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Oral liquid compounding

Laura A Calvo-Castro, Christina Schiborr, Franziska David, Heidi Ehrt, Jenny Voggel, Nadine Sus, Dariush Behnam, Anja Bosy-Westphal, Jan Frank
SCOPE: Grapevine-shoot extract Vineatrol® 30 contains abundant resveratrol monomers and oligomers with health-promoting potential. However, the oral bioavailability of these compounds in humans is low (˂1-2%). The aim of this study was to improve the oral bioavailability of resveratrol from vineatrol by micellar solubilization. METHODS AND RESULTS: Twelve healthy volunteers (6 women, 6 men) randomly ingested a single dose of 500 mg vineatrol (30 mg trans-resveratrol, 75 mg trans-ε-viniferin) as native powder or liquid micelles...
March 13, 2018: Molecular Nutrition & Food Research
Ségolène De Vaugelade, Edith Nicol, Svetlana Vujovic, Sophie Bourcier, Stéphane Pirnay, Stéphane Bouchonnet
RATIONALE: The present work is devoted to the structural elucidation of by-products issued from the direct UV-visible irradiation of dehydroacetic acid (DHA) in solution and in cosmetic emulsion. METHODS: Analyses were carried out using a gas chromatography coupled with an ion trap mass spectrometer and by a high performance liquid chromatography coupled with ultrahigh resolution Fourier transform ion cyclotron resonance mass spectrometry (LC-UHRMS). The potential toxicities of by-products were estimated by in silico calculations based on a QSAR (Quantitative Structure-Activity Relationship) approach and by in vitro bioassays conducted on Vibrio fischeri bacteria...
March 8, 2018: Rapid Communications in Mass Spectrometry: RCM
Hanumanth Srikanth Cheruvu, Navneet K Yadav, Guru R Valicherla, Rakesh K Arya, Zakir Hussain, Chetan Sharma, Kamal R Arya, Rama K Singh, Dipak Datta, Jiaur R Gayen
Eclipta alba (Bhringraj) in ayurveda has been widely used as a traditional medicine for its multi-therapeutic properties for ages. Luteolin (LTL), wedelolactone (WDL) and apigenin (APG) are the three main bioactive phytochemicals present in Eclipta alba extract. However there was a lack of sensitive bioanalytical method for the pharmacokinetics of these free compounds in plasma which majorly contributes for their activities after oral administration of Eclipta alba. The present study aims to develop a sensitive, rapid and reliable liquid chromatography tandem mass spectrometry (LC-MS/MS) method for the simultaneous estimation of mice plasma concentrations of LTL, WDL and APG using quercetin as an internal standard for the pharmacokinetic analysis...
January 31, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Eman A Alraddadi, Ryan Lillico, Jonathan L Vennerstrom, Ted M Lakowski, Donald W Miller
Creatine is an ergogenic compound used by athletes to enhance performance. Supplementation with creatine monohydrate (CM) has been suggested for musculoskeletal and neurological disorders. Until now, little is known about its pharmacokinetic profile. Our objective was to determine the oral bioavailability of CM and the influence of dose on oral absorption. Rats were dosed orally with low dose (10 mg/kg) or high dose (70 mg/kg)13 C-labeled CM. Blood samples were removed at various time points. Muscle and brain tissue were collected at the conclusion of the study...
March 8, 2018: Pharmaceutics
Mustapha Tacherfiout, Petar D Petrov, Marco Mattonai, Erika Ribechini, Joan Ribot, M Luisa Bonet, Bachra Khettal
The Mediterranean buckthorn, Rhamnus alaternus L., is a plant used in traditional medicine in Mediterranean countries. We aimed at characterizing its phenolic compounds and explore potential antihyperlipidemic activity of this plant. The profile of phenolic compounds in R. alaternus leaf crude methanolic extract (CME) and its liquid-liquid extraction-derived fractions were analyzed by high-performance liquid chromatography/electrospray ionization tandem mass spectrometry (HPLC/ESI-MS2 ). Effects of CME on: circulating lipids in rats with Triton WR-1339-induced hyperlipidemia, intracellular lipid accumulation and expression of genes of fatty acid metabolism in human hepatoma HepG2 cells, and adipogenesis in the 3T3-L1 murine adipocyte cell model were assessed...
