Volume: 16  Issue: 1 - 2019
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1.A Validated RP-UPLC Method for the Determination of Gemifloxacin Mesylate in Bulk and its Pharmaceutical Preparation.
Hebatallah A Wagdy, Mohamed Tarek, Ahmed Amer, Menna Gamal, Mohey Elmazar
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INTRODUCTION: Gemifloxacin Mesylate is a fourth generation fluoroquinolone antibacterial agent. A simple, accurate and precise reversed phase UPLC method was developed and validated for short time analysis of Gemifloxacin Mesylate in its bulk and pharmaceutical preparation.
METHODS: The optimum separation was achieved at 0.5±0.03 min using AcclaimTM RSLC 120 C18 column 2.2μm (2.1 x 100 mm) at 30°C by isocratic mobile phase at pH= 3.0 composed of acetonitrile: phosphate buffer (25mM) with ratio 75: 25 (v/v). The column effluents were monitored at 276 nm using photo diode array detector (PDA) at flow rate 0.5 mL/min. The method was validated according to ICH guidelines.
RESULTS: The linearity of the calibration curve ranged from 0.5μg/mL to 10 μg/mL and square of the regression coefficient (r2) was 0.9991. The % RSD of inter-day precision ranged from 0.081% to 1.233%, while for intra-day ranged from 0.364 % to 1.018%. The method was found accurate with % recovery ranging from 93.71% to 100.29 % and % RSD ranged from 1.054 to 2.722. The limit of detection (LOD) and the limit of quantification (LOQ) were 0.066 and 0.2 μg/mL.
DISCUSSION AND CONCLUSION: The validated method proof its ability for the assay of Gemifloxacin mesylate in its bulk and dosage form in short time (less than 1 minute). To the best of our knowledge, this is the first RP-UPLC method for the determination of Gemifloxacin mesylate.
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2.Synthesis and aldose reductase inhibitory effect of some new hydrazinecarbothioamides and 4-thiazolidinones bearing imidazo[2,1-b]thiazole moiety
Nuray Ulusoy Güzeldemirci, Selin Cimok, Net Daş-Evcimen, Mutlu Sarıkaya
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GİRİŞ ve AMAÇ: ÖZ
Amaç: Bu çalışmanın amacı, 2-[[6-(4-bromofenil)imidazo[2,1-b]tiyazol-3-il]asetil]-N-alkil/arilhidrazinkarbotiyoamit ve 3-alkil/aril-2-[((6-(4-bromofenil)imidazo[2,1-b]tiyazol-3-il)asetil)hidrazono]-5-nonsübstitüe/metil-4-tiyazolidinon türevleri’ni sentezlemek, yapılarını aydınlatmak ve aldoz redüktaz inhibitör etkilerini araştırmaktır.


YÖNTEM ve GEREÇLER: Gereç ve Yöntemler: 2-[6-(4-Bromofenil)imidazo[2,1-b]tiyazol-3-il]asetohidrazit (2)’ten hareketle 2-[[6-(4-Bromofenil)imidazo[2,1-b]tiyazol-3-il]asetil]-N-alkil/arilhidrazinkarbotiyoamit (3a-f) ve 3-alkil/aril-2-[((6-(4-bromofenil)imidazo[2,1-b]tiyazol-3-il)asetil)hidrazono]-5-nonsübstitüe/metil-4-tiyazolidinon türevleri (4a-j) sentezlenmiştir. Bileşiklerin yapıları elementel analiz ve spektroskopik bulgularla kanıtlanmıştır. Sentezlenen bileşikler sıçan böbrek aldoz redüktaz (AR) enzimini inhibe etme özellikleri açısından test edilmiştir.
BULGULAR: Bulgular: Sentezlenen bileşikler arasından, 2-[[6-(4-bromofenil)imidazo[2,1-b]tiyazol-3-il]asetil]-N-benzoilhidrazinkarbotiyoamit (3d) en iyi AR inhibitör etkiyi göstermiştir.


TARTIŞMA ve SONUÇ: Sonuç: Bu çalışmanın bulguları, bu çalışmadaki bileşiklerin farklı türevlerinin gelecek araştırmalar için ilginç adaylar olarak görülebileceğini göstermektedir.
INTRODUCTION: ABSTRACT
Objectives: The aim of this study was to synthesize and characterize 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-alkyl/arylhydrazinecarbothioamide and 3-alkyl/aryl-2-[((6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-nonsubstituted/methyl-4-thiazolidinone derivatives and evaluate them for aldose reductase inhibitory effect.


METHODS: Materials and Methods: 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-alkyl/arylhydrazinecarbothioamides (3a-f) and 3-alkyl/aryl-2-[((6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-nonsubstituted/methyl-4-thiazolidinones (4a-j) were synthesized from 2-[6-(4-bromophenyl)imidazo[2,1-b]thiazole-3-yl]acetohydrazide (2). Their structures were elucidated by elemental analyses and spectroscopic data. The synthesized compounds were tested for their ability to inhibit rat kidney aldose reductase (AR).
