Lovastatin (LOV) belongs to the class of cholesterol lowering drugs and is the first clinically used statin. It is a prodrug which lowers the cholesterol level through reversible competitive inhibition of 3-hydroxy-3-methyl-glutaryl coenzyme A (HMG-CoA) reductase, an enzyme involved in biosynthesis of cholesterol. It is available as conventional and extended release tablets, but its low aqueous solubility (4´10 -4 mg mL -1 ) finally escorts it to low oral bioavailability (less than 5 %). In addition, it undergoes extensive first pass metabolism; as a consequence of hepatic extraction it leads to low and variable availability of the drug to the general circulation. Therefore improvement in aqueous solubility of LOV is the foremost aim (1, 2). Self-microemulsifying drug delivery system (SMEDDS) of lovastatin was aimed at overcoming the problems of poor solubility and bioavailability. The formulation strategy included selection of oil phase based on saturated solubility studies and surfactant and co-surfactant screening on the basis of their emulsification ability. Ternary phase diagrams were constructed to identify the self-emulsifying region. Capryol 90 (20 %) as oil, Cremophore RH40 (40 %) as surfactant and Transcutol P (40 %) as co-surfactant were concluded to be optimized components. The prepared SMEDDS was characterized through its droplet size, zeta potential, emulsification time, rheological determination and transmission electron microscopy. The optimized formulation exhibited 94 % in vitro drug release, which was significantly higher than that of the drug solution. In vivo studies using the Triton-induced hyperlipidemia model in Wistar rats revealed considerable reduction in lipid levels compared to pure lovastatin. The study confirmed the potential of lovastatin SMEDDS for oral administration.
The Plackett-Burman design was applied to determine the factors significant for the enhancement of antitubercular compound yield from fenugreek [Trigonella foenum-graecum (Methi)] seeds crude extract. By optimizing various conditions like solid-to-solvent ratio, time, shaking rate, temperature, seed particle size, and light yield of antitubercular compounds from fenugreek seeds studied in a batch system, a mathematical model was constructed showing the influence of each variable. The optimal level of each variable and its interaction with each other were determined by response surface methodology. A highly significant model was generated, with correlation coefficients (R 2 ) of 0.9109 and 0.8307 for adjusted correlation coefficients (R 2 ). Using this model, it was possible to achieve more than 90% of anti-TB compound yield from fenugreek seed crude extract, which could be produced when solid-to-solvent ratio, temperature, and time were set at 15 ml, 30°C, and 36 hours, respectively. Resazurin microtiter assay was used to determine the in-vitro antitubercular activity of the crude seed extract against Mycobacterium tuberculosis. The model accurately predicted the percentage yield and antitubercular effect of the crude extract.
Two adult patients from a village of district Bhilwara, Rajasthan, consulted Skin Department of R. N. T. Medical College and Hospital, Udaipur, with complaints of thickening of the palms and soles and pigmentation of skin with a nonhealing ulcer on the palm. They also had complaints of loss of appetite, abdominal pain, nausea, vomiting, and loose motion. On examination, there were multiple 2–3 mm, keratotic papules on the palms, and soles on the background of diffuse keratoderma. Two irregular nonhealing ulcers were present on the hands which on excisional biopsy revealed squamous cell carcinoma. A generalized mottled pigmentation was present over the trunk and proximal parts of extremities. The clinical presentation was suggestive of arsenicosis. There was history of similar ailment in some of the fellow villagers as well. With the help of health authorities, a survey was conducted in the village and it was found that eight more villagers were suffering from similar kind of illness. The common source of arsenic was explored and found to be increased in drinking water that was taken out through hand pump. The level of arsenic in drinking water was significantly above the WHO safe limit for arsenic.
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