An Insight on the Prospect of Quinazoline and Quinazolinone Derivatives as Anti-tubercular Agents.

Multiple potential drugs have been developed based on the heterocyclic molecules for the treatment of different symptoms. Among the existing heterocyclic molecules, quinazoline and quinazolinone derivatives have been found to exhibit extensive pharmacological and biological characteristics. One significant property of these molecules is their potency as anti-tubercular agents. Thus, both quinazoline and quinazolinone derivatives are modified using different functional groups as substituents for investigating their anti-tubercular activities. We present a summary of the reported anti-tubercular drugs, designed using quinazoline and quinazolinone derivatives, in this review.

Effect of alkalizing agent on abuse deterrent potential of multiple-unit ingestion of bilayer abuse-deterrent extended-release tablets using propranolol as model drug for opioids overdose crisis.

The objective of present study is to develop bilayer abuse-deterrent extended-release tablets (ADERTs) using propranolol HCl as model drug for opioids overdose crisis. Bilayer ADERTs were fabricated by direct compression and formulated with polymer matrix in extended-release drug layer coupled with alkalizing and aversive agents in fast-disintegrating pH modifying layer. Various alkalizing agents, like magnesium hydroxide, aluminum hydroxide, calcium carbonate, and calcium hydroxide, were evaluated for their abuse-deterrent potential via in-vitro drug release and extraction studies. Based on the outcomes, magnesium hydroxide was selected as an alkalizing agent, since it raised the pH of dissolving media near to pKa of the drug studied in this investigation. The formulated bilayer ADERTs with magnesium hydroxide provided similar drug release profiles as compared to conventional extended-release tablets for single-unit ingestion. However, upon ingestion of multiple-unit bilayer ADERTs, the fast-disintegrating pH modifying layer increases pH of dissolving media, while extended-release layer increases micro-environmental pH within tablets. Retarding drug release owing to low solubility of basic drug at higher pH was observed. Therefore, the application of alkalizing agent has impact on pH-dependent solubility of drug like opioids and demonstrate its useful potential to be incorporated in bilayer ADERTs for opioids overdose crisis.

Sublingual insulin administration: application of hydroxypropyl beta-cyclodextrin and poloxamer188 as permeation enhancers.

The objective of this investigation is to investigate the feasibility of sublingual insulin administration. Insulin solutions formulated with permeation enhancers (HPßCD/poloxamer 188) and their in-vitro and in-vivo performances were evaluated. Thereafter, insulin fast-dissolving film was further developed to have similar properties, upon dissolving the film, of the optimized insulin solution. In-vitro performance was evaluated via effect of HPßCD and/or poloxamer 188 concentration across cellulose acetate membrane and porcine esophagus. In-vivo performance was evaluated via pharmacodynamic and pharmacokinetic profiles of insulin solution administered. Cumulative amounts of insulin permeated at 60 min formulated with HPßCD (5%), poloxamer 188 (0.5%), and their combination were 1.31, 3.23, and 4.99 IU/cm2, respectively, indicating an additive effect of combination of HPßCD and poloxamer 188. Insulin-induced hypoglycemic effect was observed for insulin solutions with combination of HPßCD and poloxamer 188 after sublingual administration to Sprague-Dawley rats. Microscopic evaluation of porcine oesophageal tissue indicates that HPßCD and poloxamer 188 are safe. Furthermore, the cumulative amount permeated across cellulose acetate membrane at 30 min was 1.13 and 1.00 IU/cm2 for insulin solution and fast-dissolving film, respectively, demonstrating to be similar. In conclusion, the use of HPßCD/poloxamer 188 is feasible for the development of sublingual insulin solutions/films.

Sustainable improvement of soil health utilizing biochar and arbuscular mycorrhizal fungi: A review.

Conservation of soil health and crop productivity is the central theme for sustainable agriculture practices. It is unrealistic to expect that the burgeoning crop production demands will be met by a soil ecosystem that is increasingly unhealthy and constrained. Therefore, the present review is focused on soil amendment techniques, using biochar in combination with arbuscular mycorrhizal fungi (AMF), which is an indispensable biotic component that maintains plant-soil continuum. Globally significant progress has been made in elucidating the physical and chemical properties of biochar; along with its role in carbon sequestration. Similarly, research advances on AMF include its evolutionary background, functions, and vital roles in the soil ecosystem. The present review deliberates on the premise that biochar and AMF have the potential to become cardinal to management of agro-ecosystems. The wider perspectives of various agronomical and environmental backgrounds are discussed. The present state of knowledge, different aspects and limitations of combined biochar and AMF applications (BC + AMF), mechanisms of interaction between biochar and AMF, effects on plant growth, challenges and future opportunities of BC + AMF applications are critically reviewed. Given the severely constrained nature of soil health, the roles of BC + AMF in agriculture, bioremediation and ecology have also been examined. In spite of the potential benefits, the functionality and dynamics of BC + AMF in soil are far from being fully elucidated.

Speciation, contamination, ecological and human health risks assessment of heavy metals in soils dumped with municipal solid wastes.

The main aim of this work is to assess the extent of soil contamination, potential ecological and health risks associated with the disposal of municipal solid waste (MSW) near a Ramsar site in Assam, India. Soil samples were collected and analysed for three heavy metals (HMs), namely, chromium (Cr), manganese (Mn) and zinc (Zn). The sources of HMs and their pollution levels were evaluated using different indices. The results demonstrated that Cr contamination was high near the metal scrap segregations unit within the dumping site, otherwise, the ecological risks associated with Zn and Mn were found to be low. The speciation of Cr and Zn were associated with the Fe-Mn oxide bound (F4) fraction, accounting 44.23% and 30.68%, respectively, whereas Mn (52.55%) was associated with the exchangeable fraction (F2). The fate and origin of HMs were assessed using mobility and enrichment factors and 16 out of the 20 sampling sites fell under the category of heavily polluted category for Cr, while others which were nearby the metal segregation units fell under the strongly to extremely polluted category. In few sites, significant enrichment was observed for Zn and minimal to moderate enrichment for Mn, respectively. Health risk assessment results indicated that Cr posed higher threat to human health through ingestion.

Factors Associated with Time to Full Feeds in Preterm Very Low Birth Weight Infants.

BACKGROUND: Feeding intolerance prolongs time to full feeds (TFFs) in preterm infants. We studied factors associated with TFF in preterm infants on standardized feeding regimen (SFR) and routine probiotic supplementation (RPS). METHODS: This is a prospective cohort study of preterm infants ≤1500 g. Pearson's correlation, Mann-Whitney test and multivariate analysis were used. RESULTS: In total, 37 of 304 admitted infants died before reaching full feeds. Median (interquartile range) gestation, birth weight and TFF were 31.4 (30-33.05) weeks, 1210 (1066-1400) g and 11 (8-15) days, respectively. Gestation and birthweight were inversely correlated with TFF, whereas low Apgar's, sepsis, patent ductus arteriosus (PDA) and respiratory distress syndrome were directly correlated with TFF. Growth-restricted infants had significantly shorter TFF vs. appropriate for gestational age infants, probably because of higher gestation. On multivariate analysis gestation, sepsis and PDA were significant predictors of TFF. CONCLUSION: In preterm infants managed with SFR and RPS, gestation had inverse correlation with TFF, whereas sepsis and PDA had direct correlation with TFF.

Early Discharge of Preterm Infants- An Indian Perspective.

INTRODUCTION: Early home discharge of preterm infants is a priority in developing countries due to bed shortage and poor socio-economic status. There is wide variation in home discharge policies for preterm infants. Limited data exists on optimal timing for discharging such infants. In view of the socio-economic and medico-legal importance of the issue, we aimed to study the outcomes of our ex-preterm infants discharged home 'early', to guide our clinical practice. AIM: To study the rates of re-admissions/mortality within 4 weeks after discharge in preterm (born <34 weeks) infants. MATERIALS AND METHODS: This was an analysis of retrospectively collected data on all ex-preterm infants (gestation <34 weeks at birth) discharged home from our Neonatal Intensive Care Unit (NICU) during the study period. Infants enrolled were stratified based on their gestation age: Group I (n=54): 26-29 weeks, Group II (n=181): 30-34 weeks. Data on demographic characteristics, hospital course and outcomes were analysed for infants meeting inclusion criteria. Re-admission and/or mortality within 4 weeks after discharge were studied. RESULTS: The mean±(SD) duration of stay was 42±19 vs. 19±14 days in group I vs. II infants. Five (2.7%) infants were re-admitted within the first four weeks after discharge in group II; none in group I. CONCLUSION: Early home discharge for preterm infants born <34 weeks was feasible and safe in our set-up. Large prospective studies are required to confirm these benefits.