SOLID STATE CHARACTERIZATION AND QUANTIFICATION OF ABACAVIR SULPHATE, LAMIVUDINE AND ZIDOVUDINE AND ITS TABLET FORMULATION BY X-RAY POWDER DIFFRACTION METHOD

Objective: To determine simultaneously the content of crystallinity of Abacavir sulphate (ABC), Lamivudine (LMD) and Zidovudine (ZVD) using X-ray Powder Diffraction (XRPD) technique and to validate the developed analytical methods and to statistically perform correlations by ANOVA technique.Methods: Characteristic non-interfering peaks of ABC, LMD and ZVD were identified by using X-Ray Powder Diffraction method for assessment of the content of crystallinity.Results: A working range 70 % to 130 % was taken for the establishment of linearity of the ABC, LMD and ZVD in the formulation and the coefficient of regression of ABC was 0.999, LMD was 0.998 and ZVD was 0.998. The F value by ANOVA was found to be within limits and satisfactory.Conclusion: The developed method was adapted to the samples exposed to 40 °C/75 % RH, accelerated stability conditions and hence proved that it can be used for monitoring real-time samples.Keywords: Abacavir sulphate, Lamivudine, Zidovudine, Crystallinity, XRPD, Validatio

Evaluation of antipyretic activity of ethyl acetate extract of Adenema hyssopifolium G. Don in a rat model

AbstractObjectiveTo evaluate the effect of ethyl acetate extract of Adenema hyssopifolium (AHEAE) on normal body temperature and brewer's yeast-induced pyrexia rats.MethodsPreliminary phytochemical tests, acute toxicity tests and antipyretic evaluation were carried out in ethyl acetate extract of Adenema hyssopifolium. Two doses of the extract (300 or 600 mg/kg orally) and standard antipyretic agent, paracetamol at a dose of 150 mg/kg were administered to various group of the rats. Mean rectal temperature before and after treatment was noted.ResultsThe phytochemical analysis of AHEAE revealed the presence of flavonoid and iridoid glycosides as major phytoconstituents. The administration of AHEAE at a dose of 300 or 600 mg/kg produced significant reduction (P<0.001 and P<0.01) of the body temperature in normal and pyrexia rats on a dose dependent manner. The antipyretic influence of AHEAE was comparable to that of standard antipyretic agent, paracetamol (150 mg/kg), and onset of action and reduction in pyrexia towards normal body temperature was delayed when compared to paracetamol treatment. At dose of 600 mg/kg, AHEAE reduced pyrexia to normal body temperature at 4 h after its administration compared to reduction of pyrexia to normal body temperature at 2 h by standard drug. The reduction of fever was consistent in paracetamol group from 2 to 4 h after its administration to normal body temperature compared to AHEAE treatments.ConclusionsOur present results corroborate with the traditional notion of Adenema hyssopifolium G. DON that is being used as an effective cure of fever and add authenticity to claim of indigenous healers that the taxon is a potential antipyretic agent

Antidiabetic, antihyperlipidemic and antioxidant potential of methanol extract of Tectona grandis flowers in streptozotocin induced diabetic rats

AbstractObjectiveTo investigate antidiabetic, antihyperlipidemic and antioxidant activity of methanol extract of Tectona grandis (T. grandis) flowers (METGF) in streptozotocin (STZ) induced diabetic rats to supports its traditional use.MethodsAcute toxicity study of METGF was carried out in rat to determine its dose for the antidiabetic study. Oral glucose tolerance test (OGTT) was performed to evaluate METGF effect on elevated blood glucose level. Diabetes was induced in rats by administration of STZ (60 mg/kg, ip.) and it was confirmed 72 h after induction. METGF was orally given to the diabetic rats up to 28 days and blood glucose level were estimated each week. On 28 day of the experiment, diabetic rats were sacrificed after the blood collection for the biochemical parameters analysis and liver, kidney was collected to determine antioxidants levels.ResultsIn acute toxicity, METGF did not show toxicity and death up to a dose 2 000 mg/kg in rats. Administration of METGF 100 and 200 mg/kg significantly (P<0.001) reduced blood glucose levels in OGTT and STZ-induced diabetic rats. Both doses of METGF treatment significantly (P<0.001, P<0.01 and P<0.05) increased body weight, serum insulin, haemoglobin (Hb) and total protein levels in diabetic rats. Also, MEGTF treatment reduced elevated glycosylated haemoglobin (HbA1c) and other biochemical parameters levels significantly (P<0.001) in diabetic rats. Altered lipid profiles and antioxidants levels were reversed to near normal in diabetic rats treated with METGF.ConclusionsThese results concluded that METGF possesses antidiabetic, antihyperglycemic and antioxidant activity which supports its traditional use

