Current Issue : July - September Volume : 2019 Issue Number : 3 Articles : 6 Articles
Pioglitazone, a class II BCS drug having poor water solubility and slow dissolution rate may have a negative impact on its bioavailability, sub-therapeutic plasma drug levels and thus may lead to therapeutic failure. In order to improve its solubility and thus dissolution rate, chitosan loaded nanoparticles were prepared and passed through high-pressure homogenizer with varying pressure and number of cycle. A response surface design namely Box-Behnken design was implemented to optimized the nanoparticles. Chitosan (X1), pressure (X2) and the number of cycles (X3) were selected as independent variables whereas particle size (Y1) and entrapment efficiency (Y2) were selected as dependent variables. FTIR and DSC study revealed no interaction between drug and excipients. Particle size and entrapment efficiency were found in the range of 39.1 nm to 250.3 nm and 70.78 to 93.71 % respectively. A design expert V8 software was used to determine the relationship between the dependent and independent variables were drawn out from the mathematical equations and response surface plots. Statistical analysis was performed using ANOVA which was found to be a significant and quadratic model was obtained by MLRA for particle size and for entrapment efficiency. TEM analysis shows that spherical shape of nanoparticles. In-vivo pharmacokinetic study of optimized batch shows high bioavailability as compared with the pure drug. From the above result, high-pressure homogenizer was found to be the best method of preparation for nanoparticles as well as it has wide industrial acceptance as it is reproducible and industrial scalability....
A continuous-spray granulator (CTS-SGR) is a one-step granulation technology capable of\nusing solutions or suspensions. The present research objectives were, (1) to reduce the manufacturing\noperations for solid dosage formulations, (2) to make amorphous solid dispersion (ASD) granules\nwithout pre-preparation of amorphous solids of active pharmaceutical ingredients (API), and (3) to\ncharacterize the obtained SGR granules by comprehensive pharmaceutical analysis. Rebamipide\n(RBM), a biopharmaceutical classification system class IV drug, that has low solubility or permeability\nin the stomach, was selected as a model compound. Five kind of granules with different concentrations\nof polyvinylpyrrolidone/vinyl acetate copolymer (PVP-VA) were prepared using a one-step SGR\nprocess. All of the SGR granules could be produced in amorphous or ASD form and their\nthermodynamic stability was very high because of high glass transition temperatures (>178 DegreeC).\nThey were unstable in 20 DegreeC/75%RH; however, their stability was improved according to the\nproportion of polymer. The carboxy group of RBM was ionized in the granules and interactions\nappeared between RBM and PVP-VA, with the formation of an ASD confirmed and the solubility\nwas enhanced compared with bulk RBM crystals. The SGR methodology has the possibility of\ncontributing to process development in the pharmaceutical industry....
This study reports the first case of an innovative drop-on-powder (DoP) three-dimensional\n(3D) printing technology to produce oral tablets (diameters of 10 mm and 13 mm) loaded with an\nanticancer model drug, 5-fluorouracil (FLU). For this study, a composition of the powder carrier\ncontaining CaSO4 hydrates, vinyl polymer, and carbohydrate was used as the matrix former, whereas\n2-pyrrolidone with a viscosity like water was used as a binding liquid or inkjet ink. All tablets\nwere printed using a commercial ZCorp 3D printer with modification. The resultant tablets were\nsubject to coating with various polymeric solutions containing the drug. The composition of the\npolymeric solutions was adjusted at drug: polymer(s) 1:1 (w/w) ratio. Either Soluplus® (SOL) alone\nor in combination with polyethylene glycol (PEG) was used to develop the coating solution of 2.5%\n(w/v) concentration. The particle size analysis, flow test, and particle morphology studies revealed\nmono-modal narrow size distribution, good flow properties, and porous loosely bound texture\n(of the tablets), respectively. Moreover, the advanced application of the fluorescence microscopy\nshowed a homogenous distribution of the drug throughout the surface of the 3D printed tablets.\nThe in vitro dissolution studies showed that the tablet compositions, dimensions, and the coating\nsolution compositions influenced the release of the drug from the tablets. It can be concluded that our\ninnovative DoP 3D printing technology can be used to fabricate personalized dosage forms containing\noptimized drug content with high accuracy and shape fidelity. This is particularly suitable for those\ndrugs that are highly unstable in thermal processing and cannot withstand the heat treatment, such\nas in fused deposition modeling (FDM) 3D printing....
