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ISSN (Online): 0975-8232,
ISSN (Print): 2320-5148

International Journal Of
Pharmaceutical Sciences And Research

IJPSR is indexed with Embase

An International Journal published monthly
An Official Publication of Society of Pharmaceutical Sciences and Research

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Posted by on Mar 1, 2016 in | 0 comments

SYNTHESIS OF QUINOLINE DERIVATIVES BY REACTION OF DIMETHYL(2R,3S,4R)-2-PHENYL-4-(PHENYLAMINO)-1,3,4-TRIHYDROQUINOLINE-2,3-DICARBOXYLATE WITH SOME AMINES

In this work, quinoline derivatives were synthesized from reaction of aniline, benzylaldehyde and dimethylacetylene dicarboxylate (DMAD) in sequent steps to provide quinoline derivative dimethyl (2R, 3S, 4R)-2-phenyl-4-(phenylamino)-1, 3, 4-trihydroquinoline-2,3-dicarboxylate (12). Compound (12), was reacted with some amines such as  hydrazine hydrate, urea, thiourea, ethylenediamine, diaminopropane, dinitrophenylhydrazine and o-phenylenediamine to give (3aS,9R,9aS)-2-amino-3a-phenyl-9-(phenylamino)-4,9,9a-trihydro-pyrrolo[3,4-b]quinoline-1,3-dione (13),  (3aR) – 1,3 – dioxo – 3a-phenyl-9-(phenylamino)-4,9,9a-trihydro-pyrrolo[3,4-b]quinoline-2-carboxamide (14), (3aS)-1,3-dioxo-3a-phenyl-9-(phenylamino)-4,9,9a-trihydro-pyrrolo[3,4-b] quinoline – 2-carbothioamide (15),  6a-phenyl-12-(phenylamino)-2,3,4,5,7,12,12a-heptahydro-[1,4]diazocino[6,7-b]quinoline-1,6-dione (16),  (7aS)-7a-phenyl-13-(phenylamino)-2,3,4,5,6,8,13,13a-octahydro-[1,5]diazonino[7,8-b]quinoline-1,7-dione (17),  2-((2,4-dinitrophenyl)amino)-9-(phenylamino)- 4, 9, 9 a – trihydro-pyrrolo [3,4-b] quinoline-1,3-dione (18), and 2-(2-aminophenyl)-6a-phenyl-12-(phenylamino)-2, 4,5,7,12,12a-hexahydro-diazocino[3,4-b]quinoline-1,6- dione (19) respectively. Reaction of (12) sodium metal gave methyl 3-oxo-2-phenyl-5-(phenylamino)-1,2, 4,5-tetrahydro- benzo[b]azepine-4-carboxylate(20). These reactions were carried out with different solvents like acetonitrile, ethanol, and chloroform providing good yields of the new heterocyclic compounds (13-20) of quinoline derivatives. The identification of the compounds(13-20) were based on spectroscopic analysis such as IR, UV, 1H-NMR, 13C-NMR, and the microanalysis of the elements (CHN)...

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Posted by on Mar 1, 2016 in | 0 comments

ENHANCEMENT OF DOMPERIDONE DISSOLUTION RATE VIA FORMULATION OF ADSORBATES AND CO-ADSORBATES

The aim of this study was to enhance the dissolution rate of water-insoluble, weakly basic antiemetic drug; Domperidone (DMP), through the formulation of adsorbates and co-adsorbates. Adsorption of drug onto the surface of three different adsorbents; Avicel PH 101, Florite R and Aerosil 200 was studied and Langmuir adsorption isotherms were constructed.  Adsorbates of drug with the used adsorbents were prepared in different weight ratios by physical mixing, grinding and solvent evaporation methods. Co-adsorbates of drug with Aerosil 200 and Tween 80 were prepared by solvent evaporation method in different weight ratios. The prepared systems were physico-chemically characterized by Fourier- transform Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC) and powder X-ray diffractometry (P-XRD). FT-IR data confirmed the absence of any chemical interaction between DMP and the used adsorbents. P-XRD results confirmed the transformation of some systems from the crystalline state to the amorphous state which aided in the dissolution rate enhancement. Furthermore, the in-vitro dissolution rate of drug from these systems was studied which showed marked enhancement of DMP...