March 1, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Eunsook Park, Mee-Young Lee, Woo-Young Jeon, Chang-Seob Seo, Sooseong You, Hyeun-Kyoo Shin
ETHNOPHARMACOLOGICAL RELEVANCE: Paljung-san is a traditional herbal medicine used widely for the treatment of urogenital diseases in East Asia. However, scientific evidence of the efficacy of Paljung-san and its mechanisms of action against benign prostatic hyperplasia (BPH) is not clearly established. AIM OF THE STUDY: We investigated the inhibitory effect of Paljung-san water extract (PSWE) and its mechanisms against BPH in vitro and in vivo. MATERIALS AND METHODS: Active compounds of PSWE were analyzed quantitatively by High-performance liquid chromatography (HPLC)...
February 28, 2018: Journal of Ethnopharmacology
Amany A Thabet, Fadia S Youssef, Mohamed El-Shazly, Hesham A El-Beshbishy, Abdel Nasser B Singab
Oxidative stress leads to many disorders as diabetes mellitus and liver diseases. This study evaluates the antihyperglycemic and hepatoprotective activities of Brachychiton rupestris (Malvaceae). The antihyperglycemic activity of the total methanol extract of B. rupestris leaves (BRT) and its ethyl acetate fraction (BRE) was evaluated using streptozotocin induced diabetic rats. The hepatoprotective activity was assessed using carbon-tetrachloride induced hepatotoxicity. Oral administration of 50 mg/kg b.wt (body weight) of BRT and BRE to Streptozotocin -diabetic rats caused a notable decrease in serum glucose by 39...
February 24, 2018: Food and Chemical Toxicology
De Ji, Xiaonan Su, Ziyan Huang, Qiaohan Wang, Tulin Lu
We established a rapid and sensitive ultrahigh performance liquid chromatography tandem mass spectrometry method for the simultaneous quantification of xanthones and steroidal saponins in rat plasma. Chromatographic separation was achieved on a C18 column with a mobile phase comprising acetonitrile and 0.1% formic acid. The detection was performed by negative electrospray ionization in multiple reaction monitoring mode. The validated method showed good linearity within the tested range (r > 0.9945). The intra- and inter-day precision at high, medium, and low concentrations were less than 7...
February 23, 2018: Journal of Separation Science
Yunmei Song, Zen Whey Chin, David Ellis, Ei Mon Phyo Lwin, Sean Turner, Desmond Williams, Sanjay Garg
PURPOSE: Results of a study to determine the stability of an extemporaneously compounded minoxidil oral suspension under various temperature and stress conditions are reported. METHODS: Commercially available minoxidil tablets (10 mg) were crushed to a fine powder, and predetermined amounts of 2 suspending vehicles were added to produce a 1-mg/mL suspension, which was stored in glass bottles at room temperature (25 ± 2 °C) or in a refrigerator (4 ± 2 °C). To simulate daily patient use, 5 days weekly 1 bottle of the suspension was removed from refrigerated storage and shaken and 0...
March 1, 2018: American Journal of Health-system Pharmacy: AJHP
Shailee V Tiwari, Julio A Seijas, Maria Pilar Vazquez-Tato, Aniket P Sarkate, Kshipra S Karnik, Anna Pratima G Nikalje
Herein, we report an environmentally friendly, rapid, and convenient ionic liquid ([Et₃NH][HSO₄])-promoted facile synthesis of ethyl 4-(6-substituted-4-oxo-4H-chromen-3-yl)-6-methyl-2-thioxo/oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate derivatives 4 ( a - f ) and 4-(6-substituted-4-oxo-4H-chromen-3-yl)-6-methyl-2-thioxo/oxo-1,2,3,4-tetrahydropyrimidine-5- carbohydrazide derivatives 6 ( a - f ). All the synthesized derivatives 4 ( a - f ) and 6 ( a - f ) were evaluated for their in vitro antifungal and antibacterial activity, by method recommended by National Committee for Clinical Laboratory Standards (NCCLS)...
