Posted by admin on Nov 30, 2018 in |
The aim of the present study was to improve the solubility and bioavailability of a poorly water-soluble drug in human body, using a solid dispersion technique. Solubility and dissolution rate is an important physicochemical factor affecting absorption of drug and its therapeutic effectiveness. Consequences of poor aqueous solubility would lead to failure in formulation development. The poor solubility of drug substances in water and their low dissolution rate in aqueous G.I.T fluid often leads to insufficient bioavailability. In the present investigation, an attempt was made to improve the solubility and dissolution rate of a poorly soluble drug, Eprosartan by solid dispersion method using Arosil-200 as carrier. The formulations were characterized for solubility parameters, drug release studies and solubility studies, dissolution studies. All the formulations showed marked improvement in the solubility behaviour and improved drug release. The interaction studies showed no interaction between the drug and the carrier. It was concluded that Aerosil-200 as a carrier can be very well utilized to improve the solubility of poorly soluble...
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Posted by admin on Nov 30, 2018 in |
Quinolones are the organic compounds that act against the DNA-gyrase enzyme, a type II topoisomerase. Norfloxacin is one such quinolone which is characterized by a piperazinemoiety at C-7 position. This moiety plays a significant role in determining the antibacterial spectrum and potency and serves as a site amenable to significant modification. N-Mannich bases have proved to be potential prodrug candidates for amides, urea derivatives, imides and amines. It has proved to be a versatile base in current applications of organic chemistry. Mannich bases with N-4 substituted piperazine containing moieties were biologically active. We designed and synthesized new series of Mannich bases of Norfloxacin by conventional as well as microwave method by reacting them with isatin and various aromatic aldehydes. Their chemical structures have been confirmed by IR, 1H NMR and 13C NMR spectroscopy and evaluated for antibacterial activity by Agar well diffusion method. Antimicrobial evaluation was done against gram positive bacteria B. subtilis and gram negative bacteria E. coli. Among the compounds tested, 7a (i) and 7b (i) showed...
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Posted by admin on Nov 30, 2018 in |
Antiviral properties of methanol and aqueous extracts from Morchella conica and Fomes fomentarius were assessed by colorimetric XTT test against human respiratory syncytial virus (HRSV). HEp-2 cell line was used for the cytotoxic and antiviral effects of the extracts. Non-cytotoxic concentrations of methanol and aqueous extracts of M. conica were tested in 50000 to 195 µg/mL. In contrast, the cytotoxic F. fomentarius methanol and aqueous extracts and Ribavirin were tested at concentrations from 3347-13.1 μg/mL, 4906.5-19.2 μg/mL and 86.60-0.30 μg/mL, respectively. The results showed that aqueous extract of F. fomentarius had strong anti-HRSV activity (EC50 = 358.7 μg/mL, SI = 27.4) which could be compared with ribavirin (EC50 = 15.6 μg/mL, SI = 11.1) used as a positive control against HRSV, while other extracts (M. conica methanol extract EC50 = 28055 μg/mL, SI = >1.8; F. fomentarius methanol extract EC50 = 3000 μg/mL, SI = 2.2) were found to have weak antiviral activity. As a result, it can be said that aqueous extract of F. fomentarius is worthy of...
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Posted by admin on Nov 30, 2018 in |
Thiazoles derivatives are an important class of heterocyclic compounds, reported to possess a wide spectrum of biological activities. Moreover, thiazole nucleus occupies a very important place in the field of antioxidant agents. The above observations prompted us to synthesize some novel thiazole derivatives with various substitutions at along with heterocyclic rings in the same framework for synergistic action. We here in report the synthesis, antioxidant screening & QSAR studies of the new title compounds. Concentrated research on N-((Substituted) benzylidene)-4-(4-chlorophenyl) thiazole-2-carbohydrazides GS-5i-(a-k) & were synthesized, screened for antioxidant activities & QSAR studies. All new entities have good yield and results. From antioxidant activity results, it was observed that the compounds with both electron donating and electron withdrawing groups on the aldehydic phenyl ring influenced the activity. Among all the compounds tested GS-5i-b, GS-5i-d, GS-5i-e, GS-5i-h & GS-5i-i showed the good % inhibition and were found to be more significant compound among all the compounds tested. Compounds GS-5i-j were showed moderate % inhibition and were found to be significant among all...
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Posted by admin on Nov 30, 2018 in |
The hydro dynamically balanced gastro retentive systems of Pregabalin has been formulated and evaluated which can retard the release of drug based on Super Porous Hydrogel Composites (SPHC) thereby prolong the release rate specifically in the upper part of the GIT. Fast swelling highly porous SPHCs are synthesized by gas blowing technique. The swelling property, mechanical strength and release profile of SPHCs containing drug was investigated by changing the amount of cross-linking agents such as N,N1-methylene-bis acrylamide (BIS) and Ac-Di-Sol. SPHCs to powder form was prepared, the obtained powder material used as matrix agent for the preparation of tablets. Floating tablets were prepared by wet granulation, novel melt granulation and direct compression methods using various grades of ethyl cellulose, HPMCK 100, eudragit ESPO, geleol, compritol 888 ATO and SPHC powder in different concentrations. The prepared gastro retentive floating tablets were evaluated in-vitro buoyancy studies, in–vitro and in-vivo release studies. Formulations consisting powdered SPH Ac-Di-Sol composite as matrix agent was optimized. The floating time observed >12 h at pH 1.2....
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