Bazı imidazol türevi ilaçlar üzerine çalışmalar

Bu tezin, veri tabanı üzerinden yayınlanma izni bulunmamaktadır. Yayınlanma izni olmayan tezlerin basılı kopyalarına Üniversite kütüphaneniz aracılığıyla (TÜBESS üzerinden) erişebilirsiniz.- 37 S TJ M MARY The stability of chlotrimazole in acid pH (pil = 1) at 100 O and in artificial gastric and intestinal medium at 37°C was investigated,, The degradation products at acid pH ?were identified» After the separation of the degradation productsBu çalışmada klotrimazolün asit pH 'da (pH =1) 100 C de, suni mide ve barsak vasatında 37°C de stabilitesi incelendi ve asit pH'da teşekkül eden bozunma ürünlerinin teşhisleri yapıldı» Asit pH'da bozunma ürünlerinin ince tabaka kromatografisiyle ayrılmalarını takiben değişik spektroskopik yöntemler yardımıyla yapıları aydınlatıldı» İnce tabaka kromatografisi ile incelemede enzimli ve enzimsiz suni mide vasatında asit pH'da elde edilen bozunma ürünleri yanında 3» "bir bozunma ürünü teşhis edildi. Enzimli ve enzimsiz suni barsak vasatında yapılan çalışmalara ait kromatogramlarda ilk iki leke elde edilemeyip, sadece üçüncü leke elde edildi. Ancak bu lekenin yapısı miktarının azlığı nedeniyle aydınlatılamad

Trastuzumab Tayininde HPLC-FLD Yönteminin İncelenmesi

Trastuzumab (150kDa) is a monoclonal antibody (mAbs), which is directed against the human epidermal growth factor receptor-2 (HER2) and is used in patients with metastatic breast cancer treatment. In order to use these biosimilar drugs in therapy, bioequivalence studies should be performed and the success of these studies depends on the reliability of the analytical method. Present study describes a bioanalytical method for the total Trastuzumab determination using high-performance liquid chromatography (HPLC) coupled with fluorescence detection (FLD). Trastuzumab was isolated from rat serum using protein G column and eluted with glycine and then, the eluent was injected into HPLC system where the excitation and emission wavelengths were set at 278 and 343 nm, respectively. Experimental parameters namely the flow rate, type of analytical column, type and composition of mobile phase, and the eluent used in sample preparation step were optimized by considering the peak resolution and recovery percentages. Under optimal conditions, a calibration graph was constructed and the detection limit was calculated as 5.3 µg/mL. The applicability of the method for the pharmacokinetic studies was discussed.Trastuzumab (150kDa), insan epidermal büyüme faktörü reseptörü-2'ye (HER2) karşı yönlendirilen ve metastatik meme kanseri tedavisi gören hastalarda kullanılan bir monoklonal antikordur (mAb). Bu biyobenzer ilaçların tedavide kullanılabilmesi için biyoeşdeğerlik çalışmalarının yapılması gereklidir ve bu çalışmaların başarısı da analitik yöntemin güvenilirliğine bağlıdır. Bu çalışmada, fluoresans dedektörü (FLD) ile birleştirilmiş yüksek performanslı sıvı kromatografisi (HPLC) kullanarak toplam Trastuzumab analizi için bir biyoanalitik yöntem tanımlanmıştır. Trastuzumab, protein G kolonu kullanılarak sıçan serumundan izole edildikten sonra glisinle elüe edilerek, elüent, uyarma ve emisyon dalga boylarının sırasıyla 278 ve 343 nm'ye ayarlandığı HPLC sistemine enjekte edilmiştir. Akış hızı, kolon türü hareketli faz türü ve bileşimi ve örnek hazırlama aşamasında kullanılan elüent gibi deneysel parametreler, piklerin ayrılması ve geri kazanım yüzdeleri dikkate alınarak optimize edilmiştir. Optimum koşullar altında kalibrasyon grafiği oluşturulmuş ve belirtme alt sınırı 5.3 µg/mL olarak hesaplanmıştır. Bu yöntemin farmakokinetik çalışmalar için uygulanabilirliği tartışılmıştır

Comparison of Pharmacodynamics and Celiac Effects of Olmesartan Medoxomil Formulations by using Olmesartan-induced Celiac-rat-model

