Volume 6 - Issue 4

S.NO Title & Authors Name page
1
Feedback of pharmacy students toward teaching-learning pharmacology in Northern Cyprus
Sonia SANAJOU, louai Mohammad ALSALOUMI, Bilgen BASGUT
 Abstract                  View                 Download                 XML

This study explores pharmacy students’ feedback on teaching–learning methods of pharmacology in faculties of pharmacy in Northern Cyprus universities. 150 students randomly selected and participated by filling self-administered questionnaires. The majority of participants were female and most of them were in the 4th year of their study. The results showed that high percentage of students had good understanding and grasping of pharmacology subjects in class, and the pharmacology is the most favored course in comparison with others. Moreover, participants taught that pharmacology course will have most usage in their future pharmacy practice. It can be concluded that the general attitude of students toward pharmacology were positive; however, some changes in curriculum are still required in order to make the pharmacology courses more interesting.

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2
Effect of cyclodextrin on postprandial blood glucose and triglycerides
Mitsuki Sugahara, Yutaka Inoue, Isamu Murata, Daisuke Nakata, Keiji Terao, Ikuo Kanamoto
 Abstract                  View                 Download                 XML

This study explores pharmacy students’ feedback on teaching–learning methods of pharmacology in faculties of pharmacy in Northern Cyprus universities. 150 students randomly selected and participated by filling self-administered questionnaires. The majority of participants were female and most of them were in the 4th year of their study. The results showed that high percentage of students had good understanding and grasping of pharmacology subjects in class, and the pharmacology is the most favored course in comparison with others. Moreover, participants taught that pharmacology course will have most usage in their future pharmacy practice. It can be concluded that the general attitude of students toward pharmacology were positive; however, some changes in curriculum are still required in order to make the pharmacology courses more interesting.

13-19
3
Evaluation of the Anti-cancer Activity of most potent Ethanolic fraction of Prunus avium on EAC Cells in RPMI 1640
Lopamudra Roy, Mounamukhar Bhattacharjee
 Abstract                  View                 Download                 XML

Our present study aims to determine the most potent fraction of ethanolic extract of Prunus aviun as well as to evaluate the anticancer activity of most potent fraction on EAC cells in long time incubation (by using RPMI 1640 media). Ethanolic extract of the fruit was prepared by using maceration (70% C2H5OH + 30% H20) for 10 days followed by solvent evaporation by rotary vacuum evaporator. Most potent fraction was determined by fractionation by using Chloroform, n-butanol and ethyl acetate followed by qualitative and quantitative analysis. Most potent fraction was introduced into fresh collected and sufficiently diluted EAC cells to check the cell viability under microscope by using RPMI 1640 medium. Results of fractionation shows ethyl acetate fraction is probably most potential fraction due to presence highest amount of flavonoid and phenolic compounds than the other fractions. On addition of ethyl acetate fraction to fresh collected and diluted EAC cells, it shows IC50 values 43.03 ± 0.54 µg/ml, 34.62 ± 0.21 µg/ml and 26.94 ± 0.22 µg/ml respectively on 2 hr, 4hr and 8 hrs of incubation by using RPMI 1640 medium. Results indicates that the ethyl acetate fraction of ethanolic extract of Prunus avium is the most potential fraction and it has good anti-cancer activity in long time incubation as well. Still future studies can be performed to isolate the bioactive principles.

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4
CO-CRYSTAL CHARACTERIZATION OF NICOTINAMIDE AND UREA
Yutaka Inoue, Hirotaka Onoda, Hiroyasu Sato, Isamu Murata, Ikuo Kanamoto
 Abstract                  View                 Download                 XML

Aim of this study, a co-crystal (nicotinamide and urea) was prepared, and it was used to investigate the relevance of single-crystal structure analysis in combination with other measurement techniques. Results of both single-crystal X-ray diffraction and powder X-ray diffraction confirmed that the nicotinamide and urea co-crystals had a molar ratio of 2/1 and comprised a monoclinic system. Results of differential scanning calorimetry showed that the melting point of the co-crystals was different from that of nicotinamide and urea alone. Results of Fourier transform infrared (FT-IR) absorption spectrometry showed that the co-crystals interacted between nicotinamide and urea due to amino group. Scanning electron microscopy results showed that the co-crystal and nicotinamide and urea alone have different appearances. Thus, the combination of single-crystal structure analysis with other measurement methods is very useful for analyzing the crystal structure in detail.

