Cilnidipine and Valsartan in combined dosage form has been developed and validated. Sample and standard solutions of Cilnidipine and Valsartan were applied to precoated silica gel G 60 F254 HPTLC plates and the plates were developed with Toluene: Methanol: Ethyl acetate: Glacial Acetic acid in the ratio 8:1:1:0.1 (v/v/v/v) as mobile phase. The Rf value for cilnidipine and Valsartan was found to be 0.29 min and 0.56 min respectively. The detection was performed at 240 nm. The calibration curve was found to be linear between 1000 to 6000 ng/band for cilnidipine and 8-48 μg/band for Valsartan with correlation coefficients 0.993 and 0.993 for Cilnidipine and Valsartan respectively. Accuracy and precision of the proposed method was evaluated by recovery studies (% recovery for Valsartan and Cilnidipine was 99.03 % and 99.86 %).The results have been validated statistically as per ICH guidelines. Keywords: Validation, Valsartan, Cilnidipine, HPTLC
A simple, novel, sensitive and precise validated spectrophotometric method was developed for simultaneous determination of Mebendazole (MBZ) and Levamisole Hydrochloride (LVM) in its tablet formulation. 1% H2SO4 in methanol was selected as a common solvent for estimation of MBZ and LVM. For first order derivative method, estimation of MBZ was carried out at 307nm (ZCP of LVM) and of LVM at 232.6nm (ZCP of MBZ). The linearity was obtained in the concentration ranges of 2-6 ?g/mL for MBZ and 3-9 ?g/mL for LVM with correlation coefficient(r2) value greater than 0.995 . The % RSD value for intraday & interday precision were less than 2. The detection limit and quantification limit were found to be 0.44 ?g/mL and 1.34 ?g/mL for MBZ and 0.14 ?g/mL and 0.42 ?g/mL for LVM, respectively. All the validation parameters were performed as per the ICHQ2 (R1) guidelines. The recovery study was carried out, results were 98.82 – 101.93 % for MBZ and 100.05-101.42% for LVM. So, the developed method could be applied for the routine quality control analysis of MBZ and LVM in combined tablet formulation. Keywords: Mebendazole, Levamisole Hydrochloride, First Order Derivatives, ICH guideline, Validation
The morphological changes occurring because of trituration and solid dilution have been assessed by surface electron microscopy to follow medicinally active ingredients and validation of these findings became the objective of the study. Diluted Pharmaceutical agents Silica and Potassium Chloride were analyzed for comparison. The SEM presentation of the biochemic drugs support the idea that it is the unique characteristic change of the virgin drug substances produced because of trituration and solid dilution which is responsible for the changes in medicinal properties. The high intensity electron beam caused multiple fractures on softer molecules which helps distinguishing between lactose and the drug particles. Keywords: Silica, Potassium Chloride, Sugar (Saccharum Lactis, U. S. P.), Diluted Pharmaceutical Drugs, Phase difference, Nano particles
A simple HPLC method has been developed and subsequently validated for the simultaneous determination of Eperisone hydrochloride and Diclofenac sodium. Optimum chromatographic separations among the eperisone, diclofenac sodium and stress-induced degradation products were achieved by using Waters -ODS 5 μ C18 column (250 X 4.6mm) as stationary phase with Acetonitrile and 0.05% TEA pH 3.5 (75:25% v/v) as mobile phase at a flow rate of 1.0 mL min with detection at 273 nm. ICH guidelines were used to validate the developed method. Linearity was established for Eperisone hydrochloride and Diclofenac sodium in the range of 15-75 μg/ml and 10-60 μg/ml, respectively. Eperisone hydrochloride and Diclofenac sodium were exposed to acid, base and neutral hydrolysis, oxidation and photolytic stress conditions and the stressed samples were analyzed by the proposed method. Also the kinetics of degraded sample was evaluated for all the hydrolytic conditions. As the proposed method could effectively separate the drug from its degradation products, it can be employed as stability-indicating method for the determination of instability of these drugs in combined dosage form.
