692 research outputs found

    A REVIEW ON “DRY SYRUPS FOR PAEDIATRICS”

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    Suspensions may be defined as preparations containing finely divided drug particles (the suspensoid) distributed somewhat uniformly throughout a vehicle with or without stabilizers and other additives in which drug exhibits a minimum degree of solubility hence conventional oral suspension can be administered immediately (ready to use form) and not requiring reconstitution at the time of dispensing are simply designated as “Oral Suspension”. There is an important category of suspension that are available as dry powders intended for suspension in liquid vehicles. These are dry mixtures containing the drug and suitable suspending and dispersing agents to be diluted and agitated with a specific quantity of vehicle, most often purified water. Drugs that are instable if maintained for extended periods in the presence of aqueous vehicle (eg., many antibiotic drugs) are frequently supplied as dry powder mixtures for reconstitution at the time of dispensing. This type of preparation is designated in the USP by a title “for Oral Suspension”. The reconstituted system is the formulation of choice when the drug stability is a major concern. After reconstitution, these systems have a short but acceptable life if stored at refrigerator temperatures. Reconstitutable oral systems show the adequate chemical stability of the drug during shelf life, avoids the physical stability problems related to solubility, pH and incompatibilities with other ingredients and also reduce the weight of the final product because the aqueous vehicle is absent and consequently the transportation expenses may be reduced. Dry syrup form of the drug is also useful in case of bioavailability as it has high bioavailability rather than tablets and capsules as it disintegrates in water outside of the oral cavity and directly the suspension is gone through the gastrointestinal tract. So the suspension easily absorbs in the GIT. A number of commercial and official preparations are available as dry powder mixtures. The present review gives an account of the excipients used, methods of preparation of dry syrups along with their evaluations, their packaging, examples of research articles, few marketed preparations

    Correlation of peak expiratory flow rate and single breath count in normal adults

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    Background: Spirometry mandates the requirement of equipments and skilled technicians which may be difficult to acquire in resource limited situations. Thus simple alternative tests like Peak Expiratory Flow Rate (PEFR) and Single Breath Count (SBC) can be used to assess the pulmonary functioning of an individual.Methods: Hundred healthy participants of both genders between the age group of 18-50 years were recruited for this study. They were asked to perform PEFR using the Mini Wright Peak Flow Meter and SBC using a metronome. Three reading were noted and the best of three readings were used for analysis.Results: The mean age and BMI of the participants were 31.54±10.42 years and 23.88±5.14 kg/m2 respectively. The Spearman’s correlation coefficient of PEFR and SBC was 0.7048 with p<0.001 indicating a strong positive correlation.Conclusions: SBC can be used as a simple, convenient and cost-effective alternative to PEFR to assess pulmonary function in adults.

    Design Analysis Fabrication and Testing of Progressive Air Suspension Strut

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    Ride comfort and adjustability has always been deprived on low budget suspensions. The main problems faced in the current market shocks are that, they being heavy and having no adjustability. There should be a way to provide the masses with a highly efficient shock absorber for a very low price. The project aims to provide the reader an ideal way to design, analyze, simulate and manufacture a non-conventional shock absorber having adjustability in the ride parameters

    Therapeutic Strategies and Biomarkers to Modulate PARP Activity for Targeted Cancer Therapy

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    Poly-(ADP-ribose) polymerase 1 (PARP1) is commonly known for its vital role in DNA damage response and repair. However, its enzymatic activity has been linked to a plethora of physiological and pathophysiological transactions ranging from cellular proliferation, survival and death. For instance, malignancies with BRCA1/2 mutations heavily rely on PARP activity for survival. Thus, the use of PARP inhibitors is a well-established intervention in these types of tumors. However, recent studies indicate that the therapeutic potential of attenuating PARP1 activity in recalcitrant tumors, especially where PARP1 is aberrantly overexpressed and hyperactivated, may extend its therapeutic utility in wider cancer types beyond BRCA-deficiency. Here, we discuss treatment strategies to expand the tumor-selective therapeutic application of PARP inhibitors and novel approaches with predictive biomarkers to perturb NAD+ levels and hyperPARylation that inactivate PARP in recalcitrant tumors. We also provide an overview of genetic alterations that transform non-BRCA mutant cancers to a state of “BRCAness” as potential biomarkers for synthetic lethality with PARP inhibitors. Finally, we discuss a paradigm shift for the use of novel PARP inhibitors outside of cancer treatment, where it has the potential to rescue normal cells from severe oxidative damage during ischemia-reperfusion injury induced by surgery and radiotherapy

    Synthesis, and biological screening of chloropyrazine conjugated benzothiazepine derivatives as potential antimicrobial, antitubercular and cytotoxic agents

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    A series of twenty new chloropyrazine conjugated benzothiazepines (22-41) have been synthesized with 58%–95% yields. The compounds were characterized by using different spectroscopic techniques including FT-IR, ¹H NMR, ¹³C NMR spectroscopy and mass spectrometry. The synthesized compounds (22-41) and their precursor chalcones (2-21) were evaluated for antitubercular and cytotoxic activities. Additionally, compounds 22-41 were also tested for antimicrobial activity. Among the chalcone series (2-21), compounds 7 and 14 showed significant antitubercular activities (MICs 25.51 and 23.89 µM, respectively), whereas among benzothiazepines (22-41), compounds 27 and 34 displayed significant antimicrobial (MICs 38.02 µM, 19.01 µM) and antitubercular (MIC 18.10 µM) activities. Compounds 7 and 41 displayed cytotoxic activities with IC₅₀ of 46.03 ± 1 and 35.10 ± 2 µM respectively. All the compounds were evaluated for cytotoxic activity on normal human liver cell lines (L02) and found to be relatively less selective towards this cell line. The most active compounds identified through this study could be considered as potential leads for the development of drugs with possible antimicrobial, antitubercular, and cytotoxic activities

    Design, Facile Synthesis and Characterization of Dichloro Substituted Chalcones and Dihydropyrazole Derivatives for Their Antifungal, Antitubercular and Antiproliferative Activities

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    Infectious diseases caused by fungi and mycobacteria pose an important problem for humankind. Similarly, cancer is one of the leading causes of death globally. Therefore, there is an urgent need for the development of novel agents to combat the deadly problems of cancer, tuberculosis, and also fungal infections. Hence, in the present study, we designed, synthesized, and characterized 30 compounds including 15 chalcones (2–16) and 15 dihydropyrazoles (17–31) containing dichlorophenyl moiety and also screened these compounds for their antifungal, antitubercular, and antiproliferative activities. Among these compounds, the dihydropyrazoles showed excellent antifungal and antitubercular activities whereas the chalcones exhibited promising antiproliferative activity. Among the dihydropyrazoles, compound 31 containing 2-thienyl moiety showed promising antifungal activity (MIC 5.35 µM), whereas compounds 22 and 24 containing 2,4-difluorophenyl and 4-trifluoromethyl scaffolds revealed significant antitubercular activity with the MICs of 3.96 and 3.67 µM, respectively. Compound 16 containing 2-thienyl moiety in the chalcone series showed the highest anti-proliferative activity with an IC₅₀ value of 17 ± 1 µM. The most active compounds identified through this study could be considered as starting points in the development of drugs with potential antifungal, antitubercular, and antiproliferative activities

    Complete genome sequences of seven Vibrio cholerae phages isolated in China

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    The complete genome sequences of seven closely related Vibrio cholerae phages isolated from environmental sites in southeastern China are reported here. Phages QH, CJY, H1, H2, H3, J2, and J3 are members of the Podoviridae family and are highly similar to the previously sequenced Vibrio phages VP2, VP5, and phiVC8

    Effect of physiotherapy on single breath count and breath holding time in COVID-19 patients

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    Background: The novel Coronavirus is known to primarily affect the respiratory system and physiotherapy treatment is integral to combat this infection. However, the assessment of pulmonary function poses a difficult challenge considering the risk of spread of infection and sanitisation of the devices used. Single breath count (SBC) and breath holding time (BHT) can be thus adopted as bedside assessment tests for pulmonary function following physiotherapy treatment.Method: In this a retrospective observational study of 51 COVID-19 patients, mean age 51.7±14.56 years, on room air, admitted in the step-down units of a tertiary care hospital. Patients received standard physiotherapy treatment, within safe hemodynamic limits. Pre and post treatment session SBC was recorded in 32 patients and BHT in 19 patients. Three reading were noted and the best of three readings were used for analysis.Results: The paired t test was used to analyse SBC and BHT. Mean pre and post SBC was 18.25±8.96 and 23.31±9.96 respectively with a mean difference of 5.06 and p<0.0001. Mean pre and post BHT were 19.37 and 23.05 seconds respectively with a mean difference of 3.68 and p<0.0001.  Statistically significant difference in the pre and post treatment session SBC and BHT was observed, indicating a positive effect of physiotherapy treatment on pulmonary function.Conclusion: Physiotherapy treatment shows significant improvement in the pulmonary function in COVID-19 patients. SBC and BHT tests can be used as assessment and prognostic tools for pulmonary function in COVID-19 patients

    Antitubercular activity assessment of fluorinated chalcones, 2-aminopyridine-3-carbonitrile and 2-amino-4H-pyran-3-carbonitrile derivatives: In vitro, molecular docking and in-silico drug likeliness studies

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    A series of newer previously synthesized fluorinated chalcones and their 2-amino-pyridine-3-carbonitrile and 2-amino-4H-pyran-3-carbonitrile derivatives were screened for their in vitro antitubercular activity and in silico methods. Compound 40 (MIC~ 8 μM) was the most potent among all 60 compounds, whose potency is comparable with broad spectrum antibiotics like ciprofloxacin and streptomycin and three times more potent than pyrazinamide. Additionally, compound 40 was also less selective and hence non-toxic towards the human live cell lines-LO2 in its MTT assay. Compounds 30, 27, 50, 41, 51, and 60 have exhibited streptomycin like activity (MIC~16–18 μM). Fluorinated chalcones, pyridine and pyran derivatives were found to occupy prime position in thymidylate kinase enzymatic pockets in molecular docking studies. The molecule 40 being most potent had shown a binding energy of -9.67 Kcal/mol, while docking against thymidylate kinase, which was compared with its in vitro MIC value (~8 μM). These findings suggest that 2-aminopyridine-3-carbonitrile and 2-amino-4H-pyran-3-carbonitrile derivatives are prospective lead molecules for the development of novel antitubercular drugs
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