Aim: The flavonoid compound (Acacetin) isolated from fruits of Gmelina arborea was investigated for its pharmacokinetic evaluation to find out the suitability of this compound to be formulated in any suitable dosage form. Method: The acacetin was administered intravenously and orally in Wistar rats at a dose of 2 and 10 mg/Kg body weight respectively. In a regular interval of specified time, blood samples were collected and bio-analyzed to quantify the drug concentration in the blood sample by using LC-MS. The Cmax, Tmax, T1/2, KE, Ka, and bioavailability (F) of acacetin were determined by mathematically and graphically from plasma concentration-time profile data. Absorption rate constant was determined by the method of residual. Results: From the i.v. Bolus administration data, acacetin had an area under curve (AUC) is 1.542 µg.h/ml, elimination rate constant (KE) is 0.423 h-1, and half-life (T1/2) is two hour. The oral administration of acacetin showed the peak plasma concentration (Cmax) of 1.668 µg/ml, Tmax is 1 h, AUC is 6.44 µg h/ml, KE is 0.416 h-1, T1/2 is 2 h, absorption rate constant (Ka) is 1.6 h and bioavailability of acacetin was found to be 84 %. Conclusion: From the study it could be concluded that the acacetin possessed relatively greater bioavailability; thus this drug exhibited significant satisfactory pharmacokinetic profile which would be helpful for successful designing of a suitable dosage form formulation.
In Vitro and In Vivo Evaluation of Controlled Release Tablets of Pioglitazone HCl Solid Dispersion Sruti Ranjan Mishra 1, , Bhabani Shankar Nayak , P. Ellaiah ,Gitanjali Mishra 2 Department of Pharmaceutics, Faculty in Pharmacy, Jeypore College of Pharmacy, Rondapalli, Jeypore – 764002, Koraput, Odisha, India. P.G. Department of Zoology, Berhampur University, Bhanja Bihar, Berhampur, Ganjam, Odisha, India.
Background: The plant Gmelina arborea has been traditionally used in India for several medicinal purposes like anthelmintic, diuretic, antibacterial, hepatoprotective, anti-inflammatory, antioxidant and antidiabetic. It contains phytoconstituents like alkaloids, carbohydrates, anthraquinone glycosides, gums, mucilages, tannins, phenolic compounds and flavonoids. Aims: The objective of present study is to isolate a compound from ethanolic extract of G. arborea and to explore the diuretic activity of isolated compound. Material and methods: The isolation of compound was done by column and thin layer chromatographic methods. The isolated compound was characterized to elucidate its structure by spectroscopic methods like ultraviolet, infrared, nuclear magnetic resonance and mass spectroscopy. The diuretic activity of isolated compound was evaluated by Lipschitz test methods using Wistar rats as animal model. Statistical analysis used: All data are verified for statistically significant by using one way ANOVA at 5 % level of significance (p < 0.05). Results: A flavonoidal compound was isolated as yellow color crystal with melting point 177±1 °C with molecular formula C16H15O5 and IUPAC name 5,7-dihydroxy-4-methoxy flavone. Urine volume was significantly increased in comparison to normal and standard control groups. The excretion of sodium was also increased by the compound. The diuretic effect of the compound was comparable to that of the reference standard (Furosemide). Conclusion: It could be concluded that the isolated compound is a flavonoid and it possess diuretic activity.
Objective: Ramipril is a long-acting angiotensin-converting enzyme inhibitor. The study aimed to design, formulate and evaluate the oral osmotic drug delivery dosage form of an anti-hypertensive drug, ramipril.Methods: The tablet was formulated using ramipril and different polymers like PVP- K30 and Ethyl cellulose. The microcrystalline cellulose (MCC - diluent), Potassium chloride, Mannitol (osmogen) and Magnesium stearate (lubricant) were used in all the formulations. All the tablets were manufactured by wet granulation method followed by film coating. Compatibility of the drug with excipients was determined by FT-IR spectral analysis. The granules were evaluated for bulk density, Carr’s index and Hausner’s ration to determine flow properties. The prepared compressed and coated tablets were evaluated for weight variation, thickness, hardness, friability, and drug content and in vitro drug release and release kinetic studies.Results: The FT-IR study revealed that drug was compatible with excipients. The flow properties of granules of most formulation were excellent. All osmotic tablet formulations had good tablet physiochemical properties as per Pharmacopeia. The drug content of all tablet batches was satisfactory. The in vitro drug release study revealed that the formulation F7 containing 100 mg of ethyl cellulose release 100% of drug in 24 h with zero order release kinetics.Conclusions: Ramipril osmotic tablet could be used for safe management of hypertension with greater novelty.