Eight hybridized pyrazolone analogs were designed, docked, synthesized by microwave technique and evaluated for their in-vitro antimicrobial property against four Gram positive, four Gram negative bacterial strains and two fungal strains. Chalcone derivatives of pyrazolone moiety 5a, 5b, 5f, 5g and 5h shows good antibacterial activity aganist Gram positive strains (Percentage zone of inhibition range 68 to 100% with MIC range 12.5-50 ?g/mL) compared with Ciprofloxacin (bacteria) and Clotrimazole (fungal). Compound 5h showed good binding at the active site of the protein with docking score -8.69 and shows hydrogen bonding with Arg 58, Arg 136 and electronic interactions with Asp 34, Glu 38. All other compounds shows mild to moderate activity against all the screened micro-organisms tested. Key Words: Pyrazolone, Antibacterial, Antifungal, Shikimate kinase inhibitor
A series of 5-substituted phenyl-3-(thiophen-2-yl)-4, 5-dihydro-1, 2-oxazoles (2a-l) was synthesized by reacting appropriate chalcones of 2-acetyl thiophene with hydroxylamine hydrochloride in the presence of dry pyridine. The newly synthesized compounds were characterized by IR, 1HNMR, 13CNMR and mass spectral data. All the compounds were evaluated for their antidepressant and antianxiety activities in mice by forced swimming test and elevated plus maze method respectively. Test compounds and imipramine were administered intraperitoneally in antidepressant study at dose of 10 mg/kg. Similarly to study antianxiety activity, test compounds at the dose of 10 mg/kg and diazepam at the dose of 2 mg/kg were administered intraperitoneally. However, preliminary antidepressant screening of compounds (2a-l) revealed that none of the compounds showed antidepressant activity except for compound 2k which moderately (P
Clinical efficacy of topical antifungal therapy depends on the drug ability to penetrate into the stratum corneum (SC) and the duration of treatment. The mechanism of action for antifungal activity of the bifonazole (BFZ) is the inhibition of ergo sterol biosynthesis, an essential step in the membrane formation of fungal cells. BFZ is indicated in the treatment of superficial fungal infections of the skin such as dermatophytoses, cutaneous candidiasis and pityriasis versicolor. Thus, topical gel of bifonazole with increased bioavailability will be favorable for the treatment of fungal infections and symptomatic relief. The objective of the present work is to compare the antifungal activity of BFZ gel formulated using two drug delivery system; micro emulsion and micro sponge drug delivery system. Microemulsion was prepared by oil titration method. Quassi emulsion solvent diffusion-evaporation technique was used for the preparation of micro sponges. The formed micro emulsion and micro sponges are then incorporated into gel. In vitro antifungal activity of micro sponge based gel and micro emulsion based gel was compared using cup plate method. Key words: Topical antifungal, micro sponge, micro emulsion, bifonazole, cup-plate method.
Guillain-Barre syndrome (GBS) is also known as acute idiopathic polyneuritis. It is a neuromuscular paralysis that occurs in all the age groups and has several variants. These include demyelinating polyneuropathy, acute axonal neuropathy, Bickerstaff brainstem encephalitis, pharyngo-cervical-brachial variant, Miller Fisher syndrome and polyneuritis cranialis. Miller Fisher syndrome (MFS) is a rare variant of GBS which is observed only about 1% to 5% of all cases. The incidence of the MFS is more common in males when compared to females by a ratio of 2:1. The lower and upper age groups reported with MFS are 13 and 78 years respectively. Here we report the successful management of rare form of GB syndrome.
Bioinformatics is one of the new and emerging scientific fields which deals in the biological data and established itself an important component in the field of science. Bioinformatics is comprised of a large no of software’s, tools, statistics which helps us to identify the unknown sequence of the gene, DNA, protein or any biomolecule. Bioinformatics is used to find the 3D structure of protein, DNA or any other unknown substance which may or may not have the biological activity. It reduces the cost as well as time to perform the experiment and used in the drug design of the new molecule and to find out the therapeutic activity of molecule. Key words: Bioinformatics, Protein, DNA, Therapeutic activity, Biological activity
The Levosulpiride in bulk and Pharmaceutical formulation was estimated by a validated UV-Visible spectrophotometer method. The ? max obtained for Levosulpiride was 288.1nm in 0.1 N HCl. The drug shows linearity in a concentration range of 6-36µg/ml. The correlation coefficient for standard graph was found to be 0.999. The assay percentage of marketed formulation by the proposed method was good with label claim. The accuracy of the method was checked by recovery experiment performed at three different levels 80%, 100%, 120% and the percentage recovery was in the range 98.00-102.00%. The % RSD found was low which in turn is an indication of the accuracy and reproducibility of the method. Precision study of the method carried out as intra-day, inter-day variations and repeatability which was in good agreement with %RSD. The proposed method was found to be rugged and robust. Hence the above method can be applied for routine analysis of Levosulpiride in bulk and in pharmaceutical dosage form. Keywords: Area under Curve, Levosulpiride, Validation
