Oral fast dissolving films (OFDFs) are the most innovative oral solid pharmaceutical dosage form, especially for elderly and pediatric patients who may have dysphagia. Bilastine (BLA), is a second – generation antihistamine used to manage allergy symptoms; it is very slightly soluble in water. The main objective of this research was to enhance the solubility and dissolution rate of BLA by complexation technique. Ternary complex of BLA: methyl β- cyclodextrin (M-β-CD): soluplus® 5% w/w was prepared via solvent evaporation technique as a trial to enhance its solubility to be prepared as OFDF by incorporated into aqueous polymeric solution. Seven formulas of OFDFs were prepared using the solvent casting method using Polyvinyl alcohol, Hydroxy propyl methyl cellulose E5, and Pullulan as polymers that form film, PEG 400, and glycerin as plasticizers. The prepared films were estimated for their physical, and mechanical properties, drug content, and dissolution rate. The results showed that,the prepared complex enhanced the solubility of the BLA in water (11 times more than the pure BLA in distilled water) and it was easily utilized for the preparation of the OFDFs. The PVA-based formulation in the presence of glycerin as a plasticizer (F4), showed a homogenous clear film with accepted folding endurance (300), the shortest disintegration time (16.66 seconds), and complete release within five minutes. In conclusion, complexation of BLA with M-β CD was an efficient method for enhancing its solubility and dissolution rate to be easily prepared as OFDF with acceptable physical properties.
Orphenadrine is an anticholinergic ,antimuscarinic , centrally acting skeletal muscle relaxant .It presents in the form of citrate and HCl salts which are used in treatment of the symptoms of mild Parkinson's disease and also it is used as adjuvant with other drugs in the therapy .
Many trials were made to formulate Orphenadrine citrate as a plain tablet using wet granulation or direct compression technique in order to get a satisfactory formula through studying the effect of various factors such as binders , diluents and disintegrants types .
The best formula was obtained by using Poly Vinyl Pyrolidine (PVP) as a binder also the results indicated that starch and mannitol
... Show MoreNystatin is the drug of choice for treatment of cutaneous fungal infections with main disadvantage that is the need for multiple applications to achieve complete eradication which may reduce patient compliance. Microparticles offer a solution for such issue as they are one of sustained release preparations that achieve slow release of drug over an extended period of time. The objectives of this study were to fabricate nystatin-loaded chitosan microparticles with the ultimate goal of prolonging drug release and to analyze the influence of polymer concentration on various properties of microparticles. Microparticles were prepared by chemical cross-linking method using glutaraldehyde as cross-linking agent. Five formulas, namely N1C1, N1C2,
... Show MoreBackground: 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 fo
... 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 MoreThe preferred route of drug administration is the oral route, but drugs with narrow absorption window in the gastrointestinal tract are still challenging. The ability to extend and monitor the gastric emptying time is a valuable tool for processes remaining in the stomach longer than other traditional dosage forms.
The purpose of this study was to formulate and evaluate gastroretentive superporous hydrogel (SPH) of carvedilol with view to improve its solubility and increase gastric residence time in order to get sustained release formulas via utilization of various kinds and concentrations of hydrophilic polymers then after, incorporate the best prepared formula into capsules.
Sixteenth formulae of SPH h
... Show MoreClotrimazole nail lacquer was created using this research, which also included the incorporation of two different kinds of polymers. (Eudragit RL 100 and ethyl cellulose) in various concentrations, as well as castor oil as a plasticizer, salicylic acid as a keratolytic agent, and N-acetylcysteine as a penetration enhancer. The objective was to optimize the selection of polymers and their concentrations to enhance release efficacy based on in vitro permeability experiments, while also ensuring favorable film characteristics, such as flexibility, gloss, adhesive qualities, drying time, non-volatile content, viscosity, and water resistance. Formulation F3 was selected as the superior formula considering several parameters, including excellent
... Show MoreAt present, numerous novel chemical compounds face challenges related to their limited solubility in aqueous environments. These compounds are classified under the Biopharmaceutical Classification System (BCS) as either class II or class IV substances. Different carriers were used to increase their solubility. Candesartan cilexetil (CC) is one of the most widely used antihypertensive drugs, which belongs to class II drugs. The aim of this research was to enhance the solubility and dissolution rate of CC through a complexation approach involving β-cyclodextrin and its derivatives, specifically hydroxypropyl beta cyclodextrin (HP-β-CD), methyl beta cyclodextrin (M-β-CD), and sulfonyl ether beta-cyclodextrin (SBE-β-CD), serving as
... Show MoreBilastine (BLS) is non-sedating new-brand H1 antihistamine that has selective peripheral effects, the drug has a problem of an insufficient aqueous solubility and accordingly low dissolution rate, and low bioavailability. Solid dispersion (SD) is one of the most effective techniques for improving the solubility and the dissolution rate of poorly soluble drugs by the dispersion of drug within an inert hydrophilic carrier. The aim of this study is to increase the solubility and dissolution rate of the BLS using SD technique. Twenty-nine BLS SD formulas were prepared using different carrier polymers include Pluronic 407 (Poloxamer407), Poloxamer188, Urea, Polyethylene glycol 6000 (PEG6000) and Polyvinylpyrrolidone (PVP K30) and em
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