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DEVELOPMENT OF A LIQUID CHROMATOGRAPHIC METHOD FOR PHARMACOKINETIC STUDIES OF TOLTERODINE TARTRATE ORODISPERSIBLE TABLETS IN RATS
Y Padmavathi, Sumedha Kapre, K Latha, Renuka Menda, Rohini Kagithala
 Abstract                  View                 Download                 XML

A selective and high throughput reverse phase liquid chromatographic method was developed for studying pharmacokinetics of tolterodine tartrate (TT) orodispersible tablets (ODT) in rats. Quantification is achieved by the peak-area ratio method with reference to the internal standard. Metaxalone was used as internal standard. After liquid- liquid extraction the analyte and the internal standard were chromatographed on Enable 18H (5µ, 250×4.6mm) C18 column. Mobile phase used consists of phosphate buffer pH 3 and acetonitrile (55:45 %v/v). The elute was monitored with the UV–VIS detector at 280 nm with a flow rate of 0.8 mL/min. The peaks of the drug and IS were obtained at retention times of 6.74 min and 10.5 min respectively. The method was validated according to USFDA guidelines. The absolute recovery of analyte was consistent and reproducible. The method was successfully applied to study the pharmacokinetics of tolterodine tartrate orodispersible tablets in rats.
 

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ANTIOXIDANT, BRINE SHRIMP LETHALITY AND ANTIMICROBIAL ACTIVITIES OF DIFFERENT EXTRACTS OF GALPHIMIA GRACILIS BARTL. STEM USING IN VITRO ASSAY MODELS
Md. Rakib Hasan, Nizam Uddin, Md. Monir Hossain, Sabiha Begum, Arjyabrata Sarker, D. M. Jakaria, Md. Emtiaz Yousuf, Md. Sohel Rana
 Abstract                  View                 Download                 XML

Galphimia gracilis Bartl. (Family- Malpighiaceae) is known as gold shower and available almost everywhere in Bangladesh. This plant has some medicinal properties and is used as a source of vitamins. The current study was designed to evaluate in vitro antioxidant, brine shrimp lethality and antimicrobial activities of methanol (GSM), ethyl-acetate (GSEA) and petroleum ether (GSPE) extracts of G. gracilis stem. In vitro antioxidant activity of the extracts were studied using DPPH radical scavenging assay, NO scavenging assay, total phenol, total flavonoid content, total antioxidant capacity, total tannin content and lipid peroxidation in human erythrocyte cell assays. Lethality bioassay was performed on Artemia salina Leach nauplii. Antimicrobial activity was investigated by disc diffusion technique. Presence of alkaloids, carbohydrates, flavonoids, steroids, terpenoids, tannins, saponins and glycosides were identified in the extracts. Ethyl-acetate extract showed highest activities in DPPH (IC50 22.82±0.172 µg/ml), NO (IC50 72.886±0.394 µg/ml) and total antioxidant assay (210.86±3.436 mg/gm Ascorbic Acid Equivalent). Methanol extract showed highest content in total phenol (972.02±4.56 mg/g Gallic Acid Equivalent), total flavonoid (135.98±1.103 mg/g Quercetin Equivalent) and total tannin content assays (111.454±1.462 mg/g Tannic Acid Equivalent). Ethyl acetate extract showed promising reducing capacity than other extracts in cupric reducing (correlation coefficient r= 0.99 and P<0.01) and reducing power capacity assays (r= 0.99 and P<0.001). Besides, it showed dose dependent activity in both assays. In brine shrimp lethality bioassay, methanol extract was found to be more potent than other extracts (LC50=58.583 µg/ml, ?2=170.967, P<0.001). In disk diffusion technique methanol extract showed highest zone of inhibition against maximum number of microorganisms Staphylococcus aureus, Salmonella typhi, Salmonella abony and Pseudomonas aeruginosa (6.75±0.353 mm). The present findings suggest that the stem extracts of G. gracilis can be used as a source of potential candidates for lead compounds.

