Development of hot melt pressure sensitive adhesive for transdermal use and in vitro evaluation / 中国药学杂志

OBJECTIVE: To develop hot melt pressure sensitive adhesive (HMPSA) for transdermal use, and to investigate the in vitro drug release and permeation property of HMPSA based patches. METHODS: HMPSA was prepared using styrene-isoprene-styrene triblock copolymer (SIS), C5 petroleum resin hydrogenate, lanoline, liquid paraffin, dibutyl phthalate, 2, 6-ditertbutyl-cresol as material under orthogonal design. The formulation of HMPSA was screened using stickiness, melt temperature and vapor permeation rate as index. The in vitro drug release behavior and transdermal property of the optimized HMPSA were evaluated using a-asarone as model drug. RESULTS: The optimized formulation of HMPSA (HMPSA-OP) was followed as: SIS: C5 petroleum resin hydrogenate: lanoline: liquid paraffin: dibutylphthalate: 2, 6-ditertbutyl-cresol=100:140:20:40:20:2. HMPSA-OP had shown more rapid drug release than ordinary HMPSA. And the in vitro transdermal flux of HMPSA-OP was (4.75±0.84) μg · cm-2 · h-1, higher than that of ordinary HMPSA and acrylate PSA. CONCLUSION: The HMPSA-OP shows good property and was suitable to prepare transdermal patch.

Preparation of testosterone hot melt pressure sensitive adhesive transdermal patch / 中国药学杂志

OBJECTIVE: To prepare testosterone hot melt pressure sensitive adhesive (HMPSA) transdermal patch and investigate its percutaneous permeability in vitro. METHODS: The matrix of thermoplastic elastomer styrene-isoprene-styrene(SIS) hot melt pressure sensitive adhesive was used for testosterone transdermal patch. The percutaneous permeability through excised nude mice skin or porcine skin in vitro was conducted by Franz diffusion cells. Cumulative permeation quantity (Q) and steady state permeation rate (Jss) were evaluated to optimize drug loading capacity and enhancer. The optimal transdermal patches were compared with reference patches with regard to percutaneous behaviors using excised nude mice skin and porcine skin. RESULTS: The optimal formulation contained 2% testosterone, 6% transdermal enhancer isopropyl myristate(IPM). Its permeation behavior in vitro followed zero-order kinetics. The permeation behavior of the optimal patches was better than the reference patches for excised nude mice skin and porcine skin. CONCLUSION: SIS HMPSA has a broad application potential for transdermal drug delivery system.