Background: The plant Gmelina arborea has been traditionally used in India for several medicinal purposes like anthelmintic, diuretic, anti-inflammatory, antibacterial, antioxidant and antidiabetic. Aims: The aim of the present study is to explore the anti-inflammatory activity of G. arborea fruit extracts using ethanol, ethyl acetate, n-butanol and petroleum ether as solvents. Material and methods: The anti-inflammatory activity was evaluated by Carrageenan-induced rat paw edema method at a single dose of 300 mg/Kg, b.w. The Statistical analysis used: All data are verified for statistically significant by using one way ANOVA at 1 % level of significance (p < 0.01). Results and discussion: All extracts were able to show good anti-inflammatory activity in comparison with standard drug Diclofenac sodium. The anti-inflammatory activity of all the extracts were found in the order of ethanol > nbutanol > petroleum ether > ethyl acetate. Conclusion: It could be concluded that G. arborea fruits possess anti-inflammatory activity.
G melina arborea r oxb. is found in the tribal areas of Koraput district , Odisha, Indi a . It is extensively used traditionally by the tribal people as anthelmintic, antimicrobial, antidiabetic , h epatoprotective and antiepileptic . The present study is an attempt to explore the ant iepileptic ac tivity of different fruit extracts of plant G . arb orea using ethanol, ethyl acetate, n - butanol and petroleum ether as solvents. The extracts were screened for nontoxic properties examined by acute toxicity study and evaluated for their ant iepileptic activity . The antiepileptic activity of above extracts w as evaluated by using strychnine induced tonic convulsion in Swiss albino mice. The extracts were found as nontoxic. All extracts were able to show ant iepileptic activity at a single dose of 2 0 0 mg/ k g body weight (b.w.) . The activities are comparab le with the standard drug such as Diazepam . The dose of ethyl acetate , n - butanol and petroleum ether extracts of G . arborea showed lesser ant iepileptic activity than the standard drug diazepam except ethanol extract. Among all the solvent extracts , the ethanol ext ract showed better antiepileptic activity even in comparison with the standard drug . The data were verified as statistically signifi cant by using one way ANOVA at 1 % level of significance (p < 0.01 ) followed by z - test .
Background: Moxifloxacin is a fluoroquinolone derivative extensively used for ocular infection. Objective: The main objective of study is to design and evaluate ophthalmic insert of moxifloxacin that could be use for sustained delivery of drug in to eye. Method: The moxifloxacin ophthalmic insert was prepared by solvent casting method. The chitosan, methyl cellulose and hydroxyl propyl methyl cellulose K4M were used as release rate controlling biodegradable polymers. The drug excipients compatibility study was carried out by Fourier Transform Infrared Spectroscopy (FTIR) and study suggesting no interaction between drug and polymers. The ocuserts were characterized for weight variation, thickness, surface pH, folding endurance, moisture absorption, moisture loss, drug content uniformity, in vitro drug release, drug release kinetic, stability, sterility testing and ocular toxicity study. The ophthalmic inserts were evaluated for in vivo drug release studies. Results: The uniformity of the weights of the films suggested uniform distribution of the drug and polymer in all formulations. Use of higher concentration plasticizer was observed to cause brittleness in the medicated discs, but use of greater amount of plasticizer displayed little opaqueness and good folding endurance. The ocular irritation test did not show any signs of irritation, inflammation and abnormal discharge. Conclusion: The result indicated that the ophthalmic insert, F3 containing methyl cellulose (400 mg) released 71.5 % of drug, in a constant manner following zero order kinetics with adequate stability and non-toxic to eye, suggesting Moxifloxacin eye ocusert would be used for safe management of ocular disease with lesser frequency of administration.
