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.
Clopidogrel is a prodrug that must be transformed into an active metabolite by hepatic cytochrome P450 (CYP) isoenzymes to prevent platelet clotting. Polymorphisms of the CYP2C19 gene can cause a reduction or complete loss of CYP2C19 enzyme activity resulting in inhibiting clopidogrel metabolism, effectiveness and increase stroke recurrence risk in ischemic stroke patients. This study aims to investigate the correlation between genetic polymorphisms in CYP2C19*2 and*3 and recurrent risk in patients with ischemic stroke taking clopidogrel 75mg in Kurdistan region –Iraq. This retrospective case-control study was carried out at Kurdistan, Erbil, Medicina medical center, and Rizgary general hospital from January 2021 to
... 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 MoreFrictional resistance occurs whenever sliding happens, negatively impacting treatment outcomes and duration. It is a clinical challenge and must be dealt with efficiently to achieve the best orthodontic results. Aims of this study: compare and evaluate the static frictional forces under the wet condition to mimic the oral environment produced by using a polycrystalline ceramic bracket, monocrystalline ceramic bracket, 0.014 of an inch nickel-titanium (Rhodium coated archwires, and ilusio aesthetic archwires), and 0.019 x 0.025 of an inch stainless steel (Rhodium coated archwires, and ilusio aesthetic archwires). Ninety-six aesthetic brackets (48 monocrystalline and 48 polycrystalline brackets) were used and stored in different incub
... Show MorePolymeric microsphere devices occupy a wide range in the field of controlled drug delivery. Subcutaneous injectable preparations of Poly(Lactide-co-Glycolide) (PLGA) microsphere of Daptomycine were prepared by solvent extraction/evaporation technique using different copolymers ratio and molecular weights. Four formulations were prepared (F1-F4) and characterized in term of particle size, surface morphology, bulk density and porosity in addition to the drug content. The effects of the above parameters on the in-vitro release study were evaluated. These formulas were evaluated also for their in-vivo release profile using rat (as an animal model) and
... Show MoreBackground: Coronary artery disease (CAD) is one of the leading causes of death worldwide. Clopidogrel, antiplatelet drug, has been widely used for management of CAD. Arylesterase, the activity of Paraoxonase-1 (PON-1), is mainly contributed in the biotransformation of clopidogrel to its active thiol form. The purpose of this study was to investigate the effect of receiving clopidogrel drug on the arylesterase activities in CAD patients. The effect of receiving clopidogrel drug on the antioxidant activity of arylesterase was also monitored by determination of malondialdehyde (MDA) level. Methods: One hundred CAD patients, who were followed-up for 5 days after reciving clopidogrel, and 50 healthy volunteers were included in our study
... Show MoreThe product of rn-paracompact and rn-strongly paracompact are briefly disc. ussed.
Lasmiditan (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.
This study aims to encapsulate atenolol within floating alginate-ethylcellulose beads as an oral controlled-release delivery system using aqueous colloidal polymer dispersion (ACPD) method.To optimize drug entrapment efficiency and dissolution behavior of the prepared beads, different parameters of drug: polymer ratio, polymer mixture ratio, and gelling agent concentration were involved.The prepared beads were investigated with respect to their buoyancy, encapsulation efficiency, and dissolution behavior in the media: 0.1 N HCl (pH 1.2), acetate buffer (pH 4.6) and phosphate buffer (pH 6.8). The release kinetics and mechanism of the drug from the prepared beads was investigated.All prepare
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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
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