DEVELOPMENT AND IN VITRO–IN VIVO EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF AN ANTIRETROVIRAL AGENT RITONAVIR

Objective: The present research work concerns the development of the extended release of Ritonavir floating matrix tablets, designed to prolong the gastric residence time, increase the drug bioavailability, and diminish the side effects of irritating drugs. Methods: The floating tablets of Ritonavir were prepared by direct compression method using different grades of hydroxypropyl methylcellulose (HPMC), crospovidone, Polyox WSR 303, and sodium bicarbonate, as gas generating agent. Evaluation parameters and in vivo radiographic studies were conducted in suitable model. Results: Among all formulations, F21 was chosen as optimized formulation based on evaluation parameters such as floating lag time (33 s), total floating time (>24 h), and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product were shown 98.67% and 91.46±5.02% of drug release, respectively. The main appliance of medication discharge follows zero-order kinetics and non- Fickian transport by coupled diffusion and erosion. In vivo experiments maintained the potentials in extending the gastric residence time in the fasted state in beagle dogs. The mean gastric residence time of the optimized formulation found to be 330 min±40 in the stomach, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for enhanced bioavailability. Conclusion: From in vitro and in vivo radiographic studies, Ritonavir floating tablets estimated to provide novel choice for harmless, inexpensive, and extended release for the effective management of AIDS

Drug utilization study of antihypertensive drugs in hypertensive diabetic patients in a tertiary care hospital

Background: Diabetes along with hypertension is a very common ailment afflicting millions of people worldwide. The socio-economic stress caused by the morbidity and mortality associated with it is mind boggling. Hence, this study was undertaken to study the utilization of antihypertensive drugs in hypertensive diabetic patients.Methods: A prospective study was conducted on 100 hypertensive diabetic patients aged between 18 and 90 years of either gender attending Basaveshwar Teaching and General Hospital, Kalaburagi. The data collected were statistically analyzed and presented as counts and percentages.Results: In our study, we found that majority (63%) were male patients and majority belonged to 51-70 years age group. The majority of the patients were prescribed angiotensin converting enzyme inhibitors (ACEIs) alone (19%), followed by a combination of ACEIs and calcium channel blockers (9%). The generic prescribing was only 23%, and patient’s knowledge of correct dosage was 64%.Conclusion: In this study, it has been observed that the antihypertensives drugs were prescribed rationally, but the generic prescribing was only 23% which is inappropriate prescribing behavior. Hence, physicians should be educated to prescribe drugs in the generic name so that the cost of drugs is reduced

Center to limb observations and modeling of the Ca I 4227 A line

The observed center-to-limb variation (CLV) of the scattering polarization in different lines of the Second Solar Spectrum can be used to constrain the height variation of various atmospheric parameters, in particular the magnetic fields via the Hanle effect. Here we attempt to model non-magnetic CLV observations of the $Q/I$ profiles of the Ca I 4227 A line recorded with the ZIMPOL-3 at IRSOL. For modeling, we use the polarized radiative transfer with partial frequency redistribution with a number of realistic 1-D model atmospheres. We find that all the standard FAL model atmospheres, used by us, fail to simultaneously fit the observed ($I$, $Q/I$) at all the limb distances ($\mu$). However, an attempt is made to find a single model which can provide a fit at least to the CLV of the observed $Q/I$ instead of a simultaneous fit to the ($I$, $Q/I$) at all $\mu$. To this end we construct a new 1-D model by combining two of the standard models after modifying their temperature structures in the appropriate height ranges. This new combined model closely reproduces the observed $Q/I$ at all the $\mu$, but fails to reproduce the observed rest intensity at different $\mu$. Hence we find that no single 1-D model atmosphere succeeds in providing a good representation of the real Sun. This failure of 1-D models does not however cause an impediment to the magnetic field diagnostic potential of the Ca I 4227 A line. To demonstrate this we deduce the field strength at various $\mu$ positions without invoking the use of radiative transfer.Comment: 20 pages, 10 figures, Accepted for publication in Ap

Cloning and functional validation of early inducible Magnaporthe oryzae responsive CYP76M7 promoter from rice

Cloning and functional characterization of plant pathogen inducible promoters is of great significance for their use in the effective management of plant diseases. The rice gene CYP76M7 was up regulated at 24, 48, and 72 hours post inoculation (hpi) with two isolates of Magnaporthe oryzae Mo-ei-11 and Mo-ni-25. In this study, the promoter of CYP76M7 gene was cloned from rice cultivar HR-12, characterized and functionally validated. The Transcription Start Site of CYP76M7 was mapped at 45 bases upstream of the initiation codon. To functionally validate the promoter, 5′ deletion analysis of the promoter sequences was performed and the deletion fragments fused with the β-glucuronidase (GUS) reporter gene were used for generating stable transgenic Arabidopsis plants as well as for transient expression in rice. The spatial and temporal expression pattern of GUS in transgenic Arabidopsis plants and also in transiently expressed rice leaves revealed that the promoter of CYP76M7 gene was induced by M. oryzae. The induction of CYP76M7 promoter was observed at 24 hpi with M. oryzae. We report that, sequences spanning -222 bp to -520 bp, with the cluster of three W-boxes, two ASF1 motifs and a single GT-1 element may contribute to the M. oryzae inducible nature of CYP76M7 promoter. The promoter characterized in this study would be an ideal candidate for the overexpression of defense genes in rice for developing durable blast resistance rice lines

