Current Issue : October - December Volume : 2017 Issue Number : 4 Articles : 5 Articles
Administered by an oral route, Furosemide (FUR), a diuretic used in several edematous\nstates and hypertension, presents bioavailability problems, reported as a consequence of an erratic\ngastrointestinal absorption due to various existing polymorphic forms and low and pH-dependent\nsolubility. A mucoadhesive sublingual fast-dissolving FUR based film has been developed and\nevaluated in order to optimize the bioavailability of FUR by increasing solubility and guaranteeing\na good dissolution reproducibility. The Differential Scanning Calorimetry (DSC) analyses confirmed\nthat the film prepared using the solvent casting method entrapped FUR in the amorphous state.\nAs a solid dispersion, FUR increases its solubility up to 28.36 mg/mL. Drug content, thickness, and\nweight uniformity of film were also evaluated. The measured Young�s Modulus, yield strength, and\nrelative elongation of break percentage (EB%) allowed for the classification of the drug-loaded film as\nan elastomer. Mucoadhesive strength tests showed that the force to detach film from mucosa grew\nexponentially with increasing contact time up to 7667 N/m2. FUR was quickly discharged from\nthe film following a trend well fitted with theWeibull kinetic model. When applied on sublingual\nmucosa, the new formulation produced a massive drug flux in the systemic compartment. Overall,\nthe proposed sublingual film enhances drug solubility and absorption, allowing for the prediction of\na rapid onset of action and reproducible bioavailability in its clinical application....
Conversion into the amorphous form enhances the dissolution of poorly soluble drugs, however\nthe barrier to market for medicines containing an amorphous drug is poor stability. The aim was to\nproduce the amorphous form of a drug within a capsule, without thermal or mechanical stress during\nmanufacture. To facilitate this aim, the mechanism for drug-polymer interaction was explored.\nNifedipine and polyvinylpyrrolidone were dissolved in tert-butanol at different drug/polymer ratios.\nThese solutions were dispensed into gelatin capsules and freeze-dried. Differential scanning calorimetry\n(DSC) & novel FT-IR analysis based on peak symmetry measurements confirmed the absence of\ncrystallinity when polyvinylpyrrolidone exceeded 50%w/w. Capsules containing 10 mg of nifedipine\nwere amorphous and stable for over 3 months at ââ?°Ë?40 Ã?°C. Evidence of hydrogen bonding between\nthe N-H group of nifedipine and the C=O group of PVP was observed and this interaction inhibited\nnifedipine crystallisation. PVPââ?¬â?¢s high affinity for water and the nifedipine-polymer interaction lead to\na significant dissolution rate enhancement. The freeze-dried capsule, 10%w/w nifedipine/PVP, had the\nhighest dissolution rate constant of 0.37 Ã?± 0.05 minâË?â??1, and the lowest time to achieve 50% dissolution\nor t1/2 of 1.88 Ã?± 0.05 min. This formulation reached 80% dissolved in less than 6 min whereas the\nequivalent marketed liquid filled nifedipine capsule took 3 times longer to reach 80% dissolution....
In the past decade, the discovery of active pharmaceutical substances with high therapeutic value\nbut poor aqueous solubility has increased, thus making it challenging to formulate these\ncompounds as oral dosage forms. The bioavailability of these drugs can be increased by\nformulating these drugs as an amorphous drug delivery system. Use of porous media like\nmesoporous silica has been investigated as a potential means to increase the solubility of poorly\nsoluble drugs and to stabilize the amorphous drug delivery system. These materials have\nnanosized capillaries and the large surface area which enable the materials to accommodate high\ndrug loading and promote the controlled and fast release. Therefore, mesoporous silica has been\nused as a carrier in the solid dispersion to form an amorphous solid dispersion (ASD). Mesoporous\nsilica is also being used as an adsorbent in a conventional solid dispersion, which has many useful\naspects. This review focuses on the use of mesoporous silica in ASD as potential means to\nincrease the dissolution rate and to provide or increase the stability of the ASD. First, an overview\nof mesoporous silica and the classification is discussed. Subsequently, methods of drug\nincorporation, the stability of dispersion and, much more are discussed....
An optimum carrier rugosity is essential to achieve a satisfying drug deposition efficiency for the carrier\nbased dry powder inhalation (DPI). Therefore, a non-organic spray drying technique was firstly used\nto prepare nanoporous mannitol with small asperities to enhance the DPI aerosolization performance.\nAmmonium carbonate was used as a pore-forming agent since it decomposed with volatile during\npreparation. It was found that only the porous structure, and hence the specific surface area and carrier\ndensity were changed at different ammonium carbonate concentration. Furthermore, the carrier\ndensity was used as an indication of porosity to correlate with drug aerosolization. A good correlation\nbetween the carrier density and fine particle fraction (FPF) (r2 = 0.9579) was established, suggesting\nthat the deposition efficiency increased with the decreased carrier density. Nanoporous mannitol with\na mean pore size of about 6 nm exhibited 0.24-fold carrier density while 2.16-fold FPF value of the nonporous\nmannitol. The enhanced deposition efficiency was further confirmed from the pharmacokinetic\nstudies since the nanoporous mannitol exhibited a significantly higher AUC0-8h value than the nonporous\nmannitol and commercial product Pulmicort. Therefore, surface modification by preparing\nnanoporous carrier through non-organic spray drying showed to be a facile approach to enhance the DPI\naerosolization performance....
The objective of this study was to formulate and prepare gliclazide capsule by solid dispersion method using different\nsurfactants and their in vitro evaluation. Solubilising capacity of polyethylene glycol (PEG 6000, PEG 20000) and\npolyvinylpyrrolidone (PVP K 30) was determined at 2% concentration where gliclazide was used as a model drug and water\nwas used as control for comparison. Results showed that PVP K 30 exhibited maximum solubilising capacity. Fusion method\nof solid dispersion was adopted for preparation of capsules using PEG 6000 & PEG 20000 in different ratios. Although\nthese agents are claimed to be good surfactants but our results showed that, the highest cumulative drug release was 1.81\n% for gliclazide and PEG 6000 in a ratio of 1:6. The flow property of capsule granules was determined by angle of repose.\nThe capsules were also subjected to weight uniformity test, disintegration test and moisture permeation test and the chemical\nanalysis of solid dispersions were done by FTIR. From this study, it can be concluded that it is possible to formulate and\nprepare gliclazide capsule by using solid dispersion method....
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