GASTROPROTECTIVE NSAIDs

NSAIDs suffer from a serious drawback of GI-SEs caused particularly after chronic use. There is evidence concerning the participation of ROS in the etiology & pathophysiology of digestive system disorders like GI-inflammation & gastro ulcer. With the aim to retard the adverse effects of GI-Origin, conjugates of NSAIDs (especially the carboxylic acid derivatives) with some antioxidants can be synthesized by esterification with various antioxidants of natural origin. The conjugates that show the retention or potentiating of anti-inflammatory activity with reduced ulcerogenic side effect could be potential gastroprotective co-drugs of NSAIDs. Keyboards: NSAIDs, Gastroprotective, ROS, Natural antioxidants, Conjugates, Ulcerogeni

SYNTHESIS, SPECTRAL, AND PHARMACOLOGICAL EVALUATION OF 3 AND 5 SUBSTITUTED 2,4-THIAZOLIDINEDIONE DERIVATIVES

Background: 2,4-Thiazolidinedione derivatives was launched as antidiabetics in 90's. Later the derivatives of 2,4-thiazolidinedione were banned due to hepatotoxicity. To the date, much research has been directed toward the synthesis and novel uses of 2,4-thiazolidinedione compounds.Aim: The aim of the present study is to synthesize a set of 3,5-disudstituted-2,4-thiazolidinediones as antimicrobial. These compounds were evaluated for their antimicrobial activity.Method: First, the 2,4-thiazolidinedione was substituted at the position of 3 using sodium hydroxide and ethanol and then substituted at the position of 5 in the presence of piperdine by the Knoevenagel condensation method. The structures of the compounds were established on the basis of infrared and nuclear magnetic resonance spectral studies.Result: 3,5-disubstituted-5-benzylidine-2,4-thiazolidinediones derivative was synthesized using benzyl halides and aromatic aldehydes. The results obtained showed that TZ-1 exhibited good activity against Bacillus subtilis while no activity against Escherichia coli.Conclusion: Attachment of more heterocyclic rings containing Nitrogen on the 3rd position of 2,4-thiazolidinedione can enhance the antimicrobial activity. Addition of more lipophilic agents may increase the bioavailability and efficacy of the drug. Long alkyl chains on the benzylidene ring can also increase the lipophilic character, and further attachment of these kind of agents on benzylidene chain may produce safe and effective compounds in future

Review of Journal of Cardiovascular Magnetic Resonance 2009

There were 56 articles published in the Journal of Cardiovascular Magnetic Resonance in 2009. The editors were impressed with the high quality of the submissions, of which our acceptance rate was about 40%. In accordance with open-access publishing, the articles go on-line as they are accepted with no collating of the articles into sections or special thematic issues. We have therefore chosen to briefly summarise the papers in this article for quick reference for our readers in broad areas of interest, which we feel will be useful to practitioners of cardiovascular magnetic resonance (CMR). In some cases where it is considered useful, the articles are also put into the wider context with a short narrative and recent CMR references. It has been a privilege to serve as the Editor of the JCMR this past year. I hope that you find the open-access system increases wider reading and citation of your papers, and that you will continue to send your quality manuscripts to JCMR for publication

PREPARATION AND EVALUATION OF MODIFIED TAMARIND SEED GUM AS A NOVEL SUPERDISINTEGRANT

The aim of present study was to preparation and evaluation of modified Tamarind seed as natural superdisintegrant. The extracted gum from the Tamarind seed was modified chemically by carboxymethylation of extracted gum was done to improve the hydrophilic nature of the gum. Futher, carboxymethylated gum was complexed by using calcium chloride to enhances  the wetting capacity of the gum. The modification in functional group of extracted gum, carboxymethyled gum, Calcium complexed gum was studied by FT-IR spectrophotometer. The DSC studies shows that the changes in melting point of the carboxymethyled gum and the calcium complexed gum as compared to the extracted gum without undergoing chemical modification. The modified gum was then subjected to different studies like color, pH of gum solution, swelling indexetc. The dummy tablet prepared with calcium complexed modified Tamarind seed gum to check its disintegration effect of the tablet. The various pre-compression parameters of the tablet blend was determined like bulk density, tapped density, Carr's index, angle of repose and Hausner's ratio. The disintegration time of these dummy tablet carry the calcium complexed tamarind seed gum was compared to formulate tablet with marketed superdisintegrant i.e. sodium starch glycolate . The disintegration time of calcium complexed Tamarind seed gum was observed to be 1 min. approx. 32.5 sec. -35.2 sec. showing good disintegrating property. It can be concluded that Fast disintegrating tablet using modified Tamarind seed gum as natural superdisintegrant improves the disintegration time of the tablet. Keywords: FDT tablet, Tamarind seed gum, Sodium starch glycolate, Swelling time.&nbsp

