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Multi-compartmental transdermal patch for simultaneous delivery of multiple drugs:formulation and evaluation of newly developed novel dosage form

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Journal of Coastal Life Medicine 2015年第7期 534-538页

作者： Vijayan Venugopal Jayaraja Kumar Selvadurai Muralidharan P.Vasanth Raj Unit of Pharmaceutical Technology Faculty of PharmacyAIMST UniversityBedong-08100Malaysia

Objective:To evaluate the formulation of multi-compartmental transdermal patches for simultaneous delivery of multiple drugs:aceclofenac and ***:The patch was prepared by simple solvent casting method using hydroxy propyl methyl celluloseK100Mas matrix forming agent and dimethyl sulphoxide as permeation *** prepared transdermal patch was evaluated by physiochemical parameters andin-vitro diffusion ***:The multi-compartmental transdermal patch showed sustained drug release over the period of 12 ***:Multicompartmental transdermal patches shows better bioavailability,therapeutic efficacy and very economic as compared with other dosage forms.

关键词： Multi-compartmental transdermal patch Aceclofenac Serratiopeptidase

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A continued study on the bisoprolol and isosorbide dinitrate transdermal patches:cardiovascular protection in spontaneously hypertensive rats

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Journal of Chinese Pharmaceutical Sciences 2008年第3期17卷 241-248页

作者：魏巍傅继华苏长海单英王渊孔树佳赵继会吕万良王树明王丽中国药科大学药学院江苏南京210009 北京大学药学院天然药物及仿生药物国家重点实验室北京100191 北京康倍得制药有限公司北京100029

The objective of the present study is to examine cardiovascular protective action of a newly developed transdermal patch by incorporating bisoprolol and isosorbide dinitrate in spontaneously hypertensive rats. As the combination therapy with these two synergistic drugs at low doses through a suitable form of administration could provide optimal therapeutic benefit, we further evaluated the effects of a 42 d period of anti-hypertensive treatment in spontaneously hypertensive rats. Rats were divided into the following five groups： control （blank patch）, bisoprolol fumarate tablets （BP-FT, 20.0 mg/kg, i.g.）, bisoprolol transdermal patch （BP-TP, 20.0 mg/kg）, isosorbide dinitrate transdermal patch （ISDN-TP, 20.0 mg/kg）, and the combination of BP and ISDN in a transdermal patch at low doses （8 and 12 mg/kg, respectively）. The effects of treatment were evaluated via biochemical indicators related to cardiovascular protection, structure and function. The combination therapy had synergistic anti-hypertensive effects and significantly reduced blood pressure with the benefit of controlling blood pressure variability compared to BP-FT and BP-TP. The combined treatment also reduced heart rate as well as BP-FT and BP-TP, while ISDN-TP had no evident effects on blood pressure, heart rate, and cardiovascular protection. Combination therapy was superior to BP-TP and BP-FT at increasing blood atrial natriuretic peptide and nitric oxide, while also reducing cardiac hydroxyproline and endothelin-1 with no difference in blood endothelin-1 and cardiac malondialdehyde levels. Cardiovascular remodeling differed among the groups, with the combination therapy reducing cardiac hypertrophy and the aortic media/lumen ratio. The consequential improvements in relaxation in response to cumulative concentrations of acetylcholine may explain