February 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Róli R Simões, Scheila I Kraus, Igor S Coelho, Daniela Dal-Secco, Diogo A Siebert, Gustavo A Micke, Michele D Alberton, Adair R S Santos
ETHNOPHARMACOLOGICAL RELEVANCE: Eugenia brasiliensis Lam. (Myrtaceae) is a Brazilian tree distributed throughout Atlantic rain forest, since Bahia until Santa Catarina state, and is popularly known as "grumixaba, grumixameira, cumbixaba, ibaporoiti, and cereja-brasileira". The bark and leaves of Eugenia brasiliensis are used in folk medicine as adstringent, diuretic, energizing, anti-rheumatic and anti-inflammatory. This study aimed at investigating the chemical composition, antinociceptive and anti-inflammatory effect of the hydroalcoholic extract of Eugenia brasiliensis (HEEb)...
February 17, 2018: Journal of Ethnopharmacology
Yue-Hu Wang, Min Shi, Hong-Mei Niu, Jun Yang, Meng-Yuan Xia, Ji-Feng Luo, Ying-Jie Chen, Yi-Ping Zhou, Heng Li
ETHNOPHARMACOLOGICAL RELEVANCE: Chong-lou (Paris polyphylla var. yunnanensis or P. polyphylla var. chinensis) is traditionally used as an anticancer medicine in China. It is also the material basis of some Chinese patent anticancer medicines, such as Gan-Fu-Le capsules, Bo-Er-Ning capsules, Lou-Lian capsules, Ruan-Jian oral liquid, and Qi-Zhen capsules. P. forrestii, a substitute for Chong-lou, is planted at a large scale in the Yunnan Province of China. AIM OF THE STUDY: To clarify the active chemical constituents of P...
February 15, 2018: Journal of Ethnopharmacology
Ting Liu, Xiumin Tian, Zhaoqin Li, Fei Han, Bin Ji, Yunli Zhao, Zhiguo Yu
Gegenqinlian decoction (GQLD) as a traditional Chinese medical (TCM) prescription is made from four Chinese herbs and has been used for centuries to treat pyrexia and diarrhea. In this work, an ultra-high performance liquid chromatography coupled with Fourier transform ion cyclotron resonance mass spectrometry (UHPLC-FT-ICR-MS) method was established to profile the metabolic fate of GQLD in rat plasma, urine, bile and feces. The analysis was performed on a Waters Acquity UPLC HSS T3 column (2.1 mm × 100 mm, 1...
February 6, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Cunchun Dai, Shaoqi Qu, Ruili Zhang, Li Zhao, Yuwen Li, Jiajia Zhu, Chunmei Wang, Hui Guo, Zhihui Hao
The objective of this study was to prepare a new compound fenbendazole tablet containing 29.7 % fenbendazole, 1.50 % praziquantel and 0.059 % ivermectin for oral administration. The tablets were successfully prepared using mannitol as filler agent, polyvinyl polypyrrolidone as disintegrant, 5 % povidone (PVAK30) as a binder agent and magnesium stearate as lubricant. The appearance, hardness, fragility, time limit of disintegration and fenbendazole dissolution at 45 min all met the technical standards of the Ministry of Agriculture for the People's Republic of China...
February 1, 2018: Die Pharmazie
Mingjie Gao, Zhibin Wang, Jing Yang, Liqian Wang, Chengcui Wu, Binbin Cui, Chunjuan Yang
A sensitive, specific, and accurate ultra high performance liquid chromatography with electrospray ionization tandem mass spectrometry method was developed and validated for the simultaneous quantification of purpurin, munjistin, mollugin and alizarin from Qianzhi capsules in rat plasma. Chromatographic separation was performed on an Aglient Eclipse Plus C18 RRHD column with a mobile phase consisting of methanol and 5 mM ammonium acetate/water with gradient elution. The analytes were quantified on a triple quadrupole mass spectrometer, operating in the multiple reaction monitoring mode and switching the electrospray ion source polarity with positive electrospray ionization in a single run...
