ABSTRACT
Bergenia ciliata (Family: Saxifragaceae) is a folklore remedy for the treatment of various ailments in Asian countries. Bergenin (1) has been isolated as an active constituent in many studies, however, the amount of bergenin has not been determined in all parts of the plant. A simple RP-HPLC method was developed to determine the amount of bergenin in methanol extracts of leaves, rhizomes and roots of the plant. Separation was achieved on an Agilent Eclipse XDB-C18 column maintained at 25 o C using isocratic solvent system (water: methanol: acetic acid; 62.5:37:0.5 v/v/v) adjusted at pH 2 0 at a flow rate of 1.0 mL/min. and detected at 275 nm. Correlation coefficient (0.9952) showed linearity of concentration (5-200 μg/mL) and response. The values of LOD (0.00947 μg/mL) and LOQ (0.02869 μg/mL) indicated that method was sensitive. The recovery of bergenin was 99.99-100% indicating accuracy of method. The methanol extract of rhizomes contained higher amount of bergenin (19.4%) than roots (9.2%) and leaves (6.9%). It is concluded that methanol extract of rhizomes is a better source of bergenin than other parts of the plant. The findings are useful for standardization of bergenin containing extracts and herbal preparations.
ABSTRACT
Bergenia ciliata (Family: Saxifragaceae) is a folklore remedy for the treatment of various ailments in Asian countries. Bergenin (1) has been isolated as an active constituent in many studies, however, the amount of bergenin has not been determined in all parts of the plant. A simple RP-HPLC method was developed to determine the amount of bergenin in methanol extracts of leaves, rhizomes and roots of the plant. Separation was achieved on an Agilent Eclipse XDB-C18 column maintained at 25 o C using isocratic solvent system (water: methanol: acetic acid; 62.5:37:0.5 v/v/v) adjusted at pH 2 0 at a flow rate of 1.0 mL/min. and detected at 275 nm. Correlation coefficient (0.9952) showed linearity of concentration (5-200 μg/mL) and response. The values of LOD (0.00947 μg/mL) and LOQ (0.02869 μg/mL) indicated that method was sensitive. The recovery of bergenin was 99.99-100% indicating accuracy of method. The methanol extract of rhizomes contained higher amount of bergenin (19.4%) than roots (9.2%) and leaves (6.9%). It is concluded that methanol extract of rhizomes is a better source of bergenin than other parts of the plant. The findings are useful for standardization of bergenin containing extracts and herbal preparations.
ABSTRACT
OBJECTIVE@#To evaluate in vivo antioxidant activity of latex and leaves methanol extract of Euphorbia helioscopia using mice as experimental animals.@*METHODS@#The plant was collected, identified, dried under shade, ground to fine powder and extraction was done. Latex was collected in dried bottles by cutting the stem. Oxidative stress was induced in mice with acute toxic dose of paracetamol administered intrperitoneally. Latex and leaves methanol extract (600 and 1 200 mg/kg) orally, once a day, were given to mice for two weeks. Then oxidative stress biomarkers were measured in tissue homogenates and serum.@*RESULTS@#Leaves methanol extract exhibited prominent in vivo antioxidant effect as compared to latex. Results showed significant rise in antioxidant enzymes (catalase, superoxide dismutase and glutathione) levels at 1 200 mg/kg dose of extract. Thus, extract helped to detoxify the free radicles by increasing antioxidant enzymes levels. Malondialdehyde value decreased significantly with extract (1 200 mg/kg) which was indicator of extract's power to inhibit the generation of free radicals. Extract (1 200 mg/kg) exhibited maximum cure against stress induced changes in liver, kidney, lipid profile parameters and complete blood count.@*CONCLUSIONS@#Leaves methanol extract of Euphorbia helioscopia raised antioxidant enzymes levels in mice. It showed hepatorenal-curative effect, hypolipidemic effect and hemostasis potential. Thus, it can help the biological systems to fight against stress induced pathological conditions.
ABSTRACT
Objective: To evaluate in vivo antioxidant activity of latex and leaves methanol extract of Euphorbia helioscopia using mice as experimental animals. Methods: The plant was collected, identified, dried under shade, ground to fine powder and extraction was done. Latex was collected in dried bottles by cutting the stem. Oxidative stress was induced in mice with acute toxic dose of paracetamol administered intrperitoneally. Latex and leaves methanol extract (600 and 1 200 mg/kg) orally, once a day, were given to mice for two weeks. Then oxidative stress biomarkers were measured in tissue homogenates and serum. Results: Leaves methanol extract exhibited prominent in vivo antioxidant effect as compared to latex. Results showed significant rise in antioxidant enzymes (catalase, superoxide dismutase and glutathione) levels at 1 200 mg/kg dose of extract. Thus, extract helped to detoxify the free radicles by increasing antioxidant enzymes levels. Malondialdehyde value decreased significantly with extract (1 200 mg/kg) which was indicator of extract's power to inhibit the generation of free radicals. Extract (1 200 mg/kg) exhibited maximum cure against stress induced changes in liver, kidney, lipid profile parameters and complete blood count. Conclusions: Leaves methanol extract of Euphorbia helioscopia raised antioxidant enzymes levels in mice. It showed hepatorenal-curative effect, hypolipidemic effect and hemostasis potential. Thus, it can help the biological systems to fight against stress induced pathological conditions.
