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Biomedical subjects

M Saeed Arayne

Publications and source records attributed to M Saeed Arayne.

At least 19 recordsLinked to original sources

Interactions between sparfloxacin and antacids - dissolution and adsorption studies.

Sparfloxacin is a broad-spectrum oral fluoroquinolone antimicrobial agent with a long elimination half-life, extensively used against both Gram-positive as well as Gram-negative microorganism. Concurrent administration of antacids and sparfloxacin decreases the gastrointestinal absorption of sparfloxacin and therapeutic failure may result. The present study was designed to evaluate the influence of some antacids on the availability of sparfloxacin. The release of sparfloxacin from tablets in the presence of antacids like sodium bicarbonate, calcium hydroxide, calcium carbonate, aluminum hydroxide, magnesium hydroxide, magnesium carbonate, magnesium trisilicate and magaldrate has been studied on BP 2003 dissolution test apparatus. These studies were carried out in simulated gastric and intestinal juices for three hours at 37 degrees C. The results confirmed that the dissolution rate of tablets was markedly retarded in the presence all of antacids studied, whereas magaldrate and calcium carbonate exhibited relatively higher adsorption capacities in simulated gastric juice and magnesium trisilicate and calcium hydroxide in simulated intestinal juice.

Adsorption↗

In vitro availability of metformin in presence of h(2) receptor antagonists.

Metformin is a guanidine derivative used for the treatment of NIDDM. As it is used for a long-term therapy, it may be coadministered with other drugs. Present paper deals with the in vitro availability studies of metformin in presence of commonly used H(2) receptor antagonists. The later drugs compete with histamine for H(2) receptors and block gastric acid secretion and some cardiovascular effects of histamine. These studies were carried out in simulated gastric juices, simulating empty and full stomach, simulated intestinal juice and buffers of pH 7.4 simulating blood pH at 37 degrees C on a B.P. 2003 dissolution test apparatus. Commonly prescribed H(2) receptor antagonists like cimetidine, ranitidine and famotidine were used in these studies. The present study clearly indicated that availability of metformin can be altered in presence of most of the H(2) receptor antagonists studied except in presence of famotidine at pH 4 where the drug concentration remains unaltered. The availability of metformin was increased in simulated gastric juice, pH 7.4 and pH 9 (except ranitidine at pH 9) whereas the decrease in availability was observed in presence of cimetidine and ranitidine at pH 4 and ranitidine at pH 9. On the basis of these results, it is can be suggested that metformin should be coadministered with care along with H(2) receptor antagonists especially in case of ranitidine; although chances of adverse reactions are rare but decrease availability of metformin may result in delayed effect. On the other hand, increase in metformin concentration may result in hypoglycemic effects.

Cimetidine↗

A rp-HPLC method for the assay of cefpirome and its application in drug-metal interaction studies.

An accurate, sensitive and least time consuming RP-HPLC method for the estimation of cefpirome in the presence of essential and trace metal has been developed and validated. Cefpirome was eluted from a B144A, OD-5-100, C(18) (150 x 4.6 mm) column at room temperature with a mobile phase consisting of MeOH:H2O (15:85, % v/v) at a flow rate of 1 ml/minute, while UV detection was performed at 265 nm. The detection limit of cefpirome was 10 ng. Drug metal interaction studies were carried out at 37 degrees C to monitor the complexation of drug with metal ions. These studies were beneficial to determine the drug in therapeutic concentrations inside human body as well as its complexation with metal cations. The metals essential to human body like Mg(II), Ca(II), Cr(II), Mn(II), Fe (III), Co(II), Ni(II), Cu(II), Zn(II) & Cd(II) were in the form of chlorides. The carboxylic group of the dehydrothiazine ring has more binding capacity relative to other group that augments the drug complexes with essential and trace elements. The established HPLC method is rapid, accurate, and selective, because of its sensitivity and reproducibility. The order of complexation was ferric>chromium>copper>nickel>cadmium>zinc>magnesium>manganese>calcium>cobalt.

Anti-Bacterial Agents↗

Fabrication of nanoparticles within polymeric pores for controlled release of drug.

