Karnataka

A series of novel triazole fused thienopyrimidine derivatives are synthesized by Gewald reaction, which are well characterized by IR, 1HNMR, 13CNMR and Mass spectral analysis. These compounds are screened for their in vitro anti-tubercular and antibacterial activities. Most of these compounds exhibited MIC values in the range of 20 – 100 µM against Mycobacterium tuberculosis H37Rv. In the series, compound 5c was most active with MIC 20 µM. Furthermore, the title compounds were screened for antibacterial activity against Staphylococcus aureus ATCC 29213 (gram positive) and Escherichia coli ATCC 25922 (gram negative) bacteria. Some of these compounds exhibited MIC values in the range 8 - 64µM. Compound 5c was found to be the most active with an MIC of 5 and 8µM respectively.

Colon targeted drug delivery system is capable of protecting the drug in route to the colon i.e. drug gets released and absorbed once it reaches the colon. A multiparticulate system combining pH sensitive property and biodegradability has been investigated to prepare and evaluate Eudragit S-100 coated Sodium alginate microspheres for colon targeting of Tramadol Hydrochloride. Uncoated Tramadol Hydrochloride microspheres were prepared by ionotropic gelation technique using different ratios of Tramadol Hydrochloride and Sodium alginate. Coated Tramadol Hydrochloride microspheres were prepared by coacervation phase separation technique using different ratios of uncoated Tramadol Hydrochloride and Eudragit S-100/ Eudragit L-100. Uncoated and coated Tramadol Hydrochloride microspheres were evaluated for percentage yield, particle size, surface morphology, flow properties, drug content and entrapment efficiency and were found to be within the acceptable range. The uncoated microspheres sustained the release upto 8 hrs whereas coated microspheres sustained the release upto 12 hrs in a pH progression medium mimicking the condition of GIT. The drug release from MC4 formulation coated with Eudragit S-100 (1:4) showed desired rate as there was no drug release observed upto 4-5 hrs, while in colonic fluid controlled drug release was observed releasing about 69.66 % after 12 hrs. The release kinetics followed Peppas showing Super Case II transport. Stability studies suggested formulations were stable. It is concluded from the present investigation that Eudragit S-100 coated Sodium alginate microspheres are promising controlled release carriers for colon targeted delivery of Tramadol Hydrochloride.

The present work reports on the preparation of ethyl cellulose (EC)-pluronic F127 (PF127)-based tableted floating microspheres by the oil-in-water emulsion solvent evaporation method for the controlled release of acyclovir (ACV). Microspheres of this study were characterized by Fourier transform infrared (FTIR) spectroscopy to investigate the chemical interactions of ACV with the polymer, floating behavior, scanning electron microscopy (SEM) for morphology of the microspheres, differential scanning calorimetry (DSC) for investigating their thermal properties  and X-ray diffraction (XRD) as well as. In vitro release experiments of microspheres were performed in acidic pH 1.2 media to understand the release profiles of ACV. The selected sets of microspheres were compressed into tablets using the compressible excipients and their in vitro release performances were evaluated in pH 1.2 media.

Terbinafine hydrochloride (TFH), is a potent antifungal agent of the allylamine class with broad spectrum activity against yeasts, dimorphic fungi, molds, and dermatophytes. A new, simple, rapid, selective, precise, accurate, and stability indicating high performance liquid chromatographic method has been developed for the determination of terbinafine hydrochloride (TFH) in pharmaceuticals. The assay was performed using an Zorbax Eclips XDB C-18 (3.5 µm, 4.6 × 150 mm i.d.,) column at 30ºC temperature with UV-detection at 222 nm. A mobile phase consisting of buffer (1000 mL water, 2 mL triethylamine, pH 3.4 adjusted with trifluoroacetic acid.), isopropyl alcohol and methanol (40:12:48, v/v/v), was used in the assay at a flow rate of 1 mL min-1. The method was validated and system suitability parameters were investigated. An excellent linearity was obtained over the concentration range 1 - 80 μg mL-1 TFH with limits of detection (LOD) and quantification (LOQ) values of 0.3 and 1.0 mg mL-1, respectively. The proposed method were applied successfully to the determination of TFH in tablets. The results obtained were in good agreement with those obtained by a reference method, with high precision and without any detectable interference from tablets excipients. The validity and reliability of the proposed methods were further assessed by the recovery studies via a standard addition method. In addition, forced degradation of TFH was conducted in accordance with the ICH guidelines. Acidic, basic water hydrolysis, thermal stress, peroxide and photolytic degradation were used to assess the stability indicating power of the method. Slight degradation was observed during oxidative degradation and no degradation was observed under other stress conditions.

