Mini-tablets versus pellets as promising multiparticulate modified release delivery systems for highly soluble drugs (original) (raw)
Related papers
Venlafaxine Hydrochloride Granules Using Natural Polymers as Multiparticulate Drug Delivery System
2018
Aim: The present investigation endeavors the importance of natural polymers for the sustained oral drug delivery. In an attempt to weigh up the efficiency of natural polymers in sustained oral delivery, an antidepressant venlafaxine hydrochloride, a highly water-soluble drug was selected as a challenging model. Materials and Methods: Different formulations (F1-F12) were prepared using drug, xanthan gum (XG), guar gum (GG) at 1:1, 1:2, and 1:3 ratios, and different polymer blends of chitosan, XG, and GG at 1:1, 1:4, and 4:1 ratios. Multiparticulates (granules) were prepared using wet granulation method and then were filled into empty hard gelatin capsules. The prepared multiparticulate drug delivery systems (MDDS) were characterized for drug-excipient compatibility study, physical evaluation, and in vitro drug release. Results and Discussions: Fourier-transform infrared spectroscopy study confirmed the absence of chemical interactions between drug and polymers. Differential scanning ...
Current Drug Therapy
Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor, which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for a prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in a cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl was prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium stearate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification. In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release k...
2014
The current research aims to formulate Venlafaxine Sustained Release (VHL-SR) tablets using hydrophilic-hydrophobic polymers combination blends by melt granulation technique which highlights the novelty. The polymers selected for the present study have matrix forming properties. Results of FTIR studies have shown that there were no interactions between the polymers used and the drug VHL. Various formulations of VHL-SR tablets (F1-F16) using different combinations of hydrophilic and hydrophobic polymers viz. Carbopol 71G, HPMC K15M, PEO, sodium CMC, Eudragit RS100 and precirol were formulated. Prior pre-formulation studies carried out on powder blend showed good flow properties. Routine quality evaluations of the VHL-SR tablets showed the diameter of the tablets of all formulations were found to be 9.0±0.0 mm and thickness ranged between 2.08±0.08 to 2.25±0.14 mm, hardness 4.08±0.20-5.50±0.31 kg/cm 2 , percentage friability 0.24±0.03-0.45±0.01%, weight variation from 0-1.15%, drug co...
Objective: The objective of the proposed work was to investigate the method for the efficient encapsulation of highly water soluble venlafaxine hydrochloride into poly-e-caprolactone microspheres by water-in-oil-in-oil and water-in-oil-in water double emulsification technique and comparison for its controlled release properties. Method: The Venlafaxine loaded microspheres are prepared by water-in-oil-in-oil (w/o/w) and water-in-oil-in water (w/o/o) double emulsification technique. The compatibility study of drug with polymer was performed by Differential scanning caloriemetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). The prepared microspheres are studied for their particle size, drug entrapment efficiency. The microspheres are characterised by SEM and in-vitro release of Venlafaxine was studied in phosphate buffer pH 1.2 for 12 hours and further studied for kinetic modeling. Result: The precentage yield of Venlafaxine loaded microspheres of all the formulations were found better by w/o/w method(92.21% for F 3). The particle size was found in a range of 130-135 μm and 120-125 μm for both W/O/W and W/O/O formulations. The entrapment efficiency was found in F 5 formulation prepared by W/O/O method. While the in-vitro release of Venlafaxine showed a drug release below 60% after 12 h of study whereas the marketed formulation released above 90% within 6 h and the mechanism was found to be fickian type. Conclusion: The prepared poly-ε-caprolactone microsphere is capable of delivering Venlafaxine HCl over prolonged periods, making it a potential candidate for controlled drug delivery.
Aaps Pharmscitech, 2010
Several matrix tablet formulations (hydrophilic-based, wax-based, and three-layer tablets) were designed for controlling the release of the highly water soluble drug, venlafaxine hydrochloride (VenHCl) for once-daily administration. The three-layer tablets consist of non-swellable, compritol-based middle layers containing the drug to which hydrophilic top and bottom barrier layers were applied. A 23 full-factorial design was employed for optimization and to explore the effect of different variables on the release rate of the drug from the three-layer tablets. The optimized levels of each independent variable were based on the criterion of desirability. The calculated values of f 1 and f 2 were 4.131 and 79.356, respectively; indicating that the release profile of the optimized PEO layered tablet formulation is comparable to that of the target release model. The pharmacokinetic parameters of VenHCl from the optimized three-layer tablet was compared to the marketed extended release capsule as a reference in healthy human subjects using a randomized crossover design. In this study, the 90% confidence interval for AUC0–24 and AUC0−∞ are within (0.8–1.25), which satisfied the bioequivalence criteria. It could be concluded that a promising once-daily extended-release three-layer tablet of the highly water soluble drug, VenHCl, was successfully designed.
Brazilian Journal of Pharmaceutical Sciences, 2010
Blends of aqueous dispersion of a hydrophobic and hydrophilic polymer, namely Surelease®: hydroxypropyl methylcellulose (Surelease®: HPMC E15) were used as coating materials to control the drug release from coated pellets of the highly water soluble drug metoprolol succinate. Varying the polymer blends, ranges of drug release patterns were obtained at pH 6.8. The present study dealt with diffusion of drug through plasticized Surelease®/ hydroxypropyl methylcellulose (HPMC E15) films prepared by coating of drug and polymers onto non-pareil seeds using the solution layering technique. The release of metoprolol succinate from coated pellets was decreased with increased coating load of polymer. The optimized formulation was obtained by 3² full factorial design. The release profile revealed that the optimized formulation follows zero order release kinetics. The stability data showed no interaction for storage at 25ºC and 60% relative humidity.
The present study involves the development of porous osmotic tablets of Venlafaxine Hydrochloride in order to release the drug in sustained and predictable manner. Venlafaxine Hydrochloride is a unique antidepressant that differs structurally from other currently available antidepressants. Short biological half life, low bioavailability and frequent administration of drug led for rational development of 300mg sustained release osmotic tablets of Venlafaxine Hydrochloride that releases the drug and maintain the plasma drug concentration for more than 8hrs. The method of preparation of these SR osmotic tablets follows osmotic bursting pump model. Polymers like hydroxy propyl methyl cellulose (HPMC) K15M with lactose as diluents, magnesium stearate as glidant and talc as lubricant were selected for sustaining the drug release.
FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF VENLAFAXINE HYDROCHLORIDE
The aim of study was formulate and evaluate floating microspheres of highly water soluble drug venalfaxine HCl, using cellulose acetate and eudragit RS100 polymers. The microspheres were prepared by solvent evaporation method. The prepared microsphere showed good drug loading capacity and floating ability. The particle size was ranged between 50 μm to 200 μm depends on the drug polymer ratio. The SEM study revealed that microspheres were good spherical geometry and uniform size. FTIR studies of drug loading microspheres showed no interaction of drug and polymers. The in vitro release studies were performed in 900 ml of 0.1N HCl for 12 h using USP XXIV dissolution apparatus. Release studies showed that microspheres that able to release the drug in sustain manner. Selected formulations were subjected to kinetics studies and stability studies. The release kinetics studies showed that the release the first order diffusion control and n value obtain from Higuchi model showed the release mechanism. Stability studies indicated that developed microspheres were stable and retain their pharmaceutical properties at room temperature and 40ºc/75% RH of one month.