Venlafaxine Hydrochloride Granules Using Natural Polymers as Multiparticulate Drug Delivery System (original) (raw)
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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...
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...
2013
The main objective of present work is to develop mi ni tablets filled hard gelatin capsules. Mini table ts filled hard gelatin capsules drug delivery system comprises of 5 matrix mini-tablets weighing 50 mg encapsulated i n hard gelatin capsule (size 00). For achieving the sustai ned release, various viscosity grades of Hydroxy pr opyl methyl cellulose polymer (HPMC K4M, K100M, K200M) and Kollidone were used. The mini-tablets were prepared by wet granulation method. The prepared mini-tablets were subjected for pre-compressional and post-compressio nal evaluation. The compatibility of drug with ingredie nts used were checked by DSC and FTIR studies. Accelerated stability studies were carried out as per ICH guide lines for the best formulation. The pre-compression and post compression parameters were within prescribed limits. The in vitro performance of the best formulation showed sustained drug release for a period of 12 h. The DS C and FTIR results revealed that there was no inter a...
Applications of Polymers as Pharmaceutical Excipients in Solid Oral Dosage Forms
Over the last few decades, polymers have been extensively used as pharmaceutical excipients in drug delivery systems. Pharmaceutical polymers evolved from being simply used as gelatin shells comprising capsule to offering great formulation advantages including enabling controlled/slow release and specific targeting of drugs to the site(s) of action (the " magic bullets " concept), hence hold a significant clinical promise. Oral administration of solid dosage forms (e.g., tablets and capsules) is the most common and convenient route of drug administration. When formulating challenging molecules into solid oral dosage forms, polymeric pharmaceutical excipients permit masking undesired physicochemical properties of drugs and consequently, altering their pharmacokinetic profiles to improve the therapeutic effect. As a result, the number of synthetic and natural polymers available commercially as pharmaceutical excipients has increased dramatically, offering potential solutions to various difficulties. For instance, the different polymers may allow increased solubility, swellability, viscosity, biodegradability, advanced coatings, pH dependency, mucodhesion, and inhibition of crystallization. The aim of this article is to provide a wide angle prospect of the different uses of pharmaceutical polymers in solid oral dosage forms. The various types of polymeric excipients are presented, and their distinctive role in oral drug delivery is emphasized. The comprehensive know-how provided in this article may allow scientists to use these polymeric excip-ients rationally, to fully exploit their different features and potential influence on drug delivery, with the overall aim of making better drug products.
Whether mini-tablets (tablets, diameters 6 mm) belong to single- or multiple-unit dosage forms is still questionable. Accordingly, Pharmacopoeial evaluation procedures for mini-tablets are lacking. In this study, the aforementioned points were discussed. Moreover, their potential for oral controlled delivery was assessed. The antidepressant venlafaxine hydrochloride (Vx), a highly soluble drug undergoing first pass effect, low bioavailability and short half-life was selected as a challenging payload. In an attempt to weigh up mini-tablets versus pellets as multiparticulate carriers, Vx-loaded mini-tablets were compared to formulated pellets of the same composition and the innovator Effexor1XR pellets. Formulations were prepared using various polymer hydrogels in the core and ethyl cellulose film coating with increasing thickness. Mini-tablets (diameter 2 mm) showed extended Vx release (<60%, 8 h). Indeed, release profiles comparable to Effexor1XR pellets were obtained. Remarkably higher coating thickness was required for pellets to provide equivalent retardation. Ethyl cellulose in the core ensured faster release due to polymer migration to the surface and pore formation in the coat. mini-tablets showed higher stability to pellets upon storage. Industrially speaking, mini-tablets proved to be superior to pellets in terms of manufacturing, product quality and economical aspects. Results point out the urgent need for standardized evaluation procedures for mini-tablets.