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Dalvi Avantika V.,Ravi Punna R.,Uppuluri Chandra T.,Mahajan Radhika R.,Katke Sumeet V.,Deshpande Vibha S. 한국약제학회 2021 Journal of Pharmaceutical Investigation Vol.51 No.2
Purpose Rufinamide is an anti-epileptic drug approved for use in children ≥ 4 years of age and in adults. It is marketed as Banzel in the USA. In 2015, Banzel received approval for use in pediatric patients (1–4 years of age) and the patent for which expires in 2023. It suffers from poor oral bioavailability, and hence, small amounts of the drug reach the brain. This has led to high and frequent dosage administration of rufinamide. This work aims to improve its brain bioavailability by formulating a nasal thermosensitive in situ gel using xyloglucan. Methods The formulation was optimized using rheometric analysis, texture analysis, in vitro, and in vivo studies. Pharmacokinetic studies in rats were carried out to assess direct nose to brain uptake for the optimized in situ gelling formulation of rufinamide and compared with intravenous bolus and aqueous nasal suspension of rufinamide. Finally, brain targeting indices % DTE, and % DTP were calculated. Results All the formulations showed gelation below 35 °C. The final formulation comprised 2.0% w/v xyloglucan, 0.01% v/v thiomersal (preservative), and rufinamide in suspended form. The %DTE values for the in-situ gel formulation and aqueous suspension were 1069.94 and 146.88, and the %DTP values were 90.65 and 31.91, respectively. Conclusion This work demonstrated the superiority of the nasal gel formulation over oral formulation of rufinamide. If translated to humans, this would definitely help patients suffering from epilepsy, especially pediatric population, in whose case, a high dose and frequent dosage administration via oral route is inconvenient.
General Solutions of One-Dimensional Compressible Flows
S.V.Deshpande,Y.-K.Lee(이영기),H.-D.Kim(김희동) 대한기계학회 2006 대한기계학회 춘추학술대회 Vol.2006 No.11
One dimensional flow with effects of area change, friction, heat addition and mass addition considered separately is well explored and quite good literature is available for basic academic purpose. Such flows are called Simple One Dimensional Flows. In most practical problems, these effects occur simultaneously, and, in addition, there may be present other phenomena such as chemical reaction, change of phase, changes in molecular weight and specific heat. Such flows are called Generalized One Dimensional Flows. Good literature with the solution procedures for the Generalized One Dimensional Flows is available. In most of the works, the friction factor f is considered a constant for the entire flow field which is not practical. In the present study, an attempt to solve generalized one dimensional flow with friction factor being a function of spatial coordinate x is made. Analysis is carried out for laminar and turbulent flows and variation of properties are reported.
A Parametric Study of the Dump Diffuser Flow
V.R. Sanal Kumar,S. Deshpande,김희동(H.D. Kim),T. Setoguchi 대한기계학회 2005 대한기계학회 춘추학술대회 Vol.2005 No.5
The dump diffuser produces a stable flow pattern under a wide range of operating conditions. Many experimental and numerical studies have been reported on dump diffuser flows with tremendous insight on critical flow features. Nevertheless, the design optimization of dump diffuser is still an emerging field in the modern aircraft industry. Towards meeting the design objectives, using a two-dimensional standard k-ε turbulence model, in this paper parametric studies have been carried out to examine the flow features through a straight-walled pre-diffuser with a dump.
A Computational Study of Aerodynamic Characteristics of Spinning Sphere
S.V.Deshpande,이영기(Y.?K.Lee),김희동(H.-D.Kim) 한국유체기계학회 2006 유체기계 연구개발 발표회 논문집 Vol.- No.-
Computational Study of a sphere subjected to free stream flow and simultaneously subjected to spinning motion is carried out. Three dimensional compressible Navier-Stokes equations are solved using fully implicit finite volume scheme. SST(Shear Stress Transport) k-ω turbulence model is used. Aerodynamic characteristics being affected are studied. Validation of the numerical process is done for the no spin condition. Variation of drag coefficient and shock wave strength with increase in spinning rate is reported. Changes in the wake region of the sphere with respect to spinning speed are also observed.
S. P. Sawarkar,S. G. Deshpande,A. N. Bajaj,P. S. Soni,P. Pandit,V. S. Nikam 한국약제학회 2020 Journal of Pharmaceutical Investigation Vol.50 No.2
Purpose Colonic drug targeting is an elusive goal, implicated for localized drug and systemic delivery of proteins which otherwise cannot be delivered by oral route. The purpose of the present work was to evaluate the suitability of formulation design of compression coating and potential of low molecular weight natural polysaccharides for colonic drug targeting using Gamma Scintigraphy in human subjects and to establish platform technology. Methods Before commencing with in vivo imaging studies in human by Gamma Scintigraphy, we performed in vitro release studies and scanning electron microscopy for surface topography of tablet formulations subjected to in vitro dissolution study. Results We investigated the applicability of low molecular weight and low viscosity grade Guar gum ULV 1000 and Pectin with low degree of methoxylation 9% as for site specific delivery. Gamma Scintigraphy imaging of formulation with biopolymer in human subject showed the transit of tablet intact in colon with average arrival time being 5.75 h and the activity was released continuously for 30 h. Scanning electron microscopy for surface topography of tablets subjected to simulated colonic fluid showed erosion caused by microbial flora of the colon. Conclusion Taken together, compression coating design with low molecular weight biopolymer can serve as a platform technology to deliver other potential molecules to the colonic region for local and/or systemic effects in other therapeutic areas.
Dolichos biflorus Linn attenuate progression of renal damage in alloxan-induced diabetic rats
Chidrewar, G.U.,Mane, V.S.,Ghaisas, M.M.,Deshpande, A.D. Kyung Hee Oriental Medicine Research Center 2010 Oriental pharmacy and experimental medicine Vol.10 No.2
Dolichos biflorus Linn. (Fabaceae), commonly known as Horse gram is a medicinal plant, used in folk medicine for treating kidney stones and diabetes mellitus. The purpose of the present study was to investigate the effects of daily oral feeding of various doses of methanolic extract of Dolichos biflorus seeds (DB) for 42 days on blood glucose concentrations and kidney functions in Alloxan-diabetic rats. Plasma glucose levels, body weight, serum creatinine, and urinary albumin levels were monitored on $15^{th}$, $29^{th}$, $43^{rd}$ day. Renal hypertrophy was assessed as the ratio between the kidney weight and body weight of the rats. Plasma glucose concentrations in Alloxan-diabetic rats were significantly reduced by the administration of DB (350 mg/kg) and DB (700 mg/kg) on day 15 and onwards (P < 0.01). After 15 days of Alloxan administration urinary albumin levels (UAE) were over 5 fold higher in diabetic controls as compared to normal controls. Treatment with DB significantly prevented the rise in UAE levels from day 15 to 43 in comparison to diabetic controls (P < 0.01). Renal hypertrophy was significantly higher in diabetic controls as compared to non-diabetic controls. Treatments with DB (350 mg/kg) and DB (700 mg/kg) significantly prevented renal hypertrophy (P < 0.01) as compared to diabetic controls. DB (175 mg/kg) failed to modify renal hypertrophy. Thus the present study indicates that methanolic extract of Dolichos biflorus may be useful in management of hyperglycemia and kidney functions in Alloxan-diabetic rats.
Ajit KUMAR,Mahesh S. KULYE,Mukund V. DESHPANDE,Mala RAO 한국곤충학회 2010 Entomological Research Vol.40 No.2
In this study, the inhibition of molting fluid enzymes from Helicoverpa armigera by an aspartic protease inhibitor, Alkalophilic Thermophilic Bacillus Inhibitor (ATBI) purified from Bacillus sp. is reported. The in vitro experiments showed 80% inhibition (IC50= 48 µM) of hemoglobin hydrolyzing and 95% inhibition (IC50= 35 µM) of chitin hydrolyzing activity from molting fluid by ATBI (IC50 value is the ATBI concentration for 50% inhibition of total enzymatic activity). The treatment of H. armigera larvae with 400 µM ATBI recorded 20% larval mortality, 27.77% deformed pupae and 12.22% deformed adults. The LC50 value (Concentration of ATBI calculated to give 50% mortality) calculated for insect population was found to be 330.06 µM. Similarly, significant variations in mean larval and pupal weight, no. of eggs laid per female and percent hatching of eggs were observed at higher concentrations of ATBI. The results may provide the basis for the selection of non-host inhibitors to develop a H. armigera insecticide formulation.
Chetty, R.,Gill, P.,Govender, D.,Bateman, A.,Chang, H.J.,Deshpande, V.,Driman, D.,Gomez, M.,Greywoode, G.,Jaynes, E.,Lee, C.S.,Locketz, M.,Rowsell, C.,Rullier, A.,Serra, S.,Shepherd, N.,Szentgyorgyi, W. B. Saunders Co ; Centrum Philadelphia 2012 Human pathology Vol.43 No.11
The aim of this study was to ascertain the level of concordance among gastrointestinal pathologists for regression grading in rectal cancers treated with neoadjuvant chemoradiation. Seventeen gastrointestinal pathologists participated using the Mandard, Dworak, and modified rectal cancer regression grading systems to grade 10 representative slides that were selected from 10 cases of rectal cancer treated with long-course neoadjuvant chemoradiation. The slides were scanned with a whole-slide scanner generating dynamic digitized images. The results showed very little concordance across the 3 grading systems, with κ values of 0.28, 0.35, and 0.38 for the Mandard, Dworak, and modified rectal cancer regression grading systems, respectively. In only 1 of 10 study cases was there unanimous grading concordance using the modified rectal cancer regression grading system. It was felt that these systems lacked precision and clarity for reproducible, accurate regression grading. The study concluded that there was a need for a simple, reproducible regression grading system with clear criteria, a cumulative or composite score taking into account all sections of the tumor bed that is sampled rather than the worst section (highest grade), and there should be a uniform method of sampling of these specimens.