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Posted by on Mar 1, 2016 in | 0 comments

SATURATION SOLUBILITY OF SCOPOLAMINE IN THIN FILMS OF POLYACRYLATE PRESSURE SENSITIVE ADHESIVES IS TEMPERATURE DEPENDENT

The method of drug uptake from solid solution has been used to measure the saturation solubility of scopolamine base in various pressure sensitive adhesive DURO-TAKs at elevated temperature. The saturation solubility was strongly temperature dependent, being 50 – 100 % larger at 45°C than at 25°C. The higher temperature also caused much more rapid approach to equilibrium distribution of the drug between donor, separating membrane, and acceptor layers. With a cross-linked DURO-TAK 87-2677 the saturation solubility is 10.7 ± 0.30 % (n=4) at 25 °C, rising to 16.5 ± 0.54 % at 45 °C (n=4). The non-cross-linked DURO-TAK 87-4098 gives lower values of 6.3 ± 0.27% w/w(n=4) at 25 °C, rising to 13.2 ± 1.14 % at 45 °C. The hydrophobic DURO-TAK 87-2510gives the lowest values of 4.2 ± 0.17 % w/w (n=4) at 25 °C and 8.7 ± 0.45 % (n=4) at 45°C. The thermodynamic activity of the drug in the thin polymer film will therefore decrease as temperature...

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Posted by on Jan 31, 2016 in | 0 comments

COMPARATIVE ANALYSIS OF DRUG-INDUCED PARKINSONISM LIKE BEHAVIORS IN C57BL6 BLACK MICE USING A FORCE PLATE ACTIMETER.

This study aims to compare the Parkinsonism behavior induced by two drugs: Tacrine (9-amino-1,2,3,4-tetrahydroaminoacridine hydrochloride hydrate and MPTP (1-methyl, 4-phenyl 1,2,3,6 tetrahydropyrolidine) using a Force Plate Actimeter (FPA). 25 C57BL/6 black mice were equally divided into two groups for 5mg/kg tacrine and 30mg/kg MPTP experiment. Both groups contained sham, 5mg/kg tacrine or 30mg/kg MPTP group and sinemet group (oral administration of 10mg/kg sinemet (levodopa:carbidopa in 4:1) prior to intraperitoneal injection of 5mg/kg tacrine or 30mg/kg MPTP).  Mice were immediately kept inside FPA to record their behavior. Distance travelled, bout of low mobility (BLM) and power spectra of parkinsonian symptoms shown by both drugs were computed. Both neurotoxins reduced the motor abilities of mice in comparison with sham. Oral treatment of sinemet improved their disability. According to power spectra analysis, tacrine had only one significant narrow peak from 10-12 Hz while MPTP exhibited one to four peaks from 8 to 12 Hz. This might be because the behavior expected from tacrine is lateral movement of jaw (facial part) whilst that...

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Posted by on Jan 31, 2016 in | 0 comments

THE CLINICOPATHOLOGICAL PROFILE IN PATIENTS WITH EPITHELIAL OVARIAN CARCINOMA

The malignant tumors of ovary are a group of disease with varying clinical and biological behavior. It is fifth leading cause of death from cancer in women and the leading cause of death from gynecological cancer. This retrospective study has been undertaken to analyze patients of epithelial ovarian cancers. These cases were analyzed for various features like age, stage at presentation, histological type, and treatment pattern.  Eighty seven patients with ovarian cancer registered at department of Radiotherapy -II, Pt. BDS PGIMS, Rohtak, Haryana from January 2010 to December 2011 have been evaluated in this retrospective study. Histopathological analysis showed 71(82%) cases of epithelial tumors, 5 cases (6%) of sex cord stromal tumor and 11 (13 %) of germ cell tumors. Among the individual tumors serous tumors were the commonest 51%, followed by 18% mucinous carcinoma and 20% undifferentiated carcinoma. The peak incidence was in 5th – 6th decades. Most of the patients were referred after surgery. Surgery performed was TAH & BSO in almost all patients.  All patients were...

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