Best Paper Awards

IDMA RESEARCH PAPER AWARDS - 2015

In order to encourage R & D in the country, IDMA has instituted “Research Awards for the Best Original Research Papers” published in the “Indian Drugs” every year from the year 1981-82 and the Award for the Best Review Article was instituted in 2001. The Best Original Research Papers are evaluated in the following disciplines:

  • Pharmaceutical Chemistry
  • Natural Products
  • Pharmaceutics
  • Pharmaceutical Analysis
  • Pharmacology

The Best Research PaperAward is in the form of a citation and a cash award of `3000/- in each discipline and the Best Review Article Award is in the form of a citation and special cash award of `5000/-.

These Awards are presented to the recipients during the IDMA Annual Day Celebrations every year.

REVIEW ARTICLE

Paper : Hepatic Targeting – Addressing Vital Therapeutic Needs
Author(s) : D’Souza A.A., Devarajan P.V.
Institute : Institute of Chemical Technology (Elite status) Deemed University, Matunga, Mumbai - 400 019, India
Volume : 52(10)
Page nos. : 7–15
Abstract : Hepatic afflictions continue to pose serious challenges in therapy. The liver exhibits different types of cells, mainly, kupffer cells, sinusoidal endothelial cells, stellate cells and pit cells which represent reticuloendothelial systems. hepatocytes are the non-reticuloendothelial system. While infectious diseases generally affect reticuloendothelial systems, other serious hepatic afflictions are hepatocyteresident. Targeted approaches including passive and active targeting to the various cell types can be employed as an effective strategy to overcome the current challenges. Hepatic afflictions like infectious disease, hepatocellular carcinoma, hepatitis, malaria and others could be target diseases for such improved therapy. Nanomedicine approaches could, therefore, provide a ray of hope for improved therapy of life-threatening hepatic afflictions.

PHARMACEUTICAL CHEMISTRY

Paper : Synthesis, Biological Evaluation, Qsar And Docking Studies Of 2-Amino-5-(Substituted)Phenyl-1,3,4-Thiadiazoles
Author(s) : Mahajan S. S., Gaitonde A. D.
Institute : C. U. Shah College of Pharmacy, S. N. D. T. Women’s University, Santacruz (W), Mumbai - 400 049, Maharashtra, India
Volume : 52(09)
Page nos. : 5–12
Abstract : Ten compounds from the series of 2-amino-5-(substituted)phenyl-1,3,4-thiadiazoles were synthesized and evaluated for anti-inflammatory and analgesic activities. Their structures were characterized by infrared spectroscopy and confirmed by 1 H NMR spectroscopy. Anti-inflammatory activity was carried out by carrageenan-induced rat paw oedema method using indomethacin as standard. Analgesic activity was performed by acetic-acid induced writhing method in mice using aspirin as standard. The QSAR studies were performed for the analgesic activity using the software ‘Strike’ from Schrodinger. Docking studies were carried out for COX-2 inhibition using the software ‘Glide’ from Schrodinger. The compounds were obtained in good yields and possessed good anti-inflammatory and analgesic activities. Various physicochemical parameters, contributing towards analgesic activity were identified from the QSAR studies. The Glide Scores were more or less correlated with the anti-inflammatory and analgesic activities of compounds.

NATURAL PRODUCTS

Paper : Aegle Marmelos Leaf Extract Is Protective Against Experimentally Induced Enterocolitis Via Antioxidant Mechanism
Author(s) : Mani K. G., Prasanna. G. S.
Institute : KLE University College of Pharmacy, 2nd Block, Rajajinagar, Bangalore - 560 010, Karnataka, India
Volume : 52(06)
Page nos. : 5–10
Abstract : Oxidative stress is believed to be a key factor in the pathogenesis and perpetuation of the mucosal damage in inflammatory bowel disease. The investigation was envisaged to assess the protective effect of diethyl ether extract of leaves of Aegle marmelos Corr. (DEAM) in view of reported anti-inflammatory and antioxidant properties in acetic acid-induced enterocolitis in albino Wistar rats. Enterocolitis was induced by intrarectal injection of acetic acid (5% V/V). The study comprised of five different groups consisting of six animals each and two doses [100, 200 mg / kg] were selected. The protective effect in the treatment group of animals was assessed by measuring levels of biomarkers of inflammation [MPO] and oxidative stress [CAT, SOD and GSH] in the inflamed colon and several physiological parameters. Significant and dose dependent changes in the levels of biomarkers of oxidative stress in DEAM treated animals was suggestive of the antioxidant-mechanism protective effect by Aegle marmelos.