68 Abstract: Clotrimazole is an imidazole derivative novel broad spectrum antimicrobial agent extensively used topically for fungal infection. The purpose of this study is to design and develop in situ implants containing clotrimazole that could be used in the treatment of periodontal diseases by direct periodontal intrapocket administration. The dental film of clotrimazole was prepared by solvent casting technique using hydroxyl propyl methyl cellulose, ethyl cellulose, hydroxyl propyl cellulose and chitosan in different concentrations as biodegradable rate controlling polymers. The drug polymers interaction was studied by Fourier Transform Infrared Spectroscopy (FTIR) and study suggesting no interaction between drug and polymers. The implants were characterized for weight variation, thickness, surface pH, tensile strength, folding endurance, moisture content, viscosity, drug content uniformity, in vitro drug release, mass balance, drug release kinetic, stability and in vitro antibacterial activity studies. Mean weight data showed that the different films were uniform. Minimum thickness was obtained with film containing chitosan. Almost all dental film formulations having satisfactory tensile strength. Good physicochemical properties were shown by the films. In vitro drug release data indicate that the films showed an initial burst release followed by sustained release of the drug(s). In vitro drug release rate for selected dental implant formulation (F6, containing 4.5 % w/w of chitosan) was found to sustain clotrimazole over 10 h obeying zero order kinetic. The stability study did not show any significant changes. The study suggesting the film containing chitosan is a potential drug delivery device for the topical treatment of periodontal diseases.
The Solanum Surattens Linn fruits, family, Solanaceae, is traditionally eat by local Tribes. The fruit mucilage is used as gum for pasting sheets of paper and card board. The present study is an attempt to investigate the efficacy of S. Surattens fruit mucilage as tablet binder. The mucilage was extracted with ethanol, screened phytochemically for detection of mucilage and physiochemical characteristics of mucilage were studied. The heavy metal study in soil, study of toxicity, gum-experimental tablet excipient interactions using Fourier Transform Infrared Spectroscopy and Differential Scanning Colorimetry ensured its safe use as a tablet binder. Tablets were manufactured using Diclofenac sodium and granules were prepared by wet granulation method with different concentration (4, 6, 8, 10 and 12% w/v) of mucilage as tablet binding agent. The prepared granules were evaluated for percentage of fines and flow properties. A comparison was made against the tablets prepared with 5% w/v starch paste as standard binder, based on studying the standard parameters like hardness, thickness, friability, weight variation, disintegration time and in vitro dissolution. The tablets had good tablet physiochemical properties and the drug release was more than 90% within 1.5 h. S. Surattens at 8% w/v was found to be effective as tablet binder. All the formulations were subjected to stability studies and showed stable with respect to tablet parameters. Thus this gum will be a non-toxic, biodegradable, economic WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES SJIF Impact Factor 2.786 Volume 4, Issue 03, 1370-1385. Research Article ISSN 2278 – 4357 Article Received on 05 Jan 2015, Revised on 30 Jan 2015, Accepted on 23 Feb 2015
Gmelina arborea roxb. is extensively used traditionally as anthelmintic, antimicrobial, antidiabetic, diuretic, hepatoprotective and antiepileptic agent. The present study is an attempt to explore and confirm the diuretic activity of different fruit extracts of the plant G. arborea using ethanol, ethyl acetate, n-butanol and petroleum ether as solvents. The diuretic activity of the extracts were evaluated by determining urine volume, urine pH and electrolyte (Na+) concentration in male Wistar rats at a single dose of 300 mg/Kg, b.w. Urea (1 g/Kg) was used as normal standard drug and normal saline water was 0.9 % w/v used as normal control. The extracts were found to be nontoxic. Urine volume was significantly increased by all the extracts in comparison to normal and standard control groups. The excretion of sodium was also increased by all the extracts. There was no significant change in the pH of urine after administration of the G. arborea extracts. The diuretic effect of the extracts was comparable to that of the reference standard (Urea). The n-butanol extract showed better diuretic effect in comparison to other extracts. Thus it could be concluded that the fruit extracts of G. arborea possess diuretic activity.
