Posted by admin on Nov 1, 2014 in |
Promethazine hydrochloride, one of the most effective agents for treating motion sickness, mainly acts as a strong antagonist of H1 receptor (antihistamine) and it blocks the action of acetylcholine on the receptors (anticholinergic effect). The purpose of present work was a development of fast dissolving oral film of promethazine HCl to overcome the limitation of current routes of administration, to provide faster dissolution rate and increase patient compliance, especially for outpatient setting. The amount of drug was calculated according to the area of petri plate. The amount of drug was then used for the preparation of film by solvent casting method utilizing HPMC E3, HPMC E5, HPMC E15, and HPMC E50 as a film-forming polymers. The effect of plasticizers (PEG 200, PEG 400, PEG 600, glycerine, propylene glycol, triethyl citrate) and their concentration were tested for physicomechanical properties of casted films. Aspartame was used as a sweetener. The IR spectral studies showed no interaction between drug and polymer or with other additives. Using experimental design, the prepared formulations were...
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Posted by admin on Nov 1, 2014 in |
The objective of this study was to extract ursolic acid (UA) from Ocimum sanctum,to synthesize its derivatives and to examine the improvement of antioxidative activity. Present work involved structural modification of UA at the C-3 and C-28 positions. UA derivatives namely UA-4 and UA-7 with distinct property were synthesized. Comparative evaluation of anti-oxidant activity of UA, UA-4 and UA-7 using in vitro assays and lymphocyte model system involved: (i) inhibition of liposomal lipid peroxidation by UA and its derivatives (ii) assessment of trolox equivalent antioxidative capacity (TEAC) (iii) ABTS and DPPH radicals scavenging ability and (iv) cell death (MTT assay) under hydrogen peroxide (H2O2) induced oxidative stress. Moderate increase in antioxidant activity of compound UA-4 compared to UA was observed. In contrast, significant improvement in antioxidant activity of UA-7 was observed. To evaluate antioxidant effects on lymphocytes, we exposed cells with UA and its derivatives along with hydrogen peroxide. This was followed by measurement of cell viability by trypan blue exclusion assay and cell death using MTT assay. UA-7...
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Posted by admin on Nov 1, 2014 in |
A series of some new substituted quinolines were synthesized by Doebner reaction, a three component coupling of various aromatic amines with two aldehydes and phenyl pyruvic acid, the intermediate 2, 3-diary-6-acetyl-quinoline-4-carboxylic acids were reacted with various aromatic aldehydes in the presence of basic medium using Claisen-Schmidt condensation in order to afford the corresponding chalcones. The substituted chalcones, on condensation with hydroxylamine hydrochloride in ethanol furnished isoxazoles derivatives. Another quinolines derivative were synthesized in this study by using an aryl amines with acetylacetone as Combes reaction, Knorr reaction between an aryl amines and ethylacetoacetate with heating above 100 ºC, and Conrad-Limpach quinoline synthesis a thermal condensation of an aryl amines with ethylacetoacetate. The reaction progress for all synthesized compounds was checked by thin layer chromatography (TLC) and melting point techniques, the structure of synthesized compounds were confirmed using IR, 1HNMR, 13CNMR, and GCMS. All the compounds have been screened for their antibacterial and antifungal...
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Posted by admin on Nov 1, 2014 in |
Asthma is a multi factorial disease characterized by airflow obstruction, wheezing and dysonea and for this many genes are responsible. In this study, an attempt has been made to identify genes along with the proteins encoded by them which are responsible for Asthma along with clinical trials. In the practice of Ayurveda, it’s well established that shirish (Albizia lebbeck) can be used as a treatment of Asthma. However, how the compounds of shirish bark functions at the molecular level is yet unknown. The present study shows an insilico molecular interaction studies and clinical trials as well for the compounds of shirish bark. The results show how the compounds of shirish bark affect the target proteins of asthma which actually will aid in the design of putative inhibitor. Among the screened 9 (nine) compounds of shirish, all the compounds are giving good binding affinity to the selected proteins and among them lebbecacidin interacts potentially and is also showing lowest binding energy with IL-5, one of the target proteins. Lebbecacidin has...
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Posted by admin on Nov 1, 2014 in |
Nifedipine loaded mcoadhesive micropshres were prepared by o/w/o emulsification cross linking method using natural polymer chitosan. Microsphres with particle size range b/n 50-300 µm were obtained by this method. The prepared microspheres were evaluated for its drug loading, surface properties, in-vitro release profile. The diffusion and permeation characteristic of the drug is studied by using cellophane membrane and excised porcine intestinal mucosa respectively. The mucoadhesion properties of the microsphers were determined by using modified USP disintegration test apparatus model. In vivo animal studies were studies using rabbit model indicated a controlled blood level profile in comparison with pure nifedipine. IR studies indicated no appreciable drug excipient...
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