Pns Sustained-release Tablets Preparation And In Vivo And Vitro Release Study

Cardiovascular disease is a serious threat to human health, with the characteristics of a high incidence of morbidity, high rate of recurrence, and high mortality. Panax notoginseng, traditional Chinese medicine, plays the role of selective expansion in different parts of the vascular and reducing diastolic in blood pressure lowering,which is obvious, as well as blood stasis, anti-thrombotic, anti-platelet aggregation and other effects. Panax notoginseng saponins, extracted from Panax notoginseng has a wide range of specific pharmacological activity on cardiovascular and cerebrovascular-disease. At present, there are Xuesaitong piece, Xuesaitong injectionfluid, blood clots injection, piece of Panax notoginseng saponins capsule and so on acting as a clinical pharmaceutical preparations for the treatment of cardiovascular and cerebrovascular diseases. The use of these agents has certain requirements, such as multiple times of oral dosage a day, poor patient compliance, incomplete absorbtion of oral medications, low bioavailability, high cost of injection, inconvenience of operating. There are also some adverse reactions. For Convenient clinical application of PNS, we often improve bioavailability by changing the formulation to promote absorption, increase patient medication compliance and reduce the plasma concentration fluctuations after taking the drug, so the design of a daily dose of Panax notoginseng saponins sustained release preparation is necessary. This paper combines the needs of clinical medicine and disease characteristics and use the technology of the modern pharmaceutical preparations and methods to prepare the Panax notoginseng saponins sustained release tablets according to the guiding principle of the traditional Chinese medicine theory and basis of modern pharmacy dosage form.Gel sustained release tablets prepared in this study, Panax notoginseng saponins on framework can improve the in vivo drug absorption, and effectively improve the bioavailability of the preparations. It selects Target Components of Panax notoginseng saponins ginsenoside Rgl, establish HPLC, research the release and quality of sustained release tablets and the in vivo pharmacokinetic studies. The preparation process and in vitro release characteristics research of Panax notoginseng saponins sustained release tablets in this article is of great significance on the prevention and treatment of cardiovascular and cerebrovascular diseases, and provides some basis for cardiovascular disease drugs and their preparations.1Preparation process researchThe Preparation of Panax notoginseng saponins sustained-release formulations is based on the guiding principles of sustained-release formulations of the Chinese Pharmacopoeia. To a certain extent, it is a little difficult to research the drug release due to the in vivo gastric environment factors’effect on floating sustained release formulations; The sustained-release pellets are affected by Chinese medicines’complex components, which results in the different release behavior of the active ingredients; Because of the simple process of the preparation of Sustained Release Matrix Tablets and good uniformity uniformity, we choose to prepare Panax notoginseng saponins Sustained Release Matrix Tablets. we had single factor test according to the evaluation of Ginsenoside Rgl in vitro release rate, investigated the larger accessories factors which shows the impact on the in vitro release and screen the prescription; Tests showed that the release rate of Panax notoginseng saponins sustained-release tablets slowed down with the increase of the reinforcing material in the prescription of HPMC. the smaller the viscosity is, the sooner the release is; When we add the EC and other water-insoluble materials into the reinforcing material, the release rate slowed down with the increase of water-insoluble materials and the effect of blocking and release is obvious; We add water-soluble excipient lactose and accompanied them with the wet-sensitive drugs. We found that the drug diffusion resistance decreases and drug release speeds up. So they are not suitable for skeleton filling material of Panax notoginseng saponins sustained release tablets. Wetting agents and lubricants haven’t shown great effect on the release of sustained-release tablets. Preparation and the tabletting pressure conditions also show little effect on the release of the sustained release tablets.On the basis of Single factor, we used L9(34) orthogonal experimental design to optimize the prescription form and evaluate the optimal formulation and process reproducibility and drug release homogeneity, we finally decided to use Panax notoginseng saponins sustained release tablets with the amount of HPMC (K15M) of30%for the skeleton material, the amount of MCC15%, tablet weight of300mg and developed with the Pregelatinized starch of the amount of5%.The Formulation and process reproducibility and drug release are good.2In vitro release researchWe study in vitro determination of the establishment of Panax notoginseng saponins sustained release tablets according to the evaluation in vitro release rate of ginsenoside Rgl, determine the reliability in vitro analysis method and measure ginsenoside Rgl content. we investigated the influencing factors of in vitro release, including the release of the media and the pH value, temperature, volume size, test dissolution device and the speed. we fitted the in vitro release curves of Panax notoginseng saponins sustained release tablets, and use The release profile Higuchi equation, we found that the release way is non-Fick’s diffusion, which belongs to the diffusion of the drug and skeleton dissolution synergy. According to the research of Panax notoginseng saponins sustained release tablets in vitro release of the amount-the time-pH3D release characteristics, Sustained release tablets can release well in the entire gastrointestinal tract pH range, which meet the designed satisfaction.we determine the in vitro release parameters and the release of the sampling point. In the comparison between the homemade sustained release tablets and commercially available conventional tablets, we found that Sustained release tablets in vitro sustained release, with no burst release phenomenon.3In vivo release studyIn vitro release rate determination results may not fully reflect the situation of agents in the body of the release, This chapter preliminarily study pharmacokinetics domesticated rabbits and release characteristics of Panax notoginseng saponins sustained release tablets, with the study method of Classic pharmacokinetic blood concentration method to establish Plasma concentration of Panax notoginseng saponins sustained release tablets and do the methodology research, which achieved the technical requirements of in vivo drug analysis.We did pharmacokinetic study of oral administration domesticated rabbits and in vitro evaluation with homemade Panax notoginseng saponins sustained release tablets, we used the self-control experimental design method to fit Plasma concentration and Pharmacokinetic parameters after Oral administration of domesticated rabbits, the result showed that the absorbtion of Ginsenoside Rgl in domesticated rabbits conforms two-bedroom model, compared with Conventional tablets, the amount of Cmax in the Panax notoginseng saponins sustained release tablets decreased and fmax extended, which showed obvious release effect. we also used the Loo-Riegelman method to do correlation between in vivo evaluation and found that the Sustained release tablets in vivo correlation is more significant, which showed that the preparation of Panax notoginseng saponins sustained release tablets and the release characteristics in vitro and in vivo research methods are scientifically reasonable and guaranteed the control Quality.