Nanotechnology, a multidisciplinary scientific undertaking, involves creation and utilization of materials, devices or systems on the nanometer scale. The field has enabled the development of an amazing variety of methods for fabricating nanoparticles in recent years. The technology is expected to create innovations and play a critical role in the field of bio-pharmaceuticals especially in controlled release of drug delivery. Sol-gel technique is one of the most widely used techniques to fabricate porous nanoparticles within the polymer. Such nanoparticles have also applications in vascular drug delivery and release, site-specific targeting (passive as well as active targeting), as well as transfusion medicine. This article concentrates mainly on fabrication of porous nanoparticles, its characterisation and its use for controlled release of drug. It also encompasses the strategies that have been used to translate and fabricate a wide range of particulate carriers e.g., nanospheres, liposomes, micelles, oil-in-water emulsions, with prolonged circulation and/or target specificity. With regard to the targeting issues, attention is particularly focused on the importance of physiological barriers. we have also critically reviewed and assessed the fate and activity of biodegradable/bio-erodable polymeric drug delivery vehicles because the uniformity in degradation of these polymers is questionable.

Delayed-Action Preparations↗

Degradation studies of azithromycin and its spectrophotometric determination in pharmaceutical dosage forms.

A simple, accurate and rapid spectrophotometric method for the estimation of azithromycin has been developed by the acidic hydrolysis of the drug with sulfuric acid and monitoring the absorbance at 482 nm. All variables affecting the reaction conditions such as sulfuric acid concentration, heating time, temperature and dilution solvents were carefully studied. Analytical parameters such as stability, selectivity, accuracy and precision have been established for the method and evaluated statistically to assess the application of the method. The method was applied successfully for the assay of azithromycin dihydrate in pure and pharmaceutical dosage forms as tablets, capsules and suspensions. The method was found to have the advantages for simplicity, stability, sensitivity, reproducibility and accuracy for using as an alternate to the existing non-spectrophotometric methods for the routine analysis of the drug in pharmaceutical formulations and also in pharmaceutical investigations involving azithromycin dihydrate.

Anti-Bacterial Agents↗

Synthesis and characterization of glibenclamide complexes of magnesium, chromium, cobalt, nickel, zinc and cadmium salts.

Glibenclamide is the commonly used hypoglycemic agent in NIDDM. Metal complexes of glibenclamide have been synthesized by reaction with different metals such as magnesium, chromium, cobalt, nickel, zinc and cadmium in the form of their chlorides. These complexes were characterized by their physical characteristics, 1H-NMR, IR and Atomic absorption studies.

Cadmium Chloride↗

In vitro availability of atorvastatin in presence of losartan.

Hydroxymethylglutaryl-coenzyme A reductase inhibitors (statins) are a group of cholesterol lowering agents that have become the largest selling drugs in the world. They are of proven clinical benefit in coronary heart disease, at least in those patients who do not have overt chronic heart failure (CHF). Co-administration of statins with angiotensin II receptor blockers (ARBs) is most common, since there is strong synergy between hypertension and hypercholesterolemia in terms of risk factors for the development of cardiovascular diseases. In present paper, we describe the in vitro availability of atorvastatin, a potent HMG-CoA reductase inhibitor, in presence of losartan potassium, which is a non-peptide angiotensin II receptor antagonist. These studies were carried out at 37, 48 and 60 degrees C in different pH environments simulating human body compartments. It was observed that in pH 1, 7.4 and 9 the availability of atorvastatin was very high while losartan was not at all available. However in pH 4 these effects were reversed and atorvastatin was not available at all. At 48 degrees C the availability of atorvastatin was high and that of losartan was depressed at pH 9, whereas the later was not available at pH 1, 4 and 7.4 at all. Likewise at 60 degrees C, the availability of atorvastatin at pH 7.4 and 9 was high, whereas the charge-transfer complex formed between the two drugs was broken at pH 1 at this temperature and the entire drug was available. On the other hand the availability of losartan at pH 4 and 9 was high while it was not available at pH 1 and 7.4. The availability of atorvastatin was maximum in simulated gastric juice as compared to buffer of pH 7.4 and 9. This high availability of one drug in presence of other is attributed to the formation of a charge-transfer complex, which was stable at elevated temperatures, except at 60 degrees C in pH 1.

