Objective: The aim of this study was to formulate a developed floating tablet of amlodipine using different concentrations and types of hydrophilic and hydrophobic polymers to be conserved in the stomach for modulating solubility and bioavailability, diminishes drug waste and decline side effects.Methods: Through this study, eleven innovative formulations of amlodipine floating tablets were prepared [mixture of amlodipine, sodium bicarbonate (NaHCO3), hydroxypropyl methylcellulose (HPMC) E50, HPMC K100M, ethylcellulose (EC) 5 mp. a. s.] by direct compression method. The pre-compressed mixtures were then evaluated for numerous parameters such as angle of repose, bulk density, tapped density, Carr's compressibility index and Hausner's ratio. After compression, tablets were subjected to several tests like; floating behavior of tablets, tablet thickness, hardness test, friability test, weight variation, in vitro dissolution test. In addition, the optimum formulation was evaluated for Fourier transform-infrared (FT-IR) and differential scanning calorimetry (DSC) tests. Results: From in vitro dissolution tests and kinetic assessments; F8 was selected as an optimum formula, depending on the R2 value of zero order kinetics (0.9915) and (n) value of Korsmeyer-Peppas (0.9635) which indicate purely relaxation zero order kinetic with good delaying in drug release that was reached to 14 h.Conclusion: It can be concluded that the developed formulation of a certain combination of low viscosity grades of HPMC and EC was considered an efficient floating tablet.
Objective: The aim of this study was to formulate a new developed solid dispersion (SD) containing fixed dose combination of nalidixic acid and cefdinir (500:300 mg) to improve dissolution rate of poorly soluble drugs via a new mechanism as well as the conventional mechanism of SD represented by the presence of hydrophilic carrier.Methods: Through this objective eight newly developed SD formulas of fixed dose combination of nalidixic acid and cefdinir (500:300 mg) and (polyethylene glycol 6000 and poloxamer 188) in different ratio were prepared, in addition to SD of each drug alone and simple mixture of individual SD (SMSD) prepared by means of fusion technique. Moreover, SDs beside pure drugs, simple mixture, and physical mixture (PM) were characterized by dissolution tests, solubility studies, powder X-ray diffractometer (PXRD), differential scanning calorimetry (DSC), Fourier transform-infrared (FT-IR) spectroscopy and scanning electron microscopy (SEM). Results:From in vitro dissolution tests, PXRD, DSC, FT-IR, and SEM; it is indicated the presence of a physical complex between cefdinir and nalidixic acid in their SD containing combination of fixed dose of both drugs. This will affect the crystallinity of the second drug and their dissolution behavior in addition to the conventional mechanism owing to the presence of hydrophilic carrier (poloxamer 188). Conclusion:It was concluded that the newly prepared formula of SD containing fixed dose combination of nalidixic acid and cefdinir will be promising for higher dissolution profile than that from SD of each drug alone or SMSD of each drug.
Objective: The aim of this study was to formulate enteric coated oroslippery tablets (OSTs) of naproxen to overcome the common problems of stomach irritation and swallowing difficulties which accompanied the administration of naproxen tablets.Methods: Different formulas of enteric slippery tablets were prepared by direct compression method. Various parameters were investigated like the effect of eudragit L-100 (eud.) concentration (as an enteric polymer), coating level and effect of different concentrations of croscarmellose sodium CCS (as super disintegrant) on the physical properties. Finally, in an in vitro disintegration and release study was carried out. Results:The enteric slippery optimal formula (F8) was selected to consist of double coat (17.5% eudragit (eud.)) with core tablet containing (6% CCS). It was found that this optimal formula having an acceptable physical property (friability, hardness, thickness and weight variation). Besides, the best acid resistant potential represented by the protection of the OSTs for 2 h in 0.1 N HCl without any sign of disintegration and drug release. Moreover, it was found that (F8) has a disintegration time equal to (8±1.36 min) and release of 80% (20±0.18 min) in phosphate buffer pH 6.8. Conclusion:The result revealed the successful preparation of naproxen tablets using enteric slippery coating that can be easily swallowed and prevent direct irritation of the stomach with acceptable tablet weight.
