Acute oral toxicity evaluation of aqueous ethanolic extract of Saccharum munja Roxb. roots in albino mice as per OECD 425 TG.

BACKGROUND: S. munja roots have been used in ethno medicines for the treatment of different ailments. Despite its beneficial uses no studies on its toxicity potential have been reported. OBJECTIVE: The study was designed to evaluate acute toxic potential of aqueous ethanolic extract of S. munja roots according to OECD TG No. 425. MATERIAL AND METHODS: Female mice were divided into two groups (n = 5). One group served as control while the other as treated group that received 2000 mg/kg b.w. of S. munja roots ethanolic extract orally. Then both groups were observed for 14 days. Then the blood samples were collected by cardiac puncture, under chloroform general anesthesia and were subjected to hematological and biochemical analyses. The vital organs of anesthetized animals were preserved for histopathological examination. RESULTS: The the data revealed that LD50 of the extract was greater than 2000 mg/kg b.w. There was no significant alteration found in body weight and organ to body mass index. In comparison with control group, there was significant increase in levels of ALT, AST, total proteins, globulin levels, serum urea, cholesterol, triglycerides, LDL, platelet count, MCV, MCH, WBC count and lymphocytes whereas ALP and MCHC levels were reduced significantly. CONCLUSIONS: From the data obtained in this study, It can be concluded that though LD50 is greater than 2000 mg/kg b.w. but moderate toxicity signs appeared in liver, kidney, lipid profile and CBC also showed blood dyscresias at limit dose.

Bioequivalence study of montelukast tablets in healthy Pakistani volunteers.

Montelukast is a leukotrien receptor antagonist used for asthma treatment. Objective of this study was to evaluate the bioequivalence of two montelukast 10mg tablets, Innovator drug (Singulair) as reference and other locally manufactured drug (Montiget) in 12 healthy volunteers. It was randomized, single dose, two-period crossover study with 1 week washout period. Blood samples (4-5 ml) were collected before and after drug administration and plasma was separated for analysis. Concentrations of montelukast at different time intervals were determined by validated UV-HPLC method at 345nm wavelength. Bioequivalence was assessed by using non compartmental approach and also calculated the 90% confidence interval of the least-squared pharmacokinetic parameters (Cmax, AUC0-t and AUC0-OO). On average, Cmax, AUC0-t, AUC0-inf, was 2.35µg/mL, 1.28µg.h./ml, 1.67µg.h./ml, for innovator drug and 2.53µg/mL, 1.53µg.h./ml, 1.96µg.h./ml, for test drug, respectively. Confidence interval (90%) for Cmax, AUC0-t and AUC0-inf was 89-97%, 85-91% and 81-98% respectively. No statistical difference was found between the Cmax and AUC values of test and reference drugs. The confidence intervals for Cmax, AUC0-t and AUC0-OO are fully laid within the acceptable range of FDA (80-125%), thus two formulations are considered to be bioequivalent.

Elastic liposomes bearing meloxicam-beta-cyclodextrin for transdermal delivery.

The ultra-flexible lipid vesicles, the elastic liposomes bearing meloxicam-beta-cyclodextrin complex were prepared for its topical administration with the aim of simultaneously exploiting the favorable properties of both the carriers. The prepared meloxicam-beta-cyclodextrin complex was evaluated using DSC, XRD and FT-IR, which indicates the formation of inclusion complex in a molar ratio of 1:2 of meloxicam and beta-cyclodextrin (beta-CD). The elastic liposomes were prepared by conventional rotary evaporation method and characterized for various parameters such as vesicle shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, stability and in-vitro release pattern. Permeability studies of meloxicam and meloxicam-beta-cyclodextrin complex, as such or incorporated in elastic liposomes performed both across artificial membranes and rat skin highlighted a favorable effect of cyclodextrin on drug permeation rate, due to its solubilizing action. Moreover skin-permeation enhancer property of elastic liposomes has been evidenced. Skin permeation potential of the developed formulation was assessed using confocal laser scanning microscopy (CLSM), which revealed an enhanced permeation of the formulation to the deeper layers of the skin (up to 160 microm) following channel like pathways. Skin permeation profile of elastic liposomal formulation bearing meloxicam-beta-cyclodextrin complex was observed and the investigations revealed an enhanced transdermal flux (12.48+/-0.9 microg/cm(2)/h) and decreased lag time (0.7 h) for meloxicam. The obtained flux was nearly 1.4 and 9.1 times higher than elastic liposomal formulation bearing meloxicam and plain drug solution, respectively (P<0.005). The results indicate that the elastic liposomes may be promising vehicles for the transdermal delivery of meloxicam.