RESULTS: Results: Among the synthesized compounds 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-benzoylhydrazinecarbothioamide (3d) showed the best AR inhibitor activity.
DISCUSSION AND CONCLUSION: Conclusion: The findings of this study indicate that the different derivatives of the compounds in this study may be considered as interesting candidates for future research.

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3.Antiplasmodial activity of the n-hexane extract from Pleurotus ostreatus (Jacq. Ex. Fr) P. Kumm.
Ozadheoghene Eriarie Afieroho, Xavier Siwe Noundou, Chiazor P Onyia, Osamuyi H Festus, Elizabeth C Chukwu, Olutayo M Adedokun, Michelle Isaacs, Heinrich C Hoppe, Rui WM Krause, Kio A Abo
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INTRODUCTION: Several mushrooms species have been reported to be nematophagous and anti-protozoan.This study reported the antiplasmodial and cytotoxic properties of the n-hexane extract from the edible mushroom Pleurotus ostreatus and the isolation of a sterol from the extract
METHODS: Anti-plasmodial and cytotoxicity assays were done in vitro using the plasmodium lactate dehydrogenase (pLDH) assay and human HeLa cervica cell lines respectively. The structure of the isolated compound from the n-hexane extract was elucidated using spectroscopic techniques.
RESULTS: The n-hexane extract (yield: 0.93 % w/w) showed a dose dependent anti-plasmodial activity with the trend in parasite inhibition of: chloroquine (IC50 = 0.016μg/ml) > n-hexane extract (IC50 = 25.18μg/ml). It also showed mild cytotoxicity (IC50 >100μg/ml; selectivity index >4) compared to the reference drug emetine (IC50 = 0.013 µg/ml). The known sterol: ergostan-5,7,22-trien-3-ol was isolated and characterized from the extract
DISCUSSION AND CONCLUSION: This study reporting for the first time the anti-plasmodial activity of P. ostreatus revealed its nutraceutical potential in the management of malaria.
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4.Microanatomical, Physicochemical characterization, and antioxidative activity of methanolic extract of Oudemansiella canarii (Jungh.) Höhn
Krishnendu Acharya, Sudeshna Nandi, Arun Kumar Dutta
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INTRODUCTION: Oudemansiella canarii, an edible mushroom highly appreciated throughout the world due to its gastronomic delicacy, is admiringly cultivated. Till date, no extensive work has been reported on the pharmacological and antioxidative aspect of this macrofungus. The present study focuses on the micro-morphological features, confirmation of its identity based on molecular sequence (nrITS rDNA) data, and physio-chemical parameters determination such as organoleptic features and fluorescent behaviour.
METHODS: Collected basidiocarps were powdered and used for microscopic and organoleptic evaluation. DPPH radical scavenging method, total antioxidant activity methods and ABTS assay were used for evaluating antioxidant capacities of the methanolic extract. HPLC profile was also recorded to analyse phenolic fingerprint.
RESULTS: The DPPH radical scavenging activity was determined with EC50 value of 0.912 µg, total antioxidant activity found to be 15.33 µg ascorbic acid equivalent/mg of extract and ABTS assay revealed 12.91 µm TE/mg of extract antioxidant activity. HPLC chromatogram revealed the presence of 12 peaks. Several parameters were tested for the determination of chemical composition that revealed the existence of major bioactive components in the extract in following order: phenol> flavanoid> ascorbic acid> β-carotene~ lycopene.
DISCUSSION AND CONCLUSION: The present work suggests that Oudemansiella canarii may open a novel prospect as a functional food and antioxidant supplement.
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5.Determination Of Potential Drug-Drug Interactions By Using Various Software Programs At Community Pharmacy Setting
Mesut Sancar, Aksa Kaşık, Betul Okuyan, Sevda Batuhan, Fikret Vehbi İzzettin
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GİRİŞ ve AMAÇ: Çalışmada eczaneye gelen reçetelerdeki olası ilaç-ilaç etkileşimlerinin saptanması ve farklı yazılım programları kullanılarak belirlenen olası ilaç-ilaç etkileşim sonuçlarının karşılaştırılması amaçlanmıştır.
YÖNTEM ve GEREÇLER: Çalışma Mart ila Nisan 2015 (haftada iki gün) tarihleri arasında İstanbul’da yer alan 50 eczanede yürütülmüştür. Çalışmanın yürütüleceği eczanelerde 18 yaş ve üzeri hastalara ait ve içinde en az 2 ilaç bulunan ardışık 20 reçetedeki olası ilaç-ilaç etkileşmeleri incelenmiştir. Yazılım programlarında yer almayan ilaçları içeren reçeteler çalışma kapsamına alınmamıştır. Olası ilaç-ilaç etkileşimleri ‘Micromedex 2.0® Software Drug Interactions’ (www.micromedex.com), ‘Medscape Drug Interaction Checker®’ (www.medscape.com), ve ‘Drugs’ (www.drugs.com) programları kullanılarak karşılaştırılmıştır.