Metastatic colorectal cancer remains one of the deadliest types of cancer having significant presence globally. Exhaustive research throughout the scientific fraternities worldwide is now getting focused on selectively targeting the cancer cells. One such achievement has been the recent approval of ramucirumab by USFDA which has added to the existing armamentarium of angiogenesis inhibitors. Ramucirumab is a fully humanized monoclonal antibody directed against the extracellular domain of vascular endothelial growth factor receptor 2 (VEGFR-2) which selectively inhibits the human VEGFR-2 with a much greater affinity than its natural ligands and can be used in the second-line treatment of metastatic colorectal cancer. The current review focuses on the details regarding ramucirumab, its journey from preclinical trial to clinical trial and the way forward. Keywords: Colorectal Cancer, Monoclonal antibody, Vascular endothelial growth factor receptor 2, Ramucirumab
Uncontrolled proliferation is the hall mark of cancer and abnormal cell cycle regulation in cancer. CDK plays very important role in the control of the cell cycle and its proliferation. CDK2 is the “superstar” among the CDK family.CDK2 has cyclin A and cyclin E in its complex which the cyclin A complex require to progress through S phase regulated by phosphorylation and cyclin E require to transition from the G1 to S phase in cell cycle. Also, the mechanism of binding of CDK2 with its inhibitors as well as the changes of binding mechanisms following conformational variation of CDK2 are compared. Considering this fact, inhibition or disruption of the CDK2/cyclin complexes should be possible to suppress the hyper activation of CDK2 and hold back the infinite cell proliferation. There are main four binding site of CDK inhibitors. Competitive binding sites (site 1), Noncompetitive binding sites (site 2 and 3), Allosteric binding site (site 4). CDK inhibitors are mainly used in cancers including leukemia, melanoma, solid tumors and other types are being targeted. Keywords: Cancer, CDK, CDK2, CDK2 Inhibitors
Cancer is the biggest question-mark for the medical science. However many effective drugs are available for the cancer treatment, the biggest obstacle is the selective targeting the drug to the cancer cells. Boron Neutron Capture Therapy (BNCT) is a selective therapy of the cancer, it may not affect or affect little to the normal cells, It works on 2 principles - (1)Boron can capture the neutron & getting unstable. (2) Subsequently nuclear fission of boron occurs via emitting radiation. So, Delivered the required dose of boron to the cancerous cells and triggering it with the Neutron beam to this cancer cells which contain the boron, This neutron is capture by the neutron of cancer cells, getting unstable & subsequently nuclear fission is occur, this lethal radiation ultimately kills the cancer cells & normal cells are survive. The nuclear reaction is: 10B + nth ? [11B] ? ? + 7Li + 2.31 MeV The future prospective are to limit the radiation to the cancer cells only & efficiently deliver the Boron to the cancer cell only, also evaluate the other radioactive materials like Gadolinium in place of Boron. Keywords: Cancer, BNCT, Boron, Neutron, Nuclear Fission
Introduction: In an attempt to find potent anti-cancer agents, we performed two-dimensional quantitative structure activity relationship (2D QSAR) studies, on a novel series of 3-thiocyanato-1H- indoles. Method: 2D-QSAR was performed using Vlife MDS 4.3 on a series of 3-thiocyanato-1H-indoles. Result: The statistically validated two-dimensional quantitative structure activity relationship model was obtained through k-nearest neighbors (kNN) method using Vlife molecular design suits (MDS). Statistical data of Model 3 (q2 = 0.8001, pred r2 = 0.4082) correlated with cytotoxicity activity against human cancer cell line (HL60). Validation was done with LOO method. Conclusion: Three descriptors showing positive correlation with the cytotoxicity activity have been included in the model. This validated 2D QSAR model may be used to new more potent anticancer compounds. Keywords: 2D-QSAR; anticancer agents, regression analysis; 3- thiocyanato-1H-indoles; HL60 cell line
The aim of this study was to evaluate the in vitro anthelmintic activity of 2-Arylidene-4-(substituted aryl) but-3-en-4-olides (I-IX) against Indian earthworm i.e. Pheretima posthuma. The anthelmintic activity of nine butenolide derivatives was determined by recording the mean paralyzing and death times of the worms at concentration of 2 mg/mL. The results indicated that few of the tested butenolide derivatives possess significant anthelmintic activity comparable to positive control, albendazole. Keywords: Furanone, Pheretima posthuma, Anthelmintic, Albendazole
Cancer is a class of diseases characterized by out-of-control cell growth. There are so many types of cancer. In case of Women, Breast Cancer ranks second among cancer deaths in women. Approximately 60% of all breast cancer patients have hormone dependent breast cancer, which contains estrogen receptors and requires estrogen for tumor growth. Aromatase, the enzyme responsible for estrogen biosynthesis, is a particularly attractive target in the treatment of hormone-dependent breast cancer. In the present study we have reported the synthesis of some novel Diaryl Derivatives comprising 2-Amino Thiadiazole and Imidazothiadiazole moiety. These moieties are of interest because of structural similarity with the Letrozole, which is the potent Aromatase Inhibitor and their diverse biological activities and clinical applications. We have reported the new series of Letrozole analogues to target Aromatase Enzyme. The