Evaluation of the effect of carrier material on modification of release characteristics of poor water soluble drug from liquisolid compacts

Abstract

Liquisolid compact is a novel dosage form in which a liquid medication (liquid drug, drug solution/dispersion in non-volatile solvent/solvent system) is converted to a dry, free flowing powder and compressed. Objective of the study was to elucidate the effect of carrier material on release characteristics of clopidogrel from liquisolid compacts. Different formulations of liquisolid compacts were developed using microcrystalline cellulose, starch maize, polyvinyl pyrollidone and hydroxypropyl methylcellulose as carrier material in three concentrations (40, 30 and 20%, w/w). Liquid vehicle was selected on the basis of solubility of clopidogrel. Colloidal silicondioxide was used as coating material and ratio of carrier to coating material was kept 10. A control formulation comprised of microcrystalline cellulose (diluents), tabletose-80 (diluents), primojel (disintegrant) and magnesium stearate (lubricant) was prepared by direct compression technique and was used for comparison. All the formulations were evaluated at pre and post compression level. Acid solubility profile showed higher solubility in HCl buffer pH2 (296.89±3.49 μg/mL). Mixture of propylene glycol and water (2:1, v/v) was selected as liquid vehicle. Drug content was in the range of 99–101% of the claimed quantity. All the formulations showed better mechanical strength and their friability was within the official limits (<1%). Microcrystalline cellulose and starch maize resulted in faster drug release while polyvinyl pyrollidone and HPMC resulted in sustaining drug release by gel formation. It is concluded from results that both fast release and sustained release of clopidogrel can be achieved by proper selection of carrier material.

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 ).…”

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 27,28 , gastro retentive system as oated tablets 29 , high density tablets 30 or oated osmotic capsules 31 , liquisolid compact 32,33 , micro-emulsion 34 , nano-suspension 35 , oral disintegrating tablets 36 , or fast disintegrating lms 37 , and as FDC system 38,39 .…”

Enhancement of Pioglitazone Hydrochloride Solubility Through Liquisolid Compact Formulation Using Novel Carrier Neusilin US2

“…By simply blending the liquid medication with specific powder excipients known as the carrier (cellulose, starch, lactose, etc.) and coating (silica) materials, the liquid medication can be transformed into a dry-looking, nonadherent, free-flowing, and easily compressible powder [6,7].…”