PHARMACEUTICS

Paper : Improvement of dissolution rate of febuxostat using hybrid technique of spherical crystallization and solid dispersion
Author(s) : Tandel D. B., Shah P. A., Patel K. G., Gohel M. C., Thakkar V. T. and Gandhi T. R.
Institute : Anand Pharmacy College, Opp. Town Hall, Anand - 388 001, Gujarat, India
Volume : 52(09)
Page nos. : 32-39
Abstract : The present study was carried out with an aim to improve dissolution rate of febuxostat (FBX, BCSclass II) drug. Spherical agglomerates were prepared by hybrid technique of spherical crystallization and solid dispersion using different ratios of FBX and polymer (PVP K30, HPMC E3LV and chitosan). Drug excipient compatibility study was evaluated by Fourier transform infrared spectroscopy and X-ray diffractometry. Scanning electron microscopy was used for measurement of size of agglomerate. In vitro dissolution study of prepared spherical agglomerates was compared with untreated FBX and marketed formulation in phosphate buffer pH 6.8. The ratio of drug to polymer also affected the drug dissolution results. Drug excipient compatibility study showed no interaction between FBX and PVP K30 (1:5) polymer. The use of PVP K30 (1:5) resulted in partial amorphization and improved drug dissolution. Direct compression method can be adopted in manufacturing to simplify the validation efforts. The performance of the formulated product was superior to the marketed product in the in vitro dissolution test.

PHARMACEUTICAL ANALYSIS

Paper : QBD Based RP-HPLC Method For Screening And Analysis Of Telapravir And 7 Other Antiretroviral Gents
Author(s) : Kumar N. S., Kumaraswamy R., Shantikumar S., Paul D.
Institute : National Institute of Pharmaceutical Education and Research [NIPER-Hyderabad] Balanagar, Hyderabad-500 037, India
Volume : 52(02)
Page nos. : 20–33
Abstract : The present study describes the separation and simultaneous estimation of eight anti-retroviral drugs, namely, Telaprevir (TPV), Emtricitabine (ECB), Fosamprenavir (FANV), Tenofavir (TNF), Ritonavir (RNV), Raltegravir (RGV) and Oseltamivir (OSMV) and Zidovudine (ZDV) as an active pharmaceutical ingredient, by RP-HPLC method by applying the principles of Quality by Design (QbD). An application of DoE (Design of Experiments) full factorial design was used for initial screening and optimization. The final optimized method consists of separation being carried out on a Fortis C18 column (150 mm × 4.6 mm, 5μ particle size) using acetonitrile and 10 mm ammonium formate buffer (pH 3 adjusted with formic acid) using a gradient program. The quantitative evaluation was performed with a diode array detector at 251 nm and 230 nm with a flow rate of 1 mL min–1. Suitability of this method for the quantitative determination of the drugs was proved by validation in accordance with the International Conference on Harmonization (ICH) guidelines. The method is selective, precise, robust and accurate and can be used for routine analysis of pharmaceutical formulations in quality control and counterfeit screening.

PHARMACOLOGY

Paper : Curcumin, Ocimum Sanctum and Ginkgo Biloba Improve Hemodynamic, Biochemical and Histoarchitectural Alterations In Isoproterenol Induced Cardiac Damage
Author(s) : Suresh R Naik, Vishnu N Thakare, Vandana S. Panda
Institute : Sinhgad Institute of Pharmaceutical Sciences, Kusgaon (Bk), Lonavala - 410 401, Pune, (MS), India
Volume : 52(04)
Page nos. : 5–14
Abstract : Curcumin, Ginkgo biloba and Ocimum scantum are traditionally used for the treatment of cardiovascular and hepatic disorders. The effects of curcumin, Ginkgo biloba and Ocimum sanctum were studied [acute (4 days) and chronic (60 days)] alone and in combination (60 days) on isoproterenol (ISO) induced cardiac necrosis in rats. The antioxidant related paradigms viz. cardiac malondialdehyde (MDA) formation, and cardiac glutathione, glutathione peroxidase, glutathione reductase, superoxide dismutase, catalase; serum biomarkers, and hemodynamics along with histoarchitecture alterations, were investigated in isoproterenol induced cardiac necrosis in rats. Significant elevation of serum markers; aspartate aminotransferase, lactic dehydrogenase and creatine phosphokinase, increased MDA formation and depletion of antioxidant enzymes along with significant hemodynamic alterations were observed in ISO induced cardiac necrosis in rats. Curcumin, Ginkgo biloba and Ocimum sanctum treatment reversed/ improved serum marker enzymes, elevated MDA, and restored the depleted antioxidants, hemodynamic alterations and histoarchitecture of the heart, both in acute as well as with chronic treatment. However, the combined chronic treatment of curcumin + Ocimum sanctum and Ginkgo biloba + Ocimum sanctum exhibited improvement in both cardiac antioxidants, serum biomarkers as well as hemodynamic and histoarchitecture alterations induced by ISO. Curcumin, Ocimum sanctum and Ginkgo biloba were found to elicit cardioprotective activity on ISO induced cardiac necrosis mainly though amelioration of oxidative stress and membrane stabilizing effect.