HERBS AS TRADITIONAL MEDICINES: A REVIEW

Ayurveda is believed to have originated over 6000 years ago It was designed to promote good health and long life rather than to fight disease and was practiced by physicians and surgeons (called Bheshaja or vaidya) but recently herbal medicine have attracted much attention as alternative medicines useful for treating or preventing life-style related disorders. Herbs are the nature’s gift to human being to make disease free well life. The diverse tradition of India is a prosperous source of traditional medicines, many of which are of plant origin. Herbal medicines refers to the use of any plant’s seeds, berries, roots, leaves, bark or flowers for medicinal purpose. There are different sources of drug. Broadly speaking, there are two sources of drug namely synthetic and natural. Many drugs used in medicine today are developed by chemical synthesis. A recognized number of drugs are obtained from natural sources. The most important natural sources of drugs are (1) higher plants, (2) microbes, (3) animals and (4) marine organisms. Keywords: Ayurveda, Traditional medicines, higher plants, microbes, marine organism

Review of Journal of Cardiovascular Magnetic Resonance 2015

There were 116 articles published in the Journal of Cardiovascular Magnetic Resonance (JCMR) in 2015, which is a 14 % increase on the 102 articles published in 2014. The quality of the submissions continues to increase. The 2015 JCMR Impact Factor (which is published in June 2016) rose to 5.75 from 4.72 for 2014 (as published in June 2015), which is the highest impact factor ever recorded for JCMR. The 2015 impact factor means that the JCMR papers that were published in 2013 and 2014 were cited on average 5.75 times in 2015. The impact factor undergoes natural variation according to citation rates of papers in the 2 years following publication, and is significantly influenced by highly cited papers such as official reports. However, the progress of the journal's impact over the last 5 years has been impressive. Our acceptance rate is <25 % and has been falling because the number of articles being submitted has been increasing. In accordance with Open-Access publishing, the JCMR articles go on-line as they are accepted with no collating of the articles into sections or special thematic issues. For this reason, the Editors have felt that it is useful once per calendar year to summarize the papers for the readership into broad areas of interest or theme, so that areas of interest can be reviewed in a single article in relation to each other and other recent JCMR articles. The papers are presented in broad themes and set in context with related literature and previously published JCMR papers to guide continuity of thought in the journal. We hope that you find the open-access system increases wider reading and citation of your papers, and that you will continue to send your quality papers to JCMR for publication

A review on polymers in natural or modified form used in sustained release tablet

Tablet is a solid dosage form which is used to deliver the drug to the body to make pharmacological action. The oral dosage form should disperse into small particles to deliver active ingredients in the body, the disperse time of the dosage form depends on the ingredients which are used in the tablet. To make the tablet disintegrate slow usually sustained release agents are used. The sustained release tablets helps in maintaining the drug concentration in the body for the higher time. In this review article various polymers of natural origin and their modified forms are studied, which can be used in the sustained release tablet. In this review article the polymers studied were, Psyllium husk, HPMC K100M, Cellulose polymers, Cellulose ether polymers, Xanthan gum, Guar gum, Eudragit RLPO, Eudragit RSPO, Eudragit RL 100, Eudragit RS 100, Kollidone SR and Carnauba wax. Now a day the sustained release tablets are used more than the conventional tablets because of the patient incompliance. The main part of the sustained release tablets are the polymers. In the study it was found that the modified forms of natural polymers works better than in their natural form. In the study it was found that the hydrophilic polymers also work better like Xanthan gum and Guar gum, they are effecting and non-toxic in nature. The cellulose derivatives were studied and it was found that Substituted cellulose-methylcellulose, hydroxypropylcellulose and hydroxypropylmethylcellulose works better in the combination form. Keywords: Sustained release, Xanthan gum, Guar gum, Eudragit, Kollidone, HPM

Formulation and evaluation of sustained release matrix tablet of metoprolol succinate by using xanthan gum and carbopol