ABSTRACT
Pelletized dosage forms can be prepared by different methods which, in general, are time consuming and labor intensive. The current study was carried out to investigate the feasibility of preparing the spherical pellets of omeprazole by sieving-spheronization. An optimized formulation was also prepared by extrusion-spheronization process to compare the physical parameters between these two methods. The omeprazole pellets were consisted of microcrystalline cellulose, polyvinylpyrrolidone K 30, sodium lauryl sulphate and polyethylene glycol 6000. The omeprazole delay release system was developed by coating the prepared pellets with aqueous dispersion of Kollicoat 30 DP. The moisture content, spheronization speed and residence time found to influence the final properties of omeprazole pellets prepared by extrusion-spheronization and sieving-spheronization. The Mann-Whitney test revealed that both methods produced closely similar characteristics of the pellets in terms of, friability [p=0.553], flowability [p=0.677], hardness [p=0.103] and density [bulk, p=0.514, tapped, p=0.149] except particle size distribution [p=0.004]. The percent drug release from the coated formulation prepared by sieving-spheronization and extrusion spheronization was observed to be 84.12 +/- 1.10% and 82.67 +/- 0.96%, respectively. Dissolution profiles of both formulations were similar as indicated by values of f1 and f2, 1.52 and 89.38, respectively. The coated formulation prepared by sieving-spheronization and commercial reference product, Zimore[registered] also showed similar dissolution profiles [f1=1.22, f2=91.52]. The pellets could be prepared using sieving-spheronization. The process is simple, easy, less time- and labor-consuming and economical as compared to extrusion-spheronization process.
Subject(s)
Drug Implants , Chemistry, PharmaceuticalABSTRACT
In Pakistan, a funded flour fortification program was launched for malnourished population, residing mainly in rural low income areas, but the urban population having comparatively better nutritional as well as economic status was focused wherein excessive intake of fortificants might cause complications. Therefore, the present study describes the physicochemical properties, elemental composition, nutritional components and hemoglobin/ferritin increasing potential of fortified and non-fortified flour. Domesticated chicken [Gallus gallus domesticus], either sex, age one month, weight 380 +/- 18.28 g, were randomly segregated into 4 groups [n=6]. The group I, II and III were fed on fortified flour, whereas group IV was fed on non-fortified flour for 30 days. The birds were weighed and blood samples of each of the birds were analyzed for determination of markers of iron status, hemoglobin [Hb] and serum ferritin [SF]. Moisture, ash and iron contents were found to be lower in non-fortified flour than that of the fortified samples. Hb and SF levels in groups fed on fortified flour were significantly higher than the one received non-fortified flour [P < 0.05]. The consumption of iron-fortified flour increases iron stores in the body without any further complication but long-term usage needs to be monitored.
Subject(s)
Animals , Flour , Food, Fortified , Iron , Hemoglobins , Ferritins , ChickensABSTRACT
The present study aimed to standardize the crude drug from "Euphorbia helioscopia" by doing qualitative and quantitative analysis of different pulverized plant parts and extracts. Physicochemical analysis [determination of moisture contents, total ash, water insoluble ash, sulphated ash, acid insoluble ash, and water and alcohol extractives] was done on powdered raw materials [stem and leaves]. The moisture contents and the ash value were found within the normal recommended range [moisture contents 6% and ash value 20%]. The value of water-soluble extracts was higher as compared to alcohol soluble extractives. Percentage yield was highest in methanol solvent. The phytochemical analysis i.e. total lipids, total proteins and carbohydrates of crude powder showed that lipids and proteins contents were high [2.4% and 0.91% respectively] in pulverized stem while carbohydrate contents were high [78.27%] in pulverized leaves. Qualitative analysis by FTIR fingerprints and UV-scanning showed that stem and leaves of the plant contained the same constituents because their spectra are super-imposable. Aqueous-, ethanol-, petroleum ether-, chloroform- and methanol extracts were used in the study. Quantitative analysis was done by calculating the primary and secondary metabolites [total proteins, total glycosaponins, total alkaloids, total flavonoids, and total polyphenolics] in all the extracts using suitable markers. Chloroform gave very less percentage yield and nil primary metabolites so it was eliminated from secondary metabolites estimation. The maximum value of total proteins, total glycosaponins, total alkaloids, total flavonoids and total polyphenolics were found in the leaves methanol [36.56%], stem methanol [34%], stem ethanol [41.84%], leaves methanol [108.96%], and leaves petroleum ether [7.22%] respectively. Different pharmacological activities of the plants are due to their flavonoid contents. It is concluded that methanol is the best solvent for extraction. Any arial part of the plant can be used in pharmacological evaluations prior to pre-clinical and clinical studies because leaves and stem had superimposable spectra in FTIR and UV-scanning.
