Current Issue : October - December Volume : 2017 Issue Number : 4 Articles : 6 Articles
Objective: The present study investigates the capability of preparing metronidazole loaded\nmicrospheres employing a natural chitosan extracted from oyster shells of Egeria radiata.\nMethods: Microspheres were prepared by external gelation technique using tripolyphosphate\n(TPP) as the cross-linker. The drug to polymer ratio was selected at various levels of polymer-drug\nquantities with varying amount of TPP. The prepared microspheres were characterized for % yield,\ndrug entrapment efficiency, surface morphology and drug release profile.\nResults: Almost spherical, rough and porous microspheres were obtained. % yield and drug\nentrapment efficiency were found to be in the range of 63.5 ââ?¬â?? 70.8% and 63.4 ââ?¬â?? 77.5%\nrespectively; and about 80% of the drug was released in about 6 hours.\nConclusion: The results revealed that formulation of metronidazole loaded microspheres in\nnatural chitosan from an oyster shell can be used as a potential oral drug delivery system....
The objective of this study was to compare between the in traditional in vitrotesting and dissolution\nkinetics of selected commercial brands of ibuprofen and paracetamol tablets. Ibuprofen (400 mg/Tab)\nand paracetamol tablets (500 mg/Tab) from the Gulf Cooperation Council (GCC) pharmaceutical\nmarket were evaluated for hardness, friability, uniformity of weight, disintegration and dissolution\nprofiles. The study indicated that there is a correlation between the different in vitro tests proposing that\ntablets with higher hardness value, slow disintegration time will show slower dissolution rate. The\nresults indicated a significance difference between different brands in hardness, disintegration time and\ndissolution. This difference was more prominent for ibuprofen brands compared to paracetamol brands.\nThe similarity test supported this findings where f2 for all comparisons for the ibuprofen tablets were\nless than 50. Dissolution kinetics indicated that the first order equation was best equation to give the\ngoodness of fit and therefore to represent the dissolution data. The dissolution kinetics confirmed the\ndifference between different brands of both ibuprofen and paracetamol tablets. The use of dissolution\nkinetics proved to be a good tool in studying the interchangeability of generic drugs. The study raise a\nvaluable question about the interchangeability of different brands as this in vitro difference may suggest\na more serious in vivo difference in their bioavailability....
Purpose: To evaluate the dissolution and permeation characteristics of artemether tablets formulated\nwith cashew and prosopis gums, and compare with tablets prepared with acacia gum.\nMethods: Artemether tablets containing varying concentrations (1.0 to 4.0 %w/w) of cashew and\nprosopis gums or 3 %w/w of acacia (control) gum as binders were formulated by wet granulation\nmethod. The tablets were evaluated for crushing strength, friability and disintegration time. Dissolution\nand permeation characteristics of the formulations were studied using USP methods.\nResults: Tablets formulated with prosopis gum had higher crushing strength, higher friability and higher\ndisintegration time compared to those of cashew gum at corresponding binder concentrations. Tablets\nformulated with 3 %w/w cashew gum exhibited complete drug release within 1 h, 95 % drug permeation\nin 188 min (in simulated gastric fluid [SGF]) and 95 % permeation in 224 min (under simulated intestinal\nfluid [SIF] condition) while those made with 3 %w/w prosopis gum exhibited 70.7 % drug release in 1 h,\n95 % permeation in 135 min (in SGF) and 95 % permeation in 170 min (under SIF condition).\nConclusion: Cashew gum is effective as a binder over a relatively wide range of concentrations to\nachieve fast drug release though with minimal permeation enhancement while prosopis gum is\ncharacterized by delayed drug release but enhanced permeation of the released drug....
