Liquisolid compact is the most promising technique for increasing dissolution rate and bioavailability of poorly soluble drugs.Clopidogrel bisulfate is an oral antiplatelets used for treatment and prophylaxis of cardiovacular and peripheral vascular diseases related to platelets aggreagation.Clopidogrel has low solubility at high pH media of intestine and low bioavailability of a bout 50% after oral doses.The purpose of this work was to enhance dissolution pattern of clopidogrel through its formulation into liquisolid tablets.A mathematical model was used to calculate the optimum quantities of tween 80 , carrier (Avicel PH 102) and coating material (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures.The liquisolid tablets were evaluated for hardness, percent friability, weight variation, content uniformity , disintegration time and in vitro drug release profile.DSC , FTIR , XRD and SEM were used for assessment of physicochemical properties of drug and compatibility with excipients in the liquisolid compacts.The selected formulation (F2) released 92.2% of its content during first 10 min. compared to 13.6% of directly compressed tablet and 24.2% of marketed tablet. In conclusion the dissolution rate and bioavailability of clopidogrel can be enhanced to a great extent by liquisolid technique.
Abstract
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 MoreLasmiditan (LAS) is a recently developed antimigraine drug and was approved in October, 2019 for the treatment of acute migraines; however, it suffers from low oral bioavailability, which is around 40%.
This study aimed to improve the LAS bioavailability via formulation as nanoemulsionbased in situ gel (NEIG) given intranasally and then compare the traditional aqueous-LASsuspension (AQS) with the two successful intranasal prepared formulations (NEIG 2 and NEIG 5) in order to determine its relative bioavailability (F-relative) via using rabbits.
In this paper by using δ-semi.open sets we introduced the concept of weakly δ-semi.normal and δ-semi.normal spaces . Many properties and results were investigated and studied. Also we present the notion of δ- semi.compact spaces and we were able to compare with it δ-semi.regular spaces
The aim of present study was to develop solid and liquid self-microemulsifying drug delivery system of poorly water soluble drug mebendazole using Aerosil 200 as solid carrier. Microemulsions are clear, stable, isotropic liquid mixtures of oil, water and surfactant, frequently in combination with a co-surfactant having droplet size range usually in the range of 20-250 nm. Oleic acid, tween 80 and polypropylene glycol were selected as oil, surfactant and co-surfactant respectively and for preparation of stable SMEDDS, micro emulsion region was identified by constructing pseudo ternary phase diagram containing different proportion of surfactant: co-surfactant (1:1, 2:1 and 3:1), oil and water. In brief S/ CoS mix means su
... Show More(1) Background: Plant flavonoids are efficient in preventing and treating various diseases. This study aimed to evaluate the ability of hesperidin, a flavonoid found in citrus fruits, in inhibiting lipopolysaccharide (LPS) induced inflammation, which induced lethal toxicity in vivo, and to evaluate its importance as an antitumor agent in breast cancer. The in vivo experiments revealed the protective effects of hesperidin against the negative LPS effects on the liver and spleen of male mice. (2) Methods: In the liver, the antioxidant activity was measured by estimating the concentration of glutathione (GSH) and catalase (CAT), whereas in spleen, the concentration of cytokines including IL-33 and TNF-α was measured. The in vitro expe
... Show MoreBackground: Ceramic veneers represent the treatment of choice in minimally invasive esthetic dentistry; one of the critical factors in their long term success is marginal adaptation. The aim of the present study is to evaluate the marginal gap of ceramic veneers by using two different fabrication techniques and two different designs of preparation. Material and methods: A typodont maxillary central incisor used in the preparation from which metal dies were fabricated, which were in turn used to make forty stone dies. The dies divided into four experimental groups, each group had ten samples: A1: prepared with butt-joint incisal reduction and restored with IPS e.max CAD, A2: prepared with overlapped incisal reduction and restored with IPS e.
... Show MoreThis paper deals with the F-compact operator defined on probabilistic Hilbert space and gives some of its main properties.
Oro slippery tablets (OSTs) is a technique used to improve swallowing of tablets for patients with dysphagia. The aim of this study was to formulate irbesartan and hydrochlorothiazide as Oroslippery tablets (OST) containing 150 mg irbesartan and 25 mg hydrochlorothiazide for dysphagia patients. A simple and rapid method of analysis was developed and validated according to the ICH guideline using HPLC with UV detector. Tablets were prepared by direct compression and then coated with the slippery coat of three different concentrations of the slippering substance “xanthan gum’ (2%, 3% and 4%) in Opadry Colorcone® and evaluated according to USP. Slipperiness test was performed using Albino rabbits. Results showed that 2% xanthan gum gav
... Show MoreSilybum marianum, from which silymarin (SM) is extracted, is a medicinal herb. In the Biopharmaceutics Classification System, it is of the class II type, meaning it is almost completely insoluble in water. It has a number of therapeutic properties, including anti-inflammatory as well as properties that promote wound healing.
This research target is to promote the dissolution and solubility of SM by employing a technique called solid dispersion and then incorporating the formula of solid dispersion into a topical gel that can be used for wound healing.
Solid dispersion is a technique used to enhance solubility and dissolve pharmaceuticals that are not water-soluble. This method is widely used because of its low cos
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