Current Issue : October - December Volume : 2013 Issue Number : 4 Articles : 5 Articles
Over the last three decades industrial adaptability has allowed hot-melt extrusion (HME) to gain wide acceptance and has already\r\nestablished its place in the broad spectrum of manufacturing operations and pharmaceutical research developments. HME has\r\nalready been demonstrated as a robust, novel technique to make solid dispersions in order to provide time controlled, modified,\r\nextended, and targeted drug delivery resulting in improved bioavailability as well as taste masking of bitter active pharmaceutical\r\ningredients (APIs). This paper reviews the innumerable benefits of HME, based on a holistic perspective of the equipment,\r\nprocessing technologies to the materials, novel formulation design and developments, and its varied applications in oral drug\r\ndelivery systems....
Aims: The aim of this study was to explore the practicability of preparation of solid lipid nanoparticles of Glyceryl monostearate containing Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs. The physicochemical properties of the prepared formulae like particle size, drug entrapment efficiency, drug loading capacity, yield content and in-vitro drug release behavior were also measured. \r\nMethodology: Solid lipid nanoparticles loaded with three model lipophilic drugs were prepared by high shear hot homogenization method. The model drugs used are Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide. Glyceryl monostearate was used as lipid core; Tween 20 and Tween 80 were employed as surfactants and lecithin as co-surfactant. Many formulation parameters were controlled to obtain high quality nanoparticles. The prepared solid lipid nanoparticles were evaluated by different standard physical and imaging methods. The efficiency of drug release form prepared formulae was studied using in vitro technique with utilize of dialysis bag technique. The stability of prepared formulae was studied by thermal procedures and infrared spectroscopy.\r\nResults: The mean particle diameter measured by laser diffraction technique was (194.6�±5.03 to 406.6�±15.2 nm) for Dibenzoyl peroxide loaded solid lipid nanoparticles, (220�±6.2 to 328.34�±2.5) nm for Erythromycin loaded solid lipid nanoparticles and (227.3�±2.5 to 480.6�±24) nm for Triamcinolone acetonide loaded solid lipid nanoparticles. The entrapment efficiency and drug loading capacity, determined with ultraviolet spectroscopy, were 80.5�±9.45% and 0.805�±0.093%, for Dibenzoyl peroxide, 96�±11.5 and 0.96�±0.012 for Triamcinolone acetonide and 94.6�±14.9 and 0.946�±0.012 for Erythromycin base respectively. It was found that model drugs showed significant faster release patterns when compared with commercially available formulations and pure drugs (p?0.05). Thermal analysis of prepared solid lipid nanoparticles gave indication of solubilization of drugs within lipid matrix. Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drugs and lipid matrix and being only dissolved in it. Electron microscope of scanning and transmission techniques indicated sphere form of prepared solid lipid nanoparticles with smooth surface with size below 100 nm. \r\nConclusions: Solid lipid nanoparticles with small particle size have high encapsulation efficiency, and relatively high loading capacity for Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs can be obtained by this method. - See more at: http://www.sciencedomain.org/abstract.php?iid=211&id=14&aid=1128#.UocbjsQ_szI...
The aim of this study was to optimize fluid bed granulation and tablets compression processes using design space approach. Type\r\nof diluent, binder concentration, temperature during mixing, granulation and drying, spray rate, and atomization pressure were\r\nrecognized as critical formulation and process parameters. They were varied in the first set of experiments in order to estimate\r\ntheir influences on critical quality attributes, that is, granules characteristics (size distribution, flowability, bulk density, tapped\r\ndensity, Carr�s index, Hausner�s ratio, and moisture content) using Plackett-Burman experimental design. Type of diluent and\r\natomization pressure were selected as the most important parameters. In the second set of experiments, design space for process\r\nparameters (atomization pressure and compression force) and its influence on tablets characteristics was developed. Percent of\r\nparacetamol released and tablets hardness were determined as critical quality attributes. Artificial neural networks (ANNs) were\r\napplied in order to determine design space. ANNs models showed that atomization pressure influences mostly on the dissolution\r\nprofile, whereas compression force affects mainly the tablets hardness. Based on the obtained ANNs models, it is possible to predict\r\ntablet hardness and paracetamol release profile for any combination of analyzed factors....
The role of chronotherapeutics in hypertension management is based on the recognition that blood pressure does not remain constant throughout the day. Instead, it tends to be higher in the early morning hours and lower in the evening hours. The main objective of the present studies reported here was to investigate whether compression coating could be used to produce tablets providing maximum In-vitro drug release 8 to 10 hours after an evening dose taken at approximately 6:00 pm–7.00 pm. The basic idea behind the dosage form development is to investigate effect of coating design on lag time and drug release from directly compressed time-controlled release tablet. The aim of the present study was to design time controlled tablet of Atenolol, as Chronopharmaceutical drug delivery system by press coating. Formulation design involves coating polymer blend ratio (100:0, 75:25, 50:50, 25:75, 0:100 w/w) of Eudragit L-100: HPMC K-15M which were exploited for their pulsatile drug release ability. Coating materials blend were evaluated for micromeritic properties like flow properties, compressibility index, Hausner’s ratio and also evaluated the tablet for hardness, thickness, friability and weight variation. The obtained results showed the capability of the system in delaying drug release for a programmable period of time to attain drug release after 10hours after an evening dose taken at according to a time-dependent approach....
The present study was carried out to develop oral controlled release formulations of aceclofenac employing HPMC, ethyl cellulose and methyl cellulose as release retardant materials. Tablet containing solid dispersions of aceclofenac with polyvinyl pyrolidine (PVP k30) in the ratio of 1:1 prepared by solvent evaporation method used as core material and middle layer material for tablets. Compression coated and layered tablets were prepared with release retardant polymers, in which compatibility studies between the drug and excipients were conducted by infrared spectroscopy. The prepared tablets were characterized and results were compared the compression coated with layered tablets. Release rate was described by zero order, first order, Higuchi and peppas equations. In vitro release data revealed that by increasing the concentration of coating layer by compression coating, decreased the values of K than the layer tablets, results indicated that the release rate of drug was retarded by increasing the concentration polymers, mechanism of drug release exhibits non-Fickian diffusion anomalous transport....
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