Objective of this study was to formulate directly compressible mouth dissolving tablets of piroxicam with sufficient mechanical integrity, content uniformity and acceptable palatability to assist patients of any age group for easy administration. Six batches of piroxicam disintegrating tablets were prepared by using various subliming agents in order to get required theoretical release profiles. Effect of varying concentrations of different subliming agent such as camphor, menthol on disintegration time was studied. Tablets were evaluated for weight variation, thickness, hardness, friability, drug content, in-vitro disintegrating time, wetting time and in-vitro drug release. The study reveals that the formulation prepared by direct compression F6 exhibits better dissolution, disintegration time and wetting time compared to the other orally disintegrating tablet prepared. Physical parameters of all the formulated tablets were within the acceptable limits. FTIR studies did not indicate any excipients incompatibility, either during mixing or after compression....
An optimized formulation of capsules containing Lansoprazole enteric-coated\npellets using D-Optimal design with a polynomial statistical model were prepared\nby using EudragitÃ?®L100 as an enteric coated polymer to provide resistance\nto simulated gastric acid dissolution in buffer media. D-Optimal experimental\ndesign was used to determine the optimal level for three coating layers\nthat were applied to formulate the enteric-coated pellets including a drug\nloading layer, a sub-coating, and an outer enteric coating. Dissolution studies\nwere performed on the prepared Lansoprazole capsules. Less than 5 percent of\nLansoprazole was released in 60 minutes in an acidic dissolution medium (pH\n1.2) and greater than 90 percent of active ingredient was released in the next\n60 minutes in a buffer dissolution medium (pH 6.8). The Lansoprazole capsules\nwere stable with no observable change in physico-chemical properties in\naccelerated and normal storage conditions for 6 and 18 months, respectively.\nThe pharmacokinetic parameters Cmax, Tmax, AUC0âË?â??t , and AUC0âË?â??âË?ž were determined\nafter administration of the D-Optimal design optimized capsules of\nLPZ to healthy beagle dogs and were statistically compared to GastevinÃ?® capsules\nas a reference (KRKA, Slovenia) using the non-compartmental method\nwith the aid of WinNonlin 5.2 software. The analysis of variance showed that\nthe two formulations did not demonstrate bioequivalence using a 90% confi-dence interval range (80% - 120%) of Cmax, AUC0âË?â??t, and AUC0âË?â??âË?ž. No significant\ndifference in Tmax was found at the 0.95 significance level using the Wilcoxon\nsigned-rank test. D-Optimal Experimental Design provided definitive\ndirection for an optimal formulation of capsules containing enteric-coated\npellets of lansoprazole loaded within the coating of pellets that provided similar\nbioequivalence to Gastevin....
Solubility and dissolution rate are two fundamental criteria that portray the drug performance in-vivo. Olmesartan medoxomil (OM) is an orally active angiotensin II type 1 receptor antagonist approved by FDA for the treatment of hypertension. Being classified as BCS class II; OM suffers from poor solubility and low bioavailability. Nanosuspension is a submicron colloidal dispersion of drug particles that are stabilized by ionic or polymeric stabilizers or mixture of both. This work aimed to the formulation of OM nanosuspensions using full factorial design and studying the effect of nanosizing on OM solubility and dissolution rate. Two factors (independent variables) were evaluated: type of stabilizer and drug to stabilizer ratio. The dependent responses measured were: particle size and size distribution (span value). OM nanosuspensions were prepared by simple bottom up method (antisolvent precipitation ultrasonication). The highest desirability value was observed for formula F1. The particle size, span value and zeta potential of optimized formula (F1) were 153.00±0.58 nm, 4.35±0.0036 and -22.75±0.845 mV, respectively. Optimum formulation was further characterized in-vitro regarding its saturation solubility, dissolution rate, transmission electron microscopy and differential scanning calorimetry. Saturation solubility and the %OM dissolved within 8 minutes were enhanced by about 4 and 3 folds, respectively compared to drug alone as a result of size reduction, efficient stabilization with HPMC which were confirmed by transmission electron microscopy. Decrease of crystallinity was revealed by thermal analysis. In summary, the highlighted results confirmed the efficacy of nanosuspensions in enhancing the saturation solubility and dissolution rate of OM....
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