BULGULAR: Çalışmamızda toplam 1000 elektronik reçete incelenmiş ve bu reçetelerin %39,2’sinde yazılım programların herhangi birine göre en az bir tane olası ilaç-ilaç etkileşimi tespit edilmiştir. Reçetelerde saptanan olası ilaç-ilaç etkileşimlerinin yazılımlar tarafından bulunma oranları, ‘Micromedex 2.0® Software Drug Interactions’ için %21,2, ‘Medscape Drug Interaction Checker®’ için %33,3 ve ‘Drugs’ için ise %31,3 olarak hesaplanmıştır.
TARTIŞMA ve SONUÇ: Farklı yazılım programlarını karşılaştırdıktan sonra, yazılım programları tarafından bulunan potansiyel ilaç-ilaç etkileşimlerinin birbirlerinden farklı olduklarını kanıtlanmıştır. Bu nedenle, Türkiye'de eczacılar potansiyel ilaç-ilaç etkileşimlerini tespit edebilmek için eşzamanlı olarak ikiden fazla yazılım programı kullanmalıdırlar.
INTRODUCTION: The aim of the present study is to compare various software programs in detecting potential drug-drug interactions at community pharmacy setting.

METHODS: The prescriptions have been collected from 50 community pharmacies located in Istanbul between March and April 2015 (two days/ a week). From each pharmacy, the first twenty prescriptions that included more than one drug have been collected to evaluate potential drug-drug interactions. If the prescription was for a patient younger than 18 years old, it was excluded from the study. The following software programs were utilized to detect potential drug-drug interactions, ‘Micromedex 2.0® Software Drug Interactions’, ‘Medscape Drug Interaction Checker®’, and ‘drugs.com’. Number of potential interactions detected by the software programs was determined.

RESULTS: At least one potential drug-drug interaction was detected in 39.2% of 1000 prescriptions by one of the software programs. According to the rates of total drug-drug interactions gathered from various software programs, these software programs were arranged as ‘Medscape Drug Interaction Checker®’ (33.3%,), ‘drugs.com’ (31.3%), and Micromedex 2.0® Software Drug Interactions’ (21.2%).
DISCUSSION AND CONCLUSION: After comparing different software programs, potential drug-drug interactions found by the software programs proved to be different. Therefore, pharmacists in Turkey should use more than two software programs concurrently to detect potential drug-drug interactions.
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6.Two New Factors for the Evaluation of Scientific Performance: U and U'
Tayfun Uzbay
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Araştırmacıların akademik gelişime dönüşen bilimsel performansı, üniversitelerde görev süreleri ve proje hibeleri, bazı bibliyometrik göstergeler kullanılarak değerlendirilmektedir. Bu göstergeler toplam makale sayısı ve atıflar, yayınlandıkları dergilerin etki faktörleri, her bir makalenin etkisi veya toplam makalelerin etkisi ile hesaplanabilir. Ayrıca bireylerin bilimsel etkileri de Hirsch (h) indeksi gibi bazı indeksler tarafından belirlenmektedir. Bu ölçümlerin ve indekslerin hepsinde çeşitli sınırlılıklar vardır. Bilimsel projeler ve yayınlar çoğunlukla fazla sayıda kişi ile işbirliğini gerektirir ve tüm ortak çalışanlar bu projelere ve yayınlara eşit ölçüde katkıda bulunmaz. Dolayısıyla, bir bireyin performansını kollaboratif çalışmalardan gelen çıktılarla anlamak ve analiz etmek zordur. Bu makalede bireysel bilimsel performansı değerlendirmek için yeni bir uygulama önerilmiştir. U ve U'-faktörleri, bilimcilerin araştırma projelerinden ve çalışmalarından gelen çıktıların ürün niteliğini ve nitelikli üretim kapasitesini objektif olarak tespit edebilmektedir. Bu faktörler, belirli bilimsel problemler üzerindeki kesin katkılar ve çözümler hakkında bir fikir veremese de, U faktörü, bilim insanlarının bireysel bilimsel performansı veya üretkenliği için, h faktörü ve etki faktörü gibi diğer araçlardan daha objektif bir değerlendirmeye yardımcı olacaktır. H faktörü, araştırmacıların bazı çalışmalarını göz ardı edebilmektedir ve bu makalede, daha objektif bir değerlendirme için h yerine U faktörü kullanımı önerilmektedir. U' faktörü de özellikle bilimsel ödüllerde, proje hibelerinde ve akademik personelin atanmasında objektif bir seçim için yararlı olabilir.
Scientific performance of researchers that translates into academic improvement, tenure position in universities and project grants is commonly evaluated using by some bibliometric indicators. These indicators can be calculated through total number of papers and citations, impact factors of publishing journals, impact of the each of papers or impact of total papers. In addition, scientific impact of individuals is also determined by some indexes such as Hirsch (h) index. All of these measures and indexes have several limitations. Scientific projects and publications are mostly collaborative and not all collaborators contribute to these projects and publications equally. Thus, it is difficult to understand and analyze an individual’s performance by the outputs coming from collaborative studies. Here, a new practice for evaluating individual scientific performance is proposed. U and U'-factors are able to detect a qualified article production capacity of the scientists producing from their research projects and studies objectively. Although these factors may not give an idea about their exact contributions and solutions on the specific scientific problems, U factors will assist a more objective evaluation for individual scientific performance or productivity of the scientists than other tools such as h factor and impact factor alone. Because h factor excludes certain articles of researchers, in this paper, I propose to use U factor instead of h for a more objective evaluation. Especially the U^' factor may also be helpful for an objective selection in scientific awards, project grants and in appointing academical staff.