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A PROSPECTIVE STUDY ON ADVERSE DRUG REACTIONS IN A TERTIARY CARE HOSPITAL
Sindhoosha Malay, Shanmukhi.C, Rashmitha.G, Shravani.V, Venugopal.M
 Abstract                  View                 Download                 XML

The aim of the present study was to detect and analyze the adverse drug reactions (ADRs) of antibiotics and other drugs in a tertiary care hospital. A total of 61 ADRs were reported during the study period with male predominance (51.85%) and geriatric age group. Number of ADRs was reported more from General Medicine (45.90%) and ICU (21.31%) departments in which the most affected organ systems were the GIT (34.42%), skin (18.03%) and Central Nervous System 7(11.47%). The class of drugs most commonly associated with the reported ADRs was antimicrobials 20(32.75%). The severity assessment revealed that most of them were mild level 1 (32.78%) followed by moderate and severe reactions. Of the reported reactions 57.37% of ADRs were definitely preventable, 29.50% of ADRs were probably preventable and 13.11% were not preventable. The study concluded that ADRs to antibiotics are common and less compared to other studies. Proper monitoring and reporting can ensure drug safety profile of drug.

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RP-HPLC ANALYSIS FOR SIMULTANEOUS DETERMINATION OF RABEPRAZOLE SODIUM AND DOMPERIDONE FROM TABLET AND BULK DRUG BY INTERNAL STANDARD METHOD
Seema A. Gosavi, Rasika D Bhalke, Girija B. Bhavar, Atul A. Shirkhedkar, Sanjay J. Surana
 Abstract                  View                 Download                 XML

A specific and sensitive high-performance liquid chromatographic method for the simultaneous determination of rabeprazole sodium and domperidone in bulk drug and capsules was developed. Ranitidine hydrochloride was used as an internal standard. Separation of the drugs was carried out on the Luna C18 (5µ, 250 mm X 4.60 mm i.d.) at ambient temperature using a mobile phase consisting of ammonium acetate buffer pH 7.4 and acetonitrile (60:40 v/v). Flow rate was 1.0 ml/min with an average operating pressure of 158 kg/cm2. Quantitation was achieved with UV detection at 286 nm based on peak area with linear calibration curves at concentration ranges 10-50 µg/ml and 15-75 µg/ml for rabeprazole and domperidone, respectively. The method has been successively applied to pharmaceutical formulation. No chromatographic interference from the capsule excipients was found. The method was validated in terms of precision, robustness, recovery and limit of detection and quantitation.

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ASSESSMENT OF HOMOEOPATHIC PREPARATION OF SULPHUR WITH THE HELP OF U.V SPECTROSCOPY
Dr. Parth Aphale, Dr. Atul Balasaheb Rajgurav
 Abstract                  View                 Download                 XML

Spectroscopy is a technique that uses the interaction of energy with a sample to perform an analysis. The data that is obtained from spectroscopy is called as a spectrum. A spectrum is nothing but a plot of the intensity of energy detected versus the wavelength of the energy. Often, spectra are used to identify the components of a sample (Qualitative analysis). Spectra may also be used to measure the amount of material in a sample (Quantitative analysis). The main aim of this study was to judge the efficacy of U.V. Spectroscopy in differentiating different potencies of the same medicine. [1]. 3 centesimal scale of potencies of sulphur were selected namely 30, 200 and 1M/1000. It was observed that the UV trans-mission for homeopathic preparations of Sulphur was significantly different for different potencies of Sulphur that were tested which was evident from  ?max.

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10
UPLC METHOD VALIDATION FOR 3-ACETYLPYRIDINE CONTENT IN RISEDRONIC ACID
Sagar VLN, Sharma GVR, Omprakash G, Bharat KB
 Abstract                  View                 Download                 XML

An Ultra Performance Liquid Chromatography (UPLC) impurity profile method for the Risedronic acid monohydrate was validated in the present work. The validation method utilizes an Inertsil C-8 (100X4.6 mm), 5µ column at 50°C temperature, isocratic elution with aqueous sodium phosphate buffer at pH 7.5±0.05 and methanol as the mobile phase. The mobile-phase flow rate was 0.40 mL min–1. The linearity, method precision, method ruggedness, limit of quantitation and limit of detection of the impurity profile UPLC method are found to be satisfactory. This study showed that 3-acetylpyridine peak was well resolved from the other known impurities and Risedronic acid monohydrate, the purity angle of 3-acetylpyridine is less than the purity threshold and there is no blank interference at the retention time of 3-acetylpyridine peak. Therefore the method is determined to be specific, as judged by resolving 3-acetylpyridine content in Risedronic acid monohydrate by UPLC.

