Coprocessed Excipients Prepared By The Spray Drying Technology For Direct Compression And Its Quality Evaluation

Tablet is one of the most used preparations in clinical and daily life for accurate, simple technology and convenient use, low cost, easy to transport and stability. Accessories are an important part of the tablet. The auxiliary materials directly affect the quality of the tablet. Powder production technology of direct pressure is the most potential process in preparation because of its economic advantage. Because of high demands of excipients, so excipient is one of the most factors to restrict the development of powder direct compression. Most of the single accessories can not meet the basic requirements of direct compression. Coprocessed excipient arises at the historic moment.This paper aims to prepare a coprocessed excipient for direct compression. This paper first according to tablet commonly used complementary makings, preliminarily choose appropriate single materials which can be part of the coprocessed excipient: Tablettose, PVPP and MCC. And then choose spray drying technology as the choice in the preparation method of coprocessed excipient from four technology which is spray drying, fluidized bed drying, freeze drying and common crystallization.Study the preparation process parameters of spray drying for the optimization process parameters:solid solution content is15%, and into the wind temperature setting for190℃, and into the sample weight20mL/min, the rotating speed is set at200r/min, and the outlet temperature of60℃. Under this process parameters, suspension of the compound material can be jet smoothly, less water content, roundness of the loose, best spherical degrees after the hot air drying, and also little vulnerable to serious phenomenon of adhering wall. Under this process parameters, the end certain prescription ingredients are disintegrating agent for PVPP, filling agent for MCC and Tablettose, adhesives for PVP. Finally determined prescription is:PVPP:Tablettose: MCC:PVP=3:10:6:1.The investigation of coprocessed excipient:TGA-DSC test can be seen in the coprocessed excipient of the DSC curve obvious physical mixture and all kinds of accessories than to quietly, and almost no obvious peaks. Suggest that coprocessed excipient is more stability than a single materials and its physical mixture. From XRD map can be found in Tablettose, a shift from crystallization for amorphous state, and other accessories no change. Have reports in the literature, amorphous lactose to the medication better adhesion effect. Coprocessed excipient has a wide distribution of particle size, not easy to appear stratified phenomenon. According to the rest of the determination, Kashia Angle index, chuanbei equation, coprocessed excipient liquidity and can be pressed significantly better than its physical mixture. According to the experiment the coprocessed excipient has low lubrication sensitivity. Determination of the coprocessed excipient critical relative humidity was56%.Direct compress coprocessed excipient for blank tablet and take the quality evaluation. Appearance is bright and clean and white tablet, the influence of mixed time is very small to heavy differences, friability and crumbling time of tablets. Hardness of blank tablets also had little effect on friability and disintegrating time. Coprocessed excipient batchs have little difference, it results that the preparation technology was stable.Because Breviscapine has poor liquidity, and more than40℃temperature it will lead to lower its content, so it can not make wet granules, so choose Breviscapine as the main medicine and for direct compression, including medicine tablet for quality inspection. The mixed time of Drugs and coprocessed excipient on the drug content uniformity have influence. Drug content on the hardness, tablets friability, disintegration time limit has the influence of different level, according to experiment choose the best preparation technology of Breviscapine, and carries on the drug dissolution of the determination of the homemade Breviscapine and the Breviscapine of the sold,it result that the homemade Breviscapine has better dissolution degrees under the same time. In addition, this paper study the preliminary Breviscapine stability through the influence factor experiment (light, temperature, humidity).On the condition of the bright light, it is stability. On the condition of high humidity conditions, there is no change in40℃but a little content change in60℃,and a little weight increment under the high humidity conditions. For the time being, accelerate test and the long-term test are in progress. This paper successfully developed the coprocessed excipient which can be used to direct compression, and used in the preparation of the Breviscapine. At home, though there are also a few enterprises which are developing new accessories, but the research of the coprocessed excipient is blank. This article lays a foundation for the domestic pharmaceutical raw materials and medicinal compound materials development, also be helpful for promoting direct compression in the development of our country, the research result of this paper has useful value and cortical significance for the practical application.