Hordeum Vulgare Hull in the Design of Fast Disintegrating Tablets

In the present study, fast disintegrating tablets were designed with a view to enhance patient compliance. In this method, the hull of Hordeum vulgare, cross carmellose sodium, and sodium starch glycolate were used as superdisintegrants (4 and 6%), along with microcrystalline cellulose and mannitol, to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity, wetting time, water absorption ratio and in vitro dispersion time. Based on the in vitro dispersion time, the formulations were tested for the in vitro drug release pattern. Tablets having H. vulgare hull showed the release profile comparable to those tablets having sodium starch glycolate and cross carmellose sodium

Increased mitochondrial calcium levels associated with neuronal death in a mouse model of Alzheimer's disease

Mitochondria contribute to shape intraneuronal Ca2+ signals. Excessive Ca2+ taken up by mitochondria could lead to cell death. Amyloid beta (A beta) causes cytosolic Ca2+ overload, but the effects of A beta on mitochondrial Ca2+ levels in Alzheimer's disease (AD) remain unclear. Using a ratiometric Ca2+ indicator targeted to neuronal mitochondria and intravital multiphoton microscopy, we find increased mitochondrial Ca2+ levels associated with plaque deposition and neuronal death in a transgenic mouse model of cerebral beta -amyloidosis. Naturally secreted soluble A beta applied onto the healthy brain increases Ca2+ concentration in mitochondria, which is prevented by blockage of the mitochondrial calcium uniporter. RNA-sequencing from post-mortem AD human brains shows downregulation in the expression of mitochondrial influx Ca2+ transporter genes, but upregulation in the genes related to mitochondrial Ca2+ efflux pathways, suggesting a counteracting effect to avoid Ca2+ overload. We propose lowering neuronal mitochondrial Ca2+ by inhibiting the mitochondrial Ca2+ uniporter as a novel potential therapeutic target against AD. Calvo-Rodriguez et al. show elevated calcium levels in neuronal mitochondria in a mouse model of cerebral beta -amyloidosis after plaque deposition, which precede rare neuron death events in this model. The mechanism involves toxic extracellular A beta oligomers and the mitochondrial calcium uniporter

Pulmonary drug delivery strategies: A concise, systematic review

Because of limitations associated with the conventional treatment of various chronic diseases a growing attention has been given to the development of targeted drug delivery systems. Pulmonary route of drug delivery gaining much importance in the present day research field as it enables to target the drug delivery directly to lung both for local and systemic treatment. Over the last 2 decades, the systemic absorption of a broad range of therapeutics after pulmonary application has been demonstrated in animals as well as in humans. This review was prepared with an aim to discuss the technical, physiological, and efficacy aspects of the novel pulmonary route of drug targeting. The review also focuses on the mechanisms of pulmonary drug administration along with compatibility of the excipients employed, devices used, and techniques of particulate dosage production. This review was prepared based on the method of extensive literature survey on the topics covering all the aspects discussed in the present subject. Hence, the better understanding of complexes and challenges facing the development of pulmonary drug delivery system offer an opportunity to the pharmaceutical scientist in minimizing the clinical and technical gaps

Development and validation of liquid chromatography-Mass spectrometry method for the estimation of rifampicin in plasma

A selective, rapid and sensitive liquid chromatography-mass spectrometry method was developed for the quantitative estimation of rifampicin in plasma. With phenacetin as internal standard, sample pretreatment involved a one-step extraction with ethyl acetate from plasma. The sample was analyzed using methanol: 2mM ammonium acetate: 80:20 v/v as mobile phase. Chromatographic separation was achieved on a BDS Hypersil Gold C 18 column which was followed by detection with mass spectrometry. Linear calibration curves were obtained in the concentration range of 5.021-1008.315 ng/ml. The inter- and intra-day accuracy values were below 15% at all quality control levels. Percent recoveries for rifampicin at high, middle and low quality control samples was obtained 55.15, 48.65 and 49.62%, respectively and for internal standard was 60.22%. Rifampicin was found stable through all validation parameters. Developed method was found to be simple, precise, accurate and rapid for estimation of rifampicin in plasma. Thus, the method can be employed for routine pharmacokinetic and bioequivalence studies

Design of Fast Disintegrating Tablets of Prochlorperazine Maleate by Effervescence Method

In the present work, fast disintegrating tablets of prochlorperazine maleate were designed with a view to enhance patient compliance by effervescent method. In this method, mixtures of sodium bicarbonate and anhydrous citric acid in different ratios along with crospovidone (2-10% w/w), croscarmellose sodium (2-10% w/w) were used as superdisintegrants. Estimation of prochlorperazine maleate in the prepared tablet formulations was carried out by extracting the drug with methanol and measuring the absorbance at 254.5 nm. The prepared formulations were further evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on in vitro dispersion time (approximately 13-21 s), two promising formulations (one from each super-disintegrant) were tested for in vitro drug release pattern in pH 6.8 phosphate buffer, short-term stability (at 40°/75% relative humidity for 3 mo) and drug-excipient interaction (IR spectroscopy). Among the two promising formulations, the formulation containing 10% w/w of crospovidone and mixture of 20% w/w sodium bicarbonate and 15% w/w of citric acid emerged as the overall best formulation (t50% 6 min) based on drug release characteristics in pH 6.8 phosphate buffer compared to commercial conventional tablet formulation (t50% 17.4 min). Short-term stability studies on the promising formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05)

Formulation Design and Optimization of Fast Dissolving Clonazepam Tablets

Fast dissolving tablets of clonazepam were prepared by direct compression method with a view to enhance patient compliance. A 32 full factorial design was applied to investigate the combined effect of two formulation variables: amount of crospovidone and microcrystalline cellulose. Crospovidone (2-8% w/w) was used as superdisintegrant and microcrystalline cellulose (20-40% w/w) was used as diluent, along with directly compressible mannitol to enhance mouth feel. The tablets were evaluated for hardness, friability, thickness, drug content uniformity, in vitro dispersion time, wetting time and water absorption ratio. Based on in vitro dispersion time (approximately 16 s); the formulation containing 2% w/w crospovidone and 40% w/w microcrystalline cellulose was found to be promising and tested for in vitro drug release pattern (in pH 6.8 phosphate buffer). Short-term stability (at 40°/75% relative humidity for 3 mo) and drug-excipient interaction. Surface response plots are presented to graphically represent the effect of independent variables on the invitro dispersion time. The validity of the generated mathematical model was tested by preparing two extra-design checkpoints. The optimized tablet formulation was compared with conventional commercial tablet formulation for drug release profiles. This formulation showed nearly five-fold faster drug release (t50% 3.5 min) compared to the conventional commercial tablet formulation (t50% 16.4 min). Short-term stability studies on the formulation indicated that there are no significant changes in drug content and in vitro dispersion time (P<0.05)