Metformin: Pros and Cons

Metformin was approved for the treatment of Type 2 Diabetes Mellitus in 1958 for UK, in 1972 for Canada and in 1995 by FDA in USA. Metformin is the drug of choice for patients who are obese and have type 2 diabetes mellitus. Though metformin was at first proven to treat hyperglycemia, many other uses of metformin are proven to be effective. It is also used for gestational diabetes mellitus, obesity, hyper secretion of ovarian androgen, poly-cystic ovary syndrome (PCOS), anti-psychotic therapy induced weight gain, cancer treatment and anti-aging. Metformin causes a decrease in appetite thus known to act on obesity. The other action of metformin is reduction of circulating levels of insulin and insulin like growth factor 1 (IGF-1) which is associated with anticancer action. There are ongoing researches about the effect of metformin on anti-aging properties and proved that metformin is linked with anti-aging factors. Three main factors that are related with aging are oxidation, glaciation and methylation. Metformin as all drugs, have unwanted effects as well. Many side effects of metformin are considered mild where lactic acidosis and vitamin B12 deficiency happens to be the major

EVALUATION OF ANTI-CANCER ACTIVITY IN METHANOLIC EXTRACT OF ENICOSTEMMA LITTORALE ON DEN INDUCED HEPATOCARCINOGENESIS IN RATS

The present study is aimed at evaluating the chemoprotective effect of Enicostemma littorale in DEN induced hepato-carcinogenesis in Sprague Dawley rats. The preliminary steps involved extraction, phytochemical investigation, HPTLC study and In vitro antioxidant activity using DPPH, ABTS. and Initiation of HCC was done by single i.p injection of DEN at a dose of 200mg/kg. The MEEL received treatment for 90 days after 14 days of development of HCC and continued for entire study period, whereas the other two group given normal saline, 5-flurouracil (20mg/kg ) i.p. The results showed that the injection DEN lead to the development of liver tumors in rats. Significant effect of serum biochemical parameter like SGOT, SGPT, ALP, UREA, TOTAL PROTEIN and tumor marker was observed with depletion of endogenous antioxidants SOD, CAT, GSH, there by leading to higher LPO. The result exhibited that MEEL treatment (Preventive) group offered excellent shielding against HCC and displayed all the parameter in near normal range with a maintained antioxidant enzyme system. The result obtained showed that extracts were found to containing phenols at a concentration of 70.25 mg/g and flavonoids 26.03mg/g. HPTLC Analysis showed presence of Quercetin, Mangiferin, Gallic acid, Catechin and sweroside. In the DPPH, ABTS, FRAP, TRAP radical scavenging assay MEEL has displayed the highest antiradical activity in both assays and was also comparable with the standard qucertein The present study reveal the efficacy of the MEEL to prevent malignancy induced by chemical carcinogen and the phytoconstituents responsible for activity