Abstract

7.Characterization of gamma-irradiated Rosmarinus officinalis L. (Rosemary)
Marzieh Heidarieh, Reza Rezanejad, Seyed Mahdi Ojagh, Mojtaba Raeisi, Gholamreza Rafiee, Alireza Alishahi
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INTRODUCTION: Rosmarinus officinalis L. (C), member of the Lamiaceae family has been accepted as one of the spices with the highest antioxidant activity.
METHODS: At this study, the transmission electron microscopy (TEM), X-Ray Diffraction (XRD) and fourier transform infrared spectroscopy (FTIR) physicochemical characteristics of gamma-irradiated Rosemary nano structure were investigated.
RESULTS: The particle size distribution of the gamma-irradiated Rosemary prepared under irradiation at 30 kGy in a cobalt-60 irradiator exhibit a very narrow size distribution with average size of 70 nm. Results showed that irradiated (30 KGy) and crude Rosemary had a similar pattern of FTIR spectra, typical of phenol compound, without any notable changes in the key bands and functional groups status. The irradiated Rosemary with 50 KGy and 10 KGy showed the highest and lowest crystallinity, respectively. The Rosemary crystallinity of irradiated samples decreased, as compared with the non-irradiated sample.
DISCUSSION AND CONCLUSION: Therefore, 30 KGy can be optimum for synthesis nanoparticles, average size of 70 nm, with low crystalinity and without any notable change in key bands compare to non-irradiated.
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8.Establishment and Escalation of Amino Acid Stacked Repressible Release Embedded System Using QbD
Vijay Sharma, Lalit Singh, Navneet Verma
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INTRODUCTION: Traditional approach of developing a new delivery system is an exhaustive task and requires a number of resources like man, money, material and time. To overcome this problem Quality by Design (QbD) can be utilized to get the pharmaceutical product of desired (best) quality with minimum use of above resources as well as determination of impact of one factor over the desired associated process. The present research is focused on establishing a design for formulating optimized gelatin microspheres using QbD.

METHODS: Characterization of formulated microspheres was done by infra red spectroscopy, scanning electron microscopy, percentage yield, microsphere size, drug entrapment efficiency and drug release. Impact of concentration of gelatin and ethyl cellulose was determine over dependent response like percentage yield, microsphere size and drug entrapment efficiency.

RESULTS: Response surface curve was obtained by using 32 central composite design and optimized batch was obtained with percentage yield, microsphere size and drug entrapment efficiency as 89.98, 333.32 mm and 82.61% respectively. Validation of optimized batch was done formulatin four different batches with optimzed values of independent response and a comparison of the observed responses with the predicted ones setting up and all these batches were found close to the and show validity of optimized data.

DISCUSSION AND CONCLUSION: QbD approach is quite efficient to get optimized drug delivery systems of L-Arginine without doing exhaustive study.
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9.Effect of lipid peroxidation product 4-hydroxynonenal on neuroinflammation in microglial cells: Protective role of Quercetin and Monochloropivaloylquercetin
Ahmet Cumaoğlu, Aslı Özge Ağkaya, Zehra Özkul
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GİRİŞ ve AMAÇ: Lipit peroksidasyonu ürünü aldehit, 4-hidroinonenal (HNE), nörodejeneratif hastalıklar ve yaşlanma gibi oksidatif strese bağlı inflamatuar patolojilerle ilişkilendirilmiştir. Bu bağlamda, HNE’ in nöroinflamatuvar cevap üzerine etkisini siklooksijenaz-2 (COX-2), indüklenebilir nitrik oksit sentaz (iNOS) ifadelenmeleri ve sitokin üretimi üzerinden incelenmiştir. Bunlara ek olarak, nüklear faktör eritroid 2–ilişkili faktör 2 (Nrf2)/Kelch-benzeri ECH-ilişkili protein 1 (Keap1) sinyal proteinleri, antioksidan enzimler hemoksijenaz-1 (HO-1) ve NAD(P)H dehidrojenaz, kinon 1 (NQO1) ifadelenme düzeyleri ölçüldü ve sonuçlar kersetin ve monokloropivaloilkersetin uygulanan hücrelerle karşılaştırılmıştır.
YÖNTEM ve GEREÇLER: Sitotoksisite MTT (3-(4,5-dimetiltiyazol-2-yl)-2,5-difeniltetrazolyum bromit) indirgenme yöntemi ile ölçüldü ve sitokin üretimi ise sitokin array ile belirlendi. Bununla birlikte, 2,5 µM HNE uygulanmış BV-2 hücrelerinde hücre içi Nrf2/Keap1 sinyal proteinleri, HO-1, NQO1 ve COX-2 ifadeleri Western blot ile analiz edildi. iNOS ve COX-2 mRNA düzeyleri RT-PCR ile ölçülmüştür.
