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Pan H.,Queens University of Belfast | Jing H.,Nanjing Chia Tai Tianqing Pharmaceutical Co. | Yang X.,Shenyang Pharmaceutical University | Pan W.,Shenyang Pharmaceutical University | Chen T.,Queens University of Belfast
Drug Development and Industrial Pharmacy | Year: 2016

The combination of metformin hydrochloride (MTF) and glipizide (GLZ) is second-line medication for diabetes mellitus type 2 (DMT2). In the present study, elementary osmotic pump ( EOP) tablet is designed to deliver the combination of MTF and GLZ in a sustained and synchronized manner. By analyzing different variables of the formulation, sodium hydrogen carbonate is introduced as pH modifier to improve the release of GLZ, while ethyl cellulose acts as release retardant to reduce the burst release phase of MTF. A two-factor, three-level face-centered central composite design (FCCD) is applied to investigate the impact of different factors on drug release profile. Compared with conventional tablets, the EOP tablet demonstrates a controlled release behavior with relative bioavailability of 99.2% for MTF and 99.3% for GLZ. Data also shows EOP tablet is able to release MTF and GLZ in a synchronized and sustained manner both in vitro and in vivo. © 2016 Informa UK Limited, trading as Taylor & Francis Group Source


Zhu C.-X.,Nanjing Chia Tai Tianqing Pharmaceutical Co. | Jiang Y.-R.,Jiangsu Provincial Academy of Chinese Medicine | Zhang Z.-H.,Jiangsu Provincial Academy of Chinese Medicine | Ding D.-M.,Jiangsu Provincial Academy of Chinese Medicine | Jia X.-B.,Jiangsu Provincial Academy of Chinese Medicine
Zhongguo Zhongyao Zazhi | Year: 2013

To determine the optimum process for preparing Cinnamomi Cortex oil microspheres based on porous silicon dioxide. After porous silica dioxide adsorbed Cinnamomi Cortex oil, Cinnamomi Cortex oil microspheres were prepared by the dropping method, with sodium alginate as the skeleton materials. The preparation process was optimized through the L9 (34) orthogonal test design, with microspheres diameter, distribution, drug loading capacity and entrapment efficiency as the indexes. The cinnamon volatile oil microspheres were characterized by scanning election microscope (SEM), thermogravimetric analysis (TGA), and infrared (IR) spectroscopy. An in vitro drug release experiment was conducted. The results showed that the microspheres prepared with the optimal process parameters were in good shape, even in size and good in dispersibility, with an average diameter of 1.61 mm, an average drug loading capacity of 32.85%, an entrapment efficiency of 94.79%. The maximum drug release capacity reached 72.6%, 95.0%, 97.4%, respectively, under pH 4.0, 6.8, 7.4 in 6 hours. Meanwhile, microsphere generation was tested by IR, TGA and other methods. The established optimum process for preparing Cinnamomi Cortex oil microspheres was proved to be stable and practical. Source


Song X.-F.,Center for Certification & Evaluation Jiangsu Province Food and Drug Administration | Song X.-F.,Nanjing Chia Tai Tianqing Pharmaceutical Co. | Zhao C.,Nanjing Chia Tai Tianqing Pharmaceutical Co. | Hu Z.-Y.,Institute for Food and Drug Control
Chinese Journal of New Drugs | Year: 2016

Objective: To eestablish an HPLC method for determining the related substances in montelukast sodium chewable tablets. Methods: Thermo Hypersil BDS-C18(100 mm×4.6 mm, 3 μm) column was used, and the column temperature was set at 40 ℃. The mobile phase was composed of acetonitrile and 0.02 mol·L-1 phosphate buffer [pH was adjusted to (3.7±0.1) by phosphoric acid] (20∶80 for A, and 80∶20 for B). The flow rate was 1.0 mL·min-1. The detection wavelength was 225 nm. Results: Impurities were completely separated from the main constituent. The main peak purity and material balance met the requirements. The LOD of impurities 1, 2 and 3 were 0.255 8, 0.132 1 and 0.176 0 ng. The average recoveries were 101.0%, 95.0% and 103.7%. Durability results showed that the appropriately altered detection conditions did not affect the detection of impurities. Conclusion: This method is applicable for the determination of related substance in montelukast sodium chewable tablets. © 2016, Chinese Journal of New Drugs Co. Ltd. All right reserved. Source


Cao M.,Nanjing Southeast University | Chang W.,Nanjing Southeast University | Chang W.,Nanjing Chia Tai Tianqing Pharmaceutical Co. | Zheng M.,Nanjing Southeast University | And 8 more authors.
Current Pharmaceutical Design | Year: 2015

Missing in metastasis (MIM, also MTSS1) is a member of the inverse Bin-Amphiphysin-Rvs (I-BAR) family that senses and stabilizes negative membrane protrusions. Abnormal expression of MIM has been frequently associated with a subset of human cancers and may play different roles in different stages of tumor progression. Overexpression of MIM-I-BAR in 293A cells potentiated the cell growth and increased the toxic response to paclitaxel. To modulate the function of MIM within cells, we designed several short peptide derivatives to target I-BAR dimerization. One of these derivatives had a cyclic configuration with a potency to disrupt the dimerization of MIM or ABBA proteins in vitro, and to be readily internalized into cells. Exposure of cells expressing MIM-I-BAR to this compound abolished increased susceptibility to paclitaxel and partially inhibited the I-BAR-mediated endocytosis. Our data suggests that this cyclic peptide can be used as a tool to study the function of intracellular MIM and as a lead to develop a therapy targeting human diseases involving abnormal MIM expressions. © 2015 Bentham Science Publishers. Source


Cao M.,Nanjing Southeast University | Hu H.-Y.,Huaiyin Normal University | Zhao H.-C.,Nanjing Southeast University | Zhang X.-Q.,Nanjing Chia Tai Tianqing Pharmaceutical Co. | And 6 more authors.
Chemical Papers | Year: 2014

In the current study a facile synthetic route for preparing antineoplastic drug GDC-0449 is investigated. Starting with pyridine-1-oxide and 1-iodo-3-nitrobenzene, the intermediate product 2-(2-chloro-5-nitrophenyl) pyridine was prepared by cross-coupling, deoxidation and halogenation. The final compound was then synthesised by reduction of the nitro group followed by amidation. This synthetic route avoids the use of unstable organometallic or organic boride compounds; it employs relatively inexpensive and bench-stable reagents, involves readily controllable reaction conditions, and achieves a relatively high yield. © 2014 Institute of Chemistry, Slovak Academy of Sciences. Source

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