MOSP - Macao Scientific Publishers

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Accelerated stability testing of celecoxib nanoemulsion containing Cremophor-EL

Faiyaz Shakeel*, Sanjula Baboota, Alka Ahuja, Javed Ali and Sheikh Shafiq

Abstract: Celecoxib (CXB), a selective cyclooxygenase-2 inhibitor has been recommended for the treatment of arthritis and osteoarthritis upon oral administration. However, long term oral administration of celecoxib cause serious gastrointestinal adverse effects. Therefore the aim of the present study was to enhance CXB’s physical and chemical stability using nanoemulsion formulation in order to eliminate gastrointestinal adverse effects of its oral administration. Optimized nanoemulsion formulation was prepared by spontaneous emulsification method. Nanoemulsion was characterized by droplet size, viscosity and refractive index. Stability studies were performed for the period of 3 months. Droplet size, viscosity and refractive index were determined every month. Shelf- life of nanoemulsion formulation was also determined by accelerated stability testing. It was found that droplet size, viscosity and refractive index were slightly increased at refrigerator and room temperature in 3 months period. However, the changes in these parameters were not statistically significant (p 0.05). The shelf-life of optimized nanoemulsion formulation was found to be 2.38 years at room temperature. These results indicated that both physical as well as chemical stability of celecoxib can be enhanced in nanoemulsion formulation using Cremophor-EL as surfactant.[...] Read More.

Keywords: Nanoemulsion, celecoxib, shelf life, cremophor-EL.

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Antidiabetic activity of hydro-ethanolic extracts of Nymphaea Stellata flowers in normal and alloxan induced diabetic rats

K. Rajagopal and K. Sasikala

Abstract: The antidiabetic effect of hydro-ethanolic extract (HEE) of Nymphaea stellata Willd flower was investigated in normal and alloxan-induced diabetic rats. In the present study, the animals were divided in to normal control, diabetic control, diabetic treated and control treated group (n = 6). Effect of oral administration of HEE (300 mg/kg) for 30 days on the level of blood glucose, glycosylated hemoglobin (HbA1C), total cholesterol (TC), triglycerides (TG), phospholipids, low density lipoprotein (LDL), very low density lipoprotein (VLDL), high density lipoprotein (HDL), Hexokinase, lactate dehydrogenase (LDH) and Glucose-6-phosphatase in normal and alloxan-induced diabetic rats were evaluated. When comparing the values of the HEE treated group with those of the control diabetic group, we found that the HEE significantly decreased the elevated blood glucose level, glycosylated hemoglobin, cholesterol, triglycerides, phospholipids, LDL, VLDL and it showed a significant increase in liver glycogen, insulin and HDL level. Treatment with HEE in diabetic rats increased the Hexokinase, LDH activity and decreased the glucose 6-phosphatase activity. These results clearly indicated that N. stellata flowers possess promising antidiabetic effect in diabetic rats.[...] Read More.

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Evaluation of antimicrobial potentials of stem bark extracts of Cochlospermum planchoni

Doughari, J. H.*, El-Mahmood, A. M. and Phillip, B.

Abstract: Antimicrobial activity of root extracts of Cochlospermum planchoni against some pathogenic bacteria and fungi were investigated using the filter paper disc diffusion method. Phytochemical studies revealed the presence saponins, tannins, glycosides and aikaloid as phytochemicals. Methanol extracts (40 mg/ml) exhibited the highest activity (16 - 30 mm zone diameter of inhibition, MIC and MBC values 2.5 - 22.5 mg/ml) against the test organisms. Chloroform extracts demonstrated the least activity. The activity of the extracts increased with increase in temperature (4 - 100ºC) and increasing acidity (pH 2.5 - 6), but alkaline pH (pH 10) neither enhanced nor depreciated the activity of the extracts. The plant can be used to source newer antibiotic substances and can be used for the treatment of typhoid fever, dysentery, urinary tract and wound infections and mycotic infections.[...] Read More.

Keywords: Antimicrobial activity, disc diffusion method, extracts, infections, pathogenic, phytochemicals.