IDMA RESEARCH PAPER AWARDS - 2014

In order to encourage R & D in the country, IDMA has instituted “Research Awards for the Best Original Research Articles” published in the “Indian Drugs” every year, from the year 1981-82, in the following disciplines:

  • Pharmaceutical Chemistry
  • Natural Products
  • Pharmaceutics
  • Pharmaceutical Analysis
  • Pharmacology

The award is in the form of a citation and a cash award of `3000/- in each discipline.

These Awards are presented to the recipients during the IDMA Annual Day Celebrations every year.

An Award for the Best Review Article was instituted in 2001. A citation and special cash Award of `5000/- is presented to the recipient at the time of the Annual Celebrations.

REVIEW ARTICLE

Paper : Aloe Vera – Neutraceutical to Pharmaceutical
Author(s) : Mulay S., Bele A., Borade A. and Khale A.
Institute : H.K college of Pharmacy, Pratikshnagar, Oshiwara, Jogeshwari (W), Mumbai
Volume : 51(03)
Page nos. : 5–23
Abstract : Aloe vera has been used for centuries and is presently widely exploited as a nutraceutical. It is available in the form of various health drinks and formulations such as capsules/ tablets or externally in the form of gels & creams. Being a potent immunomodulator, it can be used in various ailments as a single drug or in a combination therapy. The area of formulation research is lacking in understanding the correlation of unique active therapeutic agent acemannan - a glucomannan present in aloe vera and its dose, due to numerous physical, microbiological and biochemical factors interfering in the extraction/ processing of aloe vera juice. Studies are limited and generally becoming complicated because of not having ability to discriminate between different species, since a very few species have a therapeutic effectiveness amongst about 400 species of aloe vera found worldwide. Being sensitive to heat, enzymes and shock, it is a good subject for formulation researchers as there is a concern about aloe products having a little or no aloe in them. The current article is about chemistry of aloe vera in exploring its potential as a mainstay of chronic drug therapy.

PHARMACEUTICAL CHEMISTRY

Paper : Synthesis of Some Novel 1,2,4-Triazole Analogues as Potential Anti-Tubercular Agents
Author(s) : Somani R. R., Shinde G.K., Shirodkar P.Y. and Sanap G.J.
Institute : VES College of Pharmacy, Hashu Advani Memorial Complex, Collector’s Colony, Chembur (E), Mumbai
Volume : 51(01)
Page nos. : 41–47
Abstract : A series of 5-(N-substituted carboxamidoethylthio)-3-(3’pyridyl)-4-amino-1,2,4-triazole derivatives (6a-j) were synthesized and evaluated for anti-tubercular activity. The derivatives were purified and structures were elucidated by spectral and elemental analyses. They were screened in-vitro at 10µg/mL concentration against Mycobacterium tuberculosis H37RV (ATCC 27294). Compounds 6e and 6h were found active as they exhibited IC50 and IC90 values at < 100µg/mL.

NATURAL PRODUCTS

Paper : Quantification of Two Marker Compounds in Gmelina arborea roxb. Stem Bark Using Validated thin Layer Chromatographic – Densitometric Method
Author(s) : Vyas N., Patel M.
Institute : Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology, Charusat Campus, Changa, Gujarat
Volume : 51(11)
Page nos. : 28–35
Abstract : Gmelina arborea Roxb. (Verbenaceae) is known as Gambhari in Ayurvedic System of medicine and being used as immuno-modulator since ancient time. Plant sterols such as β-sitosterol and Lupeol are reported to have such activity. A simple, accurate, precise, rapid and reproducible TLC densitometric method was developed for simultaneous estimation of β-sitosterol and Lupeol in plant stem bark. Compounds were separated on silica gel 60 F254 HPTLC plate using Toluene: Ethyl acetate: Formic acid (8.8:1.3:0.1, V/V/V) using Anisaldehyde-Sulphuric acid as the derivatizing reagent. TLC Analysis was performed at 520 nm. Rf value of β-sitosterol and Lupeol were found to be 0.34±0.02 and 0.46±0.01 respectively. Linearity range was 150-350 ng/spot and 300-700 ng/spot with correlation coefficient 0.998 and 0.999 for β -sitosterol and Lupeol, respectively. Method was validated as per ICH guideline. The accuracy was found to be 100.55-102.86% and 99.40-101.56% for β-sitosterol and Lupeol, respectively by recovery studies. The amount of β-sitosterol and Lupeol was found to be 4.4 mg % and 3.6 mg %. This method can be employed for routine quality control analysis of β-sitosterol and Lupeol in stem bark of Gmelina arborea Roxb.

