Dissertation > Medicine, health > Pharmacy > Pharmacy

Piroxicam in two kinds of transdermal

Author DongPing
Tutor FangXiaoLing
School Fudan University
Course Pharmacy
Keywords Piroxicam Percutaneous administration Penetration enhancers Gel Microemulsion Bioavailability
Type Master's thesis
Year 2010
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Non-steroidal anti-inflammatory drug piroxicam (Piroxicam, Pir) is a strong inhibitor of prostaglandin synthesis, is mainly used in the clinical treatment of rheumatic and rheumatoid arthritis, has a long half-life (50h) small doses, and no role in the accumulation and efficacy, but because the drug is easy to produce oral gastrointestinal adverse reactions, when the long-term administration, easily lead to gastrointestinal bleeding, ulcers and other side effects, and many researchers at home and abroad committed piroxicam by transdermal drug delivery dosage forms, such as stickers ointment, ointment, liniment, gel, etc., etc. This study hopes to explore better piroxicam transdermal preparation piroxicam gel and microemulsion. This study established the accurate and reliable piroxicam recreational outer analysis method, effects of various absorption promoting agent piroxicam percutaneous behavior results of the experiment showed that, lauryl nitrogen (?) Ketone, menthol, urea could promote topiramate Luo Xi Kang's penetration of 1% lauryl nitrogen leather ketone (Azone) and 10% propylene glycol (Propyleneglycol) joint application, the effect of transdermal penetration best, be able to significantly with ground improve topiramate piroxicam of permeability (P lt; 0.01), enhanced permeability multiple of 3.32 times. Gel (Gel) having a strong adhesion, good absorption characteristics of the skin after topical administration, this study is the first consideration prepared piroxicam gel. Investigation to compare the two gel matrix with penetration enhancers Carbomer -940 and hydroxypropyl cellulose (HPC), piroxicam promoting transparent effect A superior formulation, made a further in vitro transdermal studies, screening Optimal gel prescription: hydroxypropyl cellulose as a substrate, 1% lauryl nitrogen (?) ketone and 10% propylene glycol compatibility for promoting agent. The the homemade gel with the listed domestic piroxicam gel, and original research product-Feldene Gel (Pfizer Limited) transdermal contrast through in vitro transdermal experiments, it is found that the homemade gel permeation better than the domestic product without Feldene Gel. Microemulsion (Microemulsion, ME) as a carrier for percutaneous administration, the solubility of poorly soluble drugs can be improved, the formation of a higher concentration gradient. In addition, the microemulsion of the thermodynamic activity of the drug is increased to increase the affinity of drugs to the skin. Meanwhile, a component of the microemulsion is the role of a permeation enhancer, can reduce the barrier effect of the stratum corneum, promoting the penetration of the drug in the skin. In order to further enhance the percutaneous penetration of piroxicam, improve the clinical efficacy, this study design piroxicam microemulsions, and the in vitro and in vivo transdermal nature study. Pseudo-ternary phase diagrams by drawing microemulsion, the compatibility of different surfactant and cosurfactant, select the formation of the microemulsion larger area, to determine the basic formulation of the microemulsion prepared piroxicam microemulsion and its 12 hours per unit area of ??cumulative permeation amount as a response index, formulation optimization, the optimized prescription: oil phase (Lauroglycol FCC) 10%, surfactant (Labrasol: Cremophor EL = 1:1) 26.6%, co-surfactant ( Transcutol P) 13.3%, and water 50%. Piroxicam in microemulsion average particle size of 19.4nm evenly distributed, up to 100%; viscosity for 0.079Pa s. Rat transdermal trials comparing 0.5% piroxicam microemulsion Feldene Gel percutaneous penetration kinetics. The results show that the the prepared piroxicam microemulsion percutaneous permeation rate is better than Feldene Gel, the penetration rate of 1.66 times Feldene Gel. This study further Feldene Gel reference formulation of piroxicam in microemulsion rat in vivo bioavailability evaluation. The pharmacokinetic parameters of piroxicam microemulsion: t1 / 2 was 13.5 hours, Tmax 26 hours, Cmax (35.64 ± 11.31) μg · mL-1, AUC0-t (1511.78 ± 388.38) μg · h · mL-1, piroxicam microemulsion relative bioavailability of 185.63%. Showed that piroxicam made microemulsion administration

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