BULGULAR: HNE mikroglial hücrelerde COX-2 mRNA ve protein düzeylerini, iNOS mRNA düzeylerini ve bunlarla birlikte sitokin üretimini artırdı. Buna ek olarak, HNE uygulaması Keap1 düzeyinde belirgin bir artışla birlikte, sitoplazmik Nrf2 ifadeleri ve antioksidan enzim HO-1 düzeylerini azaltmıştır. Kersetin ve monokloropivaloilkersetin ile tedavi COX-2 mRNA ifadelenme düzeylerini azaltarak nöroinflamasyonu hafifletmiştir. Monokloropivaloilkersetin sitoplazmik Keap1 seviyelerini azaltırken Nrf2’ nin nüklear translokasyonunu artırmıştır, bu durum HO-1 ve NQO1 ifadelenmelerini uyarımı ile sonuçlanmıştır.
TARTIŞMA ve SONUÇ: Bu sonuçlar BV-2 mikroglial hücrelerde HNE’ nin oksitatif stres ve inflamasyon arasında bağlayıcı olabileceğini göstermektedir. Özellikle monokloropivaloilkersetin, proinflamatuvar genlerin ifadelenme düzeylerini azaltıp, antioksidan savunma sistemini güçlendirerek inflamasyonu hafifletmiştir.
INTRODUCTION: Lipid peroxidation-derived aldehyde, 4-hydroxynonenal (HNE) has been implicated in a number of oxidative stress-induced inflammatory pathologies such as neurodegenerative diseases and aging. In this regard, we investigated the effects of HNE on neuroinflammatory responses by measuring cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) induction with cytokine production. In addition, we measured nuclear factor erythroid 2–related factor 2 (Nrf2)/Kelch-like ECH-associated protein 1 (Keap1) signaling proteins, antioxidant enzymes Heme oxygenase-1 (HO-1) and NAD(P)H dehydrogenase, quinone 1 (NQO1), and compared the results with quercetin and monochloropivaloylquercetin (MPQ) pretreated microglial cells.
METHODS: Cytotoxicity was determined by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay and production of cytokines were determined by cytokine array. Furthermore, intracellular Nfr2/Keap1 signaling proteins, HO-1, NQO1 and COX-2 expression were analyzed by western blot in 2,5 µM HNE treated BV-2 cells.
RESULTS: iNOS and COX-2 mRNA levels measured with RT-PCR. HNE induced both COX-2 mRNA and protein levels, iNOS mRNA expression and cytokine production. In addition, HNE markedly increased Keap1 levels and decreased cytoplasmic Nrf2 expression with antioxidant enzyme HO-1 levels. Quercetin and monochloropivaloylquercetin treatment alleviated neuroinflammatory responses in microglial cells, by decreasing COX-2 mRNA expression. Monochloropivaloylquercetin decreased cytoplasmic Keap1 levels and increased nuclear translocation of Nrf2 resulted in induction of HO-1 and NQO1 expression.
DISCUSSION AND CONCLUSION: These results suggest that HNE could be a link between oxidative stress and inflammation in BV-2 microglia cells. Especially, monochloropivaloylquercetin alleviated inflammation, probably by decreasing the expression on proinflammatory genes and enforcing antioxidant defense system.
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10.Enhancement of Dissolution of Fenofibrate using complexation with Hydroxy propyl β – Cyclodextrin
Sachin K Jagdale, Mohammad H Dehghan, Nilesh S Paul
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INTRODUCTION: The aim of the present study was to enhance the dissolution rate of fenofibrate using its complexation with Hydroxy prypyl β – Cyclodextrin (HPβCD).
METHODS: The phase solubility behavior of fenofibrate was studied in presence of various concentrations of (HPβCD) in aq. Solution at 37°c.
The complexes of fenofibrate were prepared with HPβ – Cyclodextrin at 1: 1 ratio by kneading and co- precipitation method. Fenofibrate – HPβCD complexes were evaluated by dissolution studies, Fourier transform infrared (FTIR) spectroscopy and Differential scanning calorimetry (DSC) studies.
RESULTS: The solubility of fenofibrate increased with increase in amount of HPβCD in aq. Solution. Gibbs free energy (ΔG0)tr values were all negative.
The complexation of fenofibrate with HPβ – Cyclodextrin exhibited enhanced dissolution rate of fenofibrate. The mean dissolution time of fenofibrate decreases significantly in complexation. The Fourier transform infrared (FTIR) spectroscopy studies showed formation of intermolecular hydrogen bonding between fenofibrate and HPβ – Cyclodextrin. The Differential scanning calorimetric studies indicated the loss in crystalline state of fenofibrate in complexes of fenofibrate with HPβ – Cyclodextrin.
