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Luo H.,Guizhou Academy of Agricultural science | Luo H.,Guizhou University | Cai Y.,Guizhou Academy of Agricultural science | Peng Z.,Guizhou Academy of Agricultural science | And 3 more authors.
Chemistry Central Journal | Year: 2014

Background: Hylocereus polyrhizus and Hylocereus undatus are two varieties of the commonly called pitaya fruits, and pitaya fruits have gained popularity in many countries all over the world. However, studies on chemical composition and the nutritional quality of pitaya flesh peel are limited.Results: Extracts of pitaya (H. polyrhizus and H. undatus) peel were extracted by supercritical carbon dioxide extraction, and analyzed by gas chromatography-mass spectrometry analysis. Their cytotoxic and antioxidant activities were investigated. The main components of H. polyrhizus extract were β-amyrin (15.87%), α-amyrin (13.90%), octacosane (12.2%), γ-sitosterol (9.35%), octadecane (6.27%), 1-tetracosanol (5.19%), stigmast-4-en-3-one (4.65%), and campesterol (4.16%), whereas H. undatus were β-amyrin (23.39%), γ-sitosterol (19.32%), and octadecane (9.25%), heptacosane (5.52%), campesterol (5.27%), nonacosane (5.02%), and trichloroacetic acid, hexadecyl ester (5.21%). Both of the two extracts possessed good cytotoxic activities against PC3, Bcap-37, and MGC-803 cells (IC50 values ranging from 0.61 to 0.73 mg/mL), and the activities of their main components were also studied. Furthermore, these extracts also presented some radical scavenging activities, with IC50 values of 0.83 and 0.91 mg/mL, respectively.Conclusion: This paper provides evidence for studying the chemical composition of supercritical carbon dioxide extracts of pitaya peel and their biological activity. © 2014 Luo et al.; licensee Chemistry Central Ltd. Source

Xiao H.,Yangtze River Pharmaceutical Group Beijing Haiyan Pharmaceutical Co. | Bai J.,Yangtze River Pharmaceutical Group Beijing Haiyan Pharmaceutical Co. | Bai J.,Peking University | Hou P.,Yangtze River Pharmaceutical Group Beijing Haiyan Pharmaceutical Co. | And 3 more authors.
Chinese Journal of New Drugs | Year: 2013

Objective: To prepare aspirin and hydrotalcite double-layer tablets, and to evaluate the quality. Methods: The formulation and preparation of aspirin and hydrotalcite double-layer tablets were studied, and the appearance, related substances, dissolution, and contents were evaluated. HPLC was used to assay content limit of free salicylic acid, and complex ometric titration was used to determine hydrotalcite. Results: The aspirin and hydrotalcite double-layer tablets had ideal release, high stability and reproducibility. Conclusion: The aspirin and hydrotalcite double-layer tablets prepared by the method have good appearance. The determination method is rapid, convenient and accurate, and can be used to control the quality of aspirin and hydrotalcite double-layer tablets. Source

Hou P.,Beijing University of Chinese Medicine | Hou P.,Yangtze River Pharmaceutical Group Beijing Haiyan Pharmaceutical Co. | Cao S.,Beijing University of Chinese Medicine | Ni J.,Beijing University of Chinese Medicine | And 7 more authors.
Drug Development and Industrial Pharmacy | Year: 2015

The goal of this study was to enhance the absorption of a new water-insoluble antitumor lead compound, T-OA (3β-hydroxyolea-12-en-28-oic acid-3, 5, 6-trimethylpyrazin-2-methyl ester). Early-stage preparation discovery concept (EPDC) was employed in this study. Based on this concept, a microemulsion system was chosen as the method of improving bioavailability. The solubility of T-OA was checked in different oils, surfactants and cosurfactants. Ternary phase diagrams were constructed to evaluate the microemulsion domain. Developed high-performance liquid chromatography method was used to determine drug content. The transparent o/w microemulsion formulation composed of oleic acid (oil), Tween 80 (surfactant), ethanol (cosurfactant) and water enhanced the solubility of T-OA up to 20 mg/mL. It was characterized in terms of appearance, content, viscosity, zeta potential, conductivity, morphology and particle size. The particle size distribution, viscosity, conductivity and zeta potential were found to be 70 nm, 15.57 MPa s, 44.1 μS cm-1 and -0.174, respectively. Oral bioavailability of T-OA microemulsion and oleic acid solution were checked by using rat model. Contrast to the solid dispersion and proto drug, the area-under-the-curve (AUC) of T-OA microemulsion and oleic acid solution were significantly enhanced. The relative bioavailability of T-OA microemulsion was found to be 5654.7%, which is 57-fold higher than the pure drug. Improved T-OA solubility in microemulsion was found sustained 48 h in dilution study. While the solid dispersion may precipitate under the gastrointestinal circumstance based on dilution results. The in-vivo and in-vitro results indicated that, compare to improve the solubility, it is more important to maintain and prolong the T-OA dissolved status, for improvement of the in-vivo absorption. © 2013 Informa Healthcare USA, Inc. Source

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