Background: Bilastine (BLA) is a second-generation H1 antihistamine used to treat allergic rhinoconjunctivitis. Because of its limited solubility, it falls under class II of the Biopharmaceutics Classification System (BSC). The solid dispersion (SD) approach significantly improves the solubility and dissolution rate of insoluble medicines. Objective: To improve BLA solubility and dissolution rate by formulating a solid dispersion in the form of effervescent granules. Methods: To create BLA SDs, polyvinylpyrrolidone (PVP K30) and poloxamer 188 (PLX188) were mixed in various ratios (1:5, 1:10, and 1:15) using the kneading technique. All formulations were evaluated based on percent yield, drug content, and saturation solubility. The formulae with the greatest solubility enhancement were subjected to in vitro dissolution studies, Fourier transform infrared, and thermal analysis to study drug crystallinity and drug-polymer interactions. The best SD formula was made as effervescent granules using wet granulation and tested further. Results: The SD3 formula, which contained PVP K30 in a 1:15 ratio, had the highest solubility and release. In phosphate buffer (pH 6.8), over 88.43% of the BLA was released within the first 15 minutes. The optimum formula's effervescent granules demonstrated excellent flow qualities, a disintegration time of 87 seconds, an acceptable pH of 5.9, and 9.7 mg of BLA dissolved in the first 5 minutes. Conclusions: BLA dissolution can be improved via the solid dispersion technique, allowing for successful effervescent granule formulation.
Bilastine (BL) is a novel non-sedating second-generation antihistamine, and its bioavailability is about 60%. Objective: To compare the bioavailability of prepared oral self-nanoemulsions of BL (BL-SNE) with that of pure BL and marketed tablets. Methods: Four groups of Wistar rats were used in this study, each with six rats weighing between 200 and 250 g. They were treated orally using a a gavage tube. The groups were fed either with conventional tablets ("Alerbix®") after being ground and dispersed with deionized water (DIW), treated with BL-SNE or fed with pure BL powder suspension. The fourth group did not receive any medication. The concentration of BL in the rat’s plasma was measured using HPLC. We used Trandolapril as an an interna
... Show MoreIn recent years, observed focus greatly on gold nanoparticles synthesis due to its unique properties and tremendous applicability. In most of these researches, the citrate reduction method has been adopted. The aim of this study was to prepare and optimize monodisperse ultrafine particles by addition of reducing agent to gold salt, as a result of seed mediated growth mechanism. In this research, gold nanoparticles suspension (G) was prepared by traditional standard Turkevich method and optimized by studying different variables such as reactants concentrations, preparation temperature and stirring rate on controlling size and uniformity of nanoparticles through preparing twenty formulas (G1-G20). Subsequently, the selected formula that pr
... Show MoreInvasomes are newly developed types of nanovesicles. A vesicular drug delivery system is considered one of the approaches for transdermal delivery to enhance permeation and improve drug bioavailability. Ondansetron is a serotonin receptor antagonist used for treating vomiting associated with different clinical cases. The study aimed to prepare invasomal dispersions for improving permeation of ondansetron across the skin with a controlled release pattern. Twenty-seven formulas of ondansetron-loaded invasomes were prepared by a modified mechanical dispersion method. These formulas were optimized by studying the effect of variables on entrapment efficiency. Vesicle size, polydispersity, zeta potential, in-vitro release and ex-vivo perm
... Show MoreWet granulation method was used instead of conventional pan coating or fluidized –bed coating technique to prepare enteric-coated diclofenac sodium granules, using ethanolic solution of EudragitTM L100 as coating, binding and granulating agent .Addition of PEG400 or di-n-butyl phthalate as a plasticizer was found to improve the enteric property of the coat.
Part of the resulted granules was filled in hard gelatin capsules (size 0), while the other part was compressed into tablets with and without disintegrant.
The release profile of these two dosage forms in 0.1N HCl (pH 1.2)for 2 hours, and in phosphate buffer (pH 6.8) for 45 minutes as well as the release kinetic were compared with that of the en
... Show MoreFilms of PMMA and copper sulphate doped PMMA have been prepared by casting method. Absorbance and transmittance spectra were recorded in the wavelength range (300-900) nm in order to calculate, single oscillator energy, dispersion energy, average oscillator strength, the refractive index at infinite wavelength, M-1 and M -3 moments of the optical spectra, it was found that all these parameters were effected by doping.
The objective of the present investigation was to enhance the solubility of practically insoluble mirtazapine by preparing nanosuspension, prepared by using solvent anti solvent technology. Mirtazapine is practically insoluble in water which act as antidepressant .It was prepared as nano particles in order to improve its solubility and dissolution rate. Twenty formulas were prepared and different stabilizing agents were used with different concentrations such as poly vinyl pyrrolidone (PVPK-90), poly vinyl alcohol (PVA), poloxamer 188 and poloxamer 407. The ratios of drug to stabilizers used to prepare the nanoparticles were 1: 1 and 1:2. The prepared nanoparticles were evaluated for
... Show MoreIntroduction: Carrier-based gutta-percha is an effective method of root canal obturation creating a 3-dimensional filling; however, retrieval of the plastic carrier is relatively difficult, particularly with smaller sizes. The purpose of this study was to develop composite carriers consisting of polyethylene (PE), hydroxyapatite (HA), and strontium oxide (SrO) for carrier-based root canal obturation. Methods: Composite fibers of HA, PE, and SrO were fabricated in the shape of a carrier for delivering gutta-percha (GP) using a melt-extrusion process. The fibers were characterized using infrared spectroscopy and the thermal properties determined using differential scanning calorimetry. The elastic modulus and tensile strength tests were dete
... Show More