DISCUSSION AND CONCLUSION: The studies indicated the loss in crystalline state of fenofibrate in complexes of fenofibrate with HPβ – Cyclodextrin. From Study, it can be concluded that Fenofibrate - HPβ-CD complexation results in an increase in solubility and dissolution rate of drug, suggesting a possible enhancement of its oral bioavailability
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11.Degradation kinetics, in-vitro dissolution studies and quantification of praziquantel anchored in emission intensity by spectrofluorimetry
Panikumar Durga Anumolu, Sunitha Gurrala, Ceema Mathew, Vasavi Panchakatla, Veda Maddala
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INTRODUCTION: A simple, rapid, specific and highly sensitive ecofriendly spectrofluorimetric method has been developed for the quantification of praziquantel.
METHODS: A linear relationship was found between fluorescence intensity and praziquantel concentration in the range of 1-20 µg/mL in water at emission wavelength of 286 nm after excitation wavelength at 263 nm with a good correlation coefficient (0.999).
RESULTS: The proposed method was validated according to ICH guidelines and statistical analysis of the results revealed high accuracy and good precision with the percentage RSD values less than 2.The detection and quantification limits were found to be 0.27 and 0.81 µg/mL, respectively.The proposed method was extended to investigate the stability of the drug and its degradation kinetics in the presence of acidic, alkaline and oxidative conditions.
DISCUSSION AND CONCLUSION: Moreover, the method was utilized to study the in-vitro dissolution studies of praziquantel tablet formulation.The suggested procedures could be used for the assessment of praziquantel in drug substance and drug products as well as in presence of its degradation products.
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12.Histone Deacetylase Inhibitors: A Prospective In Drug Discovery
Rakesh Yadav, Pooja Mishra, Divya Yadav
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Treatment of cancer is a major provocation in the entire society and follows a line of an investigation in the field of drug discovery. Therefore, there is a crucial requirement of discovering an ingenious medicinally active agent with proficiency of amending idle drug targets. Increasing pragmatic evidences implies that the histone deacetylases (HDAC) are trapped in cancer progression which increases the deacetylation and triggers malignancy changes. They provide a ground-breaking scaffolds and an attainable key for investigating chemical entity pertinent to HDAC biology as a therapeutic target in drug discovery context. Due to the gene expression, an impending requirement to prudently transfer cyto-toxicity to cancerous cells, HDAC inhibitor may be developed as an anti-cancerous agent. The present review has been focused on the basics of HDAC enzyme, their inhibitors and therapeutic outcomes.
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13.Comparison of Essential Oils of Ferula orientalis L., Ferulago sandrasica Peșmen & Quézel and Hippomarathrum microcarpum Petrov and Their Antimicrobial Activity
Songül Karakaya, Gamze Göger, Fatmagül D. Bostanlık, Betül Demirci, Hayri Duman, Ceyda Sibel Kılıç
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INTRODUCTION: To determine the chemical composition and antimicrobial activity essential oils of aerial parts of Ferula orientalis L., roots of Ferulago sandrasica Peșmen & Quézel and aerial parts of Hippomarathrum microcarpum Petrov.
METHODS: Essential oils were analysed by GC and GC/MS. The antimicrobial activity of the essential oils were determined with bioautography assay.

RESULTS: α-pinene (75.9%) and β-pinene (3.4%) were found as major components for aerial parts of F. orientalis; limonene (28.9%), α-pinene (15.6%) and terpinolene (13.9%) for F. sandrasica; β-caryophyllene (31.4%) and caryophyllene oxide (23.1%) for aerial parts of H. microcarpum, respectively. Essential oils from aerial parts of F. orientalis and roots of F. sandrasica and from aerial parts of H. microcarpum were active against Staphylococcus aureus and Candida albicans strains. However, essential oils were not active against Pseudomonas aeruginosa and Escherichia coli.
DISCUSSION AND CONCLUSION: The antimicrobial activities against Staphylococcus aureus and Candida albicans of these species may be attributed to the presence of the main components in the essential oils.
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14.Preclinical evaluation of haematinic activity of oral indiffusible mixture of Tamarindus indica L. leaf extract
Sathiya Ramu, Shwetha Krishna Murthy, Sukanya Krishna, Abhishek Lakkasandra Somashekaraiah, Vani B Nandihalli, Kanekal Mohammed Muzammil
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INTRODUCTION: Tamarindus indica L. (T. indica) is known to be a multipurpose traditional plant in India. It is used against some bacterial infections, parasitic infestations, constipation and inflammation. It is also used as a blood tonic and used for wound healing. This study was designed to substantiate the traditional claim of haematinic activity of T. indica.
METHODS: T. indica leaf extract was formulated into an oral indiffusible mixture (TIM) and evaluated for its haematinic activity in phenylhydrazine (Single dose of 10mg/kg per oral for 8 days) induced anaemia. Wistar rats were grouped into six (n=6). Groups I and II served as normal control and disease control respectively. Group III received standard drug (Haematinic suspension 2ml/kg). Groups IV, V, VI received formulated oral indiffusible mixture of T. indica at the dose of 100, 200 and 400 mg/ kg respectively.
RESULTS: TIM was formulated and pharmaceutically optimized. TIM produced significant increase in RBC, Hb and PCV while decrease in MCV.
DISCUSSION AND CONCLUSION: These results conclude that the oral indiffusible mixture of T. indica leaf extract taken for investigation was found to reverse phenylhydrazine induced anaemia.However, short duration of present study is proposed to be a limitation, thereby longer duration is required for obtaining better responses.
