Objective: The aim of this study was to formulate and in vitro evaluate fast dissolving oral film of practically insoluble bromocriptine mesylate to enhance its solubility and to improve its oral bioavailability by avoiding first pass effect as well as to produce an immediate release action of the drug from the film for an efficient management of diabetes mellitus type II in addition to an improvement of the patient compliance to this patient- friendly dosage form. Methods: The films were prepared by the solvent casting method using hydroxypropyl methylcellulose of grades (E3, E5, E15), polyvinyl alcohol (PVA), pectin and gelatin as film-forming polymers in addition to polyethene glycol 400 (PEG400), propylene glycol (PG) and glycerin were used as a plasticizer. Poloxamer 407 was used as a surfactant, sodium saccharin as a sweetening agent, citric acid as a saliva stimulating agent, vanilla as a flavouring agent and crospovidone as a super disintegrant. The prepared films then tested for physical characterization, thickness, weight uniformity, mechanical characteristics (folding endurance, tensile strength, percent elongation and Young's modulus), surface pH, in vitro disintegration time, drug content and an in vitro drug release. Results: Films were found to be satisfactory when evaluated for physical characterization, thickness, weight uniformity, mechanical tests, in vitro disintegration time, folding endurance, drug content and an in vitro drug release. The surface pH of all the films was found to be neutral or minor change. Films in vitro drug release studies were also done using USP dissolution apparatus type II (paddle type). The in vitro drug release profile in the optimized formulation F14 was gave 86.8 % of drug released at 2 min. The optimized formulation F14 was also showed satisfactory pH (6.2±0.2), drug content (99.2±0.5%), the disintegration time of 9.2±0.1 seconds and the time needed for 80% of medication to be released (T80 %) was 1.35 minute. Conclusion: The bromocriptine mesylate fast dissolving oral film was formulated. The given film disintegrates within nine seconds which release the drug rapidly and gives an action.
Diacerein (DCN) is a semi-synthetic anthraquinone derivative of Rhein that is indicated for the management of osteoarthritis. Diacerein exhibits poor dissolution in the GIT fluids and suffers from low bioavailability upon oral administration in addition to the laxative effect of Rhein metabolites. The aim of the present study was to develop novasomal vesicles with optimized entrapment efficiency and size to serve as a carrier for transdermal delivery of diacerein. Novasomal vesicles were prepared by thin film hydration method thin film hydration. The prepared vesicles were optimized utilizing different surfactant to cholesterol molar ration, sonication type, different sonication times and varying fatty acid level. The prepared vesicles were
... Show MoreOndansetron HCl (OND) is a potent antiemetic drug used for control of nausea and vomiting associated with cancer chemotherapy. It exhibits only 60 – 70 % of oral bioavailability due to first pass metabolism and has a relative short half-life of 3-5 hours. Poor bioavailability not only leads to the frequent dosing but also shows very poor patient adherence. Hence, in the present study an approach has been made to develop OND nanoparticles using eudragit® RS100 and eudragit® RL100 polymer to control release of OND for transdermal delivery and to improve patient compliance.
Six formulas of OND nanoparticles were prepared using nanoprecipitation technique. The particles sizes and zeta potential were measured
... Show MoreAbstract: The article aimed to formulate an MLX binary ethosome hydrogel for topical delivery to escalate MLX solubility, facilitate dermal permeation, avoid systemic adverse events, and compare the permeation flux and efficacy with the classical type. MLX ethosomes were prepared using the hot method according to the Box–Behnken experimental design. The formulation was implemented according to 16 design formulas with four center points. Independent variables were (soya lecithin, ethanol, and propylene glycol concentrations) and dependent variables (vesicle size, dispersity index, encapsulation efficiency, and zeta potential). The design suggested the optimized formula (MLX−Ethos−OF) with the highest desirability to perform the
... Show MoreAntacids have been widely used in the treatment of various gastric and duodenal disorders such as heartburn, reflux esophagitis, gastritis, irritable stomach, gastric and duodenal ulcers. A pH-responsive of bi-polymer of sodium alginate and pectin have been studied as raft-forming polymers using sodium bicarbonate and calcium carbonate as gas-generating and calcium ion sources. The aim of study was to formulate and evaluate mono and bilayer tablets of floating and sustained release antacid delivery systems using sodium carboxy methyl cellulose as a gel forming substance, calcium and magnesium carbonate as sources of acid neutralizing and carbon dioxide gas generators agents upon contact with acidic solution. The effect of the formulation
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Sumatriptan(ST) is a selective agonist at serotonin 5-HTI receptors, as well as 5-HT1B/1D subtypes. It is effective for acute migraine attacks, but has a short half life (about 2 hours) and low oral bioavailability (15%). The purpose of this study was to develop and optimize nasal mucoadhesive in-situ gel(IG) of ST to enhance nasal residence time for migraine management. Cold method was used to prepare different formulas of ST nasal IG, using thermosensitive polymers (poloxamer 407 alone or with poloxamer 188) with a mucoadhesive polymer hyaluronic acid (HA) which were examined for gelation temperature and gelation time, pH, drug content, gel strength, spreadability, muc
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The aim of this study was to prepare rebamipide ocular inserts in order to extend its release on the ocular surface for dry eye treatment. Solubility study was applied to the drug with or without l-arginine using different solvents. Solvent casting technique was used to prepare the inserts; l-arginine was used to solubilize the drug, hydroxypropyl methylcellulose grades (E5 and K15M) and poly ethylene glycol 200 were used as excipients. The inserts were evaluated for their physical and mechanical properties, moisture loss% and absorption %, surface pH, and in-vitro drug release. The use l-arginine exhibited an enhancement of rebamipide solubility in both deionized water and phosphate buffer (pH 7.4) by a
... Show MoreCinema artist work has not been achieved without location indications ; places are of cultured indications and its effect on behaviors and trends. Location is an important element as to convey meanings via its interaction with the personality about which it has been written may studies. Despite location occupies huge spaces within social and philosophical Drama branches , but it has a strong connection with the art world since it reflects reality of global theories in different fields. Audio and visual speech in Cinema have connected with the environmental effectiveness resulted from location which the sensual understanding interacts with in a way that suits Movie. Location consists of mixing elements of Movie and it in return interacts
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