PHARMACEUTICS

Paper : Self – emulsifying Drug Delivery System containing Aceclofenac: Design & Development using Quality by Design (QbD) Concept.
Author(s) : Suthar V., Gohel M., Butani S. and Solanki A
Institute : L.M. College of Pharmacy, Ahmedabad, Gujarat
Volume : 51(06)
Page nos. : 15–26
Abstract : The aim of the present study was to develop self-emulsifying drug delivery system (SEDDS) of aceclofenac for potential improvement in the in vitro dissolution. The Food and Drug Control Agency (FDCA) has put more stress on the quality, safety and efficacy of the dosage form. The use of design of experiments and quality by Design (QbD) in the development of self emulsifying drug delivery system (SEDDS) containing aceclofenac is demonstrated. The optimum formulation contained Labrafil M 1944 CS, Tween 80 and Transcutol P. The systematic approach enabled us in identifying the design space. The results revealed that while devising the control strategies during manufacturing, more attention should be focused on the ratios of oil to surfactant and surfactant to co-surfactant. The drug was released at a faster rate due to a large surface area. The current approach enabled us to develop a dosage form which is economic, patient-friendly and does not require assistance of a doctor or nurse, especially at remote places at odd hours.

PHARMACEUTICAL ANALYSIS

No award this year

PHARMACOLOGY

Paper : In vitro screening of Lannea coromandelica for Antifilarial Activity on Cattle Filarial Parasite Setaria cervi
Author(s) : Jain V., Kumar T. and Sahu A.
Institute : University Institute of Pharmacy, Pt. Ravishankar University, Raipur, Chattisgarh
Volume : 51(08)
Page nos. : 28–34
Abstract : The current study was aimed to investigate the antifilarial activity of aqueous and ethyl acetate extracts of the leaves of Lannea coromandelica. Both extracts were screened for their total flavonoid content chromatographically. The total amount of flavonoid present in ethyl acetate is much greater than in aqueous extract. Aqueous extract produced initial stimulation effect in whole worm followed by reversible paralysis, whereas on the nerve muscle preparation, the effect was depressant. In the same manner ethyl acetate extract produces irreversible paralysis. The concentrations required to inhibit the movement of the whole worm and nerve muscle preparation for aqueous extract of leaves of L. coromandelica were 300 and 60 µg/mL, respectively, whereas ethyl acetate extract caused inhibition of the whole worm and nerve muscle preparation at 160 and 15 µg/mL, respectively. LC50 and LC90 were 21 and 30 ng/mL, respectively for aqueous, which were 16 and 24 ng/mL for ethyl acetate extracts.

IDMA RESEARCH PAPER AWARDS - 2013

In order to encourage R & D in the country, IDMA has instituted "Research Awards for the Best Original Research Articles" published in the "Indian Drugs" every year, from the year 1981-82, in the following disciplines:

  • Pharmaceutical Chemistry
  • Natural Products
  • Pharmaceutics
  • Pharmaceutical Analysis
  • Pharmacology

The award is in the form of a citation and a cash award of Rs. 2500/- in each discipline.

Awards are presented to the recipients at the time of the Annual Celebrations of IDMA every year.

An Award for the Best Review Article in the form of a citation and special cash Award of Rs. 5000/- is presented at the time of the Annual Celebrations.

REVIEW ARTICLE

No award this year.

PHARMACEUTICAL CHEMISTRY

No award this year.

NATURAL PRODUCTS

Paper : Isolation, Identification and Characterization of Rotenoids from Cajanus cajan (L.) Millsp. (Legueminoseae)
Authors : Chaturvedi P., Khanna P. and Chowdhary A.
Institute : Haffkine Institute for Training, Testing and Research, Parel,Mumbai 400012, Maharashtra, India.
Volume : 50(08)
Page nos. : 27-31
Abstract : Natural insecticides now-a-days have a bright future because synthetic insectides are harmful to humanbeings. Among botanical pesticides, the rotenoids standout for their potency and effectiveness againstmany crop pests and are fifteen times more toxic than the nicotinic acid. Cajanus cajan primarily grownas a grain crop for human consumption (pulse, vegetable) and has not been analysed for its rotenoidalcontent. Chromatographic analysis showed the presence of four rotenoids namely elliptone, deguelin,rotenone and tephrosin, which were identified by co-tlc, melting point, GLC and IR spectral studies withthat of the standard reference compounds. In the present investigation, rotenone (0.37 mg/gdw) wasfound in maximum quantity which was followed by deguelin (0.27 mg/gdw), tephrosin (0.21 mg/gdw)and elliptone (0.15 mg/gdw).

