Assessment of Iris albicans lange as potential antimicrobial and analgesic agent.

Objective of the present work was to evaluate the presence of phytochemical constituents and pharmacological activities (antimicrobial and anti-nociceptive) of crude extract isolated from Iris albicans and its corresponding fractions. Extraction was made with methanol and extract was evaluated for the presence of different bioactive constituents, as per standard protocols. Extract and its corresponding fractions were evaluated for their antimicrobial and anti-nociceptive potential. Well diffusion method was used to evaluate the antibacterial effects while anti-nociceptive effect was studied using in-vivo models (acetic acid induced writhing, hotplate and tail immersion tests) at different dose level (100, 200 and 300 mg/kg of body weight) and compared with diclofenac sodium (dose = 10 mg/kg body weight). Results showed that the I. albicans extracts contained secondary metabolites including alkaloids, phytosterols, flavonoids, saponins, terpenoids, tannins, phenols, steroids, fixed oil, glycosides and carbohydrates. Furthermore, it was observed that different fractions in decreasing polarity order such as chloroform >n-Hexane > Ethyl acetate > Crude Methanol > Aqueous extract exhibited effective antimicrobial response against all test organisms. Results of the study showed that the extracts have significant antimicrobial and analgesic activity, providing evidence for its folklore use.

The hematological and histological studies for the hepatoprotective-like effect of the hydromethanolic extract and the fractions of Viola serpens Wall.

Traditionally, Viola serpens has been used in the treatment of several human disorders including liver diseases without any scientific evidence. As the current therapies are not very effective and face challenges of unwanted effects and patient compliance, therefore more effective and safe agents are highly needed. The current study aimed to evaluate the hepatoprotective potential of the crude extract and subsequent fractions of the whole plant in the in-vivo model using various hematological and histopathological parameters followed by an HPLC study for the identification of phenolic compounds. Rabbits (1000-1200 g) were used in the study. Paracetamol (2g) was used to induce hepatotoxicity in experimental rabbits. The plant extract was used in two doses (150 and 300 mg/kg body weights) for eight days. The hematological parameters AST, ALT and ALP values were determined along with the histopathology of the liver. Phenolic compounds were identified by high-performance liquid chromatography (HPLC) Agilent-1260 infinity from their retention time, UV spectra and available standards while quantification was done taking the percent peak area. The doses 150 and 300 mg/kg body weight seemed to be more effective. The hematological values and the histopathological slides show the hepatoprotective effect of the plant. Regeneration indicated the presence of nuclei, nuclear cleaning, prominent nucleoli, RBC's, central veins and plates of hepatocytes. The HPLC studies revealed the presence of a number of phenicol compounds. The crude extract and the subsequent fractions of the plant possess strong hepatoprotective activity, providing a scientific rationale for its uses in the treatment of liver toxicities.

Nephroprotective effect of the hydromethanolic extract and fractions of Viola serpens Wall. Histological and hematological evidence.

The current study was planned to examine the nephroprotective effect of the crude extract and its various fractions of Viola serpense Wall against paracetamol-induced toxicity in rabbits. The serum creatinine levels of all fractions, as well as the crude extract, were found to have a greater effect. The effect on urine urea by the n-hexane, ethyl acetate, n-butanol and aqueous fraction in high doses (300 mg/kg b.wt.) and crude extract and chloroform in low doses (150 mg/kg bwts.) were comparatively more effective and comparable to silymarin. The creatinine clearance of the fractions except for chloroform, aqueous at 300 mg/kg and the hydro-methanolic extracts at both doses were highly significant. The histological structures of kidneys in crude extract and chloroform-treated groups showed more improvement at the lower doses. The fractions n-hexane, ethyl acetate and n-butanolic exhibited an inverse dose relationship in the histology of the kidney. However, the aqueous fraction showed a dose-dependent nephroprotective effect. Finally, the crude extract and fractions significantly improved paracetamol-induced nephrotoxicity in rabbits.

