In vitro antioxidant and reducing capability of weight loss tablet formulation.

Antioxidants are used as an influential counteractive measure in opposing the generation of reactive oxygen species. The current study was carried out to investigate antioxidant potential and reducing capability of developed weight reducing tablet formulation. When tablets were evaluated at concentrations of 50, 100 and 500µ/ml, antioxidant activity improved in a dose depending way just similar to standard Butylated hydroxyl anisol (BHA). For evaluation of reducing ability the formulation under test evaluated at concentrations of 50, 100 and 500µ/ml and it was observed that formulation contain good reducing capability and possess considerable activity to scavenge super oxide radicals. In-vitro analysis of weight reducing tablets formulation showed considerable antioxidant and reducing capacity that will be supportive in averting the development of a variety of oxidative stress-related diseases.

Evaluation of in vitro urease and lipoxygenase inhibition activity of weight reducing tablets.

Enzyme inhibition is a significant part of research in pharmaceutical field in view of the fact that these studies have directed to the innovations of drugs having remarkable performance in diverse physiological conditions. The present study was aimed to assess urease and lipoxygenase inhibitory activity of weight reducing tablets. For evaluating the urease activity indophenol method was employed using Thiourea as the model urease inhibitor. The lipoxygenase inhibition was evaluated by measuring the hydroperoxides produced in lipoxygenation reaction using a purified lipoxygenase with lionoleic acid as substrate. When formulation of the weight reducing tablets was compared at various concentrations (50, 100 and 500µg/ml). The antiurease activity and lipoxygenase inhibition activity increased in a dose dependent manner. The formulations under test have an excellent antiurease and lipoxygenase inhibition potential and prospective to be used in the cure of a variety of complications associated with the production of urease and lipoxygenase enzymes.

Natural antiemetics: an overview.

Emesis encompasses the forceful expulsion of the contents of stomach via the mouth or sometimes the nose. The adverse effects of currently available anti-emetic agents potentiate the natural product researchers to explore the natural anti-emetics with fewer side effects. The presented communication constitutes a review on anti-emetic effect of two hundred and forty five plants belonging to seventy-eight families found in different parts of the world. It also outlined the anti-emetic effect of plant extracts and isolated secondary metabolites studied through a variety of animal models of emesis. The reported anti-emetic plants in different countries and cultures and the scientific studies on extracts may help in the identification of promising single chemical compound(s) that may be used as a potential leads for developing safe anti-emetic agents in future. Moreover the reported secondary metabolites having the same effect may open the door for the search of same secondary metabolites from other natural sources. This review will provide useful information for the discovery of natural anti-emetic compounds and fill the gaps in knowledge.

Bioactive alkaloids produced by fungi. I. Updates on alkaloids from the species of the genera Boletus, Fusarium and psilocybe.

Fungi, in particular, are able in common with the higher plants and bacteria, to produce metabolites, including alkaloids. Alkaloids, along with other metabolites are the most important fungal metabolites from pharmaceutical and industrial point of view. Based on this observation, the authors of this review article have tried to provide an information on the alkaloids produced by the species of genera: Boletus, Fusarium and Psilocybef from 1981-2009. Thus the review would be helpful and provides valuable information for the researchers of the same field.

Biopharmaceutical evaluation of oral tablet Atenolol (100 and 50 mg) on local population.

An open-label, randomized study was designed to determine the bioavailability (BA); pharmacokinetic (PK) and pharmacodynamic (PD) behaviour of Atenolol 50 mg (two pills) and 100 mg (one pill) tablet manufactured by a national pharmaceutical industry. Peak plasma concentration (Cmax): 1.33 +/- 0.31 microg/ml, time to peak plasma concentration (Tmax): 2.2 +/- 0.27 hours, AUC (area under the plasma concentration-time curve) 6.34 +/- 2.1 microg-hr/ml for 100 mg tab and Cmax: 1.07 +/- 0.23 microg/ml, Tmax: 2.5 +/- 0.35 hours, AUC 4.97 +/- 1.09 microg-hr/ml for 50 mg (two pills) tab were observed. The BA and PK parameters such as Cmax, Tmax, are comparable to previous studies, although significant decrease in diastolic and systolic blood pressure (mmHg) upto a certain limit for a considerable duration was observed. However, relation between PK and PD may not be established due to regulatory biochemical feedback mechanism.

Effects of tryptophan and valine administration on behavioral pharmacology of haloperidol.