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Determination of prednisolone, dexamethasone and hydrocortisone in pharmaceutical formulations and biological fluid samples

K. Balaji, G. V. Raghunadha Reddy, T. Madhusudana Reddy and S. Jayarama Reddy*

Abstract: A simple, sensitive and accurate voltammetric studies on prednisolone (PE), dexamethasone (DE) and hydrocortisone (HC) were carried out by using cyclic voltammetry (CV) and differential pulse voltammetry (DPV) at bare carbon paste electrode (CPE) and -cyclodextrin modified carbon paste electrode (CDMCPE) in Britton-Robinson (BR) buffer solution. PE, DE and HC show marked enhancement of peak currents at CDMCPE when compared to CPE due to the inclusion complex between keto- group from the drug and -cyclodextrin (modifier) . All these compounds exhibit a well-defined single peak in the studied pH range which is attributed to the reduction of keto-group. BR buffer of pH 3.0 was found to be reliable supporting electrolyte for the analytical estimation of these compounds. CV studies indicate that the process was irreversible and adsorption controlled. The reduction peak currents at CDMCPE for PE, DE and HC changes linearly over the concentration range from 5.6 × 10-7 M to 2 × 10-5 M (PE), 4.1 × 10-7 M to 2 × 10-5 M (DE) and 4.2 × 10-7 M to 2.5 × 10-5 M (HC) with a correlation co-efficient of 0.9991, 0.9986 and 0.9995 for the respective compounds. DPV technique is used for the determination of PE, DE and HC in pharmaceuticals and biological fluid samples. For quantification, standard addition method was carried out in both pharmaceutical formulations and biological fluid samples.[...] Read More.

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Effect of viscosity grades of ethylcellulose on the sustained release properties of indomethacin from its tablets matrix

Amri Ahmed* and Sfar Souad

Abstract: The objective of the present study was to estimate the influence of ethyl cellulose (EC) with different viscosity grades on in vitro drug release from EC matrix tablets containing Indomethacin. Four viscosity grades of EC (7, 10, 50 and 100 cp) were studied. The 90 - 125/µm particle size fraction was collected by manual dry sieving and the compression force was varied to produce tablets of equal hardness. The drug release from Indomethacin tablets was determined by dissolution testing as described in the United States Pharmacopoeia (USP). The tablets pore characteristics were studied using helium pycnometry and mercury porosimetry. The release rate constant ranged from 1.25 ± 0.98 for the 7cp viscosity grade tablets to 1.49 ± 1.02 for the 100cp viscosity grade tablets whereas porosity ranged from 5.6% ± 0.3 to 6.8 ± 0.1 when based on gaz pycnometry and from 3.9% ± 0.4 to 5.1 ± 0.2 when based on mercury intrusion. These results indicate that the release rates marginally increased with an increase in viscosity grade. The main explanation for the viscosity grade effect on release rates would be differences in tablet porosity.[...] Read More.

Keywords: Matrix, ethylcellulose, viscosity grade, indomethacin, dissolution, porosity.

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Effects of plants and medicinal plant combinations as anti-infectives

Ramesh, Putheti and Okigbo, R. N

Abstract: The ascendancy of the Human Immuno Deficiency virus (HIV) has spurred intensive investigation into plant derivatives, which may be effective, especially for use in underdeveloped nations with little access to expensive western medicines. This review describes mostly the current state of ant microbial substances of plant origin ranging from extracts commonly in use, largely by the community, to substances being prospected screened and tested by researchers and clinicians. This review focuses on plant and their extracts, which are anti microbial in nature or in other words the anti microbial substances of plant origin and their eventual therapeutic effects on human affairs. Only phytochemicals or anti microbial substances reported to have anti microbial or anti-infective properties are examined.[...] Read More.

Keywords: Phytomedicines, medicinal plants, human, diseases.

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Phytochemical screening and antibacterial evaluation of the leaf and root extracts of Cassia alata Linn

El-Mahmood, A. M.* and Doughari, J. H.

Abstract: Phytochemical screening of the leaves and roots of Cassia alata (Linn) revealed the presence of some bioactive components, which have been linked to antimicrobial properties. The effects of water, methanol and chloroform extracts on some pathogenic Staphylococcus aureus, Escherichia coli, Streptococcus pyogenes, Pseudomonas aeruginosa and Proteus mirabilis showed that the plant parts can be used to treat infections caused by these bacteria. S. aureus, S. pyogenes and P. mirabilis were more susceptible, while E. coli and P. aeruginosa were less sensitive. The effectiveness of the crude extracts were enhanced at elevated temperatures and at near neutrality pH values, which attests to its use in traditional medicine to treat skin, urinary tract and gastrointestinal infections. The aqueous extract was less effective than the organic solvents, thus suggesting the inability of the traditional medicine practitioners to exhaustively extract all the bioactive components with water. The MICs and MBCs of the extracts against the test bacteria were high and correlate with sensitivity test results. The effectiveness of the extracts were less than the conventional antibiotic, metronidazole.[...] Read More.