Metoprolol succinate is a β1 selective antagonist used as an Anti-hypertensive, Anti arrhythmic, Anti Angina. The aim of present investigation was to develop matrix tablets of Metoprolol succinate using different polymers.Metoprolol succinate matrix tablet was prepared by use of xanthan gum and carbopol-934 as a polymer initially by direct compression methods. Physicochemical compatibility of the drug with polymer was confirmed by IR spectroscopy and DSC. Metoprolol succinate matrix tablets were prepared by direct compression and wet granulation method using different polymers. All the formulations were evaluated for weight variation, thickness, hardness, friability and dissolution. The result of matrix tablets formulation (A-4) showed drug release 94.12% in 720 min. Therefore it was concluded that formulation (A-4) containing carbopol-934 and xanthan gum in the ratio of 80:20 showing promising result for sustained release of Metoprolol succinate, further for improvement of release profile in situ interpolymeric complexes of both carbopol and xanthan gum were tried. All the formulations were evaluated for weight variation, thickness, hardness, friability and dissolution. The results of IPC formulation B-11 showed drug release 96.29% in 720 min. It was concluded that tablets were prepared by using in-situ inter polymer complex formed with 70:30 ratio of Carbopol and Xanthan gum solution as binder. Formulation B-11 showed promising result because of its resistance in pH 1.2 HCL buffer for more than 2 hrs showed the maximum sustained release as compared to simple matrix tablet because of more acid resistance of the complex. Thus, sustained release matrix tablets of Metoprolol succinate using biocompatible polymers were successfully formulated, evaluated and found to be suitable candidates in extending the release of the drug from the matrix tablets. Keywords: Metoprolol succinate, Sustained release Matrix tablets, Direct compression, Wet granulation method.&nbsp

Glioblastoma invasion and NMDA receptors: A novel prospect

Purpose Glioblastoma cells create glutamate-rich tumor microenvironment, which initiates activation of ion channels and modulates downstream intracellular signaling. N-methyl-D-aspartate receptors (NMDARs; a type of glutamate receptors) have a high affinity for glutamate. The role of NMDAR activation on invasion of glioblastoma cells and the crosstalk with α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs) is yet to be explored. Main methods LN18, U251MG, and patient-derived glioblastoma cells were stimulated with NMDA to activate NMDAR glutamate receptors. The role of NMDAR activation on invasion and migration and its crosstalk with AMPAR were evaluated. Invasion and migration of glioblastoma cells were investigated by in vitro trans-well Matrigel invasion and trans-well migration assays, respectively. Expression of NMDARs and AMPARs at transcript level was evaluated by quantitative real-time polymerase chain reaction. Results We determined that NMDA stimulation leads to enhanced invasion in LN18, U251MG, and patient-derived glioblastoma cells, whereas inhibition of NMDAR using MK-801, a non-competitive antagonist of the NMDAR, significantly decreased the invasive capacity. Concordant with these findings, migration was significantly augmented by NMDAR in both cell lines. Furthermore, NMDA stimulation upregulated the expression of GluN2 and GluA1 subunits at the transcript level. Conclusions This study demonstrated the previously unexplored role of NMDAR in invasion of glioblastoma cells. Furthermore, the expression of the GluN2 subunit of NMDAR and the differential overexpression of the GluA1 subunit of AMPAR in both cell lines provide a plausible rationale of crosstalk between these calcium-permeable subunits in the glutamate-rich microenvironment of glioblastoma

PREPARATION OF CONTROLLED RELEASE METFORMIN HYDROCHLORIDE LOADED CHITOSAN MICROSPHERES AND EVALAUTION OF FORMULATION PARAMETERS

In this work an attempt was made for the preparation and evaluation of controlled release chitosan microspheres using anti-diabetes drug Metformin hydrochloride. The microspheres were prepared by Ionotropic gelation method using chitosan as polymer and Sodium Tripolyphosphate (TPP) as crosslinking agent. The compatibility of drug and polymer is analyzed by using FTIR and DSC method. There was no interaction detected by FTIR and DSC study. Further the prepared microspheres were evaluated for particle size, drug entrapment efficiency, surface morphology, drug content, drug loading and in vitro drug release. Amongst all the formulation batch 7 shows the best release when compared to other batch. SEM (Scanning electron microscopy) revealed that microspheres were spherical and porous. Finally it was concluded that Metformin hydrochloride loaded chitosan – TPP microspheres have been found suitable for controlled release formulation due to its bioavailability and biodegradability and thus lead to improved patient compliance. Keywords: Microspheres, Metformin hydrochloride, Ionotropic gelation method, chitosan