Evaluation of the effect of carrier material on modification of release characteristics of poor water soluble drug from liquisolid compacts.

Liquisolid compact is a novel dosage form in which a liquid medication (liquid drug, drug solution/dispersion in non-volatile solvent/solvent system) is converted to a dry, free flowing powder and compressed. Objective of the study was to elucidate the effect of carrier material on release characteristics of clopidogrel from liquisolid compacts. Different formulations of liquisolid compacts were developed using microcrystalline cellulose, starch maize, polyvinyl pyrollidone and hydroxypropyl methylcellulose as carrier material in three concentrations (40, 30 and 20%, w/w). Liquid vehicle was selected on the basis of solubility of clopidogrel. Colloidal silicondioxide was used as coating material and ratio of carrier to coating material was kept 10. A control formulation comprised of microcrystalline cellulose (diluents), tabletose-80 (diluents), primojel (disintegrant) and magnesium stearate (lubricant) was prepared by direct compression technique and was used for comparison. All the formulations were evaluated at pre and post compression level. Acid solubility profile showed higher solubility in HCl buffer pH2 (296.89±3.49 µg/mL). Mixture of propylene glycol and water (2:1, v/v) was selected as liquid vehicle. Drug content was in the range of 99-101% of the claimed quantity. All the formulations showed better mechanical strength and their friability was within the official limits (<1%). Microcrystalline cellulose and starch maize resulted in faster drug release while polyvinyl pyrollidone and HPMC resulted in sustaining drug release by gel formation. It is concluded from results that both fast release and sustained release of clopidogrel can be achieved by proper selection of carrier material.

Zoonotic and non-zoonotic helminths in black rats of rain-fed and irrigated areas of Swat, Khyber Pakhtunkhwa, Pakistan.

Present study was conducted to get information on helminth parasites of zoonotic importance among the black rats of district Swat, Pakistan. Two hundred and sixty nine rats were captured from agricultural ecosystem of the district using live captured traps from 2011 to 2013. Captured rats were anesthetized and surveyed for the presence of ectoparasites, then were carefully dissected for investigation of endoparsites. Helminth parasites of 8 species were identified. Presence of parasite was noticed in 23.7% of sampled rats. The infection rates of sampled rats was given in order of their infectivity as Syphacia obvelata 13(4.83%), Aspiculuris tetraptera 13(4.83%), Heterakis spumosa 12 (4.46%), Hymenolepis spp. 9(3.34%), H.diminuta 8(2.97%), Hymenolepis fusa 4(1.48%), Lutziella microacetabularae 4(1.48%) and Lutziella spp. 1 (0.37%). No significant difference (P < 0.4289) was found in prevalence of parasites among areas, crops, crop stages and sex of the host while adult rats were found more infected than sub-adults. S. obvelata and A. tetraptera were the most common species of helminths while Lutziella sp., 1 (0.37%) was found only in one host. Rattus rattus (the black rat) was regarded as the host of helminth parasites of zoonotic importance, therefore the hidden health hazards of this rodent species needed to be considered to prevent infectivity of humans. Current study was concluded that Rattus rattus harbored a wide variety of helminth parasites which shows a hidden risk to inhabitants of the region. Monitoring rats' population in settle areas and educating the local community about the risk of rat borne parasitic diseases transmission through rats appears to be absolutely essential.

Smart nanocrystal of indomethacin: Nanonization and characterization through top down method of media milling.