Letrozole (LZ) is an aromatase inhibitor, which inhibits the formation of estrogens from androgens. Nanoemulsion is a liquid emulsion formulation utilized to increase solubility, bioavailability, and drug delivery to cancer cells. This study aims to improve LZ oral delivery through formulating solid nanoemulsion (SNE). Peppermint oil, tween 80, and transcutol P were used as an oil, surfactant, and co-surfactant, respectively. The optimized nanoemulsion (NE-3) was then incorporated into solid polyethylene glycol (PEG) to formulate (SNE). The optimized (NE-3), SNE-2, and the available marketed tablet have been compared. The optimized (NE-3) was selected according to specific parameters of optimum small nano-size 80 nm, PDI of 0.181, the zeta potential of-98.2, high transmittance (99.78%), optimum pH (5.6), a high percent of LZ content (99.03 ± 1.90), the relatively low viscosity of 60.2 mPa.s, and a rapid release of LZ within 30 min. NE-3 was selected to be formulated as SNE. LZ's best release rate was 80% in 5 min with a content homogeneity of 99.85 ± 0.04 for SNE-2. Zero-order kinetics is determined to have the greatest R 2 values. Field emission scanning electron microscopy (FE-SEM) detected that SNE-2 was (36.75–96.64 nm) with a spherical form and no adhesion or aggregation. FT-IR showed no significant variations in position and shape of the absorption peaks between the pure drug and optimal formulation diagrams. This novel nanoemulsion technology aids in improving the solubility of poorly water-soluble drugs, particularly the SNE delivery method, which has a higher in-vitro release rate and expiration date of LZ than others.
Floating in situ gel as gastroretentive drug delivery system represents a revolution in oral controlled release dosage forms in comparison with conventional oral liquids, as it prolongs the residence time of the drugs that have narrow absorption windows in the absorptive sites like stomach or upper gastrointestinal tract by having a bulk density lower than gastric fluids and thus remains buoyant in the stomach without affecting the gastric emptying rate until the drug released slowly, continuously and completely. This study was undertaken to formulate furosemide oral solution, which undergoes gelation when it is in direct contact with gastric fluid by using primary polymer (sodium alginate) in addition to the secondary polymer (iota-carrageenan) at different concentrations. Different variables that affect drug release profile like cross linking agent, combination of polymer, gas generating agent and drug concentrations were studied to optimize the best formulation through measuring their effects on viscosity, gel strength, floating lag time and floating duration. The best formulation exhibited 94.9% release of the drug after 5 h with effective floating property. In vivo test was applied and demonstrated good indication to the gastroretentive property of the optimum formulation through its relation to the diuretic property of the drug, and it agreed with in vitro release and the proposed kinetic mathematical modeling.
The purpose of this study is to provide a control drug delivery system through a newly approved work to enhance absorption and bioavailability of enalapril maleate loaded floating microspheres by ionotropic gelation technique using a hydrophilic carrier. Methods: Over this study, eleven developed formulations of floating microspheres were prepared by ionotropic gelation method using different concentrations of sodium alginate, iota carrageenan, sodium bicarbonate, calcium chloride, and the drug. Characterization of these microspheres was done using a diversity of parameters like micrometric properties, percentage yield, entrapment efficiency, In-Vitro buoyancy, In-Vitro drug release, and kinetics of drug release. The optimum formula was evaluated and identified for drugexcipients compatibility using Fourier transform infrared spectroscopy (FT-IR), surface morphology, powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). Results: From the results; F4 was selected as an optimum formula since it provides a faster and premium release of drug from the matrix (91.4%). Kinetics of drug release was founded to depend on both diffusion and erosion mechanisms, as the correlation coefficient (R 2) was best fitted with Korsemeyer model and release exponent (n) shown to be between 0.43-0.84. SEM images demonstrate spherical, discrete and freely flowing microspheres with a particle size of 199.4 ± 0.04. Optimum buoyancy properties, percentage yield, and drug entrapment efficiency were achieved. FTIR decided no interaction between enalapril and the polymers. DSC and XRD ascribed the miscibility of the drug with the polymers while maintaining stable crystalline properties of enalapril loaded in the prepared microspheres. Conclusion: It can be concluded that the developed floating microspheres of enalapril maleate can be considered as a promising controlled drug delivery system; thereby improve patient compliance.
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