This research aimed to evaluate a new approach for preparation of in situ gel and to design innovative peroral delivery systems for Ranitidine Hydrochloride (RHCl) able to enhance the control release. The present study was carried out to optimize and evaluate an oral in-situ gel containing ranitidine HCl with Pluronic F-127 and hydrophilic HPMC E50 by the simple mixing method. The compatibility of the polymers was proved by FTIR. The prepared in-situ gel formulations were tested for their physicochemical characteristics such as clarity, gel strength, gelation temperature, drug content, sol-gel transition time and in vitro release studies of ranitidine HCl-loaded in-situ gel formulation in phosphate buffer (pH 1.2 and 7.4. ) were performed using a modified diffusion cell across dialysis membrane. The prepared formulations were clear and Gel strength ranges from 31±1.6 to 33±1.2. The drug content for the prepared formulations was 97.23% to 99.02%.Then the Drug release at 12 h is 98.25 and thus shown controlled release.

The eye presents unique opportunities and challenges for the delivery of pharmaceutical dosage forms. Ocular inserts of Moxifloxacin HCl were prepared with the objective of reducing frequency of administration, controlled release and greater therapeutic effect. Moxifloxacin HCl a broad spectrum fourth generation fluroquinolone used in the treatment of conjunctivitis, keratitis, kerato-conjunctivitis etc. In the present wok reservoir type of ocular inserts formulated by sandwiching poly vinyl alcohol containing Moxifloxacin HCl in between two rate controlling membranes of ethyl cellulose and PVP-K30. The reservoir types of ocular inserts containing Moxifloxacin HCl were formulated by film casting technique using PVA as drug reservoir polymer and EC: PVP-K30 as a rate controlling material. In vitro drug release revealed that the optimized (FM6) formulation showed a controlled release. In vivo studies showed a release of 97.67% over a period of 5 days with high correlation coefficient  of  In vitro-In vivo release studies. In the present study the ocular inserts of Moxifloxacin HCl (FM6) provided desired drug release for 5 days and remained stable.

Medicinal plants and their secondary metabolites have been used since last few centuries as remedies to treat diseases and disorders. As per WHO report (1993), 80% of world population continues to depend on medicine isolated from medicinal plants. Presently there is an increasing interest in herbal medicine related to isolation, characterization and pharmacological screening of extracts obtained from medicinal plants. The ethanolic extract of Leucas indica var. martinicensis was studied for preliminary phytochemical screening and anthelmintic activity at various concentrations (i.e., 10mg/ml, 25mg/ml, 50mg/ml, 100mg/ml) by using adult Indian earth worm, pheretima posthuma from in nalgonda region. Phytochemical Screening revealed the presence of Alkaloids, carbohydrates, and saponins. The mean paralysis time and mean death time for each sample was calculated and compared with the Albendazole which is taken as standard. The result was found that Leucas indica var. martinicensis had an anthelmintic activity which was greater than standard Albendazole.

Quinolines are a class of heterocyclic compounds, widely present in nature as quinoline alkaloids. Compounds having 2-quinolone moiety are associated with interesting biological activities such as antimalarial, tuberculostatic, antibacterial, antiviral, antifungal, anticancer, antidiabetic, cardiotonic and bronchodilator activity etc. The present work deals with the synthesis, characterization of substituted 7-amino-4-methyl-2-quinolone. The synthesized compounds were characterized by the IR, 1H-NMR & Mass spectral studies. Out of 10 test compounds evaluated for their antibacterial activities, four test compounds 3,6,8 & 9 were found to be active against Bacillus subtilis while amoxycillin and gentamycin were used as standard.

In the current status there is no explicit demarcation methodology on finding of substitutes (Pratinidhi Dravya). Thus here an attempt has been made to find out substitute by DNA fingerprinting on the basis of similarity and dissimilarity. In this study two samples Alysicarpus longifolius W. & A.Prodr.- Fabaceae, Desmodium laxiflorum DC i.e. of same family, same genus with different species were subjected to fingerprints. In this data we find a more similarities characteristics in both the plants i.e. up to 63%. As per the knowledge of research scientist this is a first moral attempt which throwing lights on concept of Pratinidhi Dravya (Substitution) in Ayurvedic science.

Ciprofloxacin hydrochloride is a fluoroquinolone antibiotic, widely effective in the treatment of ophthalmic disorders like, corneal ulcers and conjunctivitis. In the present study, an attempt has been made to formulate ciprofloxacin hydrochloride as sustained release in situ gel systems utilizing the concept of ion- activated gelation using Gelrite alone and with sodium alginate in combination with HPMC E50 LV. Prepared formulations were evaluated for several parameters like drug polymer compatibility, viscosity, gelling and gel retention time, clarity, pH, drug content, antimicrobial efficacy, sterility and in vitro drug release. Among all the formulations, batches G3 containing 0.6 %w/v of Gelrite, A6 and A7 containing 1% w/w of sodium alginate with 0.5 and 0.75 % w/v of HPMC E50LV respectively were selected based on their gelling properties. The drug release of A6 extended upto 7 h and that of G3 and A7 extended upto 8 h. The formulations showed pseudo plastic behaviour after gelling. G3 showed better stability and clarity than the alginate formulations and was taken for further evaluations. It showed better antimicrobial efficacy when compared with standard. The mechanism of drug release from the best formulation was further evaluated. Hence the developed in situ system may be an alternative to conventional eye drops.