Flurbiprofen (FLB), a NSAID, widely used for preventing pain generally for arthritis or dental problems. In this study, FLB loaded chitosan microspheres were prepared by ionotropic gelation method. In this method, microspheres were formed by dropping chitosan solutions containing FLB into sodium alginate solutions including sodium tripolyphosphate (TPP). A variety of formulation parameters like drug:polymer ratio, drug concentration, polymer's molecular weight, polymer concentration, pH and the concentration of TPP solutions, drying method and stirring time were analyzed. The dissolution studies were performed in a shaking water bath in pH 7.4 phosphate buffer saline (PBS) at 37 °C. Laser diffractometer was used for particle size analysis, and scanning electron microscope (SEM) was used for morphological properties. Drug loading and loading efficiency were calculated by using UV spectrophotometer. The particles obtained were spherical with 0.7-1.3 mm size range, and the loading efficiency was approximately 21-79%. The dissolution studies conducted revealed that drug:polimer ratio and the polymer type and concentration affected the drug release from microspheres. It was observed that increasing the polymer concentration, polymer's molecular weight and TPP concentration decreased the FLB release from microspheres, which was according to Higuchi kinetics.
Dissolution testing has a very vital importance for a quality control test and prediction of the in vivo behavior of the oral dosage formulation. This requires the use of a powerful analytical method to get reliable, accurate and precise results for the dissolution experiments. In this context, new signal processing approaches, continuous wavelet transforms (CWTs) were improved for the simultaneous quantitative estimation and dissolution testing of lamivudine (LAM) and zidovudine (ZID) in a tablet dosage form. The CWT approaches are based on the application of the continuous wavelet functions to the absorption spectra-data vectors of LAM and ZID in the wavelet domain. After applying many wavelet functions, the families consisting of Mexican hat wavelet with the scaling factor a 256, Symlets wavelet with the scaling factor a 512 and the order of 5 and Daubechies wavelet at the scale factor a 450 and the order of 10 were found to be suitable for the quantitative determination of the mentioned drugs. These wavelet applications were named as mexh-CWT, sym5-CWT and db10-CWT methods. Calibration graphs for LAM and ZID in the working range of 2.0-50.0 µg/mL and 2.0-60.0 µg/mL were obtained measuring the mexh-CWT, sym5-CWT and db10-CWT amplitudes at the wavelength points corresponding to zero crossing points. The validity and applicability of the improved mexh-CWT, sym5-CWT and db10-CWT approaches was carried out by the analysis of the synthetic mixtures containing the analyzed drugs. Simultaneous determination of LAM and ZID in tablets was accomplished by the proposed CWT methods and their dissolution profiles were graphically explored. Key words continuous wavelet transform; determination; dissolution testing; anti-human immunodeficiency virus (HIV) drug; tabletLamivudine (LAM), chemically named (2R,cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one or (−)-2′,3′-dideoxy, 3′-thiacytidine (3TC) is the (−)-enantiomer of a dideoxy analogue of cytidine. LAM has been used for the treatment of infections with the human immunodeficiency viruses (HIVs) and chronic hepatitis B viruses. LAM is phosphorylated to its active 5′-triphosphate metabolite (LAM triphosphate). The principal mode of action of LAM triphosphate is inhibition of reverse transcriptase via DNA chain termination after incorporation of the nucleoside analogue. LAM triphosphate is a weak inhibitor of mammalian DNA polymerases-α, -β and mitochondrial DNA polymerase-γ LAM is often given in combination whit zidovudine (ZID) in order to provide desirable therapy. ZID or azidothymidine (AZT) has been used for the treatment of HIV/AIDS infectiousness. Its chemical name is 3′-azido-3′-deoxythymidine. ZID is phosphorylated to its active 5′-triphosphate metabolite (ZID triphosphate). ZID triphosphate is inhibition of reverse transcriptase via DNA chain termination after incorporation of the nucleoside analogue. ZID triphosphate is a weak inhibitor of the mammalian DNA polymerase-α and mitochondrial DNA polymerase-γ and has been reported to be incorp...
Classical and chemometric calibration strategies based‐Ultra Performance Liquid Chromatography‐Photodiode Array (UPLC‐PDA) measurements were improved to monitor the in‐vitro dissolution profiles of lamivudine (LAM) and zidovudine (ZID) in tablets and to quantify drugs. To generate UPLC‐PDA data, UPLC analysis was done using the mobile phase containing acetonitrile‐acetate buffer pH 5.0 (18 : 82, v/v). In the classical strategy, calibration curves were obtained by using the peak area ratios detected at 274 nm for LAM and 268 nm for ZID, respectively. Principal component regression (PCR) and partial least squares (PLS) strategies were used to solve the same problem using UPLC‐PDA measurements obtained at eight different wavelengths. Both classical and chemometric approaches were successfully applied for drugs assay and in‐vitro dissolution testing. Assay results showed that the proposed chemometric tools gave better results because they helped to minimize the effect of chromatographic issues that commonly occur with the classical UPLC approach, such as the higher standard deviation of the assay results.
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