1.Aerodynamic properties, solubility and in vitro antibacterial efficacy of dry powders prepared by spray drying: Clarithromycin versus its hydrochloride salt.
Manniello MD1, Gaudio PD1, Porta A1, Aquino RP1, Russo P2. Eur J Pharm Biopharm. 2016 Apr 19. pii: S0939-6411(16)30133-3. doi: 10.1016/j.ejpb.2016.04.009. [Epub ahead of print]
Antibiotic therapy for a direct administration to the lung in cystic fibrosis patients has to provide suitable availability, possibly in the lower respiratory tract, characterized by the presence of thick secretions. One of the crucial step in the therapeutic management of the respiratory disease could be the drug solubilization directly in this site of action. The aim of the study was to prepare respirable powders of clarithromycin, while improving drug aqueous solubility. With this aim, several batches of micronized particles were prepared by spray drying different feed solutions, varying the solvent composition (water/isopropyl alcohol ratio), the drug concentration and pH of the liquid feeds. Particle size distribution of raw materials and engineered particles was determined using a light-scattering laser granulometer while particle morphology was assessed by scanning electron microscopy. The in vitro deposition of the micronized clarithromycin powders was evaluate by means of a Single-Stage Glass Impinger using the RS01 model7 by Plastiape® as device for the aersolization.
2.[The serum level of the morphogenetic protein fibroblast growth factor 23 (FGF-23) as a marker for the efficiency of hyperphosphatemia therapy with phosphate-binding agents in chronic kidney disease].
Mukhin NA1, Milovanov YS1, Kozlovskaya LV1, Dobrosmyslov IA1, Milovanova LY1. Ter Arkh. 2016;88(4):41-45.
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English, RussianРеферат Цель исследования. Изучить возможность снижения избыточной продукции фактора роста фибробластов 23-го типа (FGF-23) в сыворотке крови у больных хронической болезнью почек (ХБП) VD стадии путем воздействия на гиперфосфатемию связывающими фосфат препаратами. Материалы и методы. В исследование включили 25 пациентов с ХБП VD стадии, находящихся на регулярном гемодиализе (ГД), 12 — хроническим гломерулонефритом, 8 — тубулоинтерстициальным нефритом и 5 — гипертензивным нефросклерозом; среди них 15 мужчин и 10 женщин в возрасте от 21 года до 65 лет, средний возраст на момент включения в исследование 43±4,5 года. Проводили клиническое, лабораторное и инструментальное обследование, аналогичное таковому у больных с более ранними стадиями ХБП. У всех 25 больных изучен уровень FGF-23 в сыворотке крови (Human FGF-23 ELISA kit с использованием моноклональных антител к полной молекуле FGF-23). Забор цельной крови выполняли через 2 дня после последнего сеанса ГД перед началом очередной процедуры.
3.Terbinafine hydrochloride nanovesicular gel: In vitro characterization, ex vivo permeation and clinical investigation.
AbdelSamie SM1, Kamel AO2, Sammour OA1, Ibrahim SM3. Eur J Pharm Sci. 2016 Apr 9;88:91-100. doi: 10.1016/j.ejps.2016.04.004. [Epub ahead of print]
In this work, nanovesicular chitosan gels were prepared for dermal delivery of terbinafine hydrochloride (TBN HCl). Ethosomes and vesicles containing different types of penetration enhancers (PEs) viz. Terpenes (cineole and limonene), labrasol and transcutol were developed. The prepared vesicles were evaluated for physical characteristics as well as skin interaction. The selected vesicles were incorporated into chitosan gel. An in vivo animal study was done on rat induced superficial Candida infection model. Moreover, randomized double blind clinical study was done on patients to compare the effect of the selected nanovesicular gel against the market product. Results showed the formation of nearly spherical, mostly deformable vesicular systems with size range of 95.5-530nm, zeta potential range of -0.1 to 15mV and entrapment efficiency range of 20-96.7%. Penetration enhancer vesicles (PEVs) prepared with 4% limonene (ELI4) showed the highest percent of drug deposition in the skin (53%) and the highest local accumulation efficiency value (35.
4.Binding of fexofenadine hydrochloride to bovine serum albumin: structural considerations by spectroscopic techniques and molecular docking.
Jattinagoudar LN1, Nandibewoor ST1, Chimatadar SA1. J Biomol Struct Dyn. 2016 Apr 25:1-54. [Epub ahead of print]
The binding interaction of peripheral H1 receptor antagonist drug, fexofenadine hydrochloride to bovine serum albumin is investigated by fluorescence spectroscopy in combination with UV-absorption spectroscopy under physiological conditions. The Stern-Volmer plots at different temperatures and the steady state fluorescence suggested a static type of interaction between fexofenadine and bovine serum albumin. Binding constants were determined to provide a measure of the binding affinity between fexofenadine and bovine serum albumin. It was found that bovine serum albumin has one binding site for fexofenadine. On the basis of the competitive site marker experiments and thermodynamic results, it was considered that fexofenadine was primarily bound to the site I of bovine serum albumin mainly by hydrogen bond and vander Waals force. Utilizing Förster resonance energy transfer (FRET) the distance, r between the donor, bovine serum albumin and acceptor fexofenadine was obtained.
