Drug Invention Today最新文献

Objective

The objective of the present work is to develop a simple, precise, accurate, validated stability indicating RP-HPLC method for the determination of Atazanavir sulphate in bulk and capsule dosage form.

Method

A validated stability indicating RP-HPLC method for the estimation of Atazanavir sulphate in capsule dosage form on Agilent TC C18 (2) 250 × 4.6 mm, 5 μ column using mobile phase composition of 0.02 M ammonium dihydrogen phosphate buffer:acetonitrile:methanol (30:25:45 v/v) and pH adjusted at 2.5 with ortho-phosphoric acid. Flow rate was maintained at 1 ml/min at an ambient temperature. Quantification was achieved with ultraviolet detection at 288 nm.

Results

The retention time obtained for Atazanavir sulphate was at 3.0 min. The result obtained with the detector response was found to be linear in the concentration range of 5–50 μg/ml. This method has been validated and shown to be specific, sensitive, precise, linear, accurate, rugged, robust and fast. Atazanavir sulphate was subjected to different accelerated stress conditions. The degradation products, when anywhere well resolved from the pure drug with significantly different retention time values.

Conclusion

It is concluded that this method can be applied for routine quality control of Atazanavir sulphate in capsule dosage forms as well as in bulk drug.

New advances in different technologies have made the previously unused terahertz frequency band accessible for imaging systems. The ‘terahertz gap’ has a frequency ranges from ∼0.3 THz to ∼10 THz in the electromagnetic spectrum which in between microwave and infrared. The terahertz radiations are invisible to naked eye & in comparison with X-ray they are intrinsically safe, non-destructive and non-invasive. This is such a new field that researchers around the world race to build the first practical system. It resolves many of the questions left unanswered by complementary techniques, such as optical imaging, Raman and infrared. Terahertz spectroscopy has number of applications run from detecting defects in tablet coating, product inspection (industry), spectroscopy (chemistry, astronomy), material characterization (physics), weapons concealed under clothing (airports), detection of cancer and caries. In the pharmaceutical industries it enables nondestructive, internal, chemical analysis of tablets, capsules and other dosage forms. This paper tries therefore not only to provide a brief overview over the imaging technology, but also over the whole range of current systems and research in terahertz technology.

Objectives

To evaluate the antifungal activities of novel 1,2,3-benzotriazole derivatives synthesized by ultrasonic and solvent-free conditions.

Methods

Newer “1-(1H-benzo[d][1,2,3]triazole-1-carbonyl) derivatives” (5A–5P) were synthesized by using “1H–benzo[d][1,2,3]triazole” (1) as the starting material under ultrasonicated and solvent-free conditions. The resulting products were isolated and characterized by melting points and spectral studies. All the products were assayed for antifungal activity for various pathogenic fungi.

Results

Excellent antifungal activity was shown by derivative-5L against Candida albicans (MTCC – 3018) whereas other compounds have shown comparable activity. Except derivative-5P, all synthesized compounds have shown mild activity against Candida glabrata (MTCC – 3019). Towards Aspergillus niger (MTCC – 2638) and Aspergillus flavus (MTCC – 2737) most of the compounds were inactive and some were feebly active. All the synthesized derivatives were inactive against Saccharomyces cerevisiae (MTCC – 170). The Minimum Inhibitory Concentrations (MIC) of the most of the synthesized 1,2,3-benzotriazole derivatives for these fungi were found to be 62.5 μg/ml.

Conclusions

Some of the newer 1,2,3-benzotriazole derivatives synthesized under solvent-free and ultrasound irradiation with noteworthy advantages viz., shorter reaction times, operational simplicity, simple work-up, and eco-friendly nature, have shown antifungal activities against selected pathogenic strains. Attachment of phenyl or phenyl with electron withdrawing substituents to either nitrile or azo functional group can be attributed to the substantial antifungal activity of these benzotriazoles.

Objective

The aim of the present work was to synthesize different types of complex compounds of two Schiff base ligands with metal ions by varying pH and solvent during their synthesis.

Methods

New Schiff base ligands formed by the condensation of 3-Aldehydosalicylic acid with equimolar quantity of Isonicotinoyl hydrazide (Isoniazid) and 4-Amino-5-phenyl-3-mercapto-1,2,4-Triazole forming 2-hydroxy-3-(2-isonicotinoyl hydrazones)methyl-benzoic acid and 3-[(3-Phenyl-5-mercepto-1,2,4-triazol-4-yl amino)-methyl-2-hydroxy-benzoic acid respectively. The complexes of metal ions like Cu (II), Zn(II), Ni(II), Co(II) and Cd(II) with Schiff base ligand (LH₂) have been synthesized at various pH ranges. All the synthesized Schiff bases and metal complexes were characterized by elemental analysis, FTIR, ¹H NMR and mass spectral data.

Results

Study reveals that the Schiff base ligand involved the donor –COOH, –OH and Nitrogen atom. The ligands LH2 in metal complexes behave as monobasic bidentate at different pH ranges. The Schiff bases and metal complexes were screened for their antifungal and antibacterial activities.

Conclusion

The Cu (II) and Zn (II) complexes exhibited higher inhibition against microorganisms than the other metal complexes.

Objectives

Microbe mediated synthesis of silver nanoparticles by using Serratia nematodiphila and to explore the antibacterial activity against pathogenic bacteria Bacillus subtilis, Klebsiella planticola and Pseudomonas aeruginosa.

Methods

The present studies, 1 mM of silver nitrate was added into 100 ml of S. nematodiphila (CAA) culture supernatant. The bioreduction of pure AgNO₃ were characterized by UV–visible spectroscopy, X-ray diffraction analysis (XRD), transmission electron microscopy (TEM) and Fourier transform infra-red (FTIR) analysis.

