Formulation and Characterization of Ciprofloxacin loaded PLGA Microspheres for Applications in Orthopedic Infections.

Purpose-Osteomyelitis is a bone infection that appears as a complication after a fracture or orthopedic surgery. Ciprofloxacin is a broad spectrum antibiotic that can be used in local drug delivery systems for the treatment of bone related infections due to its bactericidal activity against both Gram-negative and Gram-positive bacteria. The purpose of the present study was to include ciprofloxacin in poly (lactic-co-glycolic acid) (PLGA) microspheres. Material and methods-Microspheres were prepared by both water/oil/water (w/o/w) solvent evaporation method and solid/oil/water (s/o/w) dispersion solvent evaporation method. The obtained microspheres were characterized by Fourier Transform Infrared Spectroscopy. High performance liquid chromatography method was deployed to determine the encapsulation ratio. Results-The solvent evaporation method chosen for this experiment resulted in microspheres with good entrapment efficiency. Furthermore the microspheres obtained by the s/o/w method displayed better entrapment efficiency. Conclusion-The particles obtained through the s/o/w technique should be further investigated in order to develop a local drug delivery system.

Plant Growth Regulating Activity of Some N-Substituted Chloroacetylanilines.

PURPOSE: The synthesis and physico-chemical characterization of six N-substituted chloroacetylanilines and testing their plant growth regulating activity. MATERIAL/METHODS: The synthesis of the six N-substituted chloroacetylanilines was accomplished by condensation of N-substituted anilines, in an acidic medium, with chloroacetylchloride. Purified compounds obtained were physico-chemical characterized by elemental analysis and spectral analysis. Five different concentrations (0.1%, 0.5%, 0.75%, 1% and 5%) of the compounds solubilized in chloroform were used to analzyed their effects on the germination and mainly on the radicular elongation of wheat caryopses, Triticum aestivum subsp. aestivum (Poaceae), Dropia variety. RESULTS: The N-substituted chloroacetylanilines were solid, differently colored, with high melting temperatures and high yields. Their structure was confirmed both by elemental analysis and by the spectral methods (UV-Vis, FTIR, 1H-NMR, 13C-NMR, GC-MS). CONCLUSIONS: For the six analyzed compounds, at five different concentrations (0.1%, 0.5%, 0.75%, 1% and 5%), the experimental data obtained by the method of linear measurement, in the Triticum assay, showed the inhibition of mean radicular elongation compared with the reference.

Simultaneous Analysis of Clopidogrel Bisulfate, Acetylsalicylic Acid and Atorvastatin calcium in Tablets by HPLC Method.

The concept of multidrug therapy with clopidogrel, acetylsalicylic acid and atorvastatin provides major advances for patients with acute coronary syndromes (ACS) treated invasively and conservatively to reduce the risk of ischemic events and improve survival. Dual antiplatelet therapy (DAPT) with acetylsalicylic acid and clopidogrel is currently the treatment of choice in acute coronary syndromes and prevention of thrombosis after coronary stent implementation. Present paper presents a simple, rapid and precise reversed phase high performance liquid chromatographic method for simultaneous estimation of clopidogrel hydrogen sulfate, acetylsalicylic acid and atorvastatin calcium from tablet dosage form. The cromatographic analysis was carried out using a ThermoFinnigan Chromatograph with UV detection and separation on an HDS Hypersil C18 column. The elution was isocratic with mobile phase consisting in mixture of 0.01M KH2PO4 buffer: acetonitrile: methanol. Chemicals were represented by clopidogrel bisulfat, atorvastatin calcium and acetylsalicylic acid standards with high purity. The quality control samples used in the accuracy and precision evaluation were spiked at low, medium and high concentration levels. Preliminary tests were performed to select optimum conditions for simultaneous separation of all three analytes such as mobile phase composition, proportion and pH. A satisfactory separation of all three drugs was achieved with a mobile phase of 0.01 M KH2PO4 buffer (pH adjusted to 2.6 with phosphoric acid):acetonitrile:methanol 20:40:40 v/v/v at flow rate of 0.8 ml/min. The proposed method was validated for linearity, precision and accuracy. The validated method can be successfully applied for simultaneous quantification of clopidogrel, acetylsalycilic acid and atorvastatin either in combination or in single dosage form in quality control analysis. The analytical conditions can also be performed for human plasma analysis.

Formulation and In Vitro Evaluation of Alendronate Sodium/PLGA Microspheres for Applications in Bone Related Disorders.

Purpose - Bisphosphonates are a group of drugs that can be used in the development of new therapies for bone disorders. Microencapsulation by solvent evaporation is a method that results in microspheres with controlled release of the drug. The purpose of the present study was to include sodium alendronate (AL) in poly (lactic-co-glycolic acid) (PLGA) microspheres with a good encapsulation rate. Furthermore it was intended to obtain a prolonged release of the drug over a period of time. Material and methods - Microspheres were prepared by water/oil/water solvent evaporation method. The microspheres were characterized by FTIR analysis using an Avatar Nicolet spectrophotometer. Both encapsulation ratio and in vitro drug release were assessed by chromatographic analysis. Results - The method chosen for sodium alendronate incorporation resulted in microspheres with a good entrapment efficiency. The in vitro drug release from PLGA/AL microspheres was maintained up to 21 days. This suggests that the microspheres had a sustained releasing tendency. Conclusion - Given the prolonged release, PLGA/AL microspheres may be used in a controlled release system with applications in bone disease treatment.

Determination of some local anesthetics in human serum by gas chromatography with solid-phase extraction.

A method of analysis based on solid-phase extraction coupled with capillary gas chromatographic system for determination of mepivacaine, bupivacaine and lidocaine from human serum was developed. As extraction sorbents were used Chromosorb 103, Tenax-GC and Chromosorb T. The best extraction sorbent proved to be Chromosorb 103. Their recoveries ranged from 91 to 94% at the target concentrations of approx. 1.5 microgml(-1) in serum. Relative standard deviation of the recoveries ranged from 3.11 to 5.30 at these concentrations. As internal standard was used lidocaine. The chromatographic analysis was performed on a gas chromatograph equipped with a capillary column, HP-Innowax, and flame ionisation detector. Samples were injected in splitless mode. This method was applied in a stomatological clinic to healthy volunteers to whom superior-posterior alveolar nerve block anesthesia with mepivacaine was administered.