A progression of Novel Quinazoline subordinates 3 (a-j) have been incorporated from 2-Amino benzo/acetophenone as beginning material. The portrayal of the recently incorporated mixes was established by IR, 1H NMR, 13C NMR ghostly examination. The final compounds were screened for their enemy of bacterial action and antifungal movement. Against parasitic and Anti-bacterial exercises were Evaluated and saw that mixes 3i, 3j, 3e have great action.
Chikkanti Jaganmohan*, R. Venkateshwarlu, K. P. Vinay Kumar, Sandeep Mohanty, Jaydeep Kumar, Akula Raghunadh, B. Venkateswara Rao, R. Mallikarjuna Rao.
Recently several methods have been developed for the determination of drugs and their impurities products by Reversed Phase liquid chromatography. The present paper describes about highly specific, linear, precise, rugged, accurate, robust and stability indicating RP-HPLC method for determination of related substances present in Hydrochlorothiazide tablets. Chromatographic separation for the separation of Hydrochlorothiazide and with Impurity-A by using Thermosil C18 column (4.5×150mm) 5.0µ, flow rate was 0.8ml/min, mobile phase ratio was 65:35% v/v methanol: water pH 3 (pH was adjusted with orthophosphoric acid), detection wavelength was 265nm. The analytical method validation was done according to ICH guidelines. The linearity study Hydrochlorothiazide and with Impurity-A was found in concentration range of 50µg-250µg and 5µg-25µg and correlation coefficient (r2) was found to be 0.999 and 0.999. Hence the suggested RP-HPLC method can be used for routine analysis of Hydrochlorothiazide and with Impurity-A in API and Pharmaceutical dosage form.
Fast dissolving tablets of Enalapril maleate has been prepared by direct compression method using the different super disintegrates: croscarmellose and sodium starch glycolate and Excipients: lactose, sucrose magnesium stearate, sodium lauryl sulphate. The prepared tablets were characterized for the pre-compression parameter UV Spectroscopy, post compression parameter such as thickness, hardness, friability, drugs contents, weight variation, water absorbance ratio, in-vitro disintegrating time, in-vitro dissolution studies. There were no chemical interaction between drugs and Excipients were confirmed by FTIR study. Fast dissolving tablets are prepared by direct compression method, 9 formulations as the F9 to be best as its shows in F9 87.10% (direct compression method) maximum drug release respectively. The prepared tablets stability tested at 40oC having 75% relativity humidity for 1month and found to be stable. Prepared fast dissolving tablets of Enalapril maleate 5mg was found to be under fasting fed condition.
A quick and reproducible superior fluid chromatography technique was created and approved for the estimation of Arterolane Maleate, Piperaquine phosphate in dosage forms. Chromatography is done isocratically on Xbridge C18 (100nm X 4.6nm X 5µm) with a 0.1% Ortho Phosphoric Acid and Acetonitrile (in the proportion of 90:10 (v/v) at a flow of 0.9 ml/min. Measurement was done utilizing a PDA locator at 290nm. The separation time of Arterolane Maleate (ART) and Piperaquine Phosphate (PQP) are 2.9, 6.9 min individually. The Linearity of the method extend and % recovery of Arterolane and Piperaquine are 20-150μg/ml and 99%, 101% separately. The regression of ART and PQP are 0.999. The % relative standard deviations for three reproduce estimations of tests in tablets are under 2%. Developed technique was seen as rapid for synchronous estimation of Arterolane Maleate and Piperaquine phosphate in Pharmaceutical dose formulations. The proposed strategy can be helpful in quality control of bulk manufacturing and Pharmaceutical formulations.
Glycyrrhiza glabra (Phytochemical - Glycyrrhiza - Flavonol A) is herbal plant uses in different countries to treat diabetes mellitus. Glycyrrhiza glabra is a pioneer species, relatively high in bioactive secondary compound and are important for a variety of functions is economically used as a source of tannins, gums, timber, fuel and fodder. Babul plant is therapeutic used as Anti-cancer, anti tumours, Antiscorbutic, Astringent, anti-oxidant, Natriuretic, Antispasmodial, Diuretic, Intestinal pains and diarrhea, Nerve stimulant, Cold, Congestion, Coughs, Dysenter, Fever, Hemorrhages, Leucorrhea, Ophthalmia and Sclerosis. The toxicity study has showed that the 24-Methyl cycloartan compound has no toxic effect on red blood cells; therefore we suggest that this compound can be successfully and safely use to treat diabetes mellitus instead of insulin.
