Current Issue : April - June Volume : 2018 Issue Number : 2 Articles : 6 Articles
Circadin 2 mg prolonged-release tablet is the only licensed melatonin product available in\nthe UK. Circadin is indicated for patients with primary insomnia aged 55 and over, but is more widely\nused ââ?¬Å?off-labelââ?¬Â to treat sleep disorders especially in the paediatric population. Children and older\npeople often have difficulty swallowing tablets and dividing the tablet is sometimes required to ease\nadministration. The aim of this study was to measure the release profile of melatonin from Circadin\ntablets when divided or crushed, and compare this with release from intact tablets. Dissolution\ntesting was also performed for unlicensed melatonin products for comparison. Dissolution tests were\nperformed using the pharmacopoeial paddle apparatus, with melatonin release analyzed by high\nperformance liquid chromatography. Melatonin content, hardness, friability, and disintegration of\nthe products were also evaluated. The prolonged release of melatonin from Circadin tablets was\nunlike that of any other product tested. When divided into halves, Circadin preserved most of\nthe prolonged-release characteristic (f2 = 58), whereas quarter-cut and crushed tablet had a more\nimmediate melatonin release profile. Circadin is significantly less expensive and should be preferred\nto unlicensed medicines which are not pharmaceutically equivalent and offer less quality assurance....
Preservatives are used to maintain the microbiological attributes of the formulation throughout the shelf life. Sodium benzoate is used as preservative in oral, parenteral and topical formulations. Antimicrobial effectiveness testing (AET) was carried out using different concentration of sodium benzoate at different pH levels. Bacteria Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and fungi Candida albicans, Aspergillus niger were challenged for the study. Sodium benzoate concentration has studied in range 0.05-0.5% and pH range of formulations has studied 4.0-6.5. Sodium benzoate had passed the AET test as per USP for pH range 4.0-6.5 and sodium benzoate concentration 0.075 to 0.5% but AET test fails at sodium benzoate concentration 0.05%....
In this work, we examined enhanced skin delivery of minoxidil applied in nanoemulsions\nincorporating skin penetration enhancers. Aliquots of fully characterized oil-in-water nanoemulsions\n(1 mL), containing minoxidil (2%) and the skin penetration enhancer oleic acid or eucalyptol as oil\nphases, were applied to full-thickness excised human skin in Franz diffusion cells, while aqueous\nsolutions (1 mL) containing minoxidil were used as controls. Minoxidil in the stratum corneum (SC),\nhair follicles, deeper skin layers, and flux through the skin over 24 h was determined, as well as\nminoxidil solubility in the formulations and in the SC. The nanoemulsions significantly enhanced the\npermeation of minoxidil through skin compared with control solutions. The eucalyptol formulations\n(NE) promoted minoxidil retention in the SC and deeper skin layers more than did the oleic acid\nformulations, while the oleic acid formulations (NO) gave the greatest hair follicle penetration.\nMinoxidil maximum flux enhancement was associated with increases in both minoxidil SC solubility\nand skin diffusivity in both nanoemulsion systems. The mechanism of enhancement appeared to be\ndriven largely by increased diffusivity, rather than increased partitioning into the stratum corneum,\nsupporting the concept of enhanced fluidity and disruption of stratum corneum lipids....
Clarithromycin has poor acceptance by pediatric and geriatric patients due to very bitter taste. Usually, in dry syrup formulations, high concentration of sugar is used for taste masking purpose. But high consumption of sugar has been related to several chronic diseases and several times is unable to mask the extreme bitter taste. Therefore this study aimed to investigate taste masking capacity of excipients other than sugar. For this purpose, initially several granulating material were evaluated for masking the bitter taste of clarithromycin. After identifying the granulating material, combination of non caloric intense sweeteners along with granulating materials were used to achieve pleasant taste. Combination of sucralose and aspartame with hydroxy propyl cellulose miraculously removed bitterness, provided sweetness and absence of aftertaste. These taste masked granules can be used in formulation of dry syrup or tablet, which can be easily accepted by pediatric as well as by geriatric patients. The result of this study provided important information for future applications of synergistic effects of sucralose and aspartame in combination with hydroxy propyl cellulose for taste masking purposes....
In this study, we attempted to prepare carbamazepine (CBZ) cocrystal through the solution\nmethod in ethanol-water solvent mixture (volume ratio 1:1) and polyvinyl pyrrolidone (PVP) solution.\nNicotinamide (NIC) and saccharin (SAC) were selected as cocrystal coformers. Cocrystal screening\nproducts were characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning\nCalorimetry (DSC), and Powder X-ray Diffraction (PXRD) techniques. Characterization results show\nthat in ethanol-water solvent mixture, pure CBZ-NIC cocrystal can be prepared, while CBZ-SAC\ncocrystal cannot be obtained. The addition of PVP can inhibit CBZ-NIC cocrystal formation and\nfacilitate CBZ-SAC cocrystal formation....
Lipid nanocarriers show occlusive properties that may be related to their ability to improve\nskin hydration. The aim of this work was to evaluate the relationship between in vitro occlusion factor\nand in vivo skin hydration for three types of lipid nanocarriers: nanoemulsions (NEs), solid lipid\nnanoparticles (SLNs) and nanostructured lipid carriers (NLCs). These lipid nanocarriers were loaded\nwith trans-resveratrol (RSV) and incorporated in gel vehicles. In vitro occlusion factor was in the\norder SLNs > NLCs > NEs. Gels containing unloaded or RSV loaded lipid nanocarriers were applied\non the back of a hand of 12 healthy volunteers twice a day for one week, recording skin hydration\nchanges using the instrument Soft Plus. An increase of skin hydration was observed for all lipid\nnanocarriers (SLNs > NLCs > NEs). RSV loading into these nanocarriers did not affect in vitro and\nin vivo lipid nanocarriers effects. A linear relationship (r2 = 0.969) was observed between occlusion\nfactor and in vivo increase of skin hydration. Therefore, the results of this study showed the feasibility\nof using the occlusion factor to predict in vivo skin hydration resulting from topical application of\ndifferent lipid nanocarriers loading an active ingredient with no inherent hydrating activity....
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