PHARMACEUTICS

Paper : Design, Development and Evaluation of Cationic Guar and Hydroxypropyl guar based In situ Gels for Ophthalmic Drugs Delivery.
Authors : Dasankoppa F.S. and Swamy N.G.N.
Institute : Department of Pharmaceutics, Government College of Pharmacy, P. Kalinga Rao Road, Subbaiah Circle, Bangalore-560027, India.
Volume : 50(01)
Page nos. : 30-41
Abstract : The poor bioavailability and therapeutic response exhibited by the conventional eye drops due to rapidcorneal loss is overcome by the use of ion-activated gel forming systems that are instilled as drops;these undergo gelation in cul-de-sac mode. The present study describes the design, development andevaluation of in situ ophthalmic drug delivery of antibacterial agent, linezolid, based on ion-activatedguar gum derivatives. Novel polymers such as Cationic guar with hydroxypropyl guar are being used asgelling as well as viscosity enhancing agents. Differential scanning calorimetric studies have revealedthat linezolid is compatible with all the excipients in the formulation. The study also aims at rheologicalcharacterization, effect of sterilization (moist heat) and effect of aging on the viscosity of in situ gels bycalculating consistency index (K), flow behaviour index (n value) using power law model. The in vitrodrug diffusion study for the developed formulations has also been carried out. The formulation CGHPG2,exhibiting good physical stability subsequent to sterilization and storage and further retaining theconsistency index (K) and flow behavior index (n value), was chosen as the optimized formulation. Thegel formed in situ revealed the sustained release of the drug for up to 12 hrs. Stability data recordedover a period of 6 months at elevated temperature conditions revealed the formulation to be stable.Invivo ocular toxicity studies revealed non irritant and non toxic nature of the formulation. Therefore, thedeveloped guar gum derivative based ophthalmic in situ gel by virtue of its prolonged corneal residencetime and sustained drug release could be considered a viable alternative to the conventional eye dropformulation in achieving enhanced bioavailability.

PHARMACEUTICAL ANALYSIS

Paper : Forced Degradation Study of Eletriptan by Using Ultra High Performance Liquid Chromatography (UHPLC)
Authors : Sahu S., Singh R.M., Mathur S.C., Sharma D. K. Saini P.K., Duggal D., Tyagi V. and Singh G. N.
Institute : Analytical Research & Development Division, Indian Pharmacopoeia Laboratory, Indian Pharmacopoeia Commission, Ministry of Health & Family Welfare, Government of India, Sec – 23, Rajnagar, Ghaziabad, Uttar Pradesh -201002, India.
Volume : 50(07)
Page nos. : 14-21
Abstract : A simple, fast, precise and accurate ultra high performance liquid chromatography method wasdeveloped for degradation study of eletriptan hydrobromide (EH) under exaggerated conditions.An Inertsil ODS C18 (250 x 4.6 mm, 5?m) column in isocratic mode was used with mobile phasecomprising of water, methanol and trifluoroacetic acid mixed in the ratio 55:45:0.1 % V/V/V,maintained at pH 3.5. The flow rate was set at 0.4 mL per minute with UV detection at 225 nm. Theretention time of EH was found to be 3.7 minutes. Linearity for EH was found in the range of 3.5-200 ?g per mL and percentage recoveries were obtained in the range of 100.2 % to 100.6 %. Themethod was capable of resolving all degradants and principle component in sample. The proposedmethod is accurate, precise, selective, reproducible, and rapid for detection of degradation ofeletriptan hydrobromide.

PHARMACOLOGY

Paper : Evaluation of Anti-diarrhoeal Activity of Punica granatum Stem Bark
Authors : Khan N., Hugar S., Patil V., Nanjappaiah H.M., Gaviraj E.N., and Kalyane N.V.
Institute : Dept. of Pharmacology, B.L.D.E.A’s College of Pharmacy, B.L.D.E. University Campus, Bijapur-586103, Karnataka. India
Volume : 50 (09)
Page nos. : 34-40
Abstract : Evaluation of anti-diarrhoeal effect of Punica granatum stem bark ethanolic extract was carried out on various experimental animal models of diarrhea. Different paragons used were castor oil induced diarrhoea, magnesium sulphate induced diarrhoea, castor oil induced enteropooling and gastrointestinal motility test. The various parameters recorded were onset of diarrhoea, mean number of fecal drops, mean weight of fecal matter, mean weight of small intestine, volume of fluid accumulation in the intestine and mean distance travelled by charcoal meal in the intestine. The test extract demonstrated dose dependent significant anti-diarrhoeal effect. The results of this investigation revealed that, 70% hydroalcoholic extract of Punica granatum stem bark contains pharmacologically active substance(s) with anti-diarrhoeal efficacy.

