microscope (HSM). A batch size of ...

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10.05.2013 | Ian M. Hodge, Journal of Pharmaceutical Sciences, 2013

Abstract Numerical simulations indicate that neglecting the canonical nonlinearity of glassy‐state annealing kinetics in pharmaceutical (and other) glasses leads to good KWW fits to the dependence of enthalpy on annealing time, but with spurious KWW parameters that are affected by ...

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09.05.2013 | Shunsuke Ozaki, Ikuo Kushida, Taro Yamashita, Takashi Hasebe, Osamu Shirai, Kenji Kano, Journal of Pharmaceutical Sciences, 2013

Abstract The impact of water‐soluble polymers on drug supersaturation behavior was investigated to elucidate the role of water‐soluble polymers in enhancing the supersaturation levels of amorphous pharmaceuticals. Hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone (PVP), and ...

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09.05.2013 | Xi Qiu, Yi‐An Bi, Larissa M. Balogh, Yurong Lai, Journal of Pharmaceutical Sciences, 2013

Abstract Species differences among membrane transporters can be remarkable and difficult to properly assess by conventional methods. Herein, we employed the first use of stable isotope labeling in mammals or stable isotope‐labeled peptides combined with mass spectrometry to identify ...

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09.05.2013 | Ming‐Liang Lai, Yu‐En Tien, Ying‐Syuan Huang, Jin‐Ding Huang, Journal of Pharmaceutical Sciences, 2013

Abstract P‐glycoprotein (P‐gp) is a drug efflux pump in many organs, including the intestine and liver. Two single nucleotide polymorphisms (SNPs) of P‐gp gene, 2677G>T and 3435C>T, were reported to influence function and expression of P‐gp and have the controversial effects on drug ...

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09.05.2013 | Xi Han, Laila Jallo, Daniel To, Chinmay Ghoroi, Rajesh Davé, Journal of Pharmaceutical Sciences, 2013

Abstract Ibuprofen micronization with dry coating is investigated to examine its influence on passivation/stabilization of high‐surface‐energy sites and reduced cohesion. A fluid energy mill was used to micronize ibuprofen particles down to 5–28 μm with or without simultaneous nanosilica ...

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