FORMULATION AND EVALUATION OF CHRONOMODULATED PULSATILE THERAPEUTIC SYSTEM FOR EARLY MORNING SURGE IN BLOOD PRESSURE

Objective: The objective of this study was to design and developed a rupturable coating type of pulsatile press coated tablet, which releases drug early in the morning hours. This delivery system was helpful to control an early morning surge in Blood Pressure because cardiovascular events occur more frequently in the morning. This delivery system would be useful for the prevention of cardiovascular events in hypertensive patients.Methods: Initially core tablet was prepared by using Captopril HCl as a model drug, which is having Angiotensin-converting enzyme inhibition activity and different concentration of cross carmellose sodium as a superdisintegrant by the direct compression method. Core tablet was press coated by using HPMC K4M and Ethyl Cellulose in different ratios as a press coating polymers.Results: Core tablet was evaluated for different evaluation parameters and the formulation which shows least disintegration time has been selected for further study. Dissolution profiles clearly indicate that Captopril released from the press-coated tablet depends on the amount of an HPMC/EC ratio used.Conclusion: From in-vitro dissolution study it was concluded that the lag time decreases with increase in concentration of HPMC K4M. When the concentration of hydrophilic polymer was increased, i.e. HPMC K4M, hydration property of the system increases, causing more rapid dissolution or rupturing of the external shell resulting in the reduction in lag time.Â

Comparison of Hermetic Storage of Wheat with Traditional Storage Methods in India

India is among the countries experiencing high postharvest losses. Four hermetic bags, two metallic bins, and two gunny bag (also known as jute or burlap bag) piles each containing 1 tonne of wheat were instrumented with temperature, relative humidity, and carbon dioxide sensors. Representative samples from each structure were collected each month and tests for moisture, germination, insect-damaged grain, and milling yield were performed. After nine months, wheat stored in hermetic bags had higher germination (87%) and lower insect-damaged grain percentages (0% to 0.33% with a mean value of 0.2%). Hermetic bags with deliberately introduced Rhyzopertha dominica successfully eliminated the pests. Gunny bag piles had infestations; metallic bins also were infested. Wheat moisture content in all structures varied depending upon ambient conditions; moisture variation was largest in gunny bag piles. Milling yields were lowest for gunny bag piles. Hermetic bags can be an effective and environmentally friendly solution for reducing storage losses of wheat in India

Comparison of Hermetic Storage of Wheat with Traditional Storage Methods in India

India is among the countries experiencing high postharvest losses. Four hermetic bags, two metallic bins, and two gunny bag (also known as jute or burlap bag) piles each containing 1 tonne of wheat were instrumented with temperature, relative humidity, and carbon dioxide sensors. Representative samples from each structure were collected each month and tests for moisture, germination, insect-damaged grain, and milling yield were performed. After nine months, wheat stored in hermetic bags had higher germination (87%) and lower insect-damaged grain percentages (0% to 0.33% with a mean value of 0.2%). Hermetic bags with deliberately introduced Rhyzopertha dominica successfully eliminated the pests. Gunny bag piles had infestations; metallic bins also were infested. Wheat moisture content in all structures varied depending upon ambient conditions; moisture variation was largest in gunny bag piles. Milling yields were lowest for gunny bag piles. Hermetic bags can be an effective and environmentally friendly solution for reducing storage losses of wheat in India

INTERNATIONAL JOURNAL OF PHARMACY & LIFE SCIENCES RP-HPLC simultaneous estimation of metronidazole and diloxanide furoate in combination

Abstract A reverse phase high performance liquid chromatography method was developed for the simultaneous estimation of diloxanide furoate and metronidazole in formulation. The separation was achieved by octadecyl C8 column and a mixture of methanol: acetonitrite: 0.05M phosphate buffer at pH 4.0 (45:25:30 v/v) as eluent, at a flow rate of 1 ml/min. detection was carried out at 277 nm. Quantitation was done by external standard method. The retention time of metronidazole and diloxanide furoate was found to be 3.28 and 6.42 min, respectively. The method has validated for linearity, accuracy and precision. Linearity of metronidazole and diloxanide furoate were in the range of 5-50 µg/ml for both the drugs The mean recoveries obtained for metronidazole and diloxanide furoate were100.01% and 99.71%, respectively. The developed method was found to be accurate, precise, selective and rapid for the simultaneous estimation of metronidazole and diloxanide furoate in tablet

