Marmara Pharmaceutical Journal最新文献

{"title":"Türkiye’de İnsüline Ait Satış Verileri ve Referans İnsülin Aspart İle Biyobenzerinin Analitik Karşılaştırılması","authors":"O. Dal, A. Sezer","doi":"10.12991/MPJ.82504","DOIUrl":"https://doi.org/10.12991/MPJ.82504","url":null,"abstract":"Son yillarda ilac sanayinin ve ilac biyoteknolojisinin en populer konularindan biri biyobenzerlerdir. Uretimleri daha karmasik surecler iceren biyoteknolojik urunler, patentlerinin de bitmeye yaklasmasi veya bitmesi ile ilgi odagi olmaktadir. Jenerik urunler ile karsilastirildiginda karmasik surecler sadece uretim ile sinirli degildir. Gelistirme, klinik surecleri ve pazara erisim surecleri de zorlu ve maliyetlidir. Bu zorluklara ragmen biyobenzer gelistiren ve gelistirme calismalari devam eden bircok sirket bulunmaktadir. Jenerikler ile iliskili olarak gectigimiz uzun yillara ait net veriler olmasina ragmen biyobenzerler icin bircok baslik jeneriklere kiyasla yeni tartisilmaya baslanmistir. Bu basliklar arasinda biyobenzerlerin ekonomik katkisi, kamu maliyetine etkileri, hasta erisimi, klinik calismalar ve referans urun ile karsilastirma calismalarini sayabiliriz. Bu arastirma kapsaminda 1982 yilinda ilk onay alip, rekombinant DNA teknolojisi ile uretilmis biyolojik urun olan insulin iceren urunlerin kuresel ve Turkiye’deki satislari ele alinmistir. Arastirmada ayrica referans insulin aspart urunu ile insulin aspart biyobenzerinin analitik olarak karsilastirilmasi ele alinmistir, gelistirme ve ruhsat sureclerinde kullanilabilecek olasi basliklar irdelenmistir.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"1 1","pages":"675-687"},"PeriodicalIF":0.0,"publicationDate":"2017-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83160144","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Metoklopramit Hidroklorür Hpmc Tabletlerinin Sürekli Salım Özelliği Gösteren Formülasyonlarını Hazırlanması ve Değerlendirilmesi","authors":"Ramesh Narayanasamy, Ramakrishna Shabaraya","doi":"10.12991/marupj.323596","DOIUrl":"https://doi.org/10.12991/marupj.323596","url":null,"abstract":"Bu calismanin amaci, hidroksipropil metilseluloz (HPMC) kullanilarak direkt basim yontemi ile metoklopramid hidroklorur’un “gunde bir kez” kullanimi amaciyla surekli salim ozelligi gosteren tabletlerini gelistirmektir. Saf ilac etken maddesi, polimerler ve karisimlar incelendiginde pik kaymasi, piklerin varligi veya kaybolmasi bakimindan belirgin bir degisiklik kaydedilmedi. Metoklopramid hidroklorur iceren surekli salinimi ve klinik kullanima sunulmus olan hemen salim ozelligine sahip tabletler, gorunus, agirlik degisimi, kalinlik, sertlik, kirilganlik ve in vitro serbest salim gibi fiziko-kimyasal parametreler acisindan degerlendirildi. Metoklopramid hidroklorur’un surekli salim ozelligi gosteren tabletlerinin fizikokimyasal ozellikleri ve ilac icerikleri dikkate alindiginda 25⁰C’de ve %60 bagil nem (RH) kosullarinda ve 40°C’de ve %75 RH sartlarini iceren uzun sureli, hizlandirilmis alti aylik saklama kosullarinda kararlidir. Metoklopramid hidroklorur’un surekli salim tabletlerinden in vitro ilac salinimi, piyasaya surulmus olan derhal salim ozellikli tabletler ile karsilastirildi. Metoklopramid hidroklorur’un surekli salim tabletlerinin cok iyi emildigi ve emilim oraninin pazarlanan tabletinkinden daha yuksek oldugu belirlendi. Surekli salim formulasyonuna kiyasla Cmax ve tmax verileri derhal salim tabletleri icin daha yuksek bulundu. Gelistirilen metoklopramid hidroklorur surekli salinma tabletlerinin, yuksek AUC, yarilanma omru ve daha dusuk eliminasyon hiz sabiti degerleri gostermesi ilacin uzun sure vucutta kaldigini ve uzamis etki belirtileri gosterdigini dusundurdu. Bu calismada, gelistirilen surekli salim ozellikli ilac verme sisteminin, plazma metoklopramid hidroklorur duzeylerinin saglanmasinda daha iyi sonuc verecegi ve bu durumun da geleneksel tedavi ile ilgili sorunlari ortadan kaldiracagi onerilmektedir.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"74 1","pages":"717-729"},"PeriodicalIF":0.0,"publicationDate":"2017-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83752089","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Study on the Antimicrobial Effects of Novel Thiazole Derivatives","authors":"M. Y. Cankilic, L. Yurttaş","doi":"10.12991/MARUPJ.323584","DOIUrl":"https://doi.org/10.12991/MARUPJ.323584","url":null,"abstract":"In this work, six 2-[(1/4-methylimidazol/triazol/tetrazol- 2/3/5-yl)thio]-N-(4-substituted thiazol-2-yl) acetamide derivatives (2a-f) were synthesized. The antimicrobial activities of these substances were examined against some foodborne Gram positive and Gram negative test bacteria, Candida albicans, Candida glabrata, Candida krusei, and Candida parapsilosis yeasts, and some Aspergillus and Penicillium filamentous fungi species. The substances were shown considerable antimicrobial effect to tested pathogenic microorganisms.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"61 1","pages":"654-659"},"PeriodicalIF":0.0,"publicationDate":"2017-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80608562","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"HPLC Assay Method Development and Validation for Quantification of Capecitabine in Tablets and Forced Degradation Samples","authors":"M. Bhatia, Jivan N Raut, Anuja Barve, Prachi Patil, S. Jadhav","doi":"10.12991/mpj.36471","DOIUrl":"https://doi.org/10.12991/mpj.36471","url":null,"abstract":"A simple, rapid accurate and forced degradation indicating RP-HPLC method was developed for the determination of Capecitabine in pure and tablet dosage form. The mobile phase used contains 0.1% Acetic acid, Methanol and Acetonitrile in the ratio of 35:60:5 v/v. The linearity range is found over the concentration range of 50-150µg/ml. The Inertsil ODS, C18, 3V, 250 x 4.6 mm, 5µm with UV detection 250 nm is used. The RT is found to be 6.4 mins. The method was statistically validated for accuracy, linearity, precision, robustness, specificity and range. Quantitative and recovery studies of the dosage form were also carried out and analyzed; the % RSD from recovery studies was found to be within limits. The specificity of the method was ascertained by forced degradation studies by acid, alkali hydrolysis and oxidation and about 35% of drug is degraded in acidic medium. Due to simplicity, rapidity and accuracy of the method, the method will be useful for routine analysis and checking purity of Capecitabine tablet. The method further can be investigated for pharmacokinetic and biopharmaceutical analysis.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"39 1","pages":"660-668"},"PeriodicalIF":0.0,"publicationDate":"2017-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87507933","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Mean Centering Method for determination of Empagliflozin and Metformin","authors":"B. Ayoub, R. Emam, M. Youssef, M. El-Kattan, M. A. Sayed, Ahmed M Kowider, Adly H Seha, E. A. Rabea, Rana M Yakout, Rolly H Faried","doi":"10.12991/MARUPJ.323590","DOIUrl":"https://doi.org/10.12991/MARUPJ.323590","url":null,"abstract":"Introduction of computer-assisted analysis to pharmaceutical products is considered a significant approach. A new method was developed for simultaneous determination of empagliflozin and metformin manipulating their ratio spectra with application on recently approved pharmaceutical combination, Synjardy ® tablets. Spiking technique was used to increase the concentration of empagliflozin after extraction from tablets to allow its simultaneous determination with metformin without prior separation. Validation parameters according to ICH guidelines were acceptable over the concentration range of 2-12 μgml -1 for both drugs. Mean centering was performed using Minitab ® program. Using computer assisted programs after spiking accompanied with direct UV measurement of the drugs was satisfactory for accurate assay without complex instrumentations. The optimized method was proved to be suitable for industrial QC labs.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"12 1","pages":"669-674"},"PeriodicalIF":0.0,"publicationDate":"2017-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81859702","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antioxidant Potential and Emulsifying Properties of Kheri (Acacia chundra, Mimosaceae) Gum Polysaccharide","authors":"R. Malviya, P. Sharma, S. Dubey","doi":"10.12991/MARUPJ.323594","DOIUrl":"https://doi.org/10.12991/MARUPJ.323594","url":null,"abstract":"Ham Kheri recinesi (KG) cozucu olarak su, cokturme ajani olarak etil alkol kullanilarak saflastirilmistir. Sicakligin ve derisimin KG’nin yuzey gerilimine olan etkileri tespit edilmistir. Recinenin emulsifiyan ozellikleri yagli faz olarak aycicek yaginin sulu faz olarak saf suyun kullanildigi bir emulsiyon sisteminde calisilmis ve damlacik buyuklugu, akis hiz, emulsiyon stabilitesi, kopuk olusturma ve kopuk stabilitesi ve kremlesme (%) parametreleri saptanmistir. Polimerin serbest radikal supurucu ozelligi radikal olarak DPPHl (1,1-difenil-2-pikril hidrazil) ve H2O2 kullanilarak calisilmis, standart olarak askorbik asit kullanilmistir. KG’nin yuksek derisimde kullanildiginda daha iyi emulsifiyan etki ve daha yuksek kopuklenme ozelligi gosterdigi azalan kaynasma ve kremlesme hizina bagli olarak yorumlanmistir. Hazirlanan emulsiyonlarin damlacik buyuklugu 1.4- 2.6μ arasinda olculmustur. Kirkbes gun sonra yapilan olcumlerde emulsiyonlarin damlacik buyuklugunde degisme gorulmemistir. DPPHl kullanilarak yapilan deneylerde olusan serbest radikalleri %50 oraninda supurmek icin yeterli etkili derisim degeri (EC50) askorbik asit ve KG icin sirasiyla 36.53 ±2.03μg/ml ve 11.09 ±3.21 μg/ml olarak bulunmustur. H2O2 kullanilarak yapilan deneylerde olusan hidroksil iyonlarini %50 oraninda supurmek icin yeterli EC50 askorbik asit ve KG icin sirasiyla 73.13± 1.98 μg/ml ve 53.96 ± 1.53 μg/ml olarak bulunmustur. Elde edilen veriler isiginda, KG’nin gida, kozmetik ve ilac endustrisinde antioksidan potansiyali de olan bir emulsiyon ajani olarak kullanilabilecegi dusunulmektedir.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"37 1","pages":"701-706"},"PeriodicalIF":0.0,"publicationDate":"2017-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90984677","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation and evaluation of a bilayer tablet comprising of diclofenac potassium as orodispersible layer and diclofenac sodium as sustained release core","authors":"Jabbar Abbas, S. Bashir, M. Samie, S. Laghari, Nargis Aman, Habibullah Jan, Imran Nazir","doi":"10.12991/MARUPJ.323595","DOIUrl":"https://doi.org/10.12991/MARUPJ.323595","url":null,"abstract":"Diklofenak, bir fenilasetik asit turevi olup uzun yillardan beri antienfamatuvar ve analjezik bir ilac olarak kullanilmaktadir ancak bu etken maddeden hareketle hemen salim icin yukleme dozu iceren geciktirilmis salim formulasyonunun hazirlanmasi istenmektedir. Bu calismanin amaci, agizda dagilan tabaka olarak diklofenak potasyum, geciktirilmis salim cekirdegi olarak diklofenak sodyum iceren iki tabakali tabletlerin formulasyonu ve degerlendirilmesidir. Diklofenak sodyum iceren cekirdek yas granulasyon yontemi ile hazirlanirken agizda dagilan dis tabaka direct basim yontemiyle ve super dagitici olarak sodyum nisasta glikolat varliginda hazirlandi. Toz karisimi hem basim oncesi hem de basim sonrasi ozellikleri acisindan degerlendirildi. Toz karisiminin ve tabletlerin fiziksel ozelliklerinin zorunlu standartlarla uyumlu oldugu goruldu. Agizda dagilan kismin 30 saniyeden kisa bir surede dagilarak yukleme dozu olan diklofenak potasyumu saldigi, cekirdek kisminin ise simule bagirsak sivisinda (pH 6.8), 10 saate kadar diklofenak sodyum salinimi sagladigi tespit edildi. Kinetik ile ilgili veriler incelendiginde, tabletin non-fickian salim gosterdigi ve Korsmeyer-Peppas modeline uygun oldugu tespit edildi. Tek bir tablet iceriginde, agizda dagilan tabaka olarak diklofenak potasyum, geciktirilmis salim cekirdegi olarak diklofenak sodyum iceren ve super dagitici olarak sodyum nisasta glikolat iceren tabletlerin formulasyonu basariyla yapildi.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"59 1","pages":"707-716"},"PeriodicalIF":0.0,"publicationDate":"2017-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91003468","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preparation and Evaluation of a Sustained Release Formulation of Metoclopramide Hydrochloride HPMC Tablets","authors":"Ramesh Narayanasamy, Ramakrishna Shabaraya","doi":"10.12991/MPJ.76647","DOIUrl":"https://doi.org/10.12991/MPJ.76647","url":null,"abstract":"The objective of the present study was to develop \"once daily\" sustained release tablets of metoclopramide by direct compression using hydroxypropyl methylcellulose (HPMC). No significant changes in terms of peak shifting, appearance or disappearance of peaks were noted with pure drug, polymers and mixtures. The developed sustained release and marketed immediate release were appraised for physico-chemical parameters such as appearance, weight variation, thickness, hardness, friability and in vitro release study. Developed sustained release tablets of metoclopramide hydrochloride with respect to its physicochemical parameters and drug conent are stable at long term storage conditions at 25 o C and 60% RH,  and accelerated  conditions at 40 o C and 75% RH for a period of  six months. The in vitro release of metoclopramide sustained  release the formulations was compared with the marketed immediate release. The sustained release tablets of metoclopramide were well absorbed and the extent of absorption was higher than that of the marketed tablet. The Cmax and Tmax data showed higher for immediate release compared to sustain release formulation. Developed sustained release demonstrated higher AUC, half-life and lower elimination rate constant values is indicative, that drug leftover in the body for extended period of time and showed signs of prolonged effect. The sustained and efficient drug delivery system developed in the present study will maintain plasma metoclopramide levels better, which resolve the drawbacks related with the conventional therapy. Keywords: Metoclopramide Hydrochloride; Sustained release; Once daily, Hydroxypropylmethyl cellulose; Dissolution study; Pharmacokinetic study. Bu calismanin amaci, hidroksipropil metilseluloz (HPMC) kullanilarak dogrudan sikistirma metoklopramidin surekli olarak birakilan \"gunde bir kez\" serbest birakilmasidir. Saf ilac, polimerler ve karisimlarda zirveye kayma, gorunum veya piklerin kaybolmasi bakimindan belirgin bir degisiklik kaydedilmedi. Gelistirilmis surekli salim ve pazarlanan derhal salinim, gorunum, agirlik degisimi, kalinlik, sertlik, kirilganlik ve in vitro serbest birakma calismasi gibi fiziko-kimyasal parametreler icin degerlendiirildi. Metoklopramid hidroklorurun fizikokimyasal parametrelerine ve uyusturucu konusuna gore gelistirilmis surekli salinimli tabletleri, 25oC ve% 60RH'de uzun vadeli saklama kosullarinda ve 40oC'de ve% 75 Bagil Nem RH'de, alti aylik bir sure boyunca hizlandirilmis kosullarda kararlidir. Metoklopramidin in vitro salinimi formulasyonlari piyasaya surulen derhal salinimla karsilastirildiginda serbest birakmistir. Metoklopramid'in surekli salim tabletleri iyi absorbe edildi ve emilim derecesi pazarlanan tabletinkinden daha yuksekti. Cmax ve Tmax verileri, surumu serbest birakma formulasyonu ile karsilastirildiginda derhal salinma icin daha yuksek gosterdi. Gelistirilmis surekli salinim, daha yuksek AUC, yarilanma omru ve daha dusuk eliminasyon hizi sabit degerlerini","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"76 1","pages":"717-729"},"PeriodicalIF":0.0,"publicationDate":"2017-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75934349","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Microemulsion based bioadhesive gel of itraconazole using tamarind gum: in-vitro and ex-vivo evaluation","authors":"K. Mali, S. Dhawale, R. Dias","doi":"10.12991/MARUPJ.323593","DOIUrl":"https://doi.org/10.12991/MARUPJ.323593","url":null,"abstract":"The current study was aimed to formulate and evaluate bioadhesive gel containing microemulsion (ME) of itraconazole (ITZ) and an attempt was made to investigate suitability of tamarind gum (TG) as a gelling agent. The solubility of ITZ in oils, surfactants and co-surfactant was evaluated for the selection of appropriate component. The ratio of surfactant and co-surfactant was optimized by constructing pseudoternary phase diagram. Ternary phase diagram was constructed using isopropyl myristate (IPM) and oleic acid (OA) as oil phase, tween 80 as surfactant and isopropyl alcohol (IPA) as cosurfactant in order to obtain ME region. The optimized ME of ITZ was characterized by its qualitative and quantitative tests and incorporated into polymeric gels of carbopol (CBP), xanthan gum (XG) and TG. The ME based ITZ gels were evaluated for pH, drug content, viscosity, ex-vivo bioadhesion, spreadability and in vitro drug release. Furthermore, antifungal activity of the gels was performed by agar cup diffusion technique using cultures of Candida albicans. ITZ showed maximum solubility in mixture of IPM and OA (1:1). Stable ME was obtained when IPM and OA was taken in the ratio of 1:1 as oil phase, Tween 80 as surfactant and isopropyl alcohol (IPA) as cosurfactant at the weight ratio of 10:45:45. The optimized ME based gels showed pH in the range of 6.11 to 6.48, spreadability in the range of 4.1 to 7.1gm.cm/sec and ex vivo bioadhesion in the range of 65 to 84gm. The viscosity study indicated pseudoplastic behaviour of all ME based gel formulations. Amongst the studied ME gels, TG containing gels exhibited fast and complete drug release at the end of 24h. Formulation F7 containing TG showed wide zone of inhibition and found to be stable for three months. These results indicate that the TG containing ME gel may be a used as vehicle for topical delivery of drugs.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"58 1","pages":"688-700"},"PeriodicalIF":0.0,"publicationDate":"2017-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83957018","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Investigation of fragment based quantitative regression on a series of substituted chromen-2-one derivatives as FXa inhibitors","authors":"Santosh S. Kumbhar, P. Choudhari, M. Bhatia","doi":"10.12991/marupj.323292","DOIUrl":"https://doi.org/10.12991/marupj.323292","url":null,"abstract":"ABSTRACT Factor Xa (FXa), a trypsin-like serine protease, is well-established target for the development of the anticoagulants. Number of molecules were reported as Factor Xa inhibitors but most of them have pharmacokinetic issues. In this present communication, we report development and validation of the group based quantitative structure activity relationship (GQSAR) studies on 48 chromen-2-one derivatives as effective inhibitors of FXa. All the molecules were fragmented into eleven functional fragments (R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11).  All the developed GQSAR models were generated using multiple linear regressions analysis (MLR). The generated GQSAR models were selected on the basis of statistical data that models having r 2 should be above 0.6 were used to check the external predictivity while the significance of the model was decided on the basis of F value. Developed GQSAR models reveled presence of lipophilic groups on fragment R6 will diminish the bio-activity while at R2 it will lead to increase in bioactivity of molecules. Additionally, minimum number of rotatable bonds at fragments R1 was fruitful for better FXa inhibition activity. The results of GQSAR models may lead to better understanding of design and development of novel FXa inhibitors.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"36 1","pages":"620-630"},"PeriodicalIF":0.0,"publicationDate":"2017-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89136064","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}