Search results for "Stability"
showing 10 items of 3085 documents
Loading, release and stability of epirubicin-loaded drug-eluting beads.
2015
Purpose The aim of this study was to determine the loading efficiency, physico-chemical stability and release of epirubicin-loaded DC Bead™ (Biocompatibles UK Ltd, a BTG International group company) (bead size 70–150 µm (=DC Bead M1™) and 100–300 µm) after loading with epirubicin solution (2 mg/ml) or reconstituted powder formulation (25 mg/ml) and controlled storage. Methods DC Bead™ were loaded with 76 mg epirubicin solution (Epimedac™, Medac GmbH) or 75 mg epirubicin powder formulation (Farmorubicin™, Pharmacia Pfizer GmbH) per 2 ml of beads. Drug loading efficiency and stability were determined by measuring the epirubicin concentration in the excess solution after predetermined interval…
Stability of tacrolimus ophthalmic solution
2017
Purpose The stability of 0.3-mg/mL tacrolimus ophthalmic solution at different storage temperatures was studied. Methods A sterile ophthalmic solution of 0.3 mg/mL tacrolimus was prepared in triplicate under aseptic conditions by diluting tacrolimus in eye drops. Three aliquots of this solution were transferred into polypropylene bottles and stored at 25, 2–8, or −15 to −25 °C. Samples were collected immediately after preparation and at selected time points and assayed in triplicate using high-performance liquid chromatography (HPLC). Samples were also visually examined for macroscopic changes. The 0.3-mg/mL tacrolimus solution was also exposed to acidic treatment and heat to force its degr…
Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Enalapril
2018
Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhibitor enalaprilat. Enalapril as the maleate salt is shown to be highly soluble, but only 60%-70% of an orally administered dose of enalapril is absorbed from the gastrointestinal tract into the enterocytes. Consequently, enalapril maleate is a Biopharmaceutics Classification System class III substance. Because in situ conversion of the maleate salt to the sodium salt is sometim…
Potential transbuccal delivery of l-DOPA methylester prodrug: stability in the environment of the oral cavity and ability to cross the mucosal tissue
2016
Levodopa (l-DOPA) is the most effective pharmacologic agent in Parkinson's disease and remains the "gold standard". Nevertheless, in long-term treatments, dyskinesias and motor complications can emerge. In this work, the combined use of l-DOPA methylester hydrochloride prodrug (LDME) with transbuccal drug delivery was supposed as a good alternative method to optimize the bioavailability of l-DOPA, to maintain constant plasma levels and to decrease the drug unwanted effects. The effects of environmental pH on buccal delivery of LDME were evaluated ex vivo. The increase of pH value from 5.8 to 6.2 implies an improvement of drug permeation. Since the pH increase causes the raising of hydrolyti…
Solid lipid nanoparticles containing tamoxifen characterization and in vitro antitumoral activity.
2005
Solid lipid nanoparticles (SLNs) containing tamoxifen, a nons- teroidal antiestrogen used in breast cancer therapy, were prepared by microemulsion and precipitation techniques. Tamoxifen loaded SLNs seem to have dimensional properties useful for parenteral administration, and in vitro plasmatic drug release studies demon- strated that these systems are able to give a prolonged release of the drug in the intact form. Preliminary study of antiproliferative ac- tivity in vitro, carried out on MCF-7 cell line (human breast cancer cells), demonstrated that SLNs, containing tamoxifen showed an antitumoral activity comparable to free drug. The results of char- acterization studies and of in vitro …
Biowaiver monograph for immediate-release solid oral dosage forms: acetylsalicylic acid.
2012
A biowaiver monograph for acetylsalicylic acid (ASA) is presented. Literature and experimental data indicate that ASA is a highly soluble and highly permeable drug, leading to assignment of this active pharmaceutical ingredient (API) to Class I of the Biopharmaceutics Classification System (BCS). Limited bioequivalence (BE) studies reported in the literature indicate that products that have been tested are bioequivalent. Most of the excipients used in products with a marketing authorization in Europe are not considered to have an impact on gastrointestinal motility or permeability. Furthermore, ASA has a wide therapeutic index. Thus, the risks to the patient that might occur if a nonbioequi…
Hexafluoro complex of rutherfordium in mixed HF/HNO3 solutions
2008
Formation of anionic fluoride-complexes of element 104, rutherfordium, produced in the 248 Cm( 18 O, 5n) 261 Rf reaction was studied by anion-exchange on an atom-at-a-time scale. It was found that the hexafluoro complex of Rf, [RfF 6 ] 2- , was formed in the studied fluoride ion concentrations of 0.0005-0.013 M. Formation of [RfF 6 ] 2- was significantly different from that of the homologues Zr and Hf, [ZrF 6 ] 2- and [HfF 6 ] 2- ; the evaluated formation constant of [RfF 6 ] 2- is at least one-order of magnitude smaller than those of [ZrF 6 ] 2- and [HfF 6 ] 2- .
Stabilization of a class of slowly switched positive linear systems: State-feedback control
2012
The main goal of this paper is to investigate the stabilization problem for a class of switched positive linear systems (SPLS) with average dwell time (ADT) switching in continuous-time context. State-feedback controllers and the corresponding switching law with ADT property are designed, which stabilize the closed-loop systems while keeping the states nonnegative. The proposed conditions, formulated as linear matrix inequalities, can be directly used for controller synthesis and switching designing. Finally, a numerical example is given to demonstrate the validity of the obtained results.
Robust H∞ reliable control for delta operator switched systems with time-varying delays under asynchronous switching
2014
The problem of robust H∞ reliable control for a class of delta operator switched systems with time-varying delays and actuator faults under asynchronous switching is considered in this paper. Asynchronous switching means that the switches between the candidate controllers and system modes are asynchronous. Based on the average dwell time approach and delta operator theory, a state feedback controller is designed such that the closed-loop system is exponentially stable with H∞ performance in the presence of actuator faults. The obtained results are formulated in the form of linear matrix inequalities (LMIs). Finally, a numerical example is provided to demonstrate explicitly the feasibility …
Stability and -Gain Control of Positive Switched Systems with Time-Varying Delays via Delta Operator Approach
2013
This paper investigates the problems of stability and -gain controller design for positive switched systems with time-varying delays via delta operator approach. The purpose is to design a switching signal and a state feedback controller such that the resulting closed-loop system is exponentially stable with -gain performance. Based on the average dwell time approach, a sufficient condition for the existence of an -gain controller for the considered system is established by constructing an appropriate copositive type Lyapunov-Krasovskii functional in delta domain. Moreover, the obtained conditions can unify some previously suggested relevant methods in the literature of both continuous- and…