Determination of drug,excipients and coating distribution in pharmaceutical tablets using NIR-CI

The growing interest of the pharmaceutical industry in Near Infrared-Chemical Imaging (NIR-CI) is a result of its high usefulness for quality control analyses of drugs throughout their production process (particularly of its non-destructive nature and expeditious data acquisition).In this work,the concentration and distribution of the major and minor components of pharmaceutical tablets are determined and the spatial distribution from the internal and external sides has been obtained.In addition,the same NIR-CI allowed the coating thickness and its surface distribution to be quantified.Images were processed to extract the target data and calibration models constructed using the Partial Least Squares (PLS) algorithms.The concentrations of Active Pharmaceutical Ingredient (API) and excipients obtained for uncoated cores were essentially identical to the nominal values of the pharmaceutical formulation.But the predictive ability of the calibration models applied to the coated tablets decreased as the coating thickness increased.

Formulation Development, in Vitro Evaluation and Stability Study of Aceclofenac Tablet

The objective of the study was to develop film coated tablets of aceclofenac using wet granulation technique. Possible drug-excipient interaction was evaluated by HPLC （high performance liquid chromatography） and FTIR （fourier infrared spectroscopy）. The tablets prepared were assessed for their physicochemical, in vitro dissolution at pH 1.2, 4.5, 6.8 and 7.5 and stability characteristics. Comparison with a commercial aceclofenac product was made in vitro and in vitro studies. There was no interaction between aceclofenac and used excipients. Furthermore, the physicochemical properties of the tablets were satisfactory. The dissolution profile of one of the formulated aceclofenac tablets （D07） was statistically similar （p 〈 0.05） to that of the commercial aceclofenac brand in all the dissolution media. The formulated products ware stable and showed no changes in physical appearance, drug content, or dissolution pattern after storage at 40 ℃/75% RH for 6 months. The results indicate that it is feasible to achieve a stable aceclofenac tablet formulation by using wet granulation technique.

Konjac glucomannan and xanthan gum as compression coat for colonic drug delivery:experimental and theoretical evaluations

Compression coated tablets for oral colon specific delivery systems were developed with a mixture polysaccharide of konjac glucomannan(KGM)and xanthan gum(XG)as the compression coat.Diffusion of cimetidine from compression coated tablets was investigated by release experiment in Vitro.0.22U/mLβ-mannanase was applied in the mimic colon solution.The structure of the mixture polysaccharide was studied by an atomic force microscope(AFM).The experimental results indicate that a KGM70 tablet with a 0.4 g coat is of good design,due to a less than 5%drug loss in the mimic upper gastrointestinal solution by the synergistic interaction between XG and KGM,and due to about 50%cumulative release in the mimic colon solution by degradation after 24 hours.The release mechanism and model are discussed based on different periods of drug release including the delay of the drug,the constant release without an enzyme and the delay of degradation.Under hydrolysis byβ-mannanase,drug release from the tablet with KGM coat shows an exponential increase,while that from the dosage with the mixture polysaccharide coat is an approximately zero-order process in which the constant release rate relates to the release velocity of a non-degraded system,the content of KGM within the coat and the average molecular weight ratio of KGM to XG.It was found that XG was the framework of the polysaccharide mixtures by AFM,which is similar to the analysis results from experiments on drug release.