Physicochemical Evaluation and Pharmacological Screening of Fernando Adenophylla Steenis Fruits.

The current study aimed to evaluate the physicochemical properties of Fernandoa adenophylla. Powder studies were carried out to estimate the quantitative physicochemical characteristics of the crude drug, including moisture content, ash content, and extractive values. Using a Soxhlet apparatus and different analytical grade solvents, 3 sample extracts of a crude drug were made. To evaluate the potentially toxic nature, an acute oral toxicity study was performed as per OECD guideline no. 423. Sample extracts were tested and analyzed by ANOVA for pharmacological potential (analgesic, antipyretic, and antidiabetic) using Wister-Albino rats. Where physicochemical analysis indicated purity, quality, and presence of organic/inorganic materials in crude drug extracts, no sign of mortality was found up to 2000 mg/kg of body weight of Fernandoa adenophyllas extracts. Analgesic activity was observed in all sample extracts, whereas only chloroform and ethanolic extracts expressed antipyretic and antidiabetic potential. Ethanolic extract was found to be most potent in pharmacological potential as 200 mg/kg extract dose exhibited %age pain inhibition of 55.12 % and reduced body temperature from 39.78±0.03 °C to 37.22±0.02 °C in hyperthermic rats. A decrease in blood glucose levels up to 57.88 % was observed on the 21st day of the treatment with 500 mg/kg ethanolic extract.

RP-HPLC Method for the Determination and Quantification of Artesunate.

A simple, rapid and cost-effective reverse phase high-performance liquid chromatographic (RP-HPLC) method was developed for the quantification of artesunate. C18 Promosil (ODS, 150 × 4.6 mm, 5 µm) column was used as stationary phase to separate the drug. Mobile phase comprised of ethanol: water (65:35) having pH 4.5 was run isocratically at a flow rate of 1 mL/min at 27°C. The method was validated according to ICH guidelines for linearity, precision, accuracy, robustness, specificity, limit of detection (LOD) and limit of quantification (LOQ). The method was found accurate, precise and robust with an average retention time of 4.509 min and 0.5357 %RSD. Good linearity was observed in the concentration range of 2-10 mg/ml with regression coefficient R2 value of 0.9995 and slope value of 369,928. Conclusively, as per ICH norms, the developed method was successfully validated and used for the quantification of artesunate in fast dissolving tablets (FDTs).

Enhancement of solubility and dissolution profile of artesunate by employing solid dispersion approach: An in-vitro evaluation.

Current study was designed with an aim to improve the solubility and dissolution profile of artesunate by preparing solid dispersions through solvent evaporation and freeze-drying techniques using polyethylene glycol 4000 (PEG4000) as solubility enhancer. Developed formulations were characterized for FTIR, XRD, TGA and SEM. Maximum increase in solubility was attained by freeze-dried solid dispersions (FD F444) i.e. 2.99 folds and 2.66 folds by solvent evaporation solid dispersion (SE F44) as compare to pure drug. Amorphous nature of artesunate in solid dispersions was confirmed from XRD diffractographs. Surface morphology indicated the existence of rough surface in freeze- dried solid dispersions (FDDs) and smooth surface in solvent evaporation solid dispersions (SEDs). Rapid dissolution rates were exhibited by fast dissolving tablets of optimized formulations. Moreover, the release of the drug was dominated by the first order kinetics (R2 = 0.9932) with the Fickian type of diffusion mechanism (n<0.450).

A mechanistic evaluation of the traditional uses of Nepeta ruderalis in gastrointestinal and airway disorders.

CONTEXT: Nepeta ruderalis Buch.-Ham. (Lamiaceae), locally known as Badranj Boya, is an aromatic herb used traditionally as an antispasmodic, antidiarrhoeal, and anti-asthamatic remedy. OBJECTIVE: Aqueous methanolic extract of N. ruderalis was studied to investigate its traditional uses. MATERIALS AND METHODS: Study was conducted from September 2015 to February 2016. In vitro spasmolytic and broncho-relaxant activity of crude extract of N. ruderalis (whole plant) was evaluated at 0.01-10 mg/mL final bath concentration in isolated rabbit jejunum and tracheal tissues, using PowerLab data acquisition system (Transonic Systems Inc., Ithaca, NY). In vivo antidiarrhoeal activity was evaluated in castor oil-induced diarrhoeal mice at the dose of 300 and 500 mg of crude extract orally. RESULTS: Crude extract of N. ruderalis completely relaxed spontaneously contracting, high K+ (80 mM) and carbachol (1 µM) induced contracted jejunum with an EC50 value of 5.85 (5.45-6.27), 4.0 (3.80-4.23) and 2.86 (2.48-3.29), similar to verapamil. Nr.Cr relaxed high K+ and carbachol induced contractions, at 5 and 10 mg/mL with an EC50 value of 2.37 (2.11-2.67) and 3.26 (2.9-3.67), respectively, and also displaced calcium concentration-response curves toward right at 0.1 and 0.3 mg/mL. Nr.Cr exhibited antidiarrhoeal protection at a dose of 300 and 500 mg/kg, similar to verapamil, whereas no acute toxicity signs were seen up to 5 g/kg in healthy mice. DISCUSSION AND CONCLUSION: Results suggest the presence of spasmolytic and broncho-relaxant effects in the crude extract of N. ruderalis, possibly mediated through calcium channel-blocking activity, providing the pharmacological basis for its traditional uses in gastrointestinal and airway disorders.