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EVALUATION OF ANTIBACTERIAL ACTIVITY OF CUSCUTA REFLEXA ROXB.
Deepti Gulati and Abhinav Mishra
 Abstract                  View                 Download                 XML

In the present study antibacterial activity of methanolic extract of stem of Cuscuta reflexa Roxb. was evaluated against Gram positive bacteria like Bacillus subtilis, Staphylococcus aureus and Gram negative bacteria like Escherichia coli, Pseudomonas aeruginosa. Extract was poured into the wells of sterile Mueller hinton agar plates and antibacterial activity was determined by agar diffusion assay. The plates were observed for the inhibition of bacterial growth that was indicated by a clear zone around the wells. The size of the zones of inhibition was measured and the antibacterial activity was expressed in terms of average diameter of the zone of inhibition in millimeters. The results showed remarkable inhibition of growth for the tested organisms. More activity was observed against Gram negative bacteria (Pseudomonas aeruginosa) as compared to Gram positive bacteria.
 

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SYNTHESIS AND EVALUATUION OF SOME NOVEL MERCAPTOBENZIMIDAZOLE DERIVATIVES
Pratik P Maske, Sunil Nalavade, Satheesh Patil
 Abstract                  View                 Download                 XML

A new class of potentially biological active mercaptobezimidazole derivatives containing Benzimidazole moiety has been synthesized. New series of acids and aldehyde substituted benzimidazoles A6–10 were synthesized by the Schiff’s Base method. Synthesized compounds A6–10 were confirmed by IR, 1H NMR, Mass and elemental analysis and further screened for antimicrobial activity and antiprotozoal activity. The in vitro antibacterial and antifungal potential of the products were also determined using bacterial strains.( E.coli ATCC 25922, S.Aureus ATCC 29213, P.aeruginosa MTCC741, C.albicansATCC 9025, A.nigerATCC 1015) The synthesized compounds exhibited significant antimicrobial & antiprotozoal activities compared to standard compounds.

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CONSUMPTION OF ARTIFICIAL SWEETENERS: BOON OR BANE
Anusha T, Ashritha D, Kiranmai M, Uma Rajeswari B
 Abstract                  View                 Download                 XML

Artificial Sweeteners (AS) having low/non-calorific value are among the most widely used food additives worldwide and also regularly consumed by lean and obese individuals alike. AS consumption is considered safe and beneficial owing to their low caloric content, yet supporting scientific data remains sparse and controversial. The objective of the present study was to review whether consumption of artificial sweetners is boon or bane to human health. It has outlined the health effects of AS with respect to their association with weight gain and other metabolic health effects. Consumption of AS in the form of carbonated beverages may cause excessive weight gain. A case control study reveals the fact that AS can induce glucose intolerance by altering gut microbiota associated with the development of metabolic syndrome such as type 2 diabetes. In conclusion, sugar based sweeteners have long been suspected as the cause of obesity and consequent cardiovascular risk.
 

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STABILITY INDICATING RP-HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF PIOGLITAZONE HYDROCHLORIDE AND ALOGLIPTIN BENZOATE IN PHARMACEUTICAL FORMULATION
T. Hemant Kumar and D. Gowri Sankar
 Abstract                  View                 Download                 XML

A simple, efficient, sensitive and stability indicating RP-HPLC method was developed and validated for the simultaneous estimation of Pioglitazone HCl and Alogliptin Benzoate in pharmaceutical formulation using Enable C 18G   column (250 ×4.6 mm, 0.5 µm) with mobile phase consisting of acetonitrile and 0.01M Ammonium acetate (pH 4.0 adjusted with acetic acid) in the ratio of 60:40 %v/v at a flow rate of 0.8 mL/min .UV detection was carried out at 269 nm. The retention time for Pioglitazone HCl and Alogliptin Benzoate were found to be 4.611 and 4.153 min respectively. The proposed method was validated for linearity, range, accuracy, precision, robustness, LOD and LOQ. Linearity was observed over a concentration range 5-220 µg/ml for Pioglitazone HCl and 15-175 µg/ml for Alogliptin Benzoate. Pioglitazone HCl and Alogliptin Benzoate were subjected to stress conditions of degradation including acidic, alkaline, oxidative, thermal and photolysis. The developed method was found to be precise and robust for the simultaneous estimation of Pioglitazone HCl and Alogliptin Benzoate in pharmaceutical formulation.

