Formulation Optimization Of Sustained-Release Pellets Prepared By Centrifugal Technology

The sustained-release pellets research in the field is an important direction of development in recent years, the field of pharmaceutical preparations prepared by centrifugal sustained-release pellets, especially prepared skeleton pills, not systematic and in-depth. This paper aims to develop a centrifugal granulator capacity in the preparation of sustained release pellets, first prepared by centrifugal model drug acetaminophen membrane control and skeleton-type sustained-release pellets, as guidance for the preparation of a water-soluble model drug metformin skeleton sustained release pill hydrochloride sustained-release pellets insoluble model drug Gliclazide membrane control, and prescription and comprehensive process optimization and filtering, the experimental results prove that prepared by centrifugal the membrane control pills and skeleton pill is feasible and controlled process.Moderate solubility of the drug is selected as a model drug acetaminophen, sustained-release pellets prepared by centrifugal comprehensive investigation, preparation Pelleted:First using the powder lamination prepared containing pills core, by the proportion of powder prescription and single factor on the drug process to determine the best on drug prescriptions and process:model drug powder, MCC, lactose50:25:25,2%HPMC as binder for powder speed of25rpm, shotcrete speed20rpm, and the lance height is10cm, the size of the blast volume of10-15Hz. Containing pills core then the coating operation, through the screening of the coating formulation and process, it is determined that the optimal formulation conditions were as follows:Eudragit RS PO/Eudragit RL PO is10:1, and the coating weight of8%, a plasticizer DBS used in an amount of20%, an amount of35%talc, the coating concentration of6%ethanol solution, the optimum conditions of:the blowing air volume of15Hz, temperature of30℃, the atomization pressure was1.Obar, shotcrete speed of10mL·min-1, the release curve pharmacokinetic model fitting, the results showed that the drug release mechanism is based on the film controlled release of the main skeleton dissolution also played a certain synergy; preparation the skeleton pills: powder lamination prepared skeleton pill, and prescription and process filter through single factor and orthogonal design experiments to determine the best prescription conditions:model drug/stearic3:1,10%PVP K30as a binder, Eudragit RL PO amount to15%, and the optimum conditions were:40rpm for powder machine speed, rotary speed of25rpm, atomization pressure of0.8Bar the shotcrete rate of20mL· min-I, the heat treatment temperature is60℃, the processing time of4h, the pharmacokinetic model release curve fitting, the results showed that the drug release mechanism for the proliferation of non-Fickian drug release is the synergy of diffusion and dissolution mechanism. Of this part of the experiment the product obtained results are satisfactory in vitro release and physical properties, and is suitable for industrial production, and laid the foundation for the the later prescription process further optimization and screening.Typical water-soluble small molecules metformin is selected as a model drug,the drug is highly water soluble, so it Coating Method to prepare its sustained-releasepellets majority of this chapter is a sustained-release pellets preparation of water-soluble drugs skeleton exploration and innovation, by referring to the upper part of the experimental results, the use of central composite design and response surface optimization method and orthogonal experimental design to further optimize the prescription process and screening been the centrifugal prepared metformin sustained-release pellets prescription process:stearic acid with model drug ratio of7.5:1, of Eudragit RL PO dosage amount of18%, the rotational speed of the powder supply machine40rpm, turntable rotational speed of35rpm, and the atomization pressure of0.8bar, shotcrete speed of10rpm, the heat treatment temperature was60℃, the time for4h, gentle the prescription process proceeds pellets drug release, process reproducibility. Select gliclazide poorly soluble model drug, With reference to part of the experimental results, the use of star point design and response surface optimization method and orthogonal experimental design the prescription process further optimization and screening. In order to improve the bioavailability, the choice of polyvinylpyrrolidone (PVP) and poloxamer ratio of1:1as a vector to prepare gliclazide solid dispersion, a solid dispersion of a drug containing an amount of50%. The optimized prescription for15%Eudragit RL, coating weight of7%, the screening process parameters:blast capacity of20Hz, a temperature of35℃, atomization pressure1.0Bar, shotcrete rate of8mL·min-1, by verifying the prepared Gliclazide sustained-release pellets process reliability, quality controlled.