Sinteza novih derivata triazola kao anti-nociceptivnih i protuuaplnih agenasa

Eight novel 1-[2-(1H-tetrazol-5-yl)ethyl]-1H-benzo[d][1,2,3]triazoles (3a-h) have been synthesized in order to obtain new compounds with potential anti-nociceptive and anti-inflammatory activity. The titled compounds were synthesized by the condensation of 1-[2-(1H-tetrazol-5-yl)ethyl]-1H-benzotriazole (2) and appropriate acid chlorides. Compound (2) was synthesized by reacting 3-(1H-benzo[d][1,2,3]triazol-1-yl)propanonitrile (1) with sodium azide and ammonium chloride in the presence of dimethylformamide. The synthesized compounds were characterized by spectroscopic methods (IR, 1H NMR, mass spectroscopy) and elemental analysis. The titled compounds were evaluated for anti-nociceptive activity by the hot plate method and the writhing response method and anti-inflammatory activity was evaluated by the carragenean induced paw edema method. 5-(2-(1H-benzo[d][1,2,3]triazo-1-yl)ethyl)-1H-tetrazol-1-yl)(4-aminophenyl)methanone (3d) and 5-(2-(1H-benzo[d][1,2,3]triazo-1-yl)ethyl)-1H-tetrazol-1-yl) (2-hydroxyphenyl)methanone (3g) exhibited significant anti-nociceptive activity. 1-(2-(1-Tosyl-1H-tetrazol-5-yl)ethyl)-1H-benzo[d][1,2,3]triazole (3c) and 4-5-(2-(1H-benzo[d][1,2,3]triazo-1-yl)ethyl)-1H-tetrazol-1-yl sulfonyl)benzenamine (3f) elicited superior anti-inflammatory activity compared to other synthesized compounds. Further investigations are needed to discern the mechanism of action.Sintetizirano je osam novih 1-[2-(1H-tetrazol-5-il)etil]-1H-benzo[d][1,2,3]triazola (3a-h), s potencijalnim anti-nociceptivnim i protuupalnim djelovanjem. Navedeni spojevi pripravljeni su kondenzacijom 1-[2-(1H-tetrazol-5-il)etil]-1H-benzotriazola (2) i odgovarajućih kiselinskih klorida. Spoj 2 dobiven je reakcijom 3-(1H-benzo[d][1,2,3]triazol-1-il)propanonitrila (1) s natrijevim azidom i amonijevim kloridom u prisutnosti dimetilformamida. Sintetizirani spojevi su karakterizirani spektroskopskim metodama (IR, 1H NMR, spektroskopijom masa) i elementarnom analizom. Anti-nociceptivno djelovanje ispitivano je metodom vruće ploče i praćenjem odgovora na bolne podražaje, dok je protuupalno djelovanje evaluirano testom s karageninom. 5-(2-(1H-benzo[d][1,2,3]triazo-1-il)etil)-1H-tetrazol-1-il)(4-aminofenil)metanon (3d) i 5-(2-(1H-benzo[d][1,2,3]triazo-1-il)etil)-1H-tetrazol-1-il) (2-hidroksifenil)metanon (3g) pokazali su značajno anti-nociceptivno djelovanje. 1-(2-(1-Tosil-1H-tetrazol-5-il)etil)-1H-benzo[d][1,2,3]triazol (3c) i 4-5-(2-(1H-benzo[d][1,2,3]triazo-1-il)etil)-1H-tetrazol-1-il sulfonil)benzenamin (3f) pokazali su superiorno protuupalno djelovanje u odnosu na druge sintetizirane spojeve. Daljnja istraživanja su nužna kako bi se razjasnio mehanizam djelovanja

Synthesis, Antinociceptive, Antiinflammatory and AntiepilepticEvaluation of Some Novel Indeno[1, 2-b] Quinoxalin-11-ylidenamines: Novel indeno quinoxalin

