Design and In-vivo Evaluation of Quercetin Nanosponges-based Buccal Tablets of Quercetin

The objective was to increase the bioavailability of quercetin by creating a controlled release formulation using nanosponges based on cyclodextrin. A 3-factor, 3-level Box-Behnken design with quercetin was loaded into nanosponges using the freeze-drying process based on the early testing. The prepared nanosponges were examined after being described and made into tablets. The quercetin-loaded nanosponges have particle sizes ranging from 36.45 to 135.27 nm, encapsulation efficiencies ranging from 42.37 to 88.44%, and drug release percentages at 6 hours ranging from 53.04 to 82.64%. The Quercetin interaction with nanosponges was validated by the FTIR, DSC, and XRD investigations. The medicine released from the nanosponges buccal tablets in vitro at a rate of 99.75 percent, and stability testing showed no significant changes within six months after the nanosponges were transformed into tablets. In-vivo studies in rats showed that quercetin optimised nanosponges tablets Cmax of 6.27±0.06 ng/ml was significantly higher (p<0.05) than the pure drug's Cmax of 3.07±0.086 ng /ml. Both the nanosponges tablet formulation and the pure drug suspension had Tmax values of 4.0±0.07 and 0.5±0.08 h, respectively. The nanosponges tablet formulation had a greater AUC0-infinity(38.54±0.65 ng.h/ml) than the pure drug suspension formulation 7.84±1.08 ng.h/ml. In comparison to the pure drug, the nanosponges tablet formulation had a considerably greater AUC0-t (p<0.05). Poorly soluble Quercetin tablets developed for regulated drug delivery shown enhanced complexing ability with increased bioavailability using cyclodextrin-based nanosponges.

Design And In Vivo Evaluation Of Manidipine By Self-Nanoemulsifying Drug Delivery Systems

The current research is aimed at developing liquid self-nanoemulsifying drug delivery system (liquid-SNEDDS) of Manidipine for enhanced solubility and oral bioavailability. The Manidipine SNEDDS are formulated with excipients comprising of Capmul MCM (oil phase), Transcutol P (surfactant) Lutrol L 300 as co-surfactant. The prepared fifteen formulations of Manidipine SNEDDS analysed for emulsification time, percentage transmittance, particle size, in vitro drug release, and stability studies. In vivo pharmacokinetic studies of the optimized formulation were carried out in Wistar rats in comparison with control (pure drug). The morphology of Manidipine SNEDDS indicates spherical shape with uniform particle distribution. The percentage drug release from optimized formulation F14 is 98.24 ± 5.14%. The particle size F14 formulation was 22.4 nm and Z-Average 23.3 nm. The PDI and zeta potential of Manidipine SNEDDS optimized formulation (F14) were 0.313 and-5.1mV respectively. From in vivo bioavailability data the optimized formulation exhibited a significantly greater Cmax and Tmax of the SNEDDS was found to be 3.42 ± 0.46ng/ml & 2.00 ± 0.05 h respectively. AUC0-∞ infinity for formulation was significantly higher (11.25 ± 3.45 ng.h/ml) than pure drug (7.45 ± 2.24ng. h/ml). Hence a potential SNEDDS formulation of Manidipine developed with enhanced solubility and bioavailability.

Determination of fenticonazole in human plasma by HPLC-MS/MS and its application to pharmacokinetic studies / 药物分析学报

Two simple and sensitive high performance liquid chromatography–tandem mass spectrometry (HPLC–MS/MS) methods were developed and validated for the determination of fenticonazole in human plasma after percutaneous and intravaginal administration. Mifepristone was used as an internal standard (IS), and simple protein precipitation by acetonitrile containing 2%acetic acid was utilized for extracting the analytes from the plasma samples. Chromatographic separation was performed on a Kinetex XB-C18 column. The quantitation was performed by a mass spectrometer equipped with an electrospray ionization source in multiple reactions monitoring (MRM) positive ion mode using precursor-to-product ion transitions of m/z 455.2–199.1 for fenticonazole and m/z 430.2–372.3 for mifepristone. The validated linear ranges of fenticonazole were 5–1000 pg/mL and 0.1–20 ng/mL in plasma for the methods A and B, respectively. For the two methods, the accuracy data ranged from 85% to 115%, the intra- and inter-batch precision data were less than 15%, the recovery data were more than 90%, and no matrix interference was observed. The methods A and B were successfully validated and applied to the pharmacokinetic studies of fenticonazole gel in Chinese healthy volunteers after percutaneous and intravaginal administration, respectively.

Review of Rhubarbs: Chemistry and Pharmacology / 中草药·英文版

Rhubarb is a perennial herb belonging to the genus Rheum L. (Polygonaceae). Rhei Radix et Rhizoma (rhubarb roots and rhizomes) is one of the most popular Chinese materia medica and has been widely used for strong laxative function. About 200 compounds with six different types of skeletons (anthraquinone, anthrone, stilbene, flavonoids, acylglucoside, and pyrone) have so far been isolated from eighteen species of the genus Rheum L. These constituents showed extensive pharmacological activities including cathartic, diuretic, anticancer, hepatoprotective, anti-inflammatory, and analgesic effects, as well as toxicological effects. Chemical fingerprint, LC-MS, and other analytical techniques have been used for the quality control of rhubarb. This comprehensive review summarizes the researches into the isolation, pharmacological activities, and phytochemical analysis reported since investigations began in the late 1940s. In addition, pharmacokinetic studies and clinical application of rhubarb are also discussed in present paper. © 2013 Tianjin Press of Chinese Herbal Medicines.

Research progress in pharmacological activities of ginsenoside Rb1 / 中国药学杂志

OBJECTIVE: To review the pharmacological effects of ginsenoside Rb1 research progress. METHODS: According to domestic and foreign research reports of ginsenoside Rb1 in recent years, the pharmacological effects of Rb1 research progress. RESULTS: This article reviewed pharmacological effects and pharmacokinetic research of ginsenosides Rb1 from the central nervous system, cardiovascular system, immune system, and anti-tumor, anti-hepatic warm ischemia-reperfusion, lowering blood sugar and other aspects. CONCLUSION: Ginsenoside Rb1 is an important chemical material with a lot of pharmacological activities, studying its pharmacological effects can provide relevant information for further its development and utilization.

Determination of evodiamine by high performance liquid chromatography-tandem mass spectrometry and pharmacokinetic studies in rats / 中国临床药理学与治疗学

AIM: To establish an LC-MS/MS method for determination of evodiamine concentration in rat plasma and to study its pharmacokinetic profile in rats. METHODS: Six rats were administrated (i.g.) evodiamine at the dose of 100 mg/kg. Blood samples were collected from eye socket. Evodiamine concentration in rat plasma was determined by LC-MS/MS method. The pharmacokinetic parameters were calculated using DAS program. RESULTS: A good linear relationship was obtained in the concentration range (0.2-50.0 ng/mL) studied (r2=0.9997). Average recoveries ranged from 96.12% to 99.46%. Intra-and inter-day relative standard deviations were 4.61%-13.51% and 5.65%-11.49%, respectively. The main pharmacokinetic parameters of evodiamine were as follows: Cmax (5.3±1.5) ng/mL; tmax (22±8) min; t1/2 (451±176) min. CONCLUSION: A selective and sensitive liquid chromatography-tandem mass spectrometric (LC-MS/MS) method for the quantification of evodiamine in rat plasma is developed and validated. This method is successfully applied for the pharmacokinetic studies of evodiamine in rats.