Preparation and In-Vitro Evaluation of Clopidogrel Bisulfate Liquisolid Compact

Abstract

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.

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“…Then compress the tablets of Atorvastatin calcium by using a Tablet punching machine. This is the general method for the preparation of the liquisolid compact 12,13 .…”

Apixaban and clopidogrel in a fixed-dose combination: Formulation and in vitro evaluation

“…Many formulations were developed later in different dosage forms to enhance CLOP solubility and bioavailability. A literature search revealed formulating CLOP as IR tablets ( Kavya et al, 2014 , Kumar et al, 2013 ), gastro retentive system as floated tablets ( Rao and Lakshmi, 2014 ), high-density tablets ( Desai and Purohit, 2017 ) or floated osmotic capsules ( Shah and Prajapati, 2019 ), liquisolid compact ( Ali et al, 2021 , Mohammed and Mohammed, 2018 ), micro-emulsion ( Patel et al, 2010 ), nano-suspension ( Jassim and Hussein, 2014 ), oral disintegrating tablets ( Mahrous et al, 2016 ), or fast disintegrating films (Alladi Saritha, 2018 ), and as FDC system ( Huang et al, 2011 , Seo and Han, 2019 ).…”

Solubility and Dissolution Rate Enhancement of Aceclofenac by Solid Dispersion Employing Kneading and Solvent Evaporation Techniques

“…The oral delivery of drugs poses a significant challenge because more than 40% of new chemical entities are practically insoluble in water. Poor aqueous solubility provides challenges, but also opportunities to scientists working in formulation development (3) . Non-steroidal anti-inflammatory drugs (NSAIDs) are the most frequently prescribed class of medication, with approximately 5-10% of all prescriptions written annually.…”