Purpose: Microneedle patches are arrays of tiny needles that painlessly pierce the skin to deliver medication into\nthe body. Biocompatible microneedles are usually fabricated via molding of a master structure. Microfabrication\ntechniques used for fabricating these master structures are costly, time intensive, and require extensive expertise to\ncontrol the structureâ??s geometry of the structure, despite evidence that microneedle geometry is a key design\nparameter. Here, a commercially available 3D printer is utilized, for the first time, to quickly and easily manufacture\nmicroneedle masters.\nDesign/methodology/approach: Because commercially available 3D printers are not typically used for micron-scale\nfabrication, the influence of three different sources of error- stair-stepping, aliasing, and light abberations- on the\nresulting structure is investigated. A custom Matlab code is written to control the light intensity projected off of each\nindividual micromirror (through grayscale) at a given time. The effect of the layer height, the number of layers, and\ngrayscale on the sharpness, surface texture, and dimensional fidelity of the final structure is described.\nFindings: The Autodesk Ember is successfully utilized to fabricate sharp microneedles with a tip radius of approximately\n15 micron in less than 30min per patch (as compared to weeks to months for existing approaches). Utilization of grayscale\nimproves surface texture and sharpness, and dimensional fidelityâ?¦â?¦....
The development of oral tablet formulation for herbal medicines has been restricted by large\ndrug loadings and the poor physicochemical and mechanical properties of dry herbal extracts (DHEs).\nHerein, statistical experimental designs were applied to herbal tablet formulation development and\noptimization usingWuzi Yanzong dry extract (WYE). The tablet disintegration time and hardness\nwere identified as the critical quality attributes (CQAs) of the product. The tablet formulation was\ndesigned to achieve a high drug loading (50% or higher of WYE), shorter tablet disintegration time\n(less than 30 minutes), and suitable hardness (6.0 to 7.5 kp). A D-optimal mixture design was used\nto evaluate the effects of excipients on CQAs to minimize the risk compression failure and improve\nthe tabletability in formulations containing WYE at 50% and 65% by weight. A partial least squares\nmodel was used to elucidate the multivariate relationships between a large number of formulation\nvariables and product CQAs, and determine the maximum possible WYE loading. From overlaid\nplots of the effects of formulation variables on CQAs, it was found that a maximum WYE loading of\n67% in tablet formulation satisfied the acceptance criteria of CQAs. In conclusion, this study shows\nthat multivariate statistical tools are useful for developing tablet formulations containing high doses\nof herbal extracts and establishing control strategies that ensure product quality....
The purpose of research was to study the “process validation of rifampicin and isoniazid film coated tablets” in tablet dosage form was carried out at Sunij Pharma Pvt. Ltd., Vatva, G.I.D.C, Ahmedabad, Gujarat. The study involves validating the process variables of this product to show that the process was under control. The study was conducted on a batch size of 3,00,000 tablets, manufactured by wet granulation method. Various critical parameters at various stages which involve sifting, dry mixing, wet granulation, drying, dry milling (sizing of dried granules), lubrication, compression of granules and coating stages were identified and evaluated. The process parameters were evaluated by validating parameters. During granulation stage various parameters such as loads of chopper and impeller, LOD (Loss on Drying) during drying, Assay, particle size analysis at blending and lubrication stage. During compression stage tablets were evaluated at different speeds at regular intervals of time for appearance, dimensions, thickness, hardness, disintegration, friability, dissolution etc. Tablets were also evaluated at coating stage. The process validation data provides you the high degree of assurance and meets its pre-determined specifications....
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