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      • KCI등재

        Solubility modulation of bicalutamide using porous silica

        Tarique Meer,Ritesh Fule,Deepak Khanna,Purnima Amin 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.4

        Objective of the present study was to explore the potential of porous silica (AEROPERL 300 Pharma)in modulating dissolution kinetics of poorly water soluble drug bicalutamide (BCL). The drug release from the developed formulation was found to be significantly higher as compared to neat BCL. This improved release kinetics of BCL may be attributed to high surface area, improved wettability and decreased crystallinity. Solid state characterization of the developed formulation was carried out with respect to IR, XRPD, SEM, DSC and dissolution. The proposed system showed a significant capability for the solubility enhancement of BCL. The dissolution profile from BCL-AEROPERL 300 Pharma (AP) system was fitted into various drug release kinetics models, in order to understand the BCL release mechanism.

      • KCI등재

        Preparation and evaluation of carbamazepine loaded fibrous electrospun mats of starch

        Tarique Ali Meer,Mirza Shehzad Baig,Purnima D. Amin 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.3

        The preset work deals with preparation of fibrous electrospun mats of starch (FEMOS) carrier, from naı¨ve starch, through a process of electrospinning. The developed FEMOS was explored for the solubility enhancement of poorly water soluble drug carbamazepine. Solid state characterization was performed with respect to Fourier transform infra-red spectroscopy, X-ray diffraction, scanning electron microscopy, contact angle determination, dissolution kinetics, and differential scanning calorimetry. Rapid release profiles were observed when the carbamazepine was loaded on FEMOS. This effect may be due to high surface area, improved wettability and reduced crystallinity of the loaded drug on FEMOS. The developed formulation was found to have a similar in vivo performance as compared to marketed formulation TegretolⓇ.

      • KCI등재

        Preparation and characterisation of lornoxicam solid dispersion systems using hot melt extrusion technique

        Ritesh Fule,Tarique Meer,Purnima Amin,Dinesh Dhamecha,Shyam Ghadlinge 한국약제학회 2014 Journal of Pharmaceutical Investigation Vol.44 No.1

        The aim of the research study was to investigatethe ability of Soluplus and surfactant individually aswell as in combination to improve the solubility, subsequentlythe dissolution profile of lornoxicam (LORX). Alaboratory size single screw rotating extruder with temperatureand speed control parameters employed during hotmelt extrusion (HME) processing of LORX along withpolymer-surfactant blends. Soluplus used as primarysolubilizing agent for preparing solid dispersion (SD). Along with Soluplus different concentrations of surfactantssuch as PEG 400, Lutrol F127, Lutrol F68 were usedto solve the permeability issues related to LORX. Encapsulationof LORX particles inside the molten matrix ofpolymer-excipient blend was confirmed by DSC, XRD andFT-IR. Drug excipient microscopic interaction was furtherconfirmed by scanning electron microscopy (SEM). Depending upon the ratio of the polymer and surfactantsused, the solubility of the hot melt extruded LORX wasimproved and found to be in the range 35–86 lg/ml (actualaqueous solubility of LORX was found to be 0.0083 lg/ml). Dissolution profile of the extruded SD was improvedand was found to be in the range of 98–104 % within20 min (actual dissolution profile of LORX was found tobe 8 % at the end of 1 h). SEM and Raman images suggestthe formation of amorphous dispersion systems. SD wassubjected to stability studies as per ICH guidelines andfound to be stable after 6 months when analyzed by HPLC. SD prepared from HME significantly improves the solubilityand dissolution profile of LORX—a BCS class IIdrug.

      • KCI등재

        Formulation of highly purified fenugreek gum based silica lipid drug delivery system for simvastatin with enhanced dissolution rate and in vitro characterization

        Ajay Kumar Sav,Meer Tarique Ali,Ritesh Amol Fule,Purnima Dhanraj Amin 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.5

        In current study, highly purified fenugreek gum (HPFG) isolated by patented method explored as emulsifier and hydrophilic solid carrier in drug delivery system. Antihyperlipidemic drug simvastatin (SIM) was selected as drug model for the study as it is associated with poorly water solubility and low bioavailability problems (\5 %). A suitable HPFG-based silica lipid system composed of SIM (1.5 %), medium chain triglyceride Capmul MCM (10 %) as lipid phase, 0.6 % HPFG as emulsifier and HPFG 2.5 %, different grades colloidal silica (7.5 %)(Aerosil 300 Pharma, Aerosil 380 Pharma and Aeroperl 300 Pharma) as hydrophilic solid carriers was developed. The optimized HPFG-based silica lipid systems were characterized for physical characteristics like flow ability,compressibility, redispersiblity, solubility and in vitro drug release using USP apparatus II in pH 6.8 phosphate buffer. The system was also characterized for Fourier transform infrared spectroscopy, powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). The developed formulation was found to have excellent flow property, readily redispersiblity, better aqueous solubility and showed 3–4-fold increase in dissolution rate as compared to plain drug and marketed formulation (Simlo 10). Transition of crystalline drug to amorphous state was confirmed by DSC,PXRD and SEM studies. Enhanced dissolution rate and solubility possibly attributed to improved wetting, amorphous drug state and facilitated diffusion from lipid-based system. Thus developed HPFG-based silica lipid system provides an alternative means for SIM with enhanced dissolution rate and stability in oral solid dosage form.

      • KCI등재

        Synthesis and evaluation of octenyl succinate anhydride derivative of fenugreek gum as extended release polymer

        Ajay Kumar Sav,Ritesh Amol Fule,Meer Tarique Ali,Purnima Amin 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.5

        In current study, fenugreek gum (FG) plant derived product was investigated as a release retarding polymer. The octenyl succincate anhydride derivative of fenugreek gum (OSFG) was synthesized to introduce hydrophobic property and investigated for its drug release retarding property with reference to FG. The reaction was carried out in anhydrous conditions at different temperature (40–98 C) using NaHCO3 as a mild base catalyst and the influences of three factors such as reagent/substrate concentration,reaction temperature and time on the degree of substitution of OSFG were studied. Highly water-soluble metoprolol succinate (MPS) and poorly water-soluble carbamazepine (CBZ) were selected as model drug as for release studies. It was observed that increase in reaction temperature and reagent concentration resulted in high degree of substitution with significant decrease in viscosity. Reaction carried out at 98 C for 2 h showed high degree of substitution (0.133) with moderate retention of viscosity compared to plain FG. FTIR, DSC, XRD, solid state CPMAS 13C-NMR, and SEM studies provide structural information of synthesized OSFG. MPS ER tablet prepared with drug:OSFG:FG at the weight of 1:4:2 and CBZ ER tablet with drug:OSFG at the weight ratio of 1:3, respectively. Both formulations showed similar drug release profile compared to marketed formulations. Optimized tablet formulations were found to be stable under stability condition according to ICH guidelines. It was concluded that the developed formulations with OSFG have a release retarding property and can be used alone or in combination with other polymers for a controlled release.

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