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.
Abstract
Locally natural occurring Iraqi rocks of Bauxite and Porcelanite (after pre calcinations at 1000oC for 1hr) were used, with the addition of different proportions of MgO and Al2O3, to prepare refractory materials. The effects of these additives on the physical and thermal properties of the prepared refractories were investigated.
Many batches of Bauxite/MgO, Bauxite/Al2O3, Bauxite/MgO/Al2O3, and Porcelanite/ MgO/Al2O3 were prepared. The mixture is milled and classified into different size fractions; fine (less than 45μm) 40%, middle (45-75μm) 40%, and coarse (75-106μm) 20% .
... Show MorePolyvinal alcohol was Cynoethylated , complex compound with Iodin in presence of Cu++ ions were preparated and their ultra violet (U.V) and infra red( IR) spectra were investigated. The prepared derivative and complexes were evaluated as antibacterial and antifungal agents following the standard dilution method. MIC(minimum inhibitory concentration) for each polymer using ten types of gram + ve and gram _ ve bacteria were determinated in addition to three types of fungi. The results obtainded showed that MIC, s were around 0.0011 × 103 molar for different polymetric derivatives tried.
The purpose of this study was to develop poloxamer-based in-situ gel of chloramphenicol aiming to increase bioavailability and prolong corneal contact time, controlling drug release, and enhancing ocular bioavailability. The in-situ gel was prepared using different concentrations of poloxamer 407 combined with hydroxypropyl methyl cellulose (HPMC) or carbapol 940 to achieve gelation temperature about physiological temperature and improve rheological behavior and gelling properties of poloxamer gel. The prepared formulations were evaluated for their appearance, pH, and sol-gel transition temperature. The formulations F2, F3, and F5 have a gelation temperature within the accepted range 35-370C an
... Show MoreA transdermal drug delivery system (TDDS) is characterized by the application of medications onto the skin's surface to deliver drugs at a controlled and predefined rate through the skin. Spanlastics, an elastic nanovesicle capable of transporting various pharmacological substances, shows promise as a drug delivery carrier. It offers numerous advantages over traditional vesicular systems applied topically, including enhanced stability, flexibility in penetration, and improved targeting capabilities. This study aims to develop meloxicam (MX)-loaded spanlastics gel as skin delivery carriers and to look into the effects of formulation factors like Tween80, Brij 35, and carbopol concentration on the properties of spanlastics gel, like pH, drug
... Show MoreThe sorption of Cu2+ ions from synthetic wastewater using crushed concrete demolition waste (CCDW) which collected from a demolition site was investigated in a batch sorption system. Factors influencing on sorption process such as shaking time (0-300min), the initial concentration of contaminant (100-750mg/L), shaking speed (0-250 rpm), and adsorbent dosage (0.05-3 g/ml) have been studied. Batch experiments confirmed that the best values of these parameters were (180 min, 100 mg/l, 250 rpm, 0.7 g CCDW/100 ml) respectively where the achieved removal efficiency is equal to 100%. Sorption data were described using four isotherm models (Langmuir, Freundlich, Redlich-Peterson, and Radke-Prausnitz). Results proved that the pure ads
... Show MorePhotonic crystal fiber interferometers are widely used for sensing applications. In this work, solid core-Photonic crystal fiber based on Mach-Zehnder modal interferometer for sensing refractive index was presented. The general structure of sensor applied by splicing short lengths of PCF in both sides with conventional single mode fiber (SMF-28). To apply modal interferometer theory; collapsing technique based on fusion splicing used to excite higher order modes (LP01 and LP11). Laser diode (1550 nm) has been used as a pump light source. Where a high sensitive optical spectrum analyzer (OSA) was used to monitor and record the transmitted. The experimental work shows that the interference spectrum of Photonic crystal fiber interferometer
... Show MoreKetoprofen is a non-steroidal anti-inflammatory (NSAID) drug with analgesic, anti-inflammatory, and antipyretic effects. It is widely used in the treatment of inflammation and pain associated with rheumatic disorders such as rheumatoid arthritis, osteoarthritis, and in soft tissue injury. The purpose of this study was to prepare an oral disintegrating tablets of ketoprofen by simple method. The tablets were prepared by direct compression method and different ratios of various subliming agents or superdisintegrants were incorporated. Then these tablets were evaluated for hardness, friability, weight variation, water absorption ratio, disintegrating time and dissolution time. The results showed that Formula F11 batch had short disint
... Show MoreBilastine (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
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