Andrographolide Solid Self-emulsifying Granules

The Self-emulsifying drug delivery systems (SEDDS) is composed of water-insoluble drugs, oil, emulsifier, co-emulsifier consisting of oral solid or liquid dosage forms. Under gentle agitation or gastrointestinal motility can spontaneously form an oil in water emulsion, can improve the water solubility of the poorly soluble and fat-soluble drugs, to improve its bioavailability. soild self-emulsifying drugdelivery (S-SEDDS) is On the basis of oil, emulsifier, co-emulsifier to mixed a suitable solid materials to repare a solid preparation. Compared with the traditional L-SEDDS, S-SEDDS has good stability and reproducibility, Patients taking conform, longer Storage time, gastrointestinal irritation reduction, Easy to take and so on advantage. Taking into account the dual advantages of solid self-emulsifying formulationAndrographolide has antibacterial, anti-inflammatory, anti-viral, immune regulation, and treatment of cardiovascular and cerebrovascular diseases, liver gallbladder and other role,Because Andrographolide is diterpene lactone compounds, insoluble in water,so have low oral bioavailability, In order to improve its bioavailability, the study is prepare Andrographolide Self-emulsifying drug delivery systems,and then make it to be emulsification granules. In the first place, Choose two poorly soluble drug diterpene Lactone compounds chuanHuning and dihydropyridine drug nifedipine as model drug.Through setting the clarity Level of turbidity standard solution, Choose10-12clarity Level prescriptions from six different ternary phase diagram,Using laser particle size scanner to determine the particle size, And using UV-visible spectrophotometry to determine its absorbance, Then draw charts to compare three methods of particle size characterization rules. Prescription in the same phase diagram form an emulsion, There is a positive correlation relationship among It’s droplet particle size, absorbance and Clarity grade But, Prescription in different phase diagram form an emulsion, There is no regularity among It’s droplet particle size, absorbance and Clarity grade.so Prescription contains the same drugs and Excipients but different proportions form emulsion, It’s droplet particle size can observe its clarity by visual method or measure its absorbance by UV-Vis spectrophotometerIn the second place,Screening excipients type excipients and excipients dosage range in Self-emulsifying region by taking the Solubility experiments, excipient compatibility compared experimental and drawing ternary phase diagram. Using central composite design-and response surface methodology to optimized the preparation. With appearance,particle size,zeta potential,emulsification time after emulsified and Preparation physical stability as indexes to do quality evaluation of Preparation. Optimum prescription of this preparation was:Tween-80:EO:Glycerin=50:26:26. particle size of this preparation is39.5nm, zeta potential is-15.18mv Self-emulsifying time is40.53s. The acquired Andrographolide Microself-emulsifying Preparation is of clear transparent and good physical stability.In the third place,we choose the Preliminary preferred self-emulsifying prescription as based prescription. To select the carrier Based on the different carrier rate of pellet formation and heavy dispersion contrast;Then Through carrier dosage, drug loading investigation to optimize the proportion of prescriptions; With the appearance of the granules, dissolution,particle size, emulsification time after emulsified as indexes to do quality evaluation of Preparation. Optimum prescription of this preparation was:Andrographolide0.1g, Self-emulsion Liquid:Poloxamer-188=1:4. particle size of this preparation Is46.1nm, Self-emulsifying time is126s. he acquired Andrographolide solid self-emulsifying Granule is of good Formability and Can significantly improve the drug dissolution.In The fourth place, To do quality evaluation of of Andrographolide Microself-emulsifying By TLC indentication, Contention determined, self-emulsifying time, particle size, dissolution and granule particle size, moisture, dissolves, the load differences in inspection.