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101.
Kandadi P Syed MA Goparaboina S Veerabrahma K 《Nanomedicine : nanotechnology, biology, and medicine》2012,8(7):1162-1171
Diclofenac lipid nanoemulsions (DLNEs) were prepared with different compositions. Based on size, PDI, zeta potential, and in vitro drug release, the optimized DLNEs (DLNE-4 and DLNE-7) were developed and evaluated for drug content, entrapment efficiencies, and stability in comparison to the control formulation (DLNE-1). The albumin was coupled to DLNE-7 globules (DLNE-8) by water soluble carbodiimide (EDC) method, purified, and quantified by modified Bradford method. The pharmacokinetic study was conducted in inflammation (granuloma air pouch model) induced rats. The maximum peak concentration of DLNE-8 was almost fourfold to fivefold in comparison to drug solution in granuloma air pouch fluid (GAPF). The therapeutic availability (TA) of DLNE-8 was 2.89, 2.34, and 1.66 times that of drug solution, DLNE-4 and DLNE-7, respectively. The GAPF/serum ratio of diclofenac from DLNE-8 was above one at all time points indicating the targeting potential of albumin ligated LNEs to inflammatory sites. FROM THE CLINICAL EDITOR: This study demonstrates targeted delivery of diclofenac to an inflammatory environment using the granuloma air pouch model and diclofenac nanoemulsions with different compositions. 相似文献
102.
Anshu?ChaudharyEmail author Anoop?Singh Prabhakar?Kumar?Verma 《Organic and medicinal chemistry letters》2014,4(1):15
Background
A rapid and sensitive ultraviolet-visible (UV-VIS) spectroscopic method was developed for the estimation of pyrimidine derivative 6-Bromo-3-(6-(2,6-dichlorophenyl)-2-(morpolinomethylamino) pyrimidine4-yl) -2H-chromen-2-one (BT10M) in bulk form.Results
Pyrimidine derivative was monitored at 275 nm with UV detection, and there is no interference of diluents at 275 nm. The method was found to be linear in the range of 50 to 150 μg/ml. The accuracy and precision were determined and validated statistically. The method was validated as a guideline.Conclusions
The results showed that the proposed method is suitable for the accurate, precise, and rapid determination of pyrimidine derivative.103.
Prabhakar K. Jadhav Matthew A. Schiffler Kostas Gavardinas EuibongJ. Kim Donald P. Matthews Michael A. Staszak D. Scott Coffey Bruce W. Shaw Kenneth C. Cassidy Richard A. Brier Yuke Zhang Robert M. Christie William F. Matter Keyun Qing Jim D. Durbin Yong Wang GaryG. Deng 《ACS medicinal chemistry letters》2014,5(10):1138-1142
104.
Liping Zhang Emily C. Cherney Xiao Zhu Tai-an Lin Johnni Gullo-Brown Derrick Maley Kathy Johnston-Allegretto Lisa Kopcho Mark Fereshteh Christine Huang Xin Li Sarah C. Traeger Gopal Dhar Aravind Anandam Sandeep Mahankali Shweta Padmanabhan Prabhakar Rajanna Venkata Murali Thanga Mariappan Robert Borzilleri Gregory Vite John T. Hunt Aaron Balog 《ACS medicinal chemistry letters》2021,12(3):494
Indoleamine 2,3-dioxygenase 1 (IDO1) has been identified as a target for small-molecule immunotherapy for the treatment of a variety of cancers including renal cell carcinoma and metastatic melanoma. This work focuses on the identification of IDO1 inhibitors containing replacements or isosteres for the amide found in BMS-986205, an amide-containing, IDO1-selective inhibitor currently in phase III clinical trials. Detailed subsequently are efforts to identify a structurally differentiated IDO1 inhibitor via the pursuit of a variety of heterocyclic isosteres, leading to the discovery of highly potent, imidazopyridine-containing IDO1 inhibitors. 相似文献
105.
Prabhakar R Haresh KP Julka PK Ganesh T Rath GK Joshi RC Sasindran M Naik KK Sridhar PS 《Australasian physical & engineering sciences in medicine / supported by the Australasian College of Physical Scientists in Medicine and the Australasian Association of Physical Sciences in Medicine》2007,30(1):42-45
The risk of inducing contralateral breast (CLB) cancer in patients undergoing tangential field irradiation for the treatment of breast cancer is a serious concern in radiation oncology. A bilateral breast phantom made of wax attached onto the Alderson Rando phantom was used for studying the CLB dose for techniques using physical wedges, EDWs, IMRT and open fields. The skin dose to the CLB was measured at four different points (3 cm from the medial border of the tangential field (P1), nipple (P3), axilla (P4), midpoint between P3 and P1 (P2)). The highest measured dose occurred at P1 with the 60 degrees physical wedges; it was 15.3% of the dose at isocentre. Similarly, the dose measured at P3 (nipple) with 60 degrees physical wedges was 1.90 times higher than the dose with 60 degrees EDWs. The dose at P1 for IMRT (7.8%) was almost the same as that for the open field (8.7%). The skin dose measured at the nipple was 2.1 - 10.9 % of the isocentre dose. The highest CLB doses were contributed by medial wedged fields. The dose to the CLB can be reduced by using IMRT or avoiding wedging the medial tangential fields. A set-up error in the longitudinal direction has little impact on the CLB dose. Set-up errors > 1 cm in the vertical and lateral directions have significant impact on the CLB dose. 相似文献
106.
Piperine, the active principle of Piper longum, Piper nigrum and Zingiber officinalis, has been reported to enhance the oral bioavailability of phenytoin in human volunteers. The objective of this study was to explore the effect of a single dose of piperine in patients with uncontrolled epilepsy on the steady-state pharmacokinetics of phenytoin. Two groups of 10 patients each receiving either a 150 mg or 200 mg twice daily dose of phenytoin were selected. Twelve hours after the night dose, venous blood samples were collected at 0, 0.5, 1, 2, 4, 6, 9, 12 h after administration of phenytoin. On the next study day, piperine 20 mg was administered along with phenytoin and samples were collected similarly. The mean plasma drug concentrations at different time points and the pharmacokinetic parameters before and after piperine administration were compared by Student's t-test. Piperine increased significantly the mean plasma concentration of phenytoin at most of the time points in both dose groups. There was a significant increase in AUC((0-12h)) (p < 0.01), C(max) (p < 0.001) and K(a) (p < 0.05) whereas the changes in K(el) and t(max) were not significant. The results showed that piperine enhanced the bioavailability of phenytoin significantly, possibly by increasing the absorption. 相似文献
107.
108.
Psychiatric morbidity in a general practice in an Indian city 总被引:1,自引:0,他引:1
C Shamasundar S K Murthy O M Prakash N Prabhakar D K Krishna 《British medical journal (Clinical research ed.)》1986,292(6537):1713-1715
Psychiatric morbidity in an Indian general practice was studied using the 12 item version of the General Health Questionnaire to screen 882 patients who represented 9000 consecutive adult patients attending the practice. The questionnaire was valid with a cutting score of 1/2 when compared with section 1 of the standardised Indian Psychiatric Survey Schedule. The probable prevalence of psychiatric morbidity was 35.9%. The general practitioner identified only about 25% of patients. Five of the 12 questions on the General Health Questionnaire had a higher discriminatory capacity, and the performance of the patients on these five questions was valid when compared to section 1 of the Indian Psychiatric Survey Schedule. 相似文献
109.
110.
Terminalia arjuna is an important cardiotonic plant described in the Ayurveda, the ancient Indian medical science. It is also believed to have the ability to cure hepatic, urogenital, venereal and viral diseases. An attempt is made here to analyse the available drug recipes using this plant from Sanskrit literature in the light of modern scientific knowledge. The chemistry and pharmacology of T. arjuna are also discussed, and areas of future investigations are identified. 相似文献