Subject(s)
Chemical Phenomena , Phytochemicals , Plant ExtractsABSTRACT
Gentamicin induces nephrotoxicity, hence the present study explores protective and curative effects of alpha-lipoic acid and selenium alone and in combination in gentamicin-induced nephrotoxicity. Forty rabbits were randomly segregated into control, protective and curative groups. The groups A and B received water [10 ml/kg/day] and gentamicin [I/M, 80 mg/kg/day], respectively as normal and gentamicin controls. Four hours before gentamicin nephrotoxic dose, the protective subgroups C, D and E received alpha-lipoic acid, selenium and combination [50 mg/kg/day alpha-lipoic acid and 10 mg/kg/day selenium], respectively and then continued for 20 days. Nephrotoxicity was induced in curative subgroups F, G and H with gentamicin sulphate for 9 days and from 10[th] day onwards, followed the same treatments as for protective group for 26 days. Blood urea nitrogen [BUN], creatinine and antioxidant activity [AOA] were measured in all the groups. Combination of alpha-lipoic acid [50 mg/kg/day] and selenium [10 mg/kg/day] significantly reduced BUN [58.64%] and creatinine [17.48%] in protective subgroups treated for 20 days as compared to control without affecting AOA [p<0.05]. Decrease of 82.19% BUN and 77.38% creatinine, and 46.66% increase in AOA was noted on day 26 in curative group treated with the combination of antioxidants. The combination of alpha-lipoic acid and selenium [50 mg/kg/day alpha-lipoic acid and 10 mg/kg/day selenium] was found to be effective in prevention and treatment of gentamicin-induced nephrotoxicity
ABSTRACT
Imatinib is an efficacious anticancer drug with a spectrum of potential antitumour applications limited by poor biodistribution at therapeutic concentrations to the tissues of interest. We assess the pharmacokinetic and tissue distribution profile of imatinib in a liposome formulation. Its single dose (6.25 mg x kg(-1)) in a liposome formulation was administered iv to male mice. Imatinib concentration was measured in plasma, spleen, liver, kidney and brain using a HPLC assay. Non-compartmental pharmacokinetic approach was used to assess the disposition parameters. The plasma disposition profile was biphasic with a plateau-like second phase. The AUC(0-->infinity) was 11.24 microg x h x mL(-1), the elimination rate constant (k(el)) was 0.348 h(-1) and the elimination half life (t(1/2)) was 2.0 h. The mean residence time (MRT) was 2.59 h, V(SS) was 1.44 L x kg(-1) and clearance was 0.56 L x h x kg(-1). Liver achieved the highest tissue exposure: CMAX = 18.72 microg x mL(-1); AUC(0-->infinity)= 58.18 microg x h x mL(-1) and longest t(1/2) (4.29 h) and MRT (5.31 h). Kidney and spleen AUC(0-->infinity) were 47.98 microg x h x mL(-1) and 23.46 microg x h x mL(-1), respectively. Half-life was 1.83 h for the kidney and 3.37 h for the spleen. Imatinib penetrated into the brain reaching approximately 1 microg x g(-1). Upon correction by organ blood flow the spleen showed the largest uptake efficiency. Liposomal imatinib presented extensive biodistribution. The drug uptake kinetics showed mechanism differences amongst the tissues. These findings encourage the development of novel imatinib formulations to treat other cancers.
Subject(s)
Animals , Male , Mice , Antineoplastic Agents , Blood , Pharmacokinetics , Area Under Curve , Benzamides , Brain , Metabolism , Drug Carriers , Chemistry , Half-Life , Imatinib Mesylate , Injections, Intravenous , Liposomes , Chemistry , Metabolic Clearance Rate , Mice, Inbred ICR , Piperazines , Blood , Pharmacokinetics , Pyrimidines , Blood , Pharmacokinetics , Tissue DistributionABSTRACT
To investigate the disposition kinetics of amoxicillin trihydrate by urinary excretion data following oral administration in normal human volunteers. Design Addressed: Evaluation of disposition kinetics of amoxicillin in local environment using urine data. Urine samples are easy to collect as compared with the blood samples and, therefore, urine data is helpful for the evaluation of disposition kinetics of drugs. Setting: Faculty of Veterinary Sciences, Agriculture University, Faisalabad-Pakistan and Department of Pharmacy, Islamia University, Bahawalpur-Pakistan. Subjects/The study was undertaken in seven normal human volunteers. Urine samples were collected over 12 hours following drug administration and analyzed for the drug by the disc diffusion method using Sarcina lutea as a test organism. The data was analyzed for computation of pharmacokinetic parameters by standard methods. A maximum amount of 29.2 +/- 3.0 mg of amoxicillin was excreted at four hours and 17.0 +/- 1.3 mg at 12 hours. The total amoxicillin cumulative amount excreted and% cumulative at the 12th hour was concluded to be 183.4 +/- 2.6 and 73.3 +/- 1.0%, respectively. Elimination rate constant of 0.60 +/- 0.03 hr and 1.18 +/- 0.05 hours in normal volunteers was observed in this study. Conclusions: Similarities and differences were both observed when the present findings were compared with the cited results. The urine data may be used as an alternative to the blood data for the estimation of pharmacokinetics of drugs