Results

In this report, biosynthesized silver nanoparticles are confirmed by color changes and it was characterized by UV–visible spectrum of surface plasmon resonance at 420 nm. Transmission electron microscopy (TEM) showed the formation of well-dispersed silver nanoparticles in the range of 10–31 nm and X-ray diffraction value obtain from range of (200) confirmed synthesized silver nanoparticles in crystalline nature. The microbe mediated synthesized silver nanoparticles shows more zone of inhibition against the pathogenic bacteria B. subtilis, K. planticola and P. aeruginosa.

Conclusion

Biosynthesis of metal nanoparticles is an expanding research area due to the biomedical application for the growth of novel biotechnologies. The report suggests that the synthesized silver nanoparticles act as eco-friendly antibacterial agent.

Objectives

To study the oculohypotensive effect of oral amlodipine in hypertensive individuals associated with increased intraocular pressure (IOP).

Method

This was a four weeks prospective study, done to assess oculohypotensive effect of oral amlodipine, in hypertensive patients with increased IOP. After obtaining written informed consent, a total of 32 (n = 32) newly diagnosed hypertensive patients (BP ≥ 140/90 mmHg) of either gender, attending the outpatient department of medicine with increased IOP (≥21 mmHg) screened by Goldmann's applanation tonometer in ophthalmology department, were included in the study. They were prescribed tab. amlodipine 5–10 mg/day by the physician depending upon the severity of hypertension. Patients were followed up every week for four weeks to monitor BP control. IOP was repeated at the end of 4 weeks.

Results

The mean basal IOPs of these individuals were 22.3 ± 1.0 mmHg in left and 21.8 ± 2.2 mmHg in right eye. After four weeks of treatment with amlodipine, the mean IOP reduced to 19.3 ± 1.8 mmHg and 18.7 ± 2.0 mmHg in left and right eye respectively in addition to significant blood pressure (BP) reduction. Analysis of IOP and blood pressure changes before and after the treatment with amlodipine, were done by paired “t” test. “t” value was found to be 9.70 and 7.14 for left and right eye respectively with the ‘p’ value of <0.001. This shows the significant oculohypotensive effect of oral amlodipine in hypertensive patients with increased IOP.

Conclusion

The present study has shown that, oral amlodipine, not only reduces BP but also acts as oculohypotensive agent in hypertensive patients with increased IOP.

The aim of this work was to estimate the total phenolic and flavonoid content, and to evaluate in-vitro antioxidant activity of flavonoids rich extract of Cassia auriculata Linn. (CAF) saponins rich extract of C. auriculata Linn. (CAS) which belongs to the family Caesalpiniaceae. Total phenolic content in CAF was found to be 67.32 μg/mg of extract calculated as gallic acid equivalent (r² = 0.976) and total flavonoids compound was found to be 31 μg/mg of extract calculated as rutin equivalent (r² = 0.985). The extract was screened for its potential antioxidant activities using tests such as DPPH free radical scavenging activity, reducing power activity, and hydrogen peroxide-scavenging activity. The in-vitro antioxidant assay showed that both CAF as well as CAS posses antioxidant activity. So C. auriculata Linn. could be useful for preparation of neutraceuticals as potent antioxidants, to treat various human diseases and its complications.

Objective

To explore the phytochemical constituents present in the leaves of Madhuca longifolia (Koenig) Linn using GC–MS and HPTLC analysis.

Method

The shade-dried leaves of M. longifolia were extracted with ethanol, the concentrated ethanolic extracts were further subjected to GC–MS. The dried powdered leaves were taken in 50% aqueous alcohol and was refluxed, filtered and dried and used for HPTLC analysis.

Results

The fluorescent band (under 254 nm and 366 nm) at R_f 0.67 in mobile phase Toluene:Ethyl acetate:Formic acid (5:4:1) was found and the marker compound Quercetin was quantified. In GC–MS analysis about twenty bioactive compounds were identified that include the presence of phenolic acids, ketones, aldehydes, carbohydrates, heterocyclic compounds and hydrocarbons.

Conclusion

The results of the present study enhance the traditional use of M. longifolia which possesses several known and unknown bioactive compounds, which may be used as an effective source against various diseases.

Objective

The aim of the present study is to investigate the antioxidant potentiality of Bacopa monniera through the synthesized gold nanoparticles (BmGNPS). The antioxidant activity of BmGNPS was evaluated in mice by assessing the oxidative stress induced by aluminum.

Method

Male albino mice were randomly divided into five groups. First group was treated as control, second group received aluminum acetate (5 mg/kg b.w), third group received B. monniera extract (5 mg/kg b.w), fourth group received BmGNPs (5 mg/kg b.w), fifth group received aluminum acetate plus BmGNPs. The lipid peroxidation (TBA-RS) levels and antioxidant enzymes such as superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidise (GPx) activities were estimated in brain, liver and kidney of albino mice.

Results and discussion

Exposure to Aluminum acetate (Al) significantly increased the lipid peroxidation (TBA-RS) levels, with a significant decrease in the antioxidant enzymes such as superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidise (GPx) activities, which may be due to the oxidative stress induced by the release of free radicals. No significant changes were observed in the BmGNPs alone treated mice when compared to control, whereas synchronous administration of BmGNPs to Al treated mice showed a significant decrease in TBA-RS levels and increase in SOD, CAT and GPx activities these results reveals the potential free radical scavenging property of BmGNPs.

Conclusion

This study suggests that the BmGNPs has the ability in counteracting Al induced oxidative stress in male albino mice.

The multicomponent reactions (MCRs) are emerging as environmental benign synthetic methods of building-up of complex molecules with maximum complexity and several level of structural diversity for diverse applications. This review article provides an overview of recent progress in MCRs of synthesis of pyrimidine derivatives covering only recent literature.