Sustained Release Tablets Of Both Sides Of Acupuncture Analgesia

Objective:To develop a theory of traditional Chinese medicine under the guidance of a significant effect,safe,reliable,advanced process formulations,quality,full control,to extend the patient's medication cycle,reducing the number of medication to improve patient compliance of Chinese medicine preparations.Optimized by orthogonal design method of sustained-release tablets pain nitidine the extraction process of total alkaloids of Zanthoxylum nitidum intestinal absorption was evaluated,using HPMC_K4M as the basic matrix material by adding microcrystalline cellulose,lactose,prepared on service twice,once the two sides of a sustained-release tablets analgesia.Developed nitidum nitidum extract and analgesic tablets, and the initial stability of quality standards for research,its quality control and provide a basis for identification of medicinal herbs.Materials and Methods:1.Materials:two sides of the needle:for plants Rutaceae Zanthoxylum nitidum Zanthoxylum nitidum(Roxb.) DC.'s Dry roots and herbs purchased in Anguo Limited.Nitidine chloride reference substance purchased in the Chinese pharmaceutical testing of biological products, the batch number:848-9901.2.Methods:(1) the use of L9(3⁴) orthogonal experimental design optimization of extraction process.An integrated score to determine the evaluation criteria,the use of visual analysis and the methods of analysis of variance of orthogonal test results for analysis.(2) study the use of single-factor method,and optimize the macroporous resin and purification of total alkaloids in Zanthoxylum nitidum the important parameters,the use of orthogonal experimental design method,and optimize the purification conditions,the use of visual analysis and variance analysis,the results of orthogonal test for analysis.(3) Determination of chloride HPLC nitidine,UV spectrophotometric determination of phenol red content,using phenol red in the systemic circulation to the demarcation of the volume of fluid calculated in the systemic circulation of mice chloride solution nitidine content.(4) the use of L9(34) orthogonal experimental design to optimize the prescription.An integrated score to determine the evaluation criteria,the use of visual analysis and the methods of analysis of variance of orthogonal test results for analysis.(5) to accelerate the test of sustained-release tablets pain nitidine preliminary stability analysis.(6) acetic acid writhing law nitidum nitidum analgesic tablets and the analgesic effect of extract for analysis.Results:1.The establishment of HPLC method nitidine nitidine chloride method for the determination, single-factor study of the extraction time,extraction of the number of solvent extraction, ethanol and acid concentrations of chloride extraction rate nitidine the effects of extraction conditions,a four-factor three-level orthogonal design method to optimize extraction conditions,to determine the optimal extraction process.2.The establishment of total alkaloids in Zanthoxylum nitidum by UV spectrophotometry method for the determination,by comparing the different types of resin for total alkaloids of Zanthoxylum nitidum static adsorption - elution rate selected for the resin;resin through the study of important parameters,such as the dynamic adsorption resin,leakage curve,elution curve to determine the total alkaloids of Zanthoxylum nitidum best purification.3.The establishment of chloride nitidine HPLC detection method and the phenol red determination of intestinal absorption of UV,the concentration of different extracts of the paragraph in the rat small intestine absorption study carried out to determine the drug absorption in vivo approach Preparation of sustained-release preparations to provide a scientific basis.4.Factors in a single study on the basis of the wetting agents and particles to determine the drying temperature.The establishment of in vitro release method,select the release medium, the test method and test to the number of different specifications of the HPMC,HPMC the dosage,the type of filler,the amount of wetting agent,the conditions of pressure producers inspected to determine the main effects of factor,and orthogonal design to optimize the prescription of the preparation process of an inspection process to determine the optimum shape.5.Nitidine quality standard sustained-release tablets pain research,the establishment of Zanthoxylum nitidum extract preparation methods and quality standards,the establishment of a sustained-release tablets pain nitidine quality standards.6.Nitidine analgesia investigated the initial stability of sustained-release tablets,in the high-temperature,high humidity,heat,light and air medium under the conditions of exposure, in the days 0,5,10 sampling,observation of appearance,check the release to determine the weight differences and levels of analgesia for sustained-release tablets nitidine packaging material selection provides a scientific basis.7.Through the acetic acid writhing test,compared with extracts from Zanthoxylum nitidum nitidum analgesic effect of analgesic tablets,resulting in a considerable analgesic effect,and with the analgesic effect of the increase in dose enhancement.Conclusion:1.To determine the best test of the extraction process is:80%ethanol concentration(by adding 0.1mol / L hydrochloric acid solution pH value adjusted to 3),increase of 8,6 times the alcohol,extracted twice,the first extraction 2h,the second extraction of 1.5h.Optimized process is stable and viable for the sustained-release tablets pain nitidine provide a reliable basis for preparation. v2.HPD 100 nitidine resin is an excellent ingredient alkaloids of the macroporous resin,the total alkaloids of Zanthoxylum nitidum dynamic adsorption capacity of up to 44.8mg / g; 5BV 80%ethanol can be adsorbed on the resin on the biological washing off,purification of total alkaloids were up to 39%purity.3.Drug absorption in mice with the drug concentration is not strong enough,by the experimental results,the low,middle and high concentrations of drug absorption was no significant difference in the percentage of drug absorption in rats is passive diffusion,the experimental results show that the small intestine of rats nitidine chloride absorption in good condition,the results of the development of drug formulations provides the basis for sustained-release preparations.4.The use of L9(3⁴) orthogonal experimental design to optimize the prescription.An integrated score to determine the evaluation criteria,the use of visual analysis and the methods of analysis of variance of orthogonal test results were analyzed to determine the best prescription.Preparation and inspection agents,and ultimately to determine the analgesic nitidine forming process of sustained-release tablets were prepared by two days served,first day of sustained-release tablets nitidine analgesia.Nitidine analgesia to sustained-release tablets in vitro release of 2h,6h,12h,respectively,to determine the release rate of 20%～30%, 50%～70%,90%.Release for good conduct,and basic to achieve complete release.5.In this paper,only the content of three batches of samples were determined from the average content of three batches of samples to fall 20%as the minimum limit,for the determination of drug content,the three smaller samples,and did not try to do zoom in,but the standard of quality so a preliminary study.6.This product is at a high temperature,light conditions,the content of the release of indicators and no significant changes in degree,in high humidity conditions,the apparent difference in the weight of the goods increased,and slightly better color,there is moisture present goods,but the content,the release of degrees no obvious changes in other indicators, show that the basic stability of the goods,but in the choice of packaging,to choose the materials to avoid moisture absorption and should be sealed to preserve.7.Writhing method is a sensitive,simple and reproducible screening method for analgesics, with acetic acid writhing method proved nitidum nitidum extract with analgesic tablets analgesic effect in mice rather,its role With the increase of the dose.