IDMA RESEARCH PAPER AWARDS - 2012

In order to encourage R & D in the country, IDMA has instituted "Research Awards for the Best Original Research Articles" published in the "Indian Drugs" every year, from the year 1981-82, in the following disciplines:

  • Pharmaceutical Chemistry
  • Natural Products
  • Pharmaceutics
  • Pharmaceutical Analysis
  • Pharmacology

The award is in the form of a citation and a cash award of Rs. 2500/- in each discipline.

Awards are presented to the recipients at the time of the Annual Celebrations of IDMA every year.

An Award for the Best Review Article in the form of a citation and special cash Award of Rs. 5000/- is presented at the time of the Annual Celebrations.

REVIEW ARTICLE

No award this year.

PHARMACEUTICAL CHEMISTRY

Paper : Synthesis, Antimalarial Activity and QSAR Studies of Chalcones, N- Benzylidenesulphonamides and Chalcone Sulfonamides
Authors : More A.H., Raul S.J. and Mahajan S.S.
Institute : C. U. Shah College of Pharmacy, S. N. D. T. Women’s University, Sir Vithaldas Vidya Vihar, Juhu Road, Santacruz (West), Mumbai- 400 049
Volume : 49 (05)
Page nos. : 20 - 34
Abstract : Malaria remains the major cause of human morbidity and mortality worldwide. Malaria, caused by Plasmodium species, is potentially life threatening, increasing in prevalence and becoming even more resistant to in-use drugs. In this article, synthesis of compounds from the series of chalcones, benzylidenesulfonamides and chalconesulfonamides, by the conventional and microwave-irradiation methods is discussed. The microwave-irradiation method was convenient, rapid and high yielding as compared to the conventional method of synthesis. The acute oral toxicity studies indicated that all the compounds were safe for administration up to 2000 mg/kg body weight of a mouse. The compounds were screened for their antimalarial activity. Two chalcones, five benzylidenesulfonamides and three chalconesulfonamides showed antimalarial activity equivalent to chloroquine. Benzylidenesulfonamides showed better antimalarial activity compared to the compounds from the other two series. Chalconesulfonamides showed better antimalarial activity than chalcones. The QSAR studies were carried out by correlating antimalarial activity of all the compounds with their physicochemical descriptors. Validation of the best QSAR model was carried out using the training set and the test set method. These studies provided guidance for the development of novel antimalarials from these series.

NATURAL PRODUCTS

Paper : Effect of Immunomodulatory Herbal Medicinal Preparations on CD4+ Lymphocyte Count and Total Viral Load in HIV- Infected Individuals
Authors : Tharakan S.T., Kuttan G, Kuttan R, Kesavan M., Sr. Austin and Rajagopalan K.
Institute : Amala Cancer Research Center, Amala Nagar, Trissur- 680555, Kerala
Volume : 49 (07)
Page nos. : 42 – 48
Abstract : This study was carried out to determine the effect of herbal medication on the clinical status of HIV infected persons especially on their CD4+ T lymphocyte count and viral load. The toxicity of the medication was also studied. 25 HIV positive individuals were taken for the study. They were treated with a herbal formulation developed in our centre, for one year. Patients were evaluated for their clinical status every month and CD4+ T lymphocyte and viral load every six months. Other parameters assessed were body weight, hematological analysis and hepatic and renal function tests. Body weight was found to be increased in 20 patients out of 25 who have undergone treatment. CD4+T lymphocyte count was increased in 15 patients and viral load was decreased in 20 patients. In six patients viral load was undetectable range. Administration of these medications significantly reduced, elevated interferon-γ and tumor necrosis factor in HIV patients. Medication did not produce any toxicity in HIV patients, as it did not show any significant change in hepatic function, renal function and haematology. Administration of herbal preparation was found to reduce clinical symptoms produced by HIV infection. This herbal formulation was found useful therapeutically for the management of HIV infection and did not produce any toxicity.

PHARMACEUTICS

Paper : Development and Characterization of Elementary Osmotic Pump Tablets for Simultaneous Release of Metformin and Glipizide
Authors : Bharadwaj P., Upaddhyay P.K., Agarwal V., Chaurasia D., Chaurasia H. and Singh R.
Institute : Adarsh Vijendra Institute of Pharmaceutical Science, Babu Vijendra Marg, Gangoh – 247 341, Saharanpur, (U.P.)
Volume : 49 (11)
Page nos. : 19 – 29
Abstract : The aim of present study was to design and evaluate an elementary osmotic pump-based drug delivery system for controlled release of metformin and glipizide simultaneously for treatment of type II noninsulin dependent diabetes mellitus. Inclusion complex of glipizide with β- cyclodextrin was prepared to enhance its solubility. Core tablets were prepared by wet granulation method. Effects of different variables like amount of plasticizer, osmogen, orifice size and dissolution media were studied on release profile for both drugs. Morphology of semi permeable was studied using electron microscope before and after dissolution test. On increasing the amount of osmogen, the release of both drugs was found to be increased. No significant effect of PVP K 30 was observed on drug release. Optimization results indicated that the release of both drugs was directly proportional to the surface porosity of the membrane. It was concluded that the osmotic pump tablets could provide more prolonged and controlled release that may result in an improved therapeutic efficacy and patient compliance.

