Study on matrix proportion of hydrophilic SIS hot melt pressure sensitive adhesive suit modified by RLPO / 中草药

Objective: To optimize the matrix proportion of SIS hot melt pressure sensitive adhesive suit for hydrophilic material releasing. Methods: By orthogonal test method, taking adhesiveness and hydrophilic drug release rate as factors, and C5 petroleum resin hydrogenate, lanoline styrene-isoprene-styrene (SIS) triblock copolymer, ethyl acrylate-methyl methacrylate-trimethylamino (RLPO), liquid paraffin, dibutyl phthalate (DOP), polyethylene glycol (PEG) 400, and Antioxidant 1010 as materials, the matrix proportion was optimized. Results: The optimized formulation was as follows: SIS-C5 petroleum resin hydrogenate-SIS-RLPO-DOP-PEG 400-Antioxidant 1010 was 3:4:6:6:5:1:0.1. The adhesiveness was proper and shows more release rate for hydrophilic material. Conclusion: The SIS hot melt pressure sensitive adhesive shows good property and is suitable to prepare transdermal patch.

Comparison on in vitro transdermal permeability, pharmacodynamics, and skin irritation of Guanjie Zhitong Patches based on two different matrixes / 中草药

Objective: To compare the differences in transdermal permeability, pharmacodynamics, and skin irritation of Guanjie Zhitong Patches based on two different formulations taking hot-melt pressure sensitive adhesive and rubber as matrixes. Methods: In vitro transdermal permeation was performed by means of Franz diffusion cells; The analgesic effect was evaluated by HAc-induced writhing response in mice and hot-plate test, while the anti-inflammatory action was assessed by xylem-induced ear edema in mice and albumin-induced paw edema in rats. The skin irritation of the two matrixes was investigated using guinea pig as model animal. Results: Patches based on hot-melt pressure sensitive adhesives showed better transdermal permeability, analgesic, and anti-inflammatory effects but less skin irritation than the rubber type patches. Conclusion: Hot-melt pressure sensitive adhesive is a kind of appropriate material to compose the patch matrix for Chinese herbal medicine, which has the good transdermal permeability and efficacy and less skin irritation.

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.

Optimization of Guanjie Zhitonggao Patch formulation using central composite design-response surface methodology / 中草药

objective To develop a new Guanjie Zhitonggao Patch using hot melt pressure sensitive adhesive (HMPSA) as matrix. Methods Amounts of tackifier and plasticizer in formulation were selected as factors. Tack force, peeling strength, and release rate of drug were selected as indexes. And the central composite design-response surface methodology was applied to optimizing the formulation. Results The model obtained from this method showed a reliable predictability. The formulation in optimized region possessed some superior properties and could be used for skin application. Conclusion Formulation optimization with advantages of less trial and higher precision could be achieved using central composite design-response surface methodology because it is suitable for multielement-nonlinear regression design.

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.