February 13, 2018: Journal of Separation Science
Thomas J McGrath, Paul D Morrison, Andrew S Ball, Bradley O Clarke
Polybrominated diphenyl ethers (PBDEs) and novel brominated flame retardants (NBFR) have been used in a range of polymers to inhibit the spread of fires but also have a propensity to migrate out of consumer materials and contaminate indoor dust. In this study, a total of 57 dust samples were collected from 12 homes, eight offices and eight vehicles in Melbourne, Australia and analysed for eight PBDEs (-28, -47, -99, -100, -153, -154, -183 and -209) and seven NBFRs (PBT, PBEB, HBB, EH-TBB, BEH-TEBP, BTBPE and DBDPE) to determine human exposure risks from dust ingestion...
February 8, 2018: Environment International
Yan-Fang Yang, You-Bo Zhang, Zhi-Jing Chen, Ying-Tao Zhang, Xiu-Wei Yang
BACKGROUND: The fruit of Psoralea corylifolia L., Psoraleae fructus (PF), is widely used in traditional Chinese medicine as a well-known herbal tonic. Previous studies have shown that PF and its major constituents may have potential values in the treatment of Parkinson and Alzheimer diseases, though their pharmacokinetics and brain distribution were largely unknown. PURPOSE: To develop a liquid chromatographic-tandem mass spectrometry (LC-MS/MS) method for simultaneous studies of the plasma pharmacokinetics and cerebral nuclei (including cerebellum, thalamus, brainstem, hippocampus, corpus striatum and cortex) distribution in rats of eleven known PF compounds following as psoralen, isopsoralen, psoralidin, bavachin, bavachinin, isobavachin, isobavachalcone, bavachalcone, neobavaisoflavone, corylifol A, and corylin...
January 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Xueju Zhang, Zifeng Pi, Zhong Zheng, Zhiqiang Liu, Fengrui Song
Gardeniae Fructus is a widely used Traditional Chinese Medicines in treating various diseases. However, the absorbed components and metabolites of its main bioactive iridoid ingredients from iridoid extract of the fruits of Gardeniae Fructus in rat plasma need further study. In this study, a systematic method based on ultra-performance liquid chromatography-quadrupole-time-of-flight/mass spectrometry (UPLC-Q-TOF/MS) technique was developed to speculate the absorbed components and metabolites of iridoid extract in rat plasma after oral administration...
February 15, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Mahamane Haidara, Mohamed Haddad, Adama Denou, Guillaume Marti, Sandra Bourgeade-Delmas, Rokia Sanogo, Geneviève Bourdy, Agnès Aubouy
BACKGROUND: Plasmodium falciparum malaria is still one of the most deadly pathology worldwide. Efficient treatment is jeopardized by parasite resistance to artemisinin and its derivatives, and by poor access to treatment in endemic regions. Anti-malarial traditional remedies still offer new tracks for identifying promising antiplasmodial molecules, and a way to ensure that all people have access to care. The present study aims to validate the traditional use of Terminalia macroptera, a Malian plant used in traditional medicine...
February 5, 2018: Malaria Journal
Liang-Tzung Lin, Ying-Jang Lai, She-Ching Wu, Wei-Hsuan Hsu, Chen-Jei Tai
Cordycepin is one of the most crucial bioactive compounds produced by Cordyceps militaris and has exhibited antitumor activity in various cancers. However, industrial production of large amounts of cordycepin is difficult. The porcine liver is abundant in proteins, vitamins, and adenosine, and these ingredients may increase cordycepin production and bioconversion during C. militaris fermentation. We observed that porcine liver extracts increased cordycepin production. In addition, air supply (2 h/d) significantly increased the cordycepin level in surface liquid-cultured C...
January 2018: Journal of Food and Drug Analysis
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