Angiotensin II Type 1 Receptor Blockers↗

Porous nanoparticles in drug delivery systems.

This article concentrates mainly on fabrication of porous nanoparticles, its characterisation and its use for controlled release of drug. It also encompasses the strategies that have been used to translate and fabricate a wide range of particulate carriers e.g., nanospheres, liposomes, micelles, oil-in-water emulsions, with prolonged circulation and/or target specificity. Sol-gel technique is one of the most widely used techniques to fabricate porous nanoparticles within the polymer. Such nanoparticles have also applications in vascular drug delivery and release, site-specific targeting, as well as transfusion medicine. With regard to the targeting issues, attention is particularly focused on the importance of physiological barriers. We have also critically reviewed and assessed the fate and activity of biodegradable polymeric drug delivery vehicles because the uniformity in degradation of these polymers is questionable. This article will highlight rational approaches in design and surface engineering of nanoscale vehicles and entities for site-specific drug delivery. Potential pitfalls or side effects associated with nanoparticles are also discussed.

Animals↗

Spectrophotometric method for quantitative determination of gliquidone in bulk drug, pharmaceutical formulations and human serum.

A quick and sensitive spectrophotometric method for quantitative determination of gliquidone in bulk drug, pharmaceutical formulations and human serum has been developed and validated. The reported method is fourteen times more sensitive than British Pharmacopoeial method. Gliquidone is a second generation sulfonyleurea derivative, indicated to improve glycemic control in NIDDM patients. The method was validated as per ICH guidelines and found advantageous for simplicity, sensitivity, reproducibility, linearity, precision and accuracy. The developed method has also been applied to the analysis of GLURENOR tablet and evaluated statistically to assess the application of the method. The limit of detection and quantification of gliquiodone at 225 nm was 68.31 ng mL-1. The, serum did not interfere with the estimation and the drug spiked in serum was totally recovered. The present method has further advantage in estimating the drug in concentrations even lower than the amount usually present in blood after oral intake. Calibration was linear in the range of 0.207-20 microg mL-1 (r2 = 0.9972). In addition, the proposed method is simple, easy to apply, low cost, requires relatively inexpensive instrument and used as an alternate to the existing spectrophotometric and non-spectrophotometric methods for the routine analysis of the drug in raw material, pharmaceutical formulations and from human serum.

Algorithms↗

In vitro interactions of captopril with NSAID's.

Captopril is effective in the treatment of hypertension of all grades of severity. Present paper deals with the in vitro availability studies of captopril in presence and absence of commonly used NSAID's likes diclofenac sodium, flurbiprofen, mefenamic acid, meloxicam and tiaprofenic acid. Since it had been established that simultaneous administration of both drugs may alter the antihypertensive effect of captopril. In order to find out the kinetics and energitics of captopril in presence of NSAID's, these studies were carried out in buffers of pH 4, 7.4 and 9 at 37 degrees C and at elevated temperatures. These studies clearly indicate that most of the NSAID's bind to captopril, forming charge-transfer complexes revealing that the availability of captopril can be affected by the concurrent administration of NSAID's. Accordingly coadministration of both the drugs should be avoided.

Angiotensin-Converting Enzyme Inhibitors↗

Development and validation of RP-HPLC method for the analysis of metformin.

The reversed-phase high-performance liquid chromatographic (RP-HPLC) method has been developed to quantify metformin hydrochloride (MfCl) in raw material and pharmaceutical formulations using C(18) analytical reverse-phase column. Diazepam was used as an internal standard. Mobile phase consisted of methanol-water (30:70 v/v), pumped at a flow rate of 0.5 ml/min at ambient temperature and the retention time was about 4.4 min with symmetrical peaks. (MfCl) was detected by ultraviolet absorbance at 233 nm with no interference of commonly used excipients. The method was linear over the concentration range 0.312-5 mug/mL (R2 = 0.9995). The limit of detection of metformin was 0.1 mug/mL and the limit of quantitation was 0.3 mug/mL. The results obtained showed a good agreement with the declared contents in case of pharmaceutical formulations. The proposed method is rapid, accurate, economical and selective and it may be used for the quantitative analysis of metformin in Neodipar tablets because of its sensitivity and reproducibility.