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15.Development of discriminative and biorelevant dissolution test method for atorvastatin /fenofibrate combination with appliance of derivative spectrophotometry.
Panukumar Durga Anumolu, Sunitha Gurrala, Subrahmanyam Chavali Venkata Satya, Santoshi Vani Polisetty, Anjana Ravindran, Radhagayathri Achanta
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INTRODUCTION: Now a days, market is flooded with combination of drugs in various dosage forms, but lack of official methods to quantify them. A single dissolution test method for the analysis of combined dosage form is preferred for simplification of quality control testing. If the developed dissolution medium mimics the bio-relevant and discriminating dissolution procedure for drug products with limited drug aqueous solubility is a useful tool for qualitative forecasting of in-vivo behavior of formulations.
METHODS: Dissolution profiles are evaluated for atorvastatin and fenofibrate in capsules, using paddle type USP dissolution apparatus in 900 mL of medium at 50 rpm and 37±0.5 °C. The best medium was 900 mL of 0.5% w/v sodium lauryl sulphate.To quantify both drugs simultaneously, a second derivative spectrophotometric was established (λmax 281 nm and 296 nm, respectively, for atorvastatin and fenofibrate) in acetate buffer, pH 2.8 solution.
RESULTS: The cumulative % dissolution was more than 85% within 45 min time for marketed tablets. The proposed dissolution test conditions have the discriminative power, dissimilarity factor (f1) are low (12-16%) and similarity (f2) factor values were also low (45-48%). Hence the use of 0.5% w/v sodium lauryl sulphate solution is justified. The dissolution method was validated (% RSD<2).
DISCUSSION AND CONCLUSION: The proposed dissolution test conditions have the discriminative power, substantiated the usefulness of this biorelevant medium for the two drugs and the dissolution method was validated (% RSD<2). The developed dissolution method can be fruitfully employed as quality control tool as well as research tool.
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16.Is There an Association Between Extreme Level of Boron Exposure and Decrease in Y: X Sperm Ratio in Men? Results of an Epidemiological Study
Can Özgür Yalçın, Aylin Üstündağ, Yalçın Duydu
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GİRİŞ ve AMAÇ: Çin’in bor madenciliği yapılan bölgesinde yürütülmüş olan bir epidemiyolojik çalışma sonucunda, erkeklerin Y: X sperm oranı ile yüksek seviyedeki bor maruziyeti arasında negatif bir ilişki olduğu belirtilmiştir. Ancak bu çalışma, çalışmanın tasarımındaki bazı zayıflıklar nedeni ile pek çok bilim insanı tarafından eleştirilmiştir. Bu çalışma, yukarıda söz edilmiş olan erkeklerin Y: X sperm oranı ile yüksek seviyedeki bor maruziyeti arasında negatif bir ilişki olduğu iddiasını doğrulamak ya da çürütmek amacıyla yapılmıştır.
YÖNTEM ve GEREÇLER: Bu çalışma Bandırma borik asit üretimi yapılan bölgede gerçekleştirilmiştir. Bu çalışmaya 163 erkek işçi gönüllü olarak katılmıştır. Borik asit üretim tesislerinde istihdam etmekte olan işçiler maruziyet grubu olarak tanımlanmışlardır (n=86). Kontrol grubu ise, buhar santrali, enerji tedarik ünitesi, demineralize su ünitesi, mekanik atölye gibi iş kollarında çalışan işçilerden oluşturulmuştur (n=77). Vardiya sonlarında çalışmaya katılan işçilerden kan ve meni örnekleri alınmıştır. Erkeklerdeki Y: X sperm oranları floresan in situ hibridizasyon (FISH) tekniği ile tespit edilmiştir. Kan ve meni örneklerindeki bor konsantrasyonları ICP-MS ile tayin edilmiştir.
BULGULAR: Olağanüstü mesleki maruziyet koşulları altında bile bor maruziyetine bağlı olarak işçilerde Y: X sperm oranlarında olumsuz bir etki gözlenmemiştir. Bizim çalışmamızın sonuçları, Y: X sperm oranı ile yüksek seviyedeki bor maruziyeti arasındaki negatif ilişkiyi reddetmektedir.
TARTIŞMA ve SONUÇ: Bizim çalışmamızdan elde etmiş olduğumuz sonuçlar, ağır mesleki bor maruziyeti koşulları altında bile bor maruziyetinin erkeklerde Y: X sperm oranları üzerinde olumsuz bir etkisinin olmadığını göstermektedir.
INTRODUCTION: A negative association between Y: X sperm ratio and high level of boron exposure was suggested in an epidemiological study conducted in boron mining areas of China. This study, however, was criticized by many authors due to some weaknesses in the study design. The present epidemiological study is designed to corroborate or refute the above mentioned negative association between boron exposure and Y: X sperm ratio in men.
