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Background@#Hydrogen bonding interaction was considered to play a critical role in controlling drug release from transdermal patch. However, the quantitative evaluation of hydrogen bonding strength between drug and polar functional group was rarely reported, and the relationship between hydrogen bonding strength and controlled release capacity of pressure sensitive adhesive (PSA) was not well understood. The present study shed light on this relationship.@*Methods@#Acrylate PSAs with amide group were synthesized by a free radical-initiated solution polymerization. Six drugs, , etodolac, ketoprofen, gemfibrozil, zolmitriptan, propranolol and lidocaine, were selected as model drugs. drug release and skin permeation experiments and pharmacokinetic experiment were performed. Partial correlation analysis, fourier-transform infrared spectroscopy and molecular simulation were conducted to provide molecular details of drug-PSA interactions. Mechanical test, rheology study, and modulated differential scanning calorimetry study were performed to scrutinize the free volume and molecular mobility of PSAs.@*Results@#Release rate of all six drugs from amide PSAs decreased with the increase of amide group concentrations; however, only zolmitriptan and propranolol showed decreased skin permeation rate. It was found that drug release was controlled by amide group through hydrogen bonding, and controlled release extent was positively correlated with hydrogen bonding strength.@*Conclusion@#From these results, we concluded that drugs with strong hydrogen bond forming ability and high skin permeation were suitable to use amide PSAs to regulate their release rate from patch.
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Objective: To prepare celecoxib hotmelt pressure sensitive adhesive (HMPSA), and investigate the quality. Methods:Celecoxib HMPSA was prepared using styrene-isoprene-styrene triblock copolymer (SIS) as the chief material, and the quality of HMP-SA was inspected with stickiness, peel strength, melt temperature and percutaneous permeation rate in vitro as the indices. Results:The stickiness of celecoxib HMPSA was (17.79 ±0.25)N, the peel strength was (2.81 ±0.49) N·cm-2, the melt temperature was 90. 8 ± 1. 9℃, and the percutaneous permeation rate in 24h was (18. 77 ± 1. 51) mg·cm-2. Conclusion: The HMPSA is suitable for the preparation of TDDS of celecoxib.
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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.
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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.
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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.
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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.
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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.
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Azone. PG combined with azone showed a higher synergic effect of enhancing effectiveness. Conclusion National Starch polyacrylate pressure-sensitive adhesive was the most effective pressure-sensitive adhesive matrix, PVP-K30 was the most effective crystallization inhibitor, PG combined with azone were the most effective penetration enhancers.