Calibration↗

Review: nanoparticles in drug delivery for the treatment of cancer.

Although the "war on cancer" is now in its fourth decade and despite much progress has been made in categorizing the environmental causes and cellular and molecular biological basis for this dreaded disease, we still do not have a precise understanding of the differences between a cancer cell and its normal counterpart. If we do not understand cancer, we cannot control, conquer, and eliminate it. The completion of the human genome sequence and its subsequent improvements in the sequence data are important steps to fully comprehend cancer cell biology. Nanotechnology, a new, novel focus of research evolved from the convergence and coalescence of many diverse scientific disciplines and as a general term for the creation, manipulation, and application of structures in the nanometer size range. In this article, nanomedicine aspects of nanotechnology will be stressed and will cover areas such as drug delivery systems and new drug therapies as they relate to cancer. One of the ultimate goals of nanomedicine is to create medically useful nanodevices that can function inside the body. It is envisioned that nanodevices will be hybrids of biologic molecules and synthetic polymers that can enter cells and the organelles to interact directly with DNA and proteins. Additionally, nanomedicine will have an impact on the key challenges in cancer therapy: localized drug delivery and specific targeting. Among the newly developed nanomedicine and nanodevices such as quantum dots, nanowires, nanotubes, nanocantilevers, and nanopores, nanoshells and nanoparticles are the most promising applications for various cancer treatments.

Animals↗

Development and validation of an HPLC-UV method for the determination of gatifloxacin in bulk material, pharmaceutical formulations, human plasma and metal complexes.

A simple reversed phase HPLC method was developed for the quantitative determination of gatifloxacin (GTX) in the bulk material, pharmaceutical formulations and human serum using Mediterranea C18 (25 x 0.46 mm, 5 mm) column. The mobile phase, acetonitrile, methanol and water (40:40:20 v/v pH 2.7 adjusted by phosphoric acid), was delivered at a flow rate of 1.0 ml/min. The eluent was monitored using spectrophotometric detection at 286 nm. The method is specific to GTX and able to resolve the drug peak from formulation excipients and metal impurities. The method is accurate (99.18-101.87%), precise (intra-day variation 0.14-1.67% and inter-day variation 0.32-1.80%) and linear within the range 0.1-25 microg/ml (R2=0.999) concentration and was successfully used in monitoring left over drug in drug-metal complexes. The detection limit of GTX at a signal-to-noise ratio of 3 was 1.73 ng/ml in human plasma while quantification limit in human serum was 5.77 ng/ml. The proposed method is applicable to routine analysis of GTX in pharmaceutical formulations as well as in human plasma samples.

Chemistry, Pharmaceutical↗

Spectrophotometric method for quantitative determination of iron (III) from iron polymaltose complex in pharmaceutical formulations.

A visible spectrophotometric method has been developed for the quantification of iron (III) from iron polymaltose complex in pure and in pharmaceutical preparations. The method is based on hydrolysis of iron polymaltose complex under acidic conditions and the formation of red colored chromogen with ammonium thiocyanate, which showed absorption peak at 471 nm. This absorption wavelength can be used for the determination of iron (III) from iron polymaltose complex. The limit of detection of iron polymaltose complex at 476 nm was 6.207 ng mL(-1). The calibration was linear in the range of 19.8-22.2 microg mL(-1). Analytical parameters such as stability, selectivity, accuracy and precision have been established for the method in HAEMOTYL syrup and evaluated statistically to assess the application of the method. The method was validated under the ICH and USP guidelines and found to comprise the advantages for simplicity, stability, sensitivity, reproducibility and accuracy for using as a method for the routine analysis of the drug in pharmaceutical formulations and in pharmaceutical investigations involving iron polymaltose complex.

Chemistry, Pharmaceutical↗

Interaction studies of omeprazole with mefloquine, pyrimethamine and sulfadoxine.

