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Studies on Self-Microemulsifying Drug Delivery Systems (SMEDDS) of Silymarin and Silymarin-Phospholipid Complex

Author: LiuLinZuo
Tutor: ZuoXiuJuan；WangSiLing
School: Shenyang Pharmaceutical University
Course: Pharmacy
Keywords: Silymarin Silybin SMEDDS Phospholipid complex Pseudo- ternary phase diagrams Bioavailability
CLC: R283
Type: Master's thesis
Year: 2007
Downloads: 37
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Abstract


Silybum thistle prime (silymarin, SM) from water flying thistle (Silybum marianum (L.) Gaertner.) Fruit extract isolated flavonoids effective ingredient by the water fly thistle Bin (silybin), water flying thistle Ning (silidianim), water milk thistle Ding (siliehristim) and silymarin alcohol (silibonol), with four kinds of isomers, silibinin as the main component, mainly used in the clinical treatment of acute and chronic hepatitis, the various liver damage, liver fibrosis and early cirrhosis, efficacy, side effects and other features. However, due to its insoluble in water, and the gastrointestinal tract instability and slow intestinal absorption, resulting in low oral bioavailability. Improve water fly thistle the dissolution speed, improve its bioavailability and increased drug loading to be made suitable for industrial production of new dosage forms, the paper design and development of silymarin self-micro-emulsifying capsule and silymarin phospholipid composite material self-micro-emulsifying capsule, and using different methods of in vivo and its scientific evaluation. Subject according to the requirements of the different studies, UV spectrophotometry spectrophotometry and high performance liquid chromatography method for silymarin and silymarin phospholipid composite material activity of the total flavonoids or water fly thistle Penn's prescription screening content determination and in vivo evaluation for SMEDDS the The quality of research has laid a solid foundation. The above method with high sensitivity, specificity, and accuracy to meet the analysis requirements of this study. Better ability to dissolve the drug and emulsifying properties accessories selected through preliminary experiments designed four factors and three levels of orthogonal experiment, appearance, add the water situation and the particle size as an indicator to determine the use of Cremophor EL as emulsifiers, Transcutol Cosurfactants by drawing a pseudo-ternary phase diagram, choose the a microemulsion region's largest prescription further determine the oil phase (ethyl oleate / MCT = 1/1). Saturated solubility final comprehensive evaluation, self-emulsifying efficiency and stability into milk, determine the the SM-SMEDDS the prescription for mixed oil (ethyl oleate: MCT = 1:1) 200g, the Cremophor EL 225g Transcutol75g, milk thistle prime 28g . Each dose of aqueous silymarin 28mg, total weight of about 0.5g. Silymarin self-micro-emulsifying capsule in vitro release characteristics were investigated by reverse dialysis method and sample separation, the results of the two dissolution methods that homemade preparations fastest dissolution, and the dissolution of the Legalon capsules no significant difference, but significantly higher in Yiganling tablet. The formulation into the milk after the average particle diameter of 120nm, ζ potential-15.2mv, 101% of the average content. The capsule contents impact factor test showed that the self-microemulsion should be stored in the dark, the thermostat accelerated experimental results show a good stability of the preparations. Select acetone as the reaction solvent, n-hexane for the collection of solvent to silymarin, soybean phospholipid mass ratio of 1:1, Preparation of phospholipid complex of silymarin result, the yield of about 65%, the recombination rate can be as high as 97%. DSC and melon analysis to identify the formation of phospholipid complex results show that a new chemical group is not formed therebetween. On the basis of water milk thistle vegetarian since the micro-emulsion research results of the draw fake three yuan phase diagram, in connection with the prescription various accessories of dissolving ability, stability since the emulsification rate and into milk, filter the water flying thistle prime phospholipid composite material self-micro-emulsifying solution of Prescription final phospholipid complexes of silymarin 70g, mixed oil (ethyl oleate: MCT 1:1) 250g, Cremophor EL 200g, the Transcutol 50g of wherein each capsule aqueous silymarin 70mg. The formulations into the milk after the average particle diameter of 146nm, using water as the diluent medium measured obtaining ζ potential-29.5mv. The in vitro release of the experimental results of complex self-microemulsifying capsule release is slow compared to the bulk drugs since the micro-emulsion. Stability of experimental studies have shown that, the good homemade complex since stability of microemulsifying capsule. Comparison of a homemade water fly thistle prime self-micro-emulsifying capsule, silymarin phospholipid composite material from micro-emulsifying capsule and commercially available Legalon capsules three formulations in dogs in vivo of differentiation, using three cycles of three cross-administration, conducted the in vivo drug pharmacokinetic study. The results are in contrast to commercial formulations, homemade relative bioavailability of two formulations (157.0 ± 53.9)% and (250.9 ± 58.3)%, respectively. Analysis of variance showed AUC 0 - ∞ and C max individuals during the week without a significant difference, the preparations there a significant difference; dual-sided t test showed that the three between any two are not bioequivalent formulations. Visible, silymarin and its phospholipid complex self-microemulsifying capsule absorbed in the body quickly and significantly improve bioavailability.

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