PHARMACEUTICAL ANALYSIS

Paper : Quantitation of Carvedilol Oxidative Metabolites in Human Plasma using Liquid Chromatography–Tandem Mass Spectrometry
Authors : Valarmathy J., Sudha T., Joshua S.L. and Senthil Kumar K.L.
Institute : Department of Pharmaceutical Analysis, The Erode College of Pharmacy, Erode-638112.
Volume : 49 (02)
Page nos. : 37 - 44
Abstract : A sensitive and efficient method was developed for the determination of carvedilol and its metabolite in human plasma by LC-MS/MS. Plasma samples were hydrolysed with β-glucuronidase and the target compounds were extracted with liquid liquid extraction using diethyl ether in dichloro methane as solvent. The extracts were completely derivatized and analysed by LC-MS/MS. The linearity of the assay ranges from 0.250 ng/mL to 200.0 ng/mL for carvedilol and from 0.500 ng/mL to 30.0 ng/mL for 4-hydroxy carvedilol. The absolute recovery of carvedilol and its metabolite added to blank plasma sample was 70.28 – 82.90%. The reproducibility was from 0.96 to 8.28 for the intraday assay and from 1.65 to 6.09 for the interday assay precision. Repetitive thawing and freezing did not have an affect on metabolite through a minimum of three cycles. Thawed samples remaining in plasma for 4h before extraction were with 5% of theoretical value. Stability of the extracted samples on the auto sampler at room temperature was evaluated for 34 h and was observed to with in 12% of a fresh analytical sample for 4–hydroxy carvedilol. The proposed LC-MS/MS method was effective for the determination of carvedilol and it metabolite in human plasma.

PHARMACOLOGY

No award this year.

IDMA RESEARCH PAPER AWARDS - 2011

In order to encourage R & D in the country, IDMA has instituted "Research Awards for the Best Original Research Articles" published in the "Indian Drugs" every year, from the year 1981-82, in the following disciplines:

  • Pharmaceutical Chemistry
  • Natural Products
  • Pharmaceutics
  • Pharmaceutical Analysis
  • Pharmacology

The award is in the form of a citation and a cash award of Rs. 2500/- in each discipline.

Awards are presented to the recipients at the time of the Annual Celebrations of IDMA every year.

An Award for the Best Review Article in the form of a citation and special cash Award of Rs. 5000/- is presented at the time of the Annual Celebrations.

REVIEW ARTICLE

Paper : Nanotechnology in Drug Delivery: A Review
Authors : Gadad A., Soni A., Dandagi P. and Mastiholimath V.
Institute : Dept. of Pharmaceutics, K.L.E.U’s College of Pharmacy, JNMC, Nehru Nagar, Belgaum-590 010, Karnataka.
Volume : 48 (11)
Page nos. : 5-16
Abstract : The field of nanotechnology is emerging worldwide and there has been tremendous investment in this area with extensive research and development efforts being focused to create new opportunities for advances in drug delivery systems. This review will discuss the various approaches in the design and development of these nanotechnology platforms that bestow such characteristics to nanoparticles. These nano-sized objects, e.g., ‘nanoparticles’, take on novel properties and functions that differ markedly from those seen from items made of identical materials. The small size, customized surface, improved solubility, and multi-functionality of nanoparticles will continue to open many doors and create new biomedical applications. This review will also focus on nanoscale based drug delivery systems that are most prominent and widely studied: hydrogels, polymersomes, nanotubes, dendrimers, quantum dots, nanoshells and nanomicelles. These drug delivery systems can be potentially translated into targeted cellular and tissue-specific clinical applications designed to achieve maximal therapeutic efficacy with minimal side effects.

PHARMACEUTICAL CHEMISTRY

Paper : Synthesis, Characterisation and Computational ADME Studies of Some Novel Analogs of (±)-2-(4-Isobutylphenyl) Propionic Acid
Authors : Velingkar V. S. and Desai D. M.
Institute : Pri. K. M. Kundnani College of Pharmacy, Jote Joy Building, Rambhau Salgaonkar Marg, Cuffe Parade, Colaba, Mumbai-400 005.
Volume : 48 (05)
Page nos. : 23 - 30
Abstract : The clinical usefulness of ibuprofen, a well known nonsteroidal anti-inflammatory drug (NSAID) is restricted by its gastrointestinal side effects like gastric irritation, ulceration and bleeding, sometimes developing into life-threatening conditions. Present work involves synthesis, purification and characterization of a series of (+)-2-(4-isobutylphenyl) propionic acid (ibuprofen) analogs by altering carboxylic acid functional group which is believed to be involved in causing gastric damage by direct contact effect. Synthesized compounds were characterized by advanced spectrometric techniques like infrared (IR), nuclear magnetic resonance (1HNMR) and mass spectroscopy and CHN analysis. The results of all the characterization techniques including melting point determination, thin layer chromatography, IR, 1HNMR, mass spectroscopy and elemental analysis positively confirm the formation of title compounds and correctness of the anticipated structures of the analogs of ibuprofen synthesized. Title compounds were also subjected to insilico ADME (absorption, distribution, metabolism and excretion) predictions using QikProp software and they presented significant values of the ADME properties studied.