Keywords: Antimicrobial bioactive, pathogenic, phytochemical, traditional medicine.

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Gender independent pharmacokinetics of levofloxacin in healthy black African subjects

Mbang A. Owolabi*, Grace E. Ukpo, Martin E. Okenne, Olayinka O. Oyeniyi, Olajumoke O. Oladipo and Smith I. Jaja

Abstract: The pharmacokinetic profile of levofloxacin in healthy black African subjects as well as the influence of gender on its pharmacokinetic parameters was investigated. Sixteen healthy adult volunteers (8 males and 8 females) enrolled in the study and took single oral dose of 500 mg levofloxacin (LevofloxÒ) after informed consent. The blood of the volunteers was withdrawn from their antecubital vein at 0, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 24 and 36 h post dosing and analysed for levofloxacin concentration. The results of this study revealed that levofloxacin was well tolerated and detectable in the plasma seventeen min after dosing being faster in female than male. Bioavailability was not affected by gender and Tmax showed no significant difference between the genders (p 0.05). The Cmax and AUC0- were higher in the female than in the male subjects, plasma clearance (CL) was lower in female than in the male thus explaining the differences in the total systemic exposure of the drug. The volume of distribution (Vd) was significantly reduced in female compared to the male. When pharmacokinetics parameters were expressed relative to mg drug/total body weight or renal function, gender-related differences were attenuated. This result indicates that subject body weight or renal function may be involved in the pharmacokinetic differences of the subjects, thus drug administration based on sex is not relevant.[...] Read More.

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Synthesis, antiviral and cytotoxic activities of some novel 2-Phenyl-3-Disubstituted Quinazolin-4(3H)-ones

Periyasamy Selvam*, K. Babu, R. Padamraj, Leentje persoons and Erik de Clercq

Abstract: The 2-phenyl-benzoxazin-4-ones were condensed with primary amine to form the 2, 3-disubstituted quinazolin-4(3H)-ones. Their chemical structure was elucidated by means of spectral (FT-IR, 1H- NMR, MS) and elemental analysis. The antiviral activity and cytotoxicity of the compounds were tested in HeLa cells (vesicular stomatitis virus, Coxsackie virus B4 and respiratory syncytial virus), HEL cells [herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2), vaccinia virus], Vero cells (parainfluenza-3, reovirus-1, Sindbis virus, Coxsackie virus B4 and Punta Toro virus). Among the new derivatives evaluated, specific antiviral activity was noted with compound QAA against vaccinia virus, parainfluenza-3 virus and Punta Toro virus, compound QOPD against HSV-1, HSV-2 and vaccinia virus, and compounds QONA and PD-NFIN against Coxsackie virus B4.[...] Read More.

Keywords: Quinazoline, antiviral, HSV, vaccinia, sulphanamides.

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Evaluation of The Effect of Colloidal Silver on The Antibacterial Activity of Ethanolic Extract of The Lichen Parmelia Perlata

Momoh, M. A.* and Adikwu, M. U.

Abstract: Substances extracted from lichens have previously been reported to possess antimicrobial activities against various groups of bacteria, fungi and viruses. Due to the high abundance of Parmelia perlata in the Eastern parts of Nigeria, we decided to explore the effect of colloidal silver on the antibacterial activity against Staphylococcus aureus. The lichen extract was obtained via cold maceration with ethanol. The phytochemical tests was carried out on the extract of lichen. The minimum inhibitory zone MICs of the ethanolic extract against S. aureus was determine and the solution of the colloidal silver was also determine separately on S. auerus, the MIC of each was noted and their admixture in the presence of concentration of colloidal silver using bore- plate method. Result of the phytochemical tests showed the presence of flavonoids, saponins, tannins, glycosides, steroidal aglycone, carbohydrates. The result also shows that, the ethanol extract of the lichen has activity on S. aureus while the colloidal silver at the dilution used, has very little activity on the S. aureus. It was also seen from the result that the zone of inhibitory of the ethanol extract was increased in the presence of colloidal silver and MICs is concentration dependent. It was therefore finally concluded that colloidal silver potentates the effect of ethanol extract of the lichen P. perlata[...] Read More.

Keywords: Parmelia perlata, lichen, Staphylococcus aureus, evaluation, colloidal silver.

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