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FORMULATION AND IN VITRO EVALUATION OF GASTRO RETENTIVE NON EFFERVESCENT TABLETS OF BALOFLOXACIN
Swaroopa Arvapalli*, D. Swapna, MD Faizal, K. Rajashekar, J.V.C. Sharma
 Abstract                  View                 Download                 XML

The purpose of present investigation was to develop and evaluate gastroretentive drug delivery system of fluoroquinolone antibiotics (Balofloxacin). These floating tablets were prepared with the objective to obtain site-specific drug delivery and to extend its duration of action. More over the non effervescent system of balofloxacin will provide increased local and systemic action in stomach. Floating non-effervescent tablets were formulated by various materials like hydroxypropyl methylcellulose HPMC (K 15M, E50), Xanthum gum, Guar gum, Carbopol 976P, polypropylene foam powder were used. All the formulations were evaluated for floating properties, swelling characteristics and drug release studies.  In  vitro drug release studies were performed and drug release kinetics evaluated using the linear regression method was  found  to  follow  zero order release  and  super case 2 transport diffusion mechanism.  The floating lag time were found to be significantly increased with the increasing concentration of the polymers. After the dissolution study of prepared balofloxacin non-effervescent floating tablet was concluded that the formulation NF9 with HPMC K15 and carbopol 976P show best controlled release effect (98.24%). The release kinetic data implies that the release mechanism of all the formulations was Zero order kinetics and super case 2 transport mechanism. The developed floating tablets of balofloxacin may be used to prolong drug release for at least 12h, thereby improving the bioavaibility and patient compliance.

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In vitro α-amylase inhibition effect of ethanol extract of Alpinia nigra (Gaertn.) leaves and molecular docking, ADME/T property studies of some of its isolated compounds.
Mohammad Shah Hafez Kabir, Syed Mohammed Tareq, Mohammad Nazmul Islam, Bishwajit Guha, Rahul Mutsuddy, Md. Mazharul Islam, Mohammad Hossain, Mohammed Shamim hasan, Arkajyoti Paul, Abul Hasanat
 Abstract                  View                 Download                 XML
The present study aims to investigate the α-amylase inhibition of ethanol extract of Alpinia nigra (EEAN) (Gaertn.) leaves by modified enzyme inhibitory action and in silico molecular docking used for five phytoconstituents namely α-fenchyl acetate, α-pinene, α-terpineol, camphene, camphor isolated from A. nigra, to identify whether these compounds interact with the responsible protein (α-amylase enzyme). And also ADME/T properties of the phytoconstituents were analyzed using Qikprop 3.2 module. EEAN had good α-amylase inhibitory activity (IC50 = 1.803±0.032 mg/ml) as compared to Acarbose. A wide range of docking score found during molecular docking by Schrodinger. α-fenchyl acetate, α-pinene, α-terpineol, camphene, camphor showed the docking score -3.938, -3.344, -3.291, -3.463, -3.547, respectively. Among all the compounds, α-fenchyl acetate showed highest docking score. So, α-fenchyl acetate is the best compounds for α-amylase inhibition, as it possessed higher value in Molecular docking. From the ADME profiles of all the tested compounds, it cleared that they might safe for human. Further in vivo investigation need to identify whether isolated compounds from A. nigra have α-amylase inhibitory activity or not.