Development of efficient designs of cooking systems. II. Computational fluid dynamics and optimization

Sections 2-6 of Part I were devoted to the analysis of heat transfer characteristics of cookers. In all the experiments, only water was employed as a working medium. Now, we extend such an analysis to the actual cooking process in order to arrive at an improved cooking device. The major strategies for the optimization of energy utilization is to design appropriate insulation that has been obtained by two cover vessels. In order to select an air gap, the flow and temperature patterns in the air gap have been extensively analyzed using computational fluid dynamics (CFD). The flow pattern and heat transfer in cooking pots have also been analyzed by CFD. This has enabled us to design suitable internals for minimizing the stratification of temperature. The understanding of fluid mechanics has also given basis for selection of heat flux, gap between burner tip and cooker bottom, and temperature of flue gases leaving the cooker. Chemical engineering principles have been used for modeling and optimization. Kinetics have been obtained in batch cookers. The knowledge of kinetics, thermal mixing, axial mixing, and optimum selection of insulation have been employed for the development of continuous cookers. The continuous mode of operation also helps in saving of energy. Systematic data have been collected for the design and scale up of continuous cookers. © 2011 American Chemical Society

Development of efficient designs of cooking systems. III. Kinetics of cooking and quality of cooked food, including nutrients, anti-nutrients, taste, and flavor

Part III of the series on cooking systems presents a qualitative description of cooking methods such as open pan cooking, pressure cooking, steam cooking, solar energy-based cooking, microwave cooking, etc. A large number of chemical and physical changes occur during the process of cooking. These changes have been comprehensively covered in published literature including some textbooks. An attempt has been made to discuss a brief coherent description regarding the changes occurring in starches, proteins, fats, etc. The kinetics of the cooking reaction has also been investigated. This information can be advantageously employed for developing a protocol for an optimum temperature-time program. Because the cooking process is practically thermally neutral, a good scope is available for the optimization of energy supply. It was also thought desirable to understand the kinetics of degradation of proteins, vitamins, anti-nutrients, and flavors in different cooking practices, including microwave ovens and pressure cookers. The mechanism of cooking of rice and lentils has been described. The cooking process involves first the transfer of water from bulk to the particle surface, where the resistance for transfer is provided by a thin film in the vicinity of grain (rice and lentils) surfaces. Second, water has to transfer from the external surface to swollen cooked mass to uncooked core. Finally, on the surface of the uncooked core, the cooking reaction occurs. All published literature regarding this mechanism has been systematically analyzed, and the procedure has been given regarding the rate controlling step(s) and the estimation of the overall rate of cooking. For this purpose, the mathematical models have been given and methods have been described for the quantitative evaluation of the model parameters. A substantial amount of additional work is needed on the mechanism of cooking and suggestions have been made for future research. © 2011 American Chemical Society

Discovery of Clinical Candidate 1‑(4-(3-(4-(1<i>H</i>‑Benzo[<i>d</i>]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), A Potent, Selective, and Efficacious Inhibitor of Phosphodiesterase 10A (PDE10A)

We report the identification of a PDE10A clinical candidate by optimizing potency and in vivo efficacy of promising keto-benzimidazole leads <b>1</b> and <b>2</b>. Significant increase in biochemical potency was observed when the saturated rings on morpholine <b>1</b> and <i>N</i>-acetyl piperazine <b>2</b> were changed by a single atom to tetrahydropyran <b>3</b> and <i>N</i>-acetyl piperidine <b>5</b>. A second single atom modification from pyrazines <b>3</b> and <b>5</b> to pyridines <b>4</b> and <b>6</b> improved the inhibitory activity of <b>4</b> but not <b>6</b>. In the in vivo LC–MS/MS target occupancy (TO) study at 10 mg/kg, <b>3</b>, <b>5</b>, and <b>6</b> achieved 86–91% occupancy of PDE10A in the brain. Furthermore, both CNS TO and efficacy in PCP-LMA behavioral model were observed in a dose dependent manner. With superior in vivo TO, in vivo efficacy and in vivo PK profiles in multiple preclinical species, compound <b>5</b> (AMG 579) was advanced as our PDE10A clinical candidate