NATURAL PRODUCTS

Paper : In Vitro Antidotal Study of Aconite
Authors : Sarkar P. K., Prajapati P. K., Shukla V. J. and Ravishankar B.
Institute : Department of Rasashastra, J. B. Roy State Ayurvedic Medical College & Hospital, 170-172, Raja Dinendra Street, Kolkata- 700004, West Bengal.
Volume : 49 (05)
Page nos. : 41 – 44
Abstract : Aconite is an extremely poisonous drug, but till no specific antidote for aconite poisoning is available. Aconite is used therapeutically in practice of Ayurvedic system of medicine. In various Ayurvedic formulations containing aconite also contain borax as an ingredient; borax is also prescribed in cases of aconite poisoning. In present study, borax was evaluated in vitro as antidote for aconite poisoning. It was found to be an effective chemical antidote for aconite poisoning.

PHARMACEUTICS

Paper : Stabilization of Amorphous form of Poorly Water-soluble drug and hence Solubility Enhancement using Poloxamer-188 and Gelucire-50/13
Authors : Kulthe V. V. and Chaudhari P. D.
Institute : Modern College of Pharmacy, Nigdi, Pune – 411 044, Maharashtra
Volume : 48 (02)
Page nos. : 25 – 37
Abstract : Improving the solubility and dissolution characteristics of potent poorly water-soluble drugs is important to achieve better in vivo performance. Physical transformation of such drug substances into its more soluble, but metastable amorphous form is one of the promising approaches in this direction. The major problem associated with etoricoxib, a selective COX – 2 inhibitor, is its poor aqueous solubility. Thus, it is a suitable candidate to study the enhancement of solubility by solid state modification. However, the underlying metastable tendency of the amorphous form needs to be circumvented to ensure stable formulations of such drug. Thus, the purpose of this work was to study the usefulness of Poloxamer-188 and Gelucire-50/13 in stabilization of amorphous form of etoricoxib by using low drug/excepient ratios such as 1: 0.5, 1: 1 and 1: 1.5. The solid dispersions prepared by rapid solvent evaporation using spray drying technique were subjected to evaluate drug content, residual solvent content (by TGA), molecular interactions (by FT- IR), morphological appearances (by SEM), physical state (by DSC and XRPD), saturation solubility and dissolution rate. Initial study revealed amorphization of etoricoxib by spray drying and significant enhancement in its solubility. Stability study was conducted for 3 months (30 0 +/_ 2 0/ 65 % RH +/_ 5 %) to evaluate physical state and solubility of etoricoxib from optimized proportions of solid dispersions. It highlighted the potential of Poloxamer-188 and Gelucire-50/13 to stabilize amorphous form of etoricoxib in solid dispersions, which was mainly responsible for observing enhanced solubility.

PHARMACEUTICAL ANALYSIS

Paper : Lower Level Determination of Epichlorohydrin Content in Drug Substance by using Dimethyl Sulfoxide as an Internal Standard with Gas Chromatography
Authors : Dubey J. K., Kolhe P. Y., Srivastava B. K., Parmar M., Tandel H., Mehta D. and Prajapati H.
Institute : CTX Life Sciences Pvt. Ltd.251-252 Sachin Magdalla Road, Sachin, Surat-394230, Gujarat.
Volume : 48 (02)
Page nos. : 38 - 42
Abstract : Epichlorohydrin is an extremely versatile chemical intermediate or raw material that is used in a wide variety of drug substances, it can occur in final products at concentration, which are hazardous to human health. This article presents an analytical technique to determine the concentration of epichlorohydrin in final drug substance, in response to the requirements of the drug regulatory, which recommends limiting the concentration to maximum of 75 mcg/g.The instrument platform used for the low-level determination of epichlorohydrin in final drug substance was the Shimadzu gas chromatograph 2010. The typical limit of quantitation of the method determined 4.56 mcg/g and limit of detection was 4.10 mcg/g. The system was successfully calibrated across a working range of 4.56 mcg/g to 10.0 mcg/g with a linear calibration curve.

PHARMACOLOGY

No award this year.

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