The present study was carried out to investigate the anti-pyretic and anticonvulsant activity of petroleum ether, ethyl acetate, n-butanol and ethanol extracts of Smilax zeylanica Linn, leaves using experimental animal models. The extracts were screened for alkaloids, steroids, proteins, flavanoids, saponins, mucilage, carbohydrates, tannins, fats and oils. Anti-pyretic activity was evaluated using the brewer's yeast-induced pyrexia in rats. The extracts in dose levels of 200 mg/kg orally were used for anti-pyretic studies. The petroleum ether extracts of leaves of Smilax zeylanica Linn produced significant (P<0.01) anti-pyretic activity. Anticonvulsant activity of above extracts was evaluated by using strychnine induced tonic convulsion of Swiss albino mice. All extracts were able to reduce convulsion in mice. The Ethyl acetate extracts of Smilax zeylanica was found to have good anticonvulsant activity in comparison to other extracts which was verified as statistically significant by using one way ANOVA at 1% level of significance *shows P value<0.01.
Smilax zeylanica Linn is found in the tribal area of Baipariguda (Dist: Koraput) Odisha, India and extensively used traditionally by the tribal people as anthelmintic, antibacterial, analgesic, impotency and antifungal agent. The present study involves the antidiabetic activity of different extracts of leaves of plant S. zeylanica using petroleum ether, ethyl acetate, n-butanol and ethanol as solvents. The various doses of solvents extracts were evaluated for their antidiabetic activity on Wister rat. All extracts exhibited the antidiabetic activity at. 250 mg/kg concentration and the activities were well comparable with the standard drug. glibenclamide. Among all the solvent extracts, ethanolic extract showed better antidiabetic activity. The data were verified as statistically significant by using one way ANOVA at 5 % level of significance (p < 0.05).
Zmelina arborea Roxb. is found in the tribal areas of Koraput and Ganjam district of Odisha, India. It is extensively used traditionally by the tribal people as anthelmintic, antimicrobial, antifungal, antidiabetic and hepatoprotective. The present study is an attempt for the preliminary investigation of phytochemical constituents and to explore the anthelmintic activity of different extracts of unripe fruits of plant 1 arborea using ethanol, ethyl acetate, n-butanol and petroleum ether as solvents. The extracts were screened for phytochemical constituents and evaluated for their anthelmintic activity on adult Indian earthworms, Pheretima posthuma. The tests for cardiac glycosides and steroids were positive for all the extracts. The ethanol and n-butanol extracts were containing most phytochemicals where as ethyl acetate extracts was containing least number of phytochemicals. All extracts were able to show anthelmintic activity at 10 mg/mL concentration. The activities are comparable with the standard drugs such as piperazine citrate and albendazole. All the doses of ethanol, ethyl acetate and petroleum ether extracts of Z. arborea showed lesser anthelmintic activity than the standard drugs piperazine citrate and albendazole except ethanol extract at 25 mg/mL of concentration which showed better anthelmintic activity than the both standard drugs. When the dose of such extract is increased, a gradual increase in anthelmintic activity was observed. Among all the solvent extracts the n-butanol extract showed better anthelmintic activity even in comparison with both the standard drugs. The data were verified as statistically significant by using one way ANOVA at 5 % level of significance (p < 0.05).
