Posted by admin on Jan 31, 2019 in |
Paracetamol is a well-known drug for its antipyretic, analgesic and anti-inflammatory activity. The drug being an OTC had been used more frequently than required. As a result of this overdosage of the drug caused a hepatotoxic effect. So to overcome this, an approach of PEGylation was chosen. PEG 1500-Paracetamol, PEG 6000-Paracetamol, PEG 1500-Glycine-Paracetamol, and PEG 6000-Glycine- Paracetamol. The Prodrugs synthesized were subjected to in- vitro dissolution at λmax 256nm at pH 1.2, 4.5 and 6.8. The studies revealed that % drug release was more at pH 6.8 rather than at pH 1.2 and 4.5, for PEG 6000-Gly-Paracetamol than PEG 1500-Gly-Paracetamol and also PEG 6000-Paracetamol % drug release was more than PEG 1500-Paracetamol. In-vivo Analgesic activity by Tail Immersion method revealed that PEG 6000-Gly-Paracetamol and PEG 1500-Gly-Paracetamol has higher analgesic activity than PEG-PEG 6000-Paracetamol and PEG 1500-Paracetamol, which indicates the influence of spacer, i.e., Glycine on drug release. In-vivo Analgesic activity by hot plate method and acetic acid methods revealed that PEG 6000-Gly-Paracetamol and PEG 6000-Paracetamol has higher analgesic activity...
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Posted by admin on Jan 31, 2019 in |
Mimosa pudica Linn. (Fabaceae) It is traditionally used to treat wounds and diabetes mellitus. The study was designed to evaluate the wound healing properties of ethyl acetate and ethanolic extracts of seeds of Mimosa pudica in streptozotocin-induced diabetes mellitus in rats at dose levels of 100, 200 and 400 mg/kg body weight. Both extracts decrease the fasting blood glucose in a dose-dependent manner. A significant decrease in blood glucose level was also observed in the ethanol and ethyl acetate extract treated rats at different dose levels. The maximum percentage contraction in wound area (25.52 to 97.37, 23.65 to 93.12) was observed in diabetic rats treated with ethanolic extract at 400 mg/kg and 200 mg/kg dose respectively and with a significant percentage contraction in wound area (21.34 to 96.87, 20.71 to 95.22) was observed in diabetic rats treated with ethyl acetate extract at 400 mg/kg and 200 mg/kg dose respectively on 15th day. The results exhibit that Mimosa pudica possesses considerable antidiabetic and wound healing activity in diabetic...
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Posted by admin on Jan 31, 2019 in |
The study aimed to develop a specific, exact, selective, precise and accurate Reversed Phase Stability Indicating Ultra-fast Liquid Chromatography (RP-UFLC) strategy is created and validated for Teneligliptin hydrobromide in the pure and marketed formulation. The method showed an adequate separation for Teneligliptin hydrobromide from their degradation products. The chromatographic separation was accomplished on Phenomenex Kinetex C18 (250 × 4.6 mm) with the mobile phase of methanol, acetonitrile, and potassium dihydrogen orthophosphate (40:20:40 v/v/v). The pH is changed by 4.6 using orthophosphoric acid. The run time was 10 min and the retention time of drug is 3.3 min. The detection is carried out at 246 nm using photodiode array detector (PDA) and ultraviolet (UV) with a flow rate of 1.0 ml/min. The drug product is exposed to acid and base stress, photolytic stress, Thermal stress, oxidative stress, and hydrolytic stress conditions, and the stressed samples were analyzed by the proposed method. The linearity of the proposed strategy is researched in the range of 2-10 µg/mL (r2 = 0.9915). The present...
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Posted by admin on Jan 31, 2019 in |
The present study was aimed to develop the effective protocol for induction roots and in-vitro regenerated plants from embryo culture of Nothapodytes nimmoniana. Excised embryos were sterilized under the aseptic condition and cultured on L2 medium fortified with different concentration (0.5 – 3 mg/L) and the combination of auxins and cytokinins. Maximum shoot initiation was observed in BAP (2 mg/L) and Kin (1 mg/L) and in a combination of BAP (0.5 mg/L) and NAA (2 mg/L). A higher number of roots were observed when the embryo was inoculated on L2 medium supplemented with NAA (1 mg/L) and 2, 4-D (0.5 mg/L). Whereas, elongated roots were observed on L2 medium fortified with BAP/KIN (0.5 mg/L) and NAA (1 mg/L). The proliferation of multiple shoots from the nodal explants of in-vitro plantlets, when sub-cultured on MS medium supplemented with BAP (2 mg/L), TZD (0.2 mg/L) and L-glutamine (100 mg/L). The obtained plantlets were hardened in soil-rite and then transferred them to a mixture of soil, sand, and manure (1:1:1). In conclusion,...
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Posted by admin on Jan 31, 2019 in |
A series of novel analogues of 2-(5-(1H-indol-3-yl)-1, 3, 4-thiadiazol-2-ylimino)- 5- (substituted benzylidene)thiazolidine-4-one have been synthesized. The structures of newly synthesized compounds were confirmed by FT-IR, 1H-NMR, 13C-NMR and Mass spectroscopy. The synthesized compounds showed significant antibacterial activity against gram-positive bacteria: Staphylococcus aureus (MTCC 3160), Bacillus subtilis (MTCC 2061), gram-negative Escherichia coli (MTCC 1652), Pseudomonas aeruginosa (MTCC 741) and antifungal activity against fungal strains: Candida albicans (MTCC 183) and Aspergillus niger (MTCC 2110). Also, their anti-inflammatory activity was evaluated by using carrageenan-induced rat paw edema method. Compounds 7d and 7h with the methoxy substitution on phenyl ring were found as active derivatives of the series, exhibited 49.86% and 49.88% inhibition respectively as compared with Diclofenac sodium. In-silico molecular docking studies of the synthesized compounds was done on crystal structures of proteins of microbes Aspergillus niger, Bacillus subtilis, Candida albicans, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and cyclooxygenase-2 using GRIP batch docking method of V-life MDS 3.0 software to study their observed activity which revealed a significant correlation between the binding...
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