Development of antipsychotics with slight/no extra-pyramidal symptoms (EPS) and/or other side effects is one of the exploring fields of drug research. Haloperidol is a high potency typical neuroleptic used in the treatment of schizophrenia but produces muscles related side effects commonly known as EPS. These effects are not produced following the administration of atypical neuroleptics such as clozapine. A severe side effect of clozapine treatment is however, agranulocytosis. This involves investigation on the mechanism by which a typical neuroleptic acting via serotonergic mechanism tends to produce less or no EPS. The present study was, therefore, designed to determine the effect of serotonin precursor tryptophan and a large neutral amino acid other than tryptophan (valine) on the modulation of haloperidol induced catalepsy and akinesia. Cataleptic effects of the drug and activity reducing effects were monitored on inclined surface and in an activity box or open field respectively. The results are discussed in the context of a role of tryptophan and valine induced changes of brain serotonin in modifying the extrapyramidal and monoaminergic effects of the typical neuroleptic haloperidol. In the present study administration of TRP and valine decreased activity in rats, haloperidol-induced catalepsy' was not modulated by prior administration of tryptophan or valine. Brain serotonin levels were elevated by haloperidol treatment and correlated very well with the behavioral response. These findings suggest a possible serotonergic involvement in neuroleptic induced tardive dyskinesia and an amelioration of the disorder through TRP supplementation.

Hypoglycemic potential of tablet Metformin 500 mg (Glucophage & Metphage): a pharmacological end point evaluation.

Quantitative determination of pharmacological response or clinical end point study is essential for successful evaluation of clinical pharmacology and Bioavailability/ Bioequivalence issues. Stride has been made for proper selection of a quality drug product from the various available therapeutic, which is the prime responsibility of Health care provider and specially pharmacist. Study was conducted in respect to investigate the Pharmacodynamics response, differences and individual variation of oral, Metphage (Metformin 500 mg tablet) as a test formulation manufactured by Efroze Chemical Industries (Pvt.) Ltd. and Glucophage (Metformin 500 mg tablet) as a reference formulation manufactured by Merck Marker. Blood glucose levels/hypoglycemic effect produced by both formulation were studied under cross over trial with respect to placebo/control treatment and result were discussed accordingly. There were no hypoglycemic episodes requiring medical intervention and/or pharmacologic therapy so the patients can easily manage it. Results of the study clearly suggest that formulation manufactured by Efroze Chemical Industries (Pvt.) Ltd. is near to the standard formulation and produced comparable results. No significant differences in pharmacodynamics was observed, however, minor differences might relate with inter individual variation in human volunteers and in different formulation as well as different pharmaceutical unit. Although this data assure the ultimate quality of Metformin 500 mg tablet manufactured by Efroze Chemical Industries (Pvt.) Ltd. but every Generic equivalent should be studied for assurance of safety and efficacy because life of patient is a matter of concern. Such type of study would provide better evaluation of the performance of a drug from a dosage form.

Bioavailability study of tablet Bezafibrate 200 mg (Lipocor).

In order to determine the ultimate quality of any formulated dosage form and rationalize the therapeutic plan as well as to individualize the prescription, in vivo measurement of drug is the modem and specialized expertise of the clinical/research area of pharmacy practice, which provides effectiveness and assures the safety of drugs. All pharmacological, therapeutic or toxic responses are subject to reaching of drug at the site of action through connective tissue. Other than physico chemical properties of drug, there are numerous factors from manufacturing process to biochemical behaviour of the individual which resist in the absorption, distribution, metabolism and elimination of drugs in the biological system. Bezafibrate Tablet 200 mg (Lipocor) an oral conventional formulation manufactured by Efroze Chemical Industries (Pvt.) Ltd. was investigated for bioavailability followed by pharmacokinetic studies on adult, male, healthy, human local population. For this purpose, a sensitive, specific and validated method was used for the estimation of bezafibrate in blood. HPLC was performed on a reversed phase C18 column (flow rate 1.5 ml/min, UV = 230 nm) with 0.02 M buffer of KH2PO4 (Adjusted pH 3.5 with Phosphoric Acid) and Methanol (40: 60) whereas extraction of the drug from the plasma was carried out by deproteinization of plasma according to classical method described in previous studies (Obaid A. et al., 1999). Peak level (Tmax) of Bezafibrate Tablet 200 mg (Lipocor) was observed at about 1.42 +/- 0.53 hours after the dose and practically free Bezafibrate Tablet 200 mg (Lipocor) could be detected in blood after 9 hours. Cmax of the investigated formulation of Lipocor register mark or target was 1732 +/- 374.2 ng/ml. Area under curve (AUC) was 5198.65 +/- 1231.8 ng. hr/ml.

Method development for analysis of gliclazide in human plasma by using high-performance liquid chromatography.

Since 1970, dissolution requirements have been included in tablets and capsules monographs, in general, in response to concerns for bioavailability of equal significance is the recognition of the immense value of dissolution testing as a tool for quality control. Thus, equivalence in dissolution behaviour was sought in the light of both bioavailability and quality control considerations (Coppack et al., 1990). Nonetheless, dissolution profiles are often considered by the industry to ascertain the release rates of drug from tablet formulations as a quality assurance tool. However, in terms of sensitivity, precision and specificity, high-performance liquid chromatographic (HPLC) method may offer additional advantages (Charles & Ravenscroft, 1984 and Nawaz, 2001).

Chemical constituents of Tagetes patula L.