METHODS: The study was conducted in boric acid production zone in Bandırma. One hundred sixty three male workers were voluntarily participated to our study. The workers employed in the boric acid production facilities were assigned as the exposed workers (n=86). The control group were composed of the workers employed in steam power plant, energy supply unit, demineralized water plant, mechanical workshop etc. (n=77). Blood and semen samples were sampled from the participated workers at the end of the work shift. Y: X sperm ratio in semen samples were determined by using fluorescence in situ hybridization (FISH) technique. Boron concentrations in semen and blood samples were determined by using Inductively Coupled Plasma Mass Spectrometry (ICP-MS).
RESULTS: Boron mediated adverse effect on the Y: X sperm ratio in workers have not been determined even under extreme occupational exposure conditions in our study. The results of our study refute the negative association between Y: X sperm ratio and high level of boron exposure which was suggested in an earlier published epidemiological study conducted in boron mining areas of China.
DISCUSSION AND CONCLUSION: The results of our study indicate that boron mediated adverse effects on the Y: X sperm ratio seem not possible even under occupational boron exposure conditions.
Abstract

17.Sub-chronic toxicity assessment of orally administered methanol (70%) seed extract of Abrus precatorius L. in Wistar albino rats
Shazia Tabasum, Swati Khare, Kirti Jain
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INTRODUCTION: Abrus precatorius L. is a famous medicinal plant of family Fabaceae and is widely used in traditional medicine for the treatment of various ailments. However, there is little toxicological data available regarding its safety following repeated exposure; therefore, the present study was designed to evaluate the 28 days sub-chronic toxicity of methanol (70%) crude extract of Abrus precatorius seeds in adult Wistar albino rats.
METHODS: Sub-chronic toxicity experiment was conducted by oral administration of graded doses (200 mg/kg and 400 mg/kg) of test extract daily for 28 days. Signs of toxicity, food and water consumption, body weight, gross pathology as well as relative organ weight were evaluated. The toxic effects were also assessed using hematological and biochemical data followed by histopathological examination of various internal organs. All data collected were expressed as mean ± standard deviation (SD). The One Way Analysis of Variance (ANOVA) followed by Bonferroni test was used for data interpretation and p ˂ 0.05 was considered as significant.
RESULTS: No deaths or evident toxic signs were found throughout the experimental period. There were no significant change in body weight, gross pathology, organ weight or food and water consumption between control and the treated groups. There were no treatment related differences in haematological and biochemical indices. Also, no gross abnormalities or histological alterations were observed.
DISCUSSION AND CONCLUSION: The methanol extract of Abrus precatorius seeds was found non-toxic in sub-chronic intake at the dosages tested. Thus, this study is expected to be beneficial for clinical and traditional applications for safe consumption and to utilize Abrus precatorius as a remedy at a recommended dosage.
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18.Quantification of Galantamine in Sterbergia Species by High Performance Liquid Chromatography
Özlem Bahadır Acıkara, Betül Sever Yılmaz, Dilhun Yazgan, Gülçin Saltan İşcan
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GİRİŞ ve AMAÇ: Bu çalışmada Türkiye’de yetişen Sternbergia türlerinin galantamin içeriklerinin kalitatif ve kantitatif analizi amaçlanmıştır.
YÖNTEM ve GEREÇLER: Galantamin S. fischeriana yumrularından izole edilmiş ve yapısı spektroskopik yöntemler kullanılarak aydınlatılmıştır. S. lutea ssp. lutea, S. lutea ssp. sicula, S. candida, S. fischeriana ve S. clusiana türlerinin galantamin içeriği kalitatif ve kantitatif olarak yeni geliştirilen ve valide edilmiş bir YPSK yöntemi kullanılarak yapılmıştır.
BULGULAR: S. lutea ssp. sicula türünün 0.0165±0.0002 g/100g olarak en yüksek galantamin içeriğine sahip olduğu belirlenmiştir. Galantamin için LOD ve LOQ değeri sırasıyla 7.5µg ve 25 µg olarak belirlenmiştir.
TARTIŞMA ve SONUÇ: Türkiye’de yetişen Sternbergia fischeriana türünden galantamin izolasyonu ilk kez bu çalışma ile rapor edilmiştir. Ayrıca bu çalışma ile Sternbergia türlerinin galantamin içeriğinin tespit edilmesi ve miktar tayini için yeni bir YPSK metodu geliştirilmiştir.
INTRODUCTION: This study describes the qualitative and quantitative analysis of galantamine in Sternbergia species growing in Turkey.
METHODS: Galantamine was isolated from S. fischeriana bulbs and structure of the compound elucidated by spectroscopic methods. The qualitative and quantitative analysis of galantamine was investigated in S. lutea ssp. lutea, S. lutea ssp. sicula, S. candida, S. fischeriana and S. clusiana using a specially developed and validated HPLC method.
RESULTS: S. lutea ssp. sicula was determined to have highest content of galantamine by 0.0165±0.0002 g/100g. The limits of detection (LOD) and quantification (LOQ) were determined as 7.5µg and 25 µg respectively.
DISCUSSION AND CONCLUSION: Isolation of galantamine from Sternbergia fischeriana growing in Turkey is reported in first time. An HPLC method was developed for identification and quantification of galantamine in Sternbergia species.
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