Feasibility of rapidly assessing reactive impurities mediated excipient incompatibility using a new method: A case study of famotidine-PEG system.

The present work demonstrates the utility of temperature controlled set up with pressurized headspace oxygen as an approach to effectively reduce the time required for solid-state drug-excipient compatibility study. To illustrate the utility, the incompatibility of polyethylene glycol (PEG) and polyethylene oxide (PEO) with Famotidine (Fam) was shown. Owing to thermal and oxidative stress, polyethylene ether moieties of PEG generated reactive impurities, resulting in the degradation of Fam. The chemical degradation was evaluated via liquid chromatography. Around 20% of degradation was observed in the pressurized oxygen set up, whereas, no degradation was found in the absence of oxidative stress. On increasing the excipient fraction, the Fam degradation increased proportionally. Formation of aldehydes and free radicals from excipients were proposed as the precursors for Fam degradation. The generation of aldehydes and free radicals was confirmed by infrared and Electron Spin Resonance (ESR) spectroscopic analysis, respectively. Overall, the present study demonstrated the utility of pressurized oxygen set up as a rapid and routine tool for studying drug-excipient incompatibility at temperatures relevant drug-product manufacture.

Effect of crude extracts and purified compounds of Alpinia galanga on nutritional physiology of a polyphagous lepidopteran pest, Spodoptera litura (Fabricius).

Secondary plant metabolites play an important role in providing protection to plants against herbivore insect pests. Keeping in view the increasing importance of biopesticides, the crude extracts from different plants are being investigated for insecticidal activities. Alpinia galanga, a medicinal plant belonging to family Zingiberaceae exhibits a wide range of biological activities. In the present study, crude extracts of A. galanga and its purified compounds i.e. 1'-acetoxychavicol acetate and galangin were evaluated for their effect on various nutritional parameters of Spodoptera litura (Fab.). All the extracts exhibited a significant influence on relative growth and consumption rates as well as efficiency of conversion of ingested and digested food. Ethyl acetate extract was found to be the most effective causing significant reduction in values of RGR, RCR, ECI and ECD of S. litura larvae in comparison to control larvae. The highest concentration of the ethyl acetate extract (2500 ppm) resulted in 44.95%, 10.99%, 38.08% and 37.04% decrease respectively in RGR, RCR, ECI and ECD in comparison to control. The purified compounds also showed inhibitory effects on various nutritional parameters. 1'-Acetoxychavicol acetate was found to be more effective in comparison to galangin.

Evaluation of anti-amnesic effect of extracts of selected Ocimum species using in-vitro and in-vivo models.

ETHNOPHARMACOLOGICAL RELEVANCE: Ocimum species are traditionally used for the treatment of anxiety, nerve pain, convulsions and a variety of neurodegenerative disorders. The present study was undertaken to evaluate the anti-amnesic effect of O. basilicum L., O. sanctum L. and O. gratissimum L. extracts using in-vitro and in-vivo models. MATERIALS AND METHODS: In-vitro acetylcholinesterase (AChE) inhibitory and antioxidant activities of hydro-methanol extracts of plants were evaluated using Ellman and DPPH and FRAP assays, respectively. The most active extract i.e. O. basilicum extract (OBE) was further explored for the possible anti-amnesic activity in mouse model of scopolamine induced amnesia using behavioral models (elevated plus maze and passive shock avoidance task). Brain AChE activity, oxidative profile and histopathological studies were assessed to outline the anti-amnesic mechanism of the extract. RESULTS: Significant antioxidant and AChE inhibition activity was observed with all prepared extracts and however, OBE showed most marked free radical scavenging, reducing power and AChE inhibition (IC50 0.65±0.15mg/ml) activity. Basil leaves were standardized with respect to content of 7 phenolic acids using a HPLC-PDA method. A TLC densitometric method was employed to determine the quercetin content in the leaves. The in-vivo studies showed that OBE pre-treatment (200 and 400mg/kg, p.o.) reversed the memory deficit induced by scopolamine in mice, evident by significant (p<0.05) decrease in the transfer latency time and increase in step down latency in elevated plus maze and passive shock avoidance task, respectively. Moreover, OBE significantly reduced the brain AChE activity and oxidative stress. Further, histopathological examination of brain tissues displayed decrease in vacuolated cytoplasm and increase in pyramidal cells in hippocampal and cortical regions with OBE pre-treatment. CONCLUSION: OBE possesses antioxidant and AChE inhibitory activity. These biochemical changes are responsible for the anti-amnesic and neuroprotective activities of O. basilicum which may be attributed to the presence of phenolic and flavonoid compounds. This can be developed as an effective anti-amnesic drug.

Two new Aromatic Glycosides from a Soil Bacterium Burkholderia gladioli OR1.

Two new aromatic glycosides, named as gladioside I (1) and II (2) were isolated from the culture broth of a soil bacterium, Burkholderia gladioli OR1. Both 1 and 2 contained one unit each of rhamnose and 3-O-methyl xylose and differed from each other in the aglycone part. Compound 1 contained an aromatic aldehyde and compound 2 contained a styrylcarbamate unit as the aglycone part. The structures of 1 and 2 were elucidated by detailed spectral analysis and chemical degradation.