Background: The plant Gmelina arborea has been traditionally used in India for several medicinal purposes like anthelmintic, diuretic, antibacterial, antioxidant and antidiabetic. Aim: The present study is an attempt to explore the antibacterial, antioxidant and antidiabetic activities of different extracts of fruits of plant G. arborea using ethanol, ethyl acetate, n‑butanol and petroleum ether as solvents. Materials and Methods: A single dose (1000 μg/ml) of extract was evaluated for their antibacterial activities on human pathogens like Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. In‑vitro antioxidant activity of G. arborea fruits was determined by 1, 1‑diphenyl‑2‑picrylhydrazil (DPPH) free radical scavenging and reducing power assay. Ascorbic acid was used as standard and positive control for both the analyses. The antidiabetic activity of above extracts was evaluated in alloxan induced diabetic model of Wistar rats. Statistical Analysis: All data are verified for statistically significant by using one way ANOVA at 1% level of significance (P < 0.01). Results: Only ethanol extract showed significant antibacterial activity against all pathogens and the activities were compared with the standard drug, streptomycin. The n‑butanol extract did not show antibacterial activity against any pathogens, whereas ethyl acetate and petroleum ether extracts showed inhibitory action against P. aeruginosa. The extracts showed significant antioxidant activities in a dose dependent manner. The ethanol extract showed good antioxidant activity when compared to the other three extracts. All the extracts were able to reduce sugar level in blood. Ethanol extract was found to have good antidiabetic activity in comparison to other extracts. Conclusion: It can be concluded that the extracts of G. arborea possess antibacterial, antioxidant and antidiabetic activities. Key words: Antibacterial, DPPH and alloxan, gmelina arborea, scavenging, streptomycin, verbenaceae
The present study involves the preliminary investigation of phytochemical constituents, acute toxicity study and the anthelmintic activity of different extracts of leaves of S. zeylanica using petroleum ether, diethyl ether, chloroform and methanol as solvents. The study was also extended to evaluate analgesic activity of different extracts of leaves of S. zeylanica using petroleum ether, chloroform and methanol as solvents. The phytochemical studies indicated that the tests for glycosides, alkaloids, tannins, triterpenoids and sterols compounds were positive for all the extracts except chloroform extract, while the tests for carbohydrate, proteins, saponins, lipids and flavonoids were negative for all extracts. The various doses of solvents extracts were evaluated for their anthelmintic activities on adult Indian earthworms, Pheretima postuma. All extracts exhibited the anthelmintic activity at 10 mg/mL concentration and the activities were well comparable with the standard drug, piperazine citrate. The analgesic activity of above extracts was evaluated by using tail immersion method in Swiss albino mice. All the extracts showed analgesic activity that was comparable with standard drug (aspirin). Among all the solvent extracts, methanolic extract showed better anthelmintic as well as analgesic activities. The data were verified as statistically significant by using one way ANOVA at 5 % level of significance (p < 0.05).
Pioglitazone hydrochloride is a novel antidiabetic drug in thiazolidinediones group and it improves insulin sensitivity in insulin resistant patients. One of the major problems with this drug is its low solubility in biological fluids, which results into poor bioavailability after oral administration. The present study is an approach to enhance the dissolution rate of pioglitazone HCl by preparing solid dispersion (solvent evaporation method) using PEG 6000 as carrier in the ratios of 1: 1, 1: 2, 1: 3 and 1: 5 respectively. The drug carrier interaction study was carried out by Fourier Transform Infrared Spectroscopy (FTIR). The prepared solid dispersions were characterized for percentage yield, bulk density, tapped density, Carr's Index, Hausner's ratio, angle of repose, drug content, in vitro drug dissolution and stability study. The FTIR study suggesting no interaction between physical mixture of drug and carrier. The solvent evaporation was found to be efficient method to obtained good yield solid dispersions with good flow properties. The drug content was found in the ranges of 72.87 +/- 0.31 to 85.23 +/- 0.22 %. The solid dispersion of pioglitazone is releasing maximum amount of drug within 60 min where as pure drug is releasing 21.80 +/- 0.85 % only. Among all the solid dispersion formulations, formulation F3 of drug carrier ratio 1: 3 was found to be best for releasing maximum drug (98.50 +/- 1.09 %) with good drug content. All pioglitazone solid dispersions were found to be stable in various storage temperatures. All data are found to be significant by applying one way ANOVA at 5 % level of significant (p<0.05).