Mefloquine hydrochloride, pyrimethamine and sulfadoxine as readily tolerated antimalarial drugs that are highly active against both usual and multidrug resistant strains of Plasmodium falciparum. Omeprazole reduce gastric acid secretion, irreversibly by inhibition of H+-K+ ATPase of the apical membrane of the parietal cell. In order to study the drug interactions of the later with antimalarials, in vitro availability of omeprazole has been studied in presence of mefloquine hydrochloride, pyrimethamine and sulfadoxine. The availability of antimalarial drugs was found to be influenced considerably in presence of omeprazole. The effect of dissolution mediums, simulating various body environments with respect to pH and the influence of temperature on these interactions has been examined in order to elucidate the mechanism of these interactions.

Antimalarials↗

Quantitation of buclizine hydrochloride in pharmaceutical formulations and human serum by RP-HPLC.

An isocratic reversed phase high-performance liquid chromatographic (HPLC) method with ultraviolet detection at 230 nm has been developed for the determination of buclizine hydrochloride in human serum and dosage formulation. Methylparaben was successfully used as an internal standard. Good chromatographic separation between buclizine and internal standard peaks was achieved by using a stainless steel analytical column Nucleosil, C18 (10 microm, 25 cm x 0.46 cm). The system was operated at room temperature using a mobile phase consisting of acetonitrile-water (1:1) (pH 2.6) with phosphoric acid 85% at a flow rate of 2 ml/min. The calibration curve for buclizine hydrochloride in human serum was linear over the tested concentration range of 10, 3, 1.5, 0.5, 0.15, 0.05, and 0.025 microg/ml with a correlation coefficient of 0.9999. The intra- and inter-run precision and accuracy results were 98.07 to 100.34. The proposed method was validated for selectivity, linearity, accuracy, and precision. The method was found to be suitable for the quality control of buclizine hydrochloride in bulk drug as well as in human serum.

Chemistry, Pharmaceutical↗

Interactions between ciprofloxacin and antacids--dissolution and adsorption studies.

Ciprofloxacin is a fluorinated quinolone antibacterial agent extensively used against both Gram-positive and Gram-negative microorganisms. In certain polytherapy programs, ciprofloxacin can be administered with some antacids that could modify its dissolution rate and reduce its absorption leading to therapeutic failure. The aim of this study was to evaluate the influence of some antacids on the availability of ciprofloxacin. The release of ciprofloxacin from tablets in the presence of antacids, such as sodium bicarbonate, calcium hydroxide, calcium carbonate, aluminum hydroxide, magnesium hydroxide, magnesium carbonate, magnesium trisilicate and magaldrate was studied on BP 2002 dissolution test apparatus. These studies were carried out in simulated gastric and intestinal juices for 3 hours at 37 degrees C. The results confirmed that the dissolution rate of tablets was markedly retarded in the presence of all the antacids studied. Magaldrate and calcium carbonate in simulated gastric juice exhibited relatively higher adsorption capacities, as did magnesium trisilicate and calcium hydroxide in simulated intestinal juice.

Adsorption↗

Determination and quantification of cetirizine HCl in dosage formulations by RP-HPLC.

A simple, sensitive, reliable and rapid HPLC method for the determination of cetirizine hydrochloride using hyoscine butyl bromide as an internal standard has been developed. The chromatographic system consisted of Shimadzu LC-10 AT VP pump, SPD-10 AV VP with UV/visible detector and a CBM-102 Bus Module integrator. Separation was achieved on the U Bondapak 125 A C18 10 microm column at room temperature. The samples were introduced through an injector valve with a 10 microl sample loop. Acetonitrile-water (1:1 v/v) was used as mobile phase, with flow rate 2 ml/minute. pH was adjusted to 2.9 with phosphoric acid. UV detection was performed at 205 nm. The results obtained showed a good agreement with the declared content. Recovery values for cetirizine hydrochloride were 99.19-100.82%. The proposed method is reliable rapid, precise, selective and may be used for the quantitative analysis of cetirizine HCl, in presence of hyoscine butyl bromide as internal standard. The method was valid was for the determination in raw materials, bulk drug and formulations. The limit of quantification was 5-30 nano grams, while the limit of detection was 0.4 nano grams.

Cetirizine↗