Amaranthus tricolor whole plants are used by folk medicinal practitioners of Bangladesh for treatment of pain, anaemia, dysentery, skin diseases, diabetes, and as a blood purifier. Thus far, no scientific studies have evaluated the antihyperglycaemic and antinociceptive effects of the plant. The present study was carried out to evaluate the possible glucose tolerance efficacy of methanolic extracts of A. tricolour whole plants using glucose-induced hyperglycaemic mice, and antinociceptive effects with acetic acid-induced gastric pain models in mice. In antihyperglycaemic activity tests, the extract at different doses was administered one hour prior to glucose administration and blood glucose level was measured after two hours of glucose administration (p.o.) using glucose oxidase method. The statistical data indicated the significant oral hypoglycaemic activity on glucose-loaded mice at all doses of the extracts tested. Maximum antihyperglycaemic activity was shown at 400 mg extract per kg body weight, which was comparable to that of a standard drug, glibenclamide (10 mg/kg body weight). In antinociceptive activity tests, the extract also demonstrated a dose-dependent significant reduction in the number of writhings induced in mice through intraperitoneal administration of acetic acid. Maximum antinociceptive activity was observed at a dose of 400 mg extract per kg body weight, which compared favourably with that of a standard antinociceptive drug, aspirin, when administered at a dose of 200 mg per kg body weight. The results validate the folk medicinal use of the plant for reduction of blood sugar in diabetic patients as well as the folk medicinal use for alleviation of pain. The results suggest that this plant may possess further potential for scientific studies leading to possible discovery of efficacious antihyperglycaemic and antinociceptive components.
The main objective of the study was to alter the dissolution profile of a practically insoluble Biopharmaceutics Classification System class II drug, aceclofenac, by formulating into lipid semisolid matrix (SSM) formulations using liquid filling technology in hard gelatin capsules, for both immediate and sustained release. SSM formulations of aceclofenac were prepared by melt fusion technique, using Gelucires (44/14, 50/13, 33/01 and 43/01), polyethylene glycols (4000 and 6000) and Poloxamer 188 at different levels. Role of additives like docusate sodium, Tween 80, Aerosil 200 and polyvinylpyrrolidone K-30 in enhancement of drug release was investigated. The optimized immediate and sustained SSM capsules were characterized in terms of assay, in vitro drug release, moisture uptake and differential scanning calorimetry. More than 80% of the drug was released within 15 min in various dissolution media studied, from Gelucire 44/14-based immediate release formulations. Incorporation of docusate sodium and Tween 80 provided further enhancement in drug dissolution when compared to plain drug and marketed tablet. SSM formulations based on Gelucire blends of 50/13 and 43/01 and 44/14 and 43/01 sustained the release of the drug for a period of 24 h following zero-order kinetics. The in vivo study of the optimized immediate release and sustained release formulations revealed significant enhancement in anti inflammatory activity (p50.01) in rats. From these findings, liquid fill technique in hard gelatin capsules using Gelucire and their blends might be an efficacious approach for designing immediate or sustained drug release profiles for poorly soluble drugs like aceclofenac.
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