FORMULATION AND EVALUATION OF ORAL SUSTAINED IN SITU GELLING SYSTEM OF ROXATIDINE

Gel dosage forms are successfully used as drug delivery systems to control drug release and protect the medicaments from a hostile environment. The main objective of this present work is to formulate and evaluate in situ gels of roxatidine for the treatment of peptic ulcer. This system utilizes polymers that exhibit sol-to-gel phase transition due to change in specific physico-chemical parameters. In the present work in situ gels have been developed by using gellan gum and sodium alginate based on the concept of ion activated systems. Sol-to-gel transformation occurred in the presence of monovalent/divalent cations. Formulations were evaluated for clarity, drug content, in vitro gelling capacity, determination of pH, in situ release study, viscosity, gel strength, ex vivo gelation and stability study. All the results found to be satisfactory. Experimental part showed that viscosity of sols and gel strength was increased with increase in the concentration of polymers, also drug release gets sustaining. The formulations were therapeutically efficacious, sterile and provided sustained release of the drug over a period of time. These results demonstrated that the developed system is an alternative to conventional drug delivery systems and can improve patient compliance.Key words: In situ gels, Roxatidine, Peptic ulcer

Anti-bacterial activity of neoandrographolide derivatives: In silico interaction with the bacterial target

157-164Natural products and their semi synthesized molecules have been used as efficient antibiotics since a long time. The present global health scenario has raised the demand for novel antimicrobial agents and drug targets that are effective against drug resistant pathogens, emerging infections etc. The current study has promoted the antibacterial activity of the glucoside labdane ‘neoandrographolide’, isolated from the methanolic extract of the medicinal plant Andrographis paniculata. Further modification at its glucoside hydroxyl groups to generate ester and acetonide derivatives was done and the antibacterial potential of these compounds was screened against common bacterial pathogens. Among various derivatives, 4,6-O-(4-methoxybenzylidene) neoandrographolide exhibited promising results. In addition, molecular modeling study of the active compound was also explored to identify its probable binding mode on the bacterial target. The present study reported antibacterial activity of neoandrographolide derivatives for first time and also the bioactive molecule, 4,6-O-(4-methoxybenzylidene) neoandrographolide was examined as a potent antibacterial agent against different strains

Anti-bacterial activity of neoandrographolide derivatives: In silico interaction with the bacterial target

Natural products and their semi synthesized molecules have been used as efficient antibiotics since a long time. The present global health scenario has raised the demand for novel antimicrobial agents and drug targets that are effective against drug resistant pathogens, emerging infections etc. The current study has promoted the antibacterial activity of the glucoside labdane ‘neoandrographolide’, isolated from the methanolic extract of the medicinal plant Andrographis paniculata. Further modification at its glucoside hydroxyl groups to generate ester and acetonide derivatives was done and the antibacterial potential of these compounds was screened against common bacterial pathogens. Among various derivatives, 4,6-O-(4-methoxybenzylidene) neoandrographolide exhibited promising results. In addition, molecular modeling study of the active compound was also explored to identify its probable binding mode on the bacterial target. The present study reported antibacterial activity of neoandrographolide derivatives for first time and also the bioactive molecule, 4,6-O-(4-methoxybenzylidene) neoandrographolide was examined as a potent antibacterial agent against different strains

Camphor sulphonic acid mediated quantitative 1,3–diol protection of major Labdane diterpenes isolated from <i>Andrographis paniculata</i>

<p>Phytochemical survey of the methanol extract of the dried aerial parts of <i>Andrographis paniculata</i> led to the isolation of major labdane diterpenes, namely 14-deoxy-11,12-didehydroandrographolide, andrographolide and neoandrographolide. Andrographolide was found to be the major phytoconstituent of the plant which was biologically active. For better physiochemical characteristics and bioefficacy, andrographolide is subjected to semi-synthetic modifications. However, presence of several free hydroxyl groups associated with this molecule make it quite polar and poorly soluble in many organic solvents and hence unsuitable for synthetic modifications. One way of resolving its solubility issue is to protect 1,3-diol quantitatively under mild reaction condition without effecting other functional groups. Reaction conditions were optimised using different solvent systems and catalysts towards this direction. X-ray structure of 3,19-isopropylidene-14-deoxy-11,12-didehydroandrographolide is being reported here for the first time. Isolated compounds and derivatives were confirmed by spectral analysis or X-ray data analysis.</p

Synthesis and antimicrobial evaluation of novel 3-(arylideneamino)-3a,8a-dihydroxy-1,3,3a,8a-tetrahydroindeno[1,2-<i>d</i>]imidazole-2,8-diones and their 2-thioxo analogues

<p>The preparation of some novel 3-(arylideneamino)-3a,8a-dihydroxy-1,3,3a,8a-tetrahydroindeno[1,2-<i>d</i>]imidazole-2,8-diones <b>8(i–xiv)</b> and 3-(arylideneamino)-3a,8a-dihydroxy-2-thioxo-1,3,3a,8a-tetrahydroindeno[1,2-<i>d</i>]imidazol-8(2<i>H</i>)-ones <b>9(i–xiv)</b> have been reported through one-pot catalyst-free reaction of aldehydes, semicarbazide hydrochloride/thiosemicarbazide with ninhydrin. All the synthesized compounds have been screened for antimicrobial activity and some of them were observed to possess broad spectrum antibacterial potential as well as significant antagonistic potential against fungal pathogens.</p