A series of novel indeno[1, 2-b]quinoxalin-11-ylidenamines 2-9 have been synthesized via condensation of indane[1, 2-b]quinoxalin-11-one (1) with various primary aromatic amines in presence of AcOH for 3 h. Compound 1 was synthesized by condensation of indane-1,2,3-trione with benzene-1,2-diamine in presence of AcOH. The synthesized compounds were characterized by IR, 1H-NMR, mass pectra and elemental analysis. Compounds 2-9 were screened for anti-nociceptive, anti-inflammatory and antiepileptic activity by AcOH induced writhing method ,carrageenan induced paw edema method and maximal electroshock induced convulsion method respectively. Out of the eight synthesized compounds, indeno[1,2-b]quinoxalin-11-ylidine (4-nitrophenyl)amine (3) exhibited promising anti-inflammatory activity and anti-nociceptive activity. N-(2,4-dinitrophenyl)-N'-(indeno[1,2-b]quinoxalin-11-ylidene)hydrazine (7) showed promising anti-inflammatory activity, anti-nociceptive activity, and antiepileptic activity, whereas N4-indeno[1, 2-b]quinoxalin-11-ylidene biphenyl-4,4'-diamine (8) showed promising anti-inflammatory activity

Hepatoprotective effect of ethanolic extract of <it>Trichosanthes lobata</it> on paracetamol-induced liver toxicity in rats

<p>Abstract</p> <p>Background</p> <p><it>Trichosanthes lobata</it> (family cucurbitaceae) is used to treat malarial fever and liver disorders. This study aims to investigate possible hepatoprotective activities of ethanolic extract of <it>Trichosanthes lobata</it> against paracetamol-induced hepatotoxicity.</p> <p>Methods</p> <p>Hepatotoxicity was induced in Wistar male rats by oral administration, 2 g/kg body weight on 7th day after the administration of ethanolic extract of <it>Trichosanthes lobata</it> and silymarin (100 mg/kg). Ethanolic extract of <it>Trichosanthes lobata</it> was administered orally at doses of 200 mg/kg and 400 mg/kg body weight daily for 7 days. Several serum markers, aspartate transaminase, alanine transaminase, alkaline phosphatase, bilirubin, total protein was measured to assess the effect of the extract on paracetamol (acetaminophen)-induced hepatic damage. The study included histopathological examination of liver sections.</p> <p>Results</p> <p>Blood samples from rats treated with ethanolic extract of <it>Trichosanthes lobata</it> (200 mg/kg body weight and 400 mg/kg body weight) had significant reductions in serum markers in paracetamol administered animals, indicating the effect of the extract in restoring the normal functional ability of hepatocytes. Silymarin (100 mg/kg, p.o.) was used as a reference drug.</p> <p>Conclusion</p> <p>The ethanolic extract of <it>Trichosanthes lobata</it> exhibits protective effects against paracetamol‒induced hepatotoxicity.</p

Synthesis and characterization of some novel azetidinone derivatives as anti-bacterial and anti-convulsant agents

Several novel azetedinones have been synthesized by condensation of 2, 4-dinitro phenyl hydrazine with various substituted aromatic aldehydes in presence of zinc chloride and methanol followed by the reaction with chloroacetyl chloride and triethylamine. The synthesized compounds were characterized by IR and PMR analysis. The titled compounds were evaluated for anti-bacterial and anticonvulsant activity by cup plate method and maximal electroshock induced convulsion method respectively. Compounds 3-chloro-1-(2,4-dinitrophenylamino)-4-(3-hydroxy-4-methoxyphenyl)azetidin-2-one 2c, 3-chloro-4-(4-chlorophenyl)-1-(2,4-dinitrophenyl amino)azetidin-2-one 2d, 3-chloro-1-(2,4-dinitrophenylamino)-4-(3-nitrophenyl)azetidin-2-one 2f and 3-Chloro-1-(2,4-dinitrophenylamino)- 4-p-tolyl-azetidin-2-one 2g showed good anti-bacterial activity. Compounds 3-chloro-1-(2,4-dinitro phenylamino)-4-(3-nitrophenyl)azetidin-2-one 2f and 3-chloro-4-(2,4-dichloro phenyl)-1-(2,4-dinitro phenylamino)azetidin-2-one 2h elicited good anti-convulsant activity when compared with control. Compound 3-chloro-1-(2,4-dinitrophenylamino)-4-(4-hydroxyphenyl)azetidin-2-one 2e elicited moderate anti-convulsant activity when compared with control. Journal of Pharmacy & Bioresources Vol. 2(2) 2005: 162-16