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Calculation of predominant drug release mechanism using Peppas-Sahlin model (substitution method): A linear regression approach
B. Ravindra Babu and K. Naveen Babu
 Abstract                  View                 Download                 XML
The objective of this study was to develop NCRD controlled release floating tablets using combination of hydrophilic and hydrophobic polymers by melt granulation technique. The in vitro drug release characteristics were determined using USP XXII type 2 (paddle type) apparatus, in a medium of 0.1N HCl. The dissolution profile of all the batches were extended up to 24 hrs. To study and model the drug delivery from polymeric floating tablets, the dissolution data was fitted to a pioneered method Korsmeyer-Peppas equation. The results indicate that, all the formulations followed super Case-II release mechanism, except MCS4 which followed non-Fickian or anomalous release mechanism. In order to determine the predominant mechanism (diffusion/ relaxation model), drug release data was incorporated into Peppas-Sahlin model. The results revealed that, Fickian release contribution was preponderance than corresponding Case-II relaxational contribution in all the formulations. In addition to this, the relaxational contribution was observed with negative sign in all the formulations but, only at specific time intervals. Relaxational contribution with negative values indicates the Fickian release mechanism was more pronounced than relaxation i.e. almost the relaxational mechanism was absent.
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DEVELOPMENT AND VALIDATION OF STABILITY INDICATING RP-HPLC METHOD FOR THE SIMULTANEOUS ESTIMATION OF METFORMIN HYDROCHLORIDE AND EMPAGLIFLOZIN IN BULK AND IN A SYNTHETIC MIXTURE
C. Rupasi Pratyusha, M. Bhagavan Raju
 Abstract                  View                 Download                 XML

The purpose of the investigation was to develop a simple, rapid and accurate RP-HPLC method to determine assay of Metformin Hydrochloride And Empagliflozin in Bulk and synthetic mixture. The chromatographic separation was performed on Kromosil 250 x 4.6 mm, 5µm. Eluents were monitored on PDA detector at a wavelength of 233 nm using a Buffer: Acetonitrile (45:55v/v). The column temperature was maintained at 30°C. Validation parameters such as system suitability, linearity, precision, accuracy, specificity, limit of detection (LOD), limit of quantification (LOQ), Stability of sample and standard stock solutions and robustness were studied as reported in the ICH guidelines. The retention time for Metformin Hydrochloride And Empagliflozin was 2.270 min and 3.413 min  respectively. Assay method further evaluated for Metformin Hydrochloride and Empagliflozin   analysis at low concentration of analyte and found limit of detection is 0.48 and 0.016 ppm respectively and limit of Quantitation is 1.49 and 0.049 ppm respectively. The percentage recovery of Metformin Hydrochloride   And Empagliflozin was 99.64% and 99.47% respectively. The %RSD for Metformin Hydrochloride And Empagliflozin was less than 2. Linearity of Metformin Hydrochloride and Empagliflozin performed from 25% to150% and the R2 is 0.999, intercept and slope found to be y = 26850x + 439840 and y = 47664x + 9394.7 respectively. The method was fast, accurate, precise and sensitive hence it can be employed for routine quality control of Metformin Hydrochloride and  Empagliflozin containing drug in quality control laboratories and pharmaceutical industries.

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Anti-Inflammatory, Anti-Arthritic Activity of Cobalt Derivative of 3-Methoxysalicylaldehyde-2-AminoBenzoylhydrazone in Rats
Imad Uddin MD, Firasat Ali, Parvinder Singh, Chandrashekhar VM, Gudasi KB, Badiger DS
 Abstract                  View                 Download                 XML
This study was piloted to screen anti-inflammatory, anti-arthritic effect of Cobalt (Co) derivative of 3-methoxysalicylaldehyde-2-aminobenzoylhydrazone (AQF). Acute oral toxicity study was conducted according to guidelines OECD-425. Widely accepted carrageenan model was adopted in this study to evaluate Anti-inflammatory effect of Co-AQF. Freunds Complete Adjuvant (FCA) was used for screening anti-arthritic effect and was evaluated by paw edema volume, paw width, paw height, Development of Arthritis (DOA), vascular permeability, release of histamine from blood, Erythrocyte Sedimentation Rate (ESR), Radiographic Analysis and Histopathological assessment. Reference standard Diclofenac Sodium (DS) and Co-AQF have shown significant decrease in all Arthritis evaluating parameters as compared to control group. Pathological changes and histopathological abnormalities which occurred in control group animals were treated with DS and Co-AQF. Hence, based on the results Co-AQF was recognized as anti-arthritic compound and further it can be elucidated at molecular level to establish its potency.
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