Tagetes patula (Asteraceae) is a medicinal plant which is indigenous to Tropical America but cultivated in Pakistan. During the chemical study, conducted on the different parts of T. patula (roots, leaves and flowers) are found thiophenes, steroidal and terpenoidal type of constituents. Their structures were characterized by different spectroscopic. Among the thiophenes triterpens and steroids are two thiophenes, one triterpene and one steroid first time isolated from the genes Tegetes methods.

Antibacterial screening of Citrullus colocynthis.

Crude ethanolic extracts of fruits, leaves, stems and roots of Citrullus colocynthis Schrad were examined for their antibacterial potentialities against Gram positive and Gram negative bacilli. Ethanolic extracts of fruits, leaves, stems and roots were found to be active against Gram positive bacilli, viz., Bacillus pumilus and Staphylococcus aureus, while fruit and root extracts in double strength gave positive results against Gram positive bacillus (Bacillus subtilis). The Gram negative bacilli viz., Escherichia coli and Pseudomonas aeruginosa showed no response.

Effect of co administration of haloperidol and large neutral amino acids (tryptophan and valine) on rats striatal dopamine, serotonin and their metabolism.

Haloperidol is a high potency typical neuroleptic used in the treatment of schizophrenia. Administration of haloperidol produces muscles related side effects commonly known as extrapyramidal effects (EPS). These effects are not produced following the administration of atypical neuroleptics such as clozapine. A severe side effect of clozapine treatment is however, agranulocytosis. Development of antipsychotics with little/no EPS and/or other side effects is one of the exploring fields of drug research. This involves investigation on the mechanism by which a typical neuroleptic acting via serotonergic mechanism tends to produce less or no EPS. The present study is, therefore, designed to determine the effect of serotonin precursor tryptophan and a large neutral amino acid (valine) other than tryptophan on the modulation of neurochemical changes in the striatum. Neurochemical estimation were done by HPLC-EC. Present study showed that administration of tryptophan increased tryptophan, 5HT, 5HIAA and DA concentration in the striatum. DOPAC and HVA were not effected. Administration of valine increased DOPAC concentration in the striatum and did not alter tryptophan, 5HT, 5HIAA, DA and HVA concentration. Administration of the haloperidol increased HVA, 5HT and 5HIAA concentration. No effect was produced on tryptophan, DOPAC and DA levels. Valine administration followed by haloperidol injection did not alter striatal tryptophan, 5HT, DA, DOPAC and HVA concentration but decreased 5HIAA concentration. Administration of tryptophan followed by haloperidol injection increased tryptophan and 5HT concentrations and decreased DA levels. No effect was produced on 5HIAA, DOPAC and HVA concentrations. Administration of TRP increased plasma and brain concentration as well as DA levels in the striatum. Administration of valine did not decrease striatal TRP concentration while Haloperidol increased striatal 5-HT and 5-HIAA concentrations and no change in DA levels after haloperidol administration. whereas prior injection of TRP that increased 5HT concentration did not alter haloperidol-induced DA turnover in the brain.

Kinetic studies on Zingiber officinale.

The present investigation deals with the isolation, purification and characterization of gingerol, the major pungent constituent of ginger (Zingiber officinale) and its kinetic of extraction using a number of organic solvents. The characterization was carried out through GC and GC-MS. Gingerol has been assayed in the plant material during extraction with various solvents by a HPLC method. In order to develop a relationship between solvent characteristics such as viscosity and dielectric constant and the rates of extraction, the kinetics of extraction of gingerol has been studied by using twelve different solvents in order to evaluate the solvent efficacy in the extraction processes. It has been observed that both solvent viscosity (1/v) and dielectric constant (epsilon) show a linear relationship with the rates of extraction (k). An increase in solvent viscosity leads to a decrease in the rates of extraction, similarly an increase in dielectric constant also leads to a decrease in the rates of extraction. This appears to be largely due to an unionizable character of gingerol which does not interact with polar solvents. Thus solvent viscosity and dielectric constant both play an important role in the choice of solvents for the extraction of gingerol. Solvents with relatively low viscosity and dielectric constant are more suitable for the extraction of gingerol from plant material.

Pharmacokinetic differences of some generic tablet gliclazide 80 mg on Pakistani population.

The goal of rational drug therapy is to produce a desired pharmacological response in an acceptable and predictable manner while minimizing the occurrence of undesired events. The Pharmacokinetics of different generics of tablet gliclazide 80 mg was investigated on healthy (10 x 2), Pakistani subjects. For this exploration an open-label, randomized, two-period crossover (Balanced in Complete Block Design) study, was conducted The out come of the said study suggests that all generics were found analogous regarding pharmacokinetic behavior in-spite of having different excipients, concentration of excipients, sources of raw material, manufacturing process, machinery, resources and also inter individual variation of the study. Results of the study also undoubtedly advocate that generics manufactured in different manufacturing units of Pakistan are near to the standard formulation and produce comparable results. No significant differences in pharmacokinetics parameters were observed, however, minor differences might narrate with inter individual variation in human volunteers and in different generic as well as different pharmaceutical unit.