| Oxymatrine(OMT) has antiarrhythmic action, it can significantly improve cardiac diastolic excitation threshold,it could markedly prolong the effective refractory period (ERP) of actionpotential. But it eliminate fast in human body, and well absorbed in the intestinum tenue. Arrhythmia is not easy to check and sudden death can be a serious threat to human life. The arrhythmia mainly happens in the nights and mornings. There are some limitations in the treatment of common preparations. Therefore, in this paper, oxymatrine was used as pharmaceutical raw materials, According to the principle of chronopharmacology, this paper designs the pulsed drug delivery system of the Oxymatrine.In this paper, the prescription and technology of pulse patch was determined by single factor test and orthogonal experiment. In order to make the patients in the incidence of the highest time to reach therapeutic serum concentrations, this experiment through the coating technology and fast Sakya intestinal adhesion sustained-release tablets core of the preparations. And it can effectively avoid the oxidation of matrine and gastric acid reaction, increase intestinal absorption, bioavailability and reduce the frequency of administration, reduce side effects.The best prescription process of this subject is as following:First of all, mix equal amounts of 10% of OMT,30% PVPP,36% starch and 24% dextrin by incremental approach,80% ethanol as a wetting agent, wet granulation, adding an appropriate amount of magnesium stearate after granulated and then tableting with the pressure of 7N, weighing 135mg/tablet. Second of all, mix 4.25% stearyl alcohol,24.75% carbomer and 1% magnesium stearatea ccording to the method of increasing the same amount, after that the powder can be obtained. Place the pre-prepared immediate release tablet core into the tableting machine and press the 400mg powder into undershoot and then obtain core tablets weighing 535mg/tablets.The ratio of acrylic resin and ethyl cellulose is 65:35, and the ratio of PEG 6000 is 15%, coating weight increased 6%. Adding acrylic resin into an appropriate amount of 95% ethanol solution while stiring. After the solution was completely dissolved, ethyl cellulose and PEG6000 should be added by prescription while stirring. Continue stirring the solution for 3 hours after dissolution, then obtain a coating solution. Put the core into the high efficient coating pan which the speed should regulator, and set coatings pot temperature of 40 ℃, when the tablet healed up to the temperature of 40 ℃, pulping and coating procedure should be started, while adjusting the coating pan speed to 18 Hz, until the end of the coating produre. After coating, the tablets were hot hatched for another 20mins. The prescription process reproduced the good type, and the delay time is 4h, which reaching the experimental design requirements.The prescription has good reproducibility, in order to achieve the desired effect of the experimental program, applying the coating technology, the preparation can reach the delayed-release effect. Through the rapid release tablet core to make the drug at the highest incidence of time to achieve the ideal blood drug concentration. Blood concentration was maintained by intestinal adhesive tablets core, reducing the dosage of the patient, so as to reduce the side effects of drugs. It laid the foundation for the development and the usage of OMT and pulse sheets. Later, it is necessary to improve the pharmacokinetics of this agent in vivo in order to achieve the purpose of improving the formulation. |
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