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.
Isradipine related to dihydropyridine (DHP) class of calcium channel blockers (CCBs). It is used to treat hypertension, angina pectoris, as well as Parkinson disease. It goes under the BCS class II drug (low solubility-high permeability). The drug will experience extensive first-pass metabolism in liver, thus, oral bio-availability will be approximately15 to 24 %.
The aim of the study is preparing stable oral oil in water (o/w) nanoemulsion of isradipine to promote the colloidial dispersion of isradipine in the nano range, so that it may be absorded by intestinal lymphatic transport in order to avoid hepatic first-pass metabolism (israpidi
... Show MoreDrug solubility and dissolution remain a significant challenge in pharmaceutical formulations. This study aimed to formulate and evaluate repanglinide (RPG) nanosuspension-based buccal fast-dissolving films (BDFs) for dissolution enhancement. RPG nanosuspension was prepared by the antisolvent-precipitation method using multiple hydrophilic polymers, including soluplus®, polyvinyl alcohol, polyvinyl pyrrolidine, poloxamers, and hydroxyl propyl methyl cellulose. The nanosuspension was then directly loaded into BDFs using the solvent casting technique. Twelve formulas were prepared with a particle size range of 81.6-1389 nm and PDI 0.002-1 for the different polymers. Nanosuspensions prepared with soluplus showed a favored mean particle size o
... Show MoreFast dissolving film can be defined as a dosage form, which when placed in the oral cavity. It will rapidly disintegrate and dissolves to release the medication for oral mucosal absorption or allow for the gastrointestinal absorption to be achieved when swallowed.
Flurbiprofen is non-steroidal anti-inflammatory agent with antipyretic and analgesic properties and can be used in low doses 8.75 mg as analgesic and anti inflammatory agent in sore throat infection. This study aims to formulate flurbiprofen as oral dissolving films, to improve the effective relief of pain with severe sore throats with little or no adverse effect.
Nine formulas were prepared using solvent-casting method, and t
... Show MoreThe objective of the study was to develop microneedle (MN) patch, with suitable properties to ensure the delivery of a therapeutic level of lornoxicam (LXM) in a period suitable to replace parenteral administration in patients, especially those who fear needles. The used polymers were cold water-soluble polyvinyl alcohol (PVA) and polyvinylpyrrolidone (PVP) of low molecular weight with PEG 400 as plasticizer and Tween 80 (to enhance the release) using micro molding technique. Patches were studied for needle morphology, drug content, axial fracture force measurement and drug release while the optimized formulas were further subjected to pH measurement, folding endurance, ex vivo permeation study, histopathology study, stability study and
... Show MoreOndansetron hydrochloride (ONH) is a very bitter, potent antiemetic drug used for the treatment and/or prophylaxis of chemotherapy or radiotherapy or postoperative induced emesis. The objective of this study is to formulate and evaluate of taste masked fast dissolving tablet (FDTs) of ONH to increase patient compliance.
ONH taste masked granules were prepared by solid dispersion technique using Eudragit E100 polymer as an inert carrier. Solvent evaporation and fusion melting methods were used for such preparation.
Completely taste masking with zero release of drug in phosphate buffer pH 6.8was obtained from granules prepared by solvent evaporation method using drug: polymer ratio of 1:2, from which four formulas pas
... Show MoreAzithromycin is the drug of choice in the treatment of several bacterial infections, most often those causing middle ear infection, bronchitis, pneumonia, typhoid and sinusitis. It’s also effective against certain urinary tract infections and venereal diseases. This study was carried out to prepare an acceptable suspension either as dry physical mixture powder or granules to be reconstituted, through studying the effect of various type and concentration of suspending agent (xanthan gum, hydroxypropyl methylcellulose (HPMC), either alone or in combination) on the release profile of the drug. The best prepared suspension formulas (H& III) were selected depending on the dissolution profile of each formulas and then compared with
... Show MoreMetoprolol is a β1 adrenergic blocker used in treatment of heart diseases. Metoprolol (100mg) tablets was formulated as a modified release oral system utilizing the concept of bilayer system, first layer contained (30mg) as immediate release and the other (70mg) in the sustained release matrix. The immediate release layer consisted of lactose or microcrystalline cellulose as diluents with sodium starch glycolate or sodium croscarmellose as disintegrants. The result showed that the layer contains microcrystalline cellulose and 2% sodium starch glycolate gave disintegration time similar to that of conventional metoprolol tartrate tablet. This result was subjected in the subsequent preparation of the bilayer tablet. The
... Show MoreBackground: Simvastatin (SIM) is a lipid-lowering agent to prevent disorders caused by clogged blood vessels. Because of its low solubility, it has low bioavailability. The adsorption technique is effective in improving drug solubility and dissolution rate. Objective: To use magnesium aluminum silicate (MAS) as an adsorbent in combination with Soluplus® as a hydrophilic polymer to formulate SIM as immediate-release tablets (IRTs). Methods: We used the solvent evaporation method to make MAS-loaded SIM in the presence of Soluplus®, making sure that the ratio of SIM to MAS to SOLU was 1:6:3. We then used this mixture to make IRTs. Using the direct compression method, we made all of the SIM-IRT formulas. We used diluents like Avicel
... Show MoreObjective: The objective of this study was to prepare nanosuspension of a practical water insoluble antiulcer drug which is lafutidine to enhance the solubility, dissolution rate with studying the effect of different formulation variables to obtain the best formula with appropriate physical properties and higher dissolution rate.Methods: Nanosuspension of lafutidine was prepared using solvent anti-solvent precipitation method using Polyvinylpyrrolidone K-90(PVP K-90) as the stabilizer. Ten formulations were prepared to show the effect of different variables in which two formulations showed the effect of stabilizer type, three formulations showed the effect of stabilizer concentration, two formulations showed the effect of combinatio
... Show MoreBackground: Bilastine is a non-sedating, second-generation antihistamine used to treat urticaria and allergic conjunctivitis. Objective: to formulate and test bilastine as a mucoadhesive ophthalmic in situ gel in order to extend its presence at site for longer time and help treat conjunctivitis and allergic rhinitis. Methods: We prepared formulations using different concentrations of poloxamers (Poloxamer 407 (P407) and Poloxamer 188 (P188)) in combination with hydroxypropyl methyl cellulose (HPMC). The prepared formulas were evaluated for their physicochemical properties, sol-gel transition temperature, viscosity, mucoadhesive strength, drug release, and kinetic modeling. Results: The prepared in situ gels were clear and transparen
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