Object Sub-Categorization and Common Framework Method using Iterative AdaBoost for Rapid Detection of Multiple Objects

Object detection and tracking in real time has numerous applications and benefits in various fields like survey, crime detection etc. The idea of gaining useful information from real time scenes on the roads is called as Traffic Scene Perception (TSP). TSP actually consists of three subtasks namely, detecting things of interest, recognizing the discovered objects and tracking of the moving objects. Normally the results obtained could be of value in object recognition and tracking, however the detection of a particular object of interest is of higher value in any real time scenario. The prevalent systems focus on developing unique detectors for each of the above-mentioned subtasks and they work upon utilizing different features. This obviously is time consuming and involves multiple redundant operations. Hence in this paper a common framework using the enhanced AdaBoost algorithm is proposed which will examine all dense characteristics only once thereby increasing the detection speed substantially. An object sub-categorization strategy is proposed to capture the intra-class variance of objects in order to boost generalisation performance even more. We use three detection applications to demonstrate the efficiency of the proposed framework: traffic sign detection, car detection, and bike detection. On numerous benchmark data sets, the proposed framework delivers competitive performance using state-of-the-art techniques

Gesture Recognition for Enhancing Human Computer Interaction

Gesture recognition is critical in human-computer communication. As observed, a plethora of current technological developments are in the works, including biometric authentication, which we see all the time in our smartphones. Hand gesture focus, a frequent human-computer interface in which we manage our devices by presenting our hands in front of a webcam, can benefit people of different backgrounds. Some of the efforts in human-computer interface include voice assistance and virtual mouse implementation with voice commands, fingertip recognition and hand motion tracking based on an image in a live video. Human Computer Interaction (HCI), particularly vision-based gesture and object recognition, is becoming increasingly important. Hence, we focused to design and develop a system for monitoring fingers using extreme learning-based hand gesture recognition techniques. Extreme learning helps in quickly interpreting the hand gestures with improved accuracy which would be a highly useful in the domains like healthcare, financial transactions and global busines

Overall Survival with Fulvestrant plus Anastrozole in Metastatic Breast Cancer

BACKGROUND We previously reported prolonged progression-free survival and marginally prolonged overall survival among postmenopausal patients with hormone receptor-positive metastatic breast cancer who had been randomly assigned to receive the aromatase inhibitor anastrozole plus the selective estrogen-receptor down-regulator fulvestrant, as compared with anastrozole alone, as first-line therapy. We now report final survival outcomes. METHODS We randomly assigned patients to receive either anastrozole or fulvestrant plus anastrozole. Randomization was stratified according to adjuvant tamoxifen use. Analysis of survival was performed by means of two-sided stratified log-rank tests and Cox regression. Efficacy and safety were compared between the two groups, both overall and in subgroups. RESULTS Of 707 patients who had undergone randomization, 694 had data available for analysis. The combination-therapy group had 247 deaths among 349 women (71%) and a median overall survival of 49.8 months, as compared with 261 deaths among 345 women (76%) and a median overall survival of 42.0 months in the anastrozole-alone group, a significant difference (hazard ratio for death, 0.82; 95% confidence interval (CIS, 0.69 to 0.98; P=0.03 by the log-rank test). In a subgroup analysis of the two strata, overall survival among women who had not received tamoxifen previously was longer with the combination therapy than with anastrozole alone (median, 52.2 months and 40.3 months, respectively; hazard ratio, 0.73; 95% CI, 0.58 to 0.92); among women who had received tamoxifen previously, overall survival was similar in the two groups (median, 48.2 months and 43.5 months, respectively; hazard ratio, 0.97; 95% CI, 0.74 to 1.27) (P=0.09 for interaction). The incidence of long-term toxic effects of grade 3 to 5 was similar in the two groups. Approximately 45% of the patients in the anastrozole-alone group crossed over to receive fulvestrant. CONCLUSIONS The addition of fulvestrant to anastrozole was associated with increased long-term survival as compared with anastrozole alone, despite substantial crossover to fulvestrant after progression during therapy with anastrozole alone. The results suggest that the benefit was particularly notable in patients without previous exposure to adjuvant endocrine therapy.National Cancer Institute; AstraZeneca6 month embargo; published 28 March 2019.This item from the UA Faculty Publications collection is made available by the University of Arizona with support from the University of Arizona Libraries. If you have questions, please contact us at [email protected]