Formulation Optimization of Rutaecarpine Transdermal Patch
- Author:
Sen WANG
1
Author Information
- Publication Type:Journal Article
- Keywords: Azone; Dibutyl sebacate; Eudragit E100; Oleic acid; Rutaecapine; Succinic acid; Transdermal patch
- From: Chinese Pharmaceutical Journal 2018;53(6):439-444
- CountryChina
- Language:Chinese
- Abstract: OBJECTIVE: To screen pressure sensitive adhesive system and penetration enhancer of rutaecarpine transdermal patch. METHODS: The patch was prepared by solvent evaporation method. The ratio between pressure sensitive adhesive (Eudragit E100), crosslinking agent (succinic acid) and plasticizer (dibutyl sebacate) of the rutaecarpine patch were screened through Box-Behnken design by using adhesion (stick power, shear strength, peel force) as the index. The ratio between pressure sensitive adhesives and chemical enhancers (azone and oleic acid) were screened by adhesion and permeation experiments in vitro using custom design, which were carried out by using improved Franz diffusion cells through excised mice skin. RESULTS: The optimized formulation of rutaecarpine transdermal patch consisted of 83% pressure sensitive adhesives (63.5% Eudragit E100, 5.5% succinic acid, 14% dibutyl sebacate), 10% azone, 6.4% oleic acid and 0.6% rutaecarpine. The stick power, shear strength, and peel force of the patch were 15 steel balls, (10.97 ± 0.32) h and (0.16 ± 0.02) kN•M-1, respectively. The cumulative permeation amount and permeation rate of the patch were (29.71 ± 1.19) μg•cm-2 and (1.36 ± 0.10) μg•cm -2•h -1, respectively. CONCLUSION: The optimized rutaecarpine patch show increased permeation and appropriate adhesion. This study provides the basis for future research.
