Posted by admin on May 1, 2014 in |
The main objective of this work is to study the stereostructures and biological activity of some highly substituted cyclohexenes, cyclohexanols and the intermediates there in. In order to get the desired cyclohexenes, the synthesis of cyclohexanols 2,4-bis(4-chlorobenzoyl)-1-(4-chlorophenyl)-3,5-bis(4-methoxyphenyl)-and 2,4-bis(4-chlorobenzoyl)-1,3,5-tris(4-chlorophenyl)-cyclohexan-1-ols (1b and 2b) from 4’- chloro-4-methoxy- and 4,4’- dichlorochalcones(1 and 2) via 1,5-bis(4-chlorophenyl)-3-(4-methoxyphenyl)- and 1,3,5-tris(4-chlorophenyl)-pentan-1,5-diones(1a and 2a ) using p-chloroacetophenone in the presence of sodium hydroxide(molar ratio, 2:1:10) is first described. These are then dehydrated with p-TsOH which afford typical cyclohexenes, 4,6-bis(4-chlorobenzoyl) -1- (4-chlorophenyl) – 3,5 –bis (4-methoxyphenyl) and 4,6 –bis(4-chlorobenzoyl)-1,3,5 –tris (4-chlorophenyl) –cyclohex-1-enes (1c) and (2c) in quantitative yields containing β,γ-unconjugated double bond following stereoselective syn elimination. Also, in an attempt to synthesize dithiazolidin-4-one (3), the reaction of 1, 5-dione (1a) with mercapto acetic acid and ammonium carbonate is adopted. However, it fails to produce (3) and only a pyridine derivative, 2, 6-bis (4-chlorophenyl)-4-(4-methoxyphenyl) pyridine (4) is obtained.in 87% yield. Structural assignment, stereochemistry and biological assays are discussed. The characterization is done by modern spectroscopic...
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Posted by admin on May 1, 2014 in |
The present work is aimed to formulate Itopride HCl sustained release pelletsusing ethyl cellulose N50 such ashydrophobic polymer by employing the solution/suspension layer technique. The drug excipients compatibility study was carried out by Furor Transform Infrared spectroscopy (FTIR) which reveals no interaction between drug and excipients. Total 12 batches were formulated. Six formulations were prepared by using each natural polymer like ethyl cellulose N50. All the formulations were evaluated for micromeritic properties, physical evaluation, which includes particle size analysis, percentage yield, drug content, drug entrapment efficacy, percent moisture loss and swelling index, in vitro dissolution studies, scanning electron microscopy, and drug polymer interaction studies. The formulated pellets were evaluated for various pellet properties, like hardness, bulk density, tapped density, cars index and dissolution rate. Comparative evaluation of the above-mentioned parameters established the superiority of the pellets formulated with Ethyl cellulose those formulated with different grades. The Optimized batch F3 was found to release the drug for 12 h (96.46%) and follows Higuchi Matrix model in dissolution studies, indicating the...
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Posted by admin on May 1, 2014 in |
Sustained release matrix tablets reduce the frequency of the dosing and increase the effectiveness of the drug by localization at the site of action, providing uniform drug delivery. Sustained release matrix tablets of verapamil hydrochloride were prepared by using HPMC K15M, Xanthan and Guar Gum polymers with different concentration in various batches of the formulations to facilitate the drug release which cause patient compliance as the dosing frequency is reduced. Verapamil HCl was considered as an ideal drug for designing sustained release formulation because of the high frequency of administration and short biological half-life. The sustained release matrices of Verapamil HCl were prepared by wet granulation technique. Drug release was studied by using Dissolution testing apparatus 2 (paddle method) with 0.1 N HCl buffer for 2 hours followed by pH 6.8 Phosphate buffer for 8 hours. The in vitro drug release of various formulations was performed and compared. The results shows that the tablets formulated with HPMC K15M polymer shows more sustained action when compared to that of Xanthan...
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Posted by admin on May 1, 2014 in |
The objective of the present work was to development and validation of stability indicating RP-HPLC assay by applying different stress degradation conditions on lornoxicam in Self Emulsifying Drug Delivery System (SEDDS) formulation. HPLC separation was achieved on analytical technique using C-18 column and mobile phase of Acetonitrile: Methanol (65:35, v/v) at a UV detector. The lornoxicam drug consist in SEDDS formulation was subjected to acid, alkali, oxidation, dry heat and photo degradation treatment apply as stress degradation condition. The method was linear in the drug concentration range of 10-60 μg/ml with a correlation coefficient 0.999. The stress degradation studies showed that Lornoxicam contains in Self Emulsifying Drug Delivery System (SEDDS) formulation undergoes degradation in acid, alkali, oxidation and dry heat condition respectively within the limit as per ICH guidelines and stable in photo-degradation...
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Posted by admin on May 1, 2014 in |
The study aimed to assess the efficacy and safety of Amoxicillin/Clavulanate 625 mg and Amoxicillin/Clavulanate 1 gram in chronic bronchitis patients. Chronic bronchitis, a type of COPD defined by a productive cough that lasts for 3 months or more for at least 2 years, other symptoms include wheezing and breathlessness, upon exertion. It is caused by recurring irritation to the epithelium of bronchi, resulting in chronic inflammation, edema and increased production of mucus by goblet. Clavulanate has high affinity for and binds to certain β-lactamases that generally inactivate amoxicillin by hydrolyzing its β-lactam ring. Combining Clavulanate potassium with amoxicillin extends the antibacterial spectrum of Amoxicillin. The objective is to evaluate the efficacy of monotherapy, adverse drug reaction and perform the comparison of both in Amoxicillin/Clavulanate 625 mg and Amoxicillin/Clavulanate 1 gram. A prospective observational study design was used and the Clinical symptoms, X-ray, PFT (FVC, FEV1, FEF, (FEV1/FVC) and Bacteriologic assessment were assessed to monitor its efficacy and safety. Hence the study concluded that Amoxicillin/Clavulanate 625 mg group was...
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