reaction was monitored by Thin Layer Chromatography using suitable mobile phase. The Rf values were compared and the Melting Point of the derivatives was determined. It was found that they were different from each others. Further, these derivatives were characterized and confirmed by IR, 1H-NMR, 13C-NMR and Mass Spectral Studies. For Anticancer activity, the selected compounds were submitted to National Cancer Institute (NCI) for in vitro anticancer assay and were evaluated for their anticancer activity. Primary in vitro dose anticancer assay was performed in full NCI 60 Cell panel in accordance with the protocol of the NCI, USA. Compound 1 has a 73.7 % and Compound 4 has a 52.56 % growth Inhibition of Breast Cancer cell lines Keywords: Anticancer, Breast Cancer, Aromatase Enzyme, Letrozole, Thiadiazole, Imidazothiadiazole, NCI-USA
The use of performance enhancing drugs in sports is prohibited by World Anti-doping Agency (WADA).(1) Herbal preparations are usually considered safe due to least side effects but may contain substances which are prohibited in sports. Athletes often take these preparations for therapeutic purpose without considering the risks of an inadvertent doping. A study on the screening of various labelled and unlabelled Indian Ayurvedic herbal preparations to identify the substance of abuse was conducted. A total of hundred and two labelled and sixteen unlabelled herbal Ayurvedic preparations used for different therapeutic indications were tested for screening of approximately one twenty drugs prohibited by WADA. Out of hundred and two labelled herbal preparations, sixteen showed presence of Strychnine. However, out of these sixteen herbal preparations, only four preparations declared presence of strychnine on the label. Strychnine is a stimulant which is prohibited by WADA during in competition testing. Out of sixteen unlabelled preparations, two showed presence of Nicotine. The study shows that the labelled/unlabelled herbal preparations may contain undeclared substances prohibited by WADA. The excretion study showed levels of strychnine above WADA Minimum Required Performance Levels (MRPL) thereby leading to positive dope test. Keywords: Sports, Doping, WADA, Prohibited List, Herbal Preparations, Adulteration
Present work deals with the investigation of corrosion inhibition of mild steel using two expired drugs namely Atenolol and Nifedipine in 1 M HCl solution. Their inhibition properties were evaluated using electrochemical, scanning electron microscopy (SEM) and DFT methods. Atenelol and Nifidipine showed efficiency of 91.30 and 93.91% at low concentration of 200 ppm respectively. Polarization study reveals that the expired drugs inhibit corrosion of mild steel by suppressing both anodic and cathodic reactions occurring on the mild steel surface thus acting as mixed type inhibitors. EIS study shows that the investigated drug increases the polarization resistance by adsorbing on the metal/electrolyte interface. The electrochemical results were well supported by SEM as well as DFT study. Keywords: Expired Drugs, Mild steel, Acid corrosion, SEM, DFT
India is a country which is full of natural recourses on all direction of land such as snow fall on northern India, highest rainfall in northeast, hot desert on west and damp sea air on remaining costal area. Such types of climates are hardly available in any country in the world. Due to all this three seasons are observed in India, like summer, Rainy season, and winter. Because of change in climates there will be sudden growth of microorganism in atmosphere and chances to increase the illness in common people. The illness due to change in season is called as viral infections. Generally viral infections include sneezing, coughing, cold, fever, body ache etc. Depending upon the immunity of individual number of patients are cure within in few days either by oral analgesic, anticold, or basic antibiotics or by simply OTC medicines but few were treated with IV antibiotics. Majority of people complaint with sore throat, patches in throat, because of cold air entered in respiratory tract and produces running nose and irritation in throat. Number of viruses is pathogenic in human being producing a variety of syndromes. In a large majority of the cases, viral infections are not apparent or subclinical; only in some of them is a clinical disease produced. Clinical illness following a virus infection depends upon factors in the virus and the host. The very important factor in a virus is genomic alterations. The factors in the host mostly depend upon the nutritional status and the immune system. The life cycle of a virus starts with its entry into a host; it reaches the susceptible target cell, enters it, replicates and causes cell injury, and may be cell death. At any of these steps the life cycle of the virus can be aborted by various body mechanisms, mainly by the immune response. A single cough can release hundreds of droplets, a single sneeze thousands (up to 40 000) each droplet containing millions of viral particles. Keywords: Viral Infection, Antiviral Drugs, Cold and
The low income countries are having a number of issues related to public health. One such very important issue is the practice of self-medication which is prevalent in such countries. There are multiple factors present in these countries that have led to widespread self-medication. The present article highlights this grave problem prevalent in the low income countries. Keywords: Healthcare information to all by 2015, Low income countries, Non-prescription drugs, Prescription drugs, Self-medication.
