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Wang N.-N.,Chongqing Medical University | Zhang D.-L.,Chongqing Pharmaceutical Research Institute Co. | Jiang X.-H.,Chongqing Medical University
Chirality | Year: 2015

A high-performance liquid chromatography (HPLC) method was established to detect Xeljanz enantiomers in active pharmaceutical ingredients (APIs) and tablets. The separation was achieved on a Chiralpak IC column using a mobile phase of hexane-ethanoldiethylamine (65:35:0.1, v/v). The detection wavelength was 289 nm. The peak areas and the enantiomer concentrations in the range of 0.15-2.25μg·mL-1 were in high linearity, with correlation coefficients higher than 0.999. The recoveries were 86.44% at the concentrations of 7.5, 18.75, and 37.5μg·mL-1. The limit of detection (LOD) and limit of quantification (LOQ) were 0.042 and 0.14μg·mL-1, respectively. This HPLC method is suitable for detecting the enantiomers of Xeljanz in its APIs and tablets. © 2014 Wiley Periodicals, Inc.

Zong T.,University of Sichuan | Zong T.,Chongqing Pharmaceutical Research Institute Co. | Mei L.,University of Sichuan | Gao H.,University of Sichuan | And 6 more authors.
Journal of Pharmaceutical Sciences | Year: 2014

The development of a drug delivery strategy that can not only cross the blood-brain barrier (BBB) rapidly, but also target the glioma and reach the core of glioma is essential and important for glioma treatment. To achieve this goal, we established a dual-targeting liposomal system modified with TAT (AYGRKKRRQRRR) and T7 (HAIYPRH), in which the specific ligand T7 could target BBB and brain glioma tumor and the nonspecific ligand TAT could enhance the effect of passing through BBB, and elevate the penetration into the tumor. The dual-targeting effects were evaluated by both in vitro and in vivo experiments. To identify the targeting effect, in vitro cellular uptake and BBB model were performed. Tumor spheroid penetration was performed to evaluate the penetration characteristics of the dual-targeting liposomes. In vivo pharmacokinetic studies were utilized to evaluate the influence of T7 and TAT peptides on the behavior of nanoparticle drug delivery system, and tissue distribution was further utilized to evaluate the glioma-targeting efficiency of the dual-targeting liposomes. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.

Liu C.,The Seventh People Hospital of Chengdu | Zhang Y.-L.,University of Sichuan | Huang H.,Chongqing University | Zhang T.,Fuan Pharmaceutical Group Chongqing Lybon PharmTeb Co. | And 2 more authors.
Chinese Journal of New Drugs | Year: 2015

Objective: To establish preparation methods of dutasteride solid self-microemulsion drug delivery system (S-SMEDDS), and to evaluate its qualities in vivo and in vitro. Methods: The effects of solid carriers on self-micromulsion's internal microstructure, drug loading, dispersion and precipitation in vitro were determined. S-SMEDDS of dutasteride was prepared by freeze-drying, and its physical properties, such as appearance, particle size and dissolution in vitro, were assessed. The pharmacokinetic behaviors of dutasteride S-SMEDDS were compared with those of Avodart in Beagle dogs. Results: The solid carriers had little effect on microstructure of L-SMEDDS but largely affected drug loading, dispersion and precipitation in vitro. Proper carriers were arabic and mannitol with the weight ratio of 1∶1. The mean diameter of dutasteride solid self-microemulsion after re-dispersing was 80 nm in spherical form. The dissolution of S-SMEDDS was significantly higher than that of Avodart in four media. Its dissolution profile was demonstrated to be rapid and pH-independent. In vivo pharmacokinetic study showed that dutasteride S-SMEDDS was bioequivalent with its market soft-capsules. Conclusion: Dutasteride S-SMEDDS is able to well maintain L-SMEDDS characteristics, and extends the range of applications in pharmaceutics. ©, 2015, Chinese Journal of New Drugs Co. Ltd. All right reserved.

Chen Y.-N.,Chongqing Medical University | Zhao X.-D.,Fochon Pharma Inc. | Deng J.,Chongqing Pharmaceutical Research Institute Co. | Li Q.-G.,Chongqing Medical University
Acta Crystallographica Section E: Structure Reports Online | Year: 2012

The title compound, C14H19N3O3, was synthesized by the reaction of 3-methoxy-propionitrile, tert-butyl bromo-acetate and eth-oxy-methyl-enemalononitrile. In the crystal, N - H⋯O hydrogen bonds link the molecules into chains propagating along the b axis. © Chen et al. 2012.

Zong T.,University of Sichuan | Zong T.,Chongqing Pharmaceutical Research Institute Co. | Mei L.,University of Sichuan | Gao H.,University of Sichuan | And 7 more authors.
Molecular Pharmaceutics | Year: 2014

Therapeutic outcome for the treatment of glioma was often limited due to low permeability of delivery systems across the blood-brain barrier (BBB) and poor penetration into the tumor tissue. In order to overcome these hurdles, we developed the dual-targeting doxorubicin liposomes conjugated with cell-penetrating peptide (TAT) and transferrin (T7) (DOX-T7-TAT-LIP) for transporting drugs across the BBB, then targeting brain glioma, and penetrating into the tumor. The dual-targeting effects were evaluated by both in vitro and in vivo experiments. In vitro cellular uptake and three-dimensional tumor spheroid penetration studies demonstrated that the system could not only target endothelial and tumor monolayer cells but also penetrate tumor to reach the core of the tumor spheroids and inhibit the growth of the tumor spheroids. In vivo imaging further demonstrated that T7-TAT-LIP provided the highest tumor distribution. The median survival time of tumor-bearing mice after administering DOX-T7-TAT-LIP was significantly longer than those of the single-ligand doxorubicin liposomes and free doxorubicin. In conclusion, the dual-ligand liposomes comodified with T7 and TAT possessed strong capability of synergistic targeted delivery of payload into tumor cells both in vitro and in vivo, and they were able to improve the therapeutic efficacy of brain glioma in animals. © 2014 American Chemical Society.

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