Indomethacin is potent and effective drug belongs to NSAID group having low bioavailability. To address this issue the novel method is Nanosuspensions which can be achieved through bottom up and top down methods. The drug concentration, batch size and crystallinity retention are the problems associated with bottom up method consequently top down method was applied. In current project batch size of 350 ml was prepared by mixing 3.5% of Indomethacin with polymer solution. Then it was introduced into Dena⌖ having 0.2µm yttrium reinforced zirconium beads. The effect of milling time was observed for sixty minutes. Stable nanocrystals with particle size of 161nm ±1.90 with PDI of 0.229 ±0.06 were produced. The DSC and PXRD confirmed the crystallinity of created nanocrystals. The pattern of particle size reduction was initially abrupt and then gradual. The two months Stability studies at 4°C and at 25°C revealed that polymers combination (PVP-K30, HPMC-6cps, SDS) were effective in marinating the stability. The SEM and TEM studies unfastened that nanocrystals were homogenously distributed with discrete crystalline morphology. The fabricated nanocrystals demonstrated marked dissolution rate compared to the raw and marketed formulations. It is demonstrated that it is useful for industry due to high drug concentration, large batch size and retention of distinct characteristics.

Enhanced dissolution rate of Ketoprofen by fabricating into smart nanocrystals.

The low bioavailability of Ketoprofen is associated with its hydrophobic nature that can be solved by nanonization. For this purpose, a polymeric solution with drug concentration of 3.5% w/w was formulated. The produced solution was milled for 60 minutes in DENA® mill which contains 0.2µ m yttrium reinforced zirconium beads. The Physicochemical properties, characterization including stability studies of the prepared nanoparticles were carried out using pharmacopeial techniques of zeta potential, PXRD, DSC, SEM and TEM. Results suggest that stable crystalline nanocrystals with a size of 169±1.98nm with PDI of 0.194±0.04 and zeta potential of -22.0±2.25mV were produced. Moreover, enhances in-vitro release rate of 78.6% for the processed Ketoprofen was achieved in first 5 min as compared to raw form and marketed drug which released only 22.9% and 33.1% of drug respectively. The 60 days stability studies at 4oC & 25°C revealed that polymers PVP-K30-HPMC-6cps-SDS were effective in stabilizing the nanocrystals. Comparatively stable ketoprofen nanocrystals were successfully produced by DENA® mill with marked enhanced dissolution rate. It proved a useful for commercialization technique due to high drug concentration and retention of distinct characteristics at large scale.

Pharmacokinetic interaction of ciprofloxacin with diclofenac: a single-dose, two-period crossover study in healthy adult volunteers.

BACKGROUND AND OBJECTIVE: Ciprofloxacin is a broad-spectrum, synthetic antibacterial used for the treatment of various bacterial infections. In multidrug therapy, ciprofloxacin is commonly prescribed with analgesics for the management of infection, pain and inflammation. The objective of this study was to evaluate the pharmacokinetic properties of ciprofloxacin tablets with concurrent administration of diclofenac tablets in healthy adult human volunteers. METHODS AND DESIGN: The disposition pharmacokinetics of a single oral dose of ciprofloxacin 500 mg alone and with co-administration of a diclofenac 50 mg tablet in 12 healthy male volunteers was investigated using a two-period, crossover design. The blood samples were collected at 0 (predose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16 and 24 hours after administration of the drugs and the concentration of ciprofloxacin in serum was determined using reversed phase high-performance liquid chromatography. The pharmacokinetic parameters were calculated using a noncompartmental model and a two-compartment model. RESULTS: The maximum plasma concentration (C(max)) of ciprofloxacin increased from 2.48 +/- 0.33 microg/mL when administered alone to 3.91 +/- 0.8 microg/mL with co-administration of diclofenac. Time to reach C(max) (t(max)) with ciprofloxacin reduced from 2.02 +/- 0.3 hours when administered alone to 1.49 +/- 0.2 h with co-administration of diclofenac. Significant increases in ciprofloxacin area under the serum concentration-time curve (AUC) and elimination half-life, together with a significant decrease in total body clearance of ciprofloxacin, were observed with concurrent administration of diclofenac. CONCLUSION: Oral co-administration of ciprofloxacin tablets with diclofenac tablets increased ciprofloxacin AUC and C(max), and reduced ciprofloxacin t(max) and total body clearance.