Study on the Fu Ante Oral-nano Granular Formulation
|School||Huazhong University of Science and Technology|
|Keywords||Fu Ante Nano oral Orthogonal design Quality standards Stability|
Fu Ante pentacyclic triterpenoids, is one of the main active ingredient of many herbal compound. It has anti-tumor, anti-diabetic, lipid-lowering, anti-inflammatory, antioxidant and other biological effects, especially anti-tumor, anti-oxidation, anti-hepatitis significant, is expected to become the anti-tumor, anti-hepatitis drug. Fu Ante has strong hydrophobicity so that its bioavailability is significantly reduced. Already Fu Ante made of nano freeze-dried powder as liver targeted drug coverage, we expect developed a preparation process is simple, fast, and easy to take solid oral nano formulations to increase its clinical application formulations. This thesis is carried out on the preparation of the Fu Ante solid nano oral granules prescription process, quality standards and stability. We found through experiments pure PEG-4000, PEG-6000, traditional materials such as PVP-K30 can not be prepared ideal Fuan Te solid dispersion limited Fu Ante solubilizing effect. By adding lipids, solid surface active agent to improve the dispersibility of Fu Ante found that not only can increase the extent and rate of its dissolution in water, and the formation of stable long-term placement of the nanoemulsion. The Orthogonal Design prescription best prescription: soybean lecithin 25%, Z-15 50% Z-7 12.5% ??PVP-k30 23%, Fu Ante 2%. 2 the process for preparing solid stars study were investigated by rotary evaporation of the solvent method, the influence of the freeze-drying method, vacuum drying method on a solid sub-state and dissolution effects, better results show that the solvent effect of rotary evaporation, we choose rotary evaporation of the solvent method to prepare the composite solid dispersion. 3. 福安特纳米 oral granules quality analysis includes the traits of the preparation, identification, inspection, determination of which content and dissolution was determined by high performance liquid chromatography (HPLC), through exploring the chromatographic conditions and method was validated, the method accurate precise determination of the content of the sample; developed on the basis of the quality standards of the the 福安特纳米 oral granules; quality check Click the quality standards of pilot batches of preparations, the indicators are in line with the requirements of the in vitro within 45 min Dissolution of up to 90% or more, and has a good immediate-release properties. 4 test preparation the stability study include: the impact factor test (high temperature, high humidity, light) and accelerated test. Test of the influence factors the pilot 福安特纳米 oral granules (batch number 100123), the product trial of high temperature and light detection indicators did not significantly change. Dissolution conditions and the dissolution of the preparations and preparations humidity test in 0 days more obvious changes, no significant changes in other indicators. The formulation unstable under the high-humidity conditions, we choose a good resistance to moisture and low toxicity of polyethylene material as a packaging material, can be a good moisture resistance, to ensure the storage stability of the preparation. The accelerated test results show that the indicators are in line with the requirements. The test results show that the form nanoemulsion 福安特纳米 oral granules all parameters were ideal in vitro dissolution and has good immediate release performance will improve Fu Ante bioavailability increase the dosage form of a simple and practical for clinical applications.