Study On The Dissolution Characteristics And Impurity Spectra

Dissolution means that under certain conditions, the provisions of the medium,the drug from solid dosage forms like tablets or capsules dissolution rate and extent [1].Dissolution testing of drugs is not only an important indicator of quality of preparation of solid control, it is an effective means of drug release and absorption latent in vivo evaluation[2]. The active ingredient in an oral formulation within the gastrointestinal tract after release before the dissolution transmembrane transport, to reach the body or the target site, the content, if not better qualified drug release in the body, they can not achieve the desired therapeutic effect, therefore, need to ensure that the drug The bioavailability. By simple dissolution test in vitro, in vivo dissolution formulations reflect the situation, so as to achieve the preparation of quality control to ensure that the purpose of its bioavailability.In the process of manufacture and storage of drugs, often it will be some impurities introduced to drugs, thus affecting the purity of the drug. Any material affect the purity of drugs are called impurities [3]. Impurity profile[4] it is unknown to all known impurities and total impurities present in the drug product description.Impurities in drugs control concept of change, divided into three stages: purity control,limit control and impurity profile control[5]. By studying the impurity profile of the drug, to determine the ownership of its impurities and structure information, in order to avoid or reduce the generation of the impurities and control within safe limits for each impurity, thereby improving the quality of medicines.In this paper, dissolution characteristics and impurity profile trepibutone sheet were studied, the main work are:First, a review of the relevant literature, their methods were investigated to optimize the determination, the establishment of a HPLC chromatographic conditions and determination. As justification methods were linear range, recovery, stability,precision and so on method validation. Japan’s Orange Book with reference to therecommended four kinds of dissolution media and national existing standards were contained in dissolution media of different domestic and foreign manufacturers produce trepibutone slices in vitro dissolution test to measure the dissolution curve,and its dissolution profile factors were studied, with f2 determine their similarity factor calculation. The results showed that domestic formulations and reference that in the preparation of inconsistencies; dissolution behavior of domestic agents between different manufacturers are not similar, within the same batch dissolution behavior between similar plants. Different dissolution media affect its dissolution tablets large,integrated results for each condition, final dissolution method chosen for: paddle method rotating at 75 rev / min, 0.2% SDS 900 ml of dissolution medium, 45 minutes sampling limits of the labeled amount of 70%.Second, the chromatographic conditions trepibutone sheet related substances are selected to establish the concentration of the sample solution and the detection wavelength, and verify the specificity of its methods, durability, detection limits and repeatability. Use good test method that determines samples tested at home and abroad, domestic and international comparative analysis of impurities in the preparation, formulation and domestic accelerated test inspection. Raw materials and preparations by forced degradation tests, combined with synthetic technology,prescription tablet composition and impurities in raw materials test results, identify and vested its impurities. Using LC-MS samples were analyzed using inferred structure impurities. Analysis trepibutone raw mass spectrometry fragmentation patterns with positive ion mode. The results showed that: HPLC method for the determination trepibutone film has five main impurity, in addition to the relative retention time of 2 times the impurity of degradation impurities, the remaining four impurities as raw materials into synthetic impurities, five impurities are trapidil Bouton change the chemical structure of benzoyl branched chain generated; tablets compared with other countries, the number of cloth through the film trapidil impurity domestic enterprises produce more, but to a lesser impurities, both total miscellaneous more than 0.5%; trepibutone accelerated test piece produced by impurity less. Under related substances, and control the proposed new monohetero not more than 0.2% ofthe total hybrid should not exceed 0.5%.Comparative study paper analyzes the domestic formulation and reference formulation dissolution profile for generic drugs to provide a basis to evaluate the agreement. Analysis of the current quality controllable dissolution method, provided the basis for the rational development of trepibutone tablets dissolution methods.Establish trepibutone and related substances tablet inspection methods, to systematically study the impurity profile of impurities determine the basic structure of the home and provide a theoretical basis for the control of impurities varieties.