Olmesartan Medoxomil (OM) is an angiotensin receptor blocker and has the adverse effect of celiac like enteropathy which was accepted by the FDA in 2013. This disease is characterized by severe diarrhea, weight loss and enteropathy. Although there are many case reports associated with olmesartan-related enteropathy in humans, it has not been described in a long-term animal model study so far. We developed a self-microemulsifying drug delivery system (OM-SMEDDS) in our previous study to reduce this side effect of the drug and to enhance bioavailability. In this study, an artificial hypertension model was established with a dose of 185 mu mol /kg L-NAME (N omega-nitro-L-arginine methyl ester) twice in a day intraperitoneally in Wistar albino rats. To determine and compare side effects, the OM-Suspension and OM-SMEDDS were administered at 1.3 mg/kg therapeutic dose during one-month period to the rats. Tension of rats was recorded by measuring from their tails with non invasive blood pressure system. We observed celiac like enteropathy findings like villous atrophy and intraepithelial lymphocytosis and clinical changes like weight loss and severe diarrhea after the treatment with OM-Suspension during one-month experiment. It was also observed that the antihypertensive efficacy of the OM-SMEDDS formulation was higher than the suspension during the experiment, which did not cause enteropathy, diarrhea and weight loss by reducing intestinal exposure. Hereby, we evaluated the side effects of two different pharmaceutical forms by designing a sustainable and reproducible celiac rat model that can be induced with olmesartan medoxomil

Sodium hyaluronate dry powder inhalation in combination with sodium cromoglycate prepared using optimized spray drying conditions

Sodium hyaluronate (SHA) is an anti-inflammatory and protective agent against bronchoconstriction, and sodium cromoglicate (SCG) prevents exercise-induced bronchoconstriction and inflammation. Based on the pharmacological properties of both substances, this study aimed to develop a dry powder inhaler (DPI) of SHA alone and in combination with SCG. The target of the study was to develop flowable formulations without any surfactants by using the spray drying method. To obtain respirable SHA and SCG:SHA particles, variables of the spray dryer, such as inlet temperature, atomized air flow, and feed solution, were changed. The particles 1-8 mu m in size were produced with high yield by spray drying and increasing the ethanol percentage of the feed solution (60%), which is the most remarkable parameter. After that, physicochemical characterizations were performed. The aerosol performance of DPI formulations prepared using lactose was evaluated using Handihaler (R) DPI. The fine particle fraction (FPF) was 36% for the SHA formulation, whereas it was 52 and 53% for SCG and SHA, respectively, in the SCG:SHA formulation. Consequently, both particles were produced reproducibly by spray drying, and inhaled SHA and SCG:SHA dry powder formulations were developed due to their high FPF and flowability with lactose.The authors acknowledge the support of NEUTEC ILAC SAN. TIC.A.S. (NEUTEC) for providing insight into the study, financial sup-port, advice, and assistance on the use of the inhaler quality control laboratory. We are grateful to Ege University Planning and Monitoring Coordination of Organizational Development and Directorate of Library and Documentation for their support in editing and proofreading service of this studyNEUTEC ILAC SAN; TIC.A.S. (NEUTEC

Analysis of Chemical Compositions of 15 Different Cold-Pressed Oils Produced in Turkey: A Case Study of Tocopherol and Fatty Acid Analysis

Many people tend to prefer natural foods and supplements nowadays. Considering this tendency, this study assessed the most significant in quality and purity parameters tocopherol and fatty acid compositions of cold-pressed oils, namely black cumin, sesame, sunflower, poppy, pomegranate, nettle, pumpkin, grape, safflower, flax, canola seed, wheat germ, peanut, hazelnut, and walnut. This study deals with the sample preparation and validation of tocopherols using an HPLC-FLD method for simultaneous determination of ?-?-?-, and ?-tocopherols, and analysis of fatty acid methyl esters (FAME) with using GC-FID. the validated HPLC method was applied for the tocopherols’ analysis and measurement uncertainty was calculated for tocopherols and some fatty acids. the obtained data were evaluated by using principal component analysis to show the relationship between quality parameters and seed oils. Wheat germ, hazelnut, safflower, and sunflower oils have the highest tocopherol contents respectively with a predominance of ?-tocopherol. Seed oils’ fatty acid compositions were classified according to proportions of oleic, linoleic, and other fatty acids. This study shows that the evaluated seeds are valuable sources of natural antioxidants and some specific and polyunsaturated fatty acids. the applied method can also be helpful for the industry to obtain quality analysis approach