Anticancer drugs selectivity is improved by strategy called Antibody-directed enzyme prodrug therapy. It is a two-step process which benefits over radioimmunoconjugate, chemo-toxin etc. The main functions of Antibody-directed enzyme prodrug therapy are prodrug activation by enzyme and targets cancer cells by the conjugates and selectivity characteristics of prodrug/drugs/enzymes are reviewed. Generation of cytotoxic agents at tumor sites by antibody vectored enzyme from non-toxic pro-drugs. The traditional approach improves the properties of prodrugs which include solubility, permeability, stability, distribution etc. but this therapy improves selectivity. The activation of prodrugs is mainly governed by enzymes that are at higher amounts in tumors, which leads to selective antitumor activity.
Quantum chemical parameters molecular geometry, vibrational frequencies and bonding features were calculated for the molecule 2-[2-ethylaminothiazol-5-oyl]-N-methyl-6-chlorobenzimidazole. The computed geometrical parameters are in close agreement with the experimental data. Charge transfer taking place within the molecule can be carried out using FMO analysis. Besides HOMO-LUMO and Mulliken atomic charges have been computed using DFT calculations.
A Specific, precise, and accurate RP-HPLC method has been developed and validated for the quantitative analysis of Obeticholic acid in tablet formulation by using refractive index detector and UV detector. An isocratic separation was achieved in RI detector using an Inertsil ODS 3V, 150 x 4.6mm; 5µ column with a flow rate of 1.2ml/min and Mobile phase pH 3.0 formic acid Buffer: Acetonitrile (30:70% v/v). An isocratic separation was achieved in UV detector using Cortecs C18+, 150 x 4.6mm; 2.7µ column with 0.7ml/min flow rate at 192nm. Isocratic elution was performed with Mobile phase A and mobile phase B as 0.05% OPA Buffer and Acetonitrile respectively in the ratio of 45:55% v/v. These methods were validated for specificity, linearity, precision, accuracy and robustness. These methods were linear over the concentration range 125-1000ppm and 240- 1500PPM (r2 = 1.0) using RI and UV detectors respectively. The accuracy of the methods was between 98.1-101.7%. These methods were found to be Robust and suitable for the quantitative analysis of Obeticholic acid in a tablet formulation.
The aim of the present work was to formulate and characterize the lamivudine and stavudine loaded nanoparticles. Nanoparticles of Lamivudine and stavudine were prepared by using nanoprecipitation method using Eudragit RL 100 and Poloxamer 407 as polymers. Nanoparticles were prepared by varying parameters like drug to Polymer ratio, centrifugation time to optimize them. The drug loaded optimized lamivudine nanoparticles showed particle size in the range of 80-90nm. Drug entrapment efficiency ranged from 62.8%‐81.4%. In vitro release studies revealed that the rate of drug release from NP 1 optimised formulation was found to be 96.88% in 24 hours which can overcome the side effects associated with the conventional dosage forms. Release of drug followed first order and the mechanism is super case II transport, indicates swelling of polymer with diffusion.
P. Pravalika Reddy*, B. Madhava Reddy, D. Jaya Prakash.
Three simple, accurate and precise spectrophotometric methods have been developed for simultaneous determination of Rabeprazole (RAB) and Ondansetron (OND) in a laboratory mixture. Simultaneous equation method (Method I) shows absorbance at 284.5 nm (λ1) and 307 nm (λ2) corresponding to the absorbance maxima of RAB and OND respectively. In absorbance ratio method (Method II) isobestic point is observed at 291nm. Isobestic point 291 nm is considered as (λ1) and absorbance maxima of OND at 307nm is considered as (λ2). In First order derivative zero crossing method (Method III) (λ1) 247nm (for RAB) and (λ2) 320.5 nm (for OND) was carried out. All dilutions were prepared in distilled water and methanol (50:50). Linearity range was observed in the concentration range of solution 2.5‐12.5μg/ml for RAB and 4-12μg/ml for OND. The methods were validated statistically and recovery study was performed to confirm the accuracy of both drugs. The developed methods are simple, economic, accurate, precise and reproducible. They can be adopted for routine quality control analysis of these drugs in pharmaceutical combined dosage form.
Yogeshwari T. Jambhulkar*, V. P. Rode, N. V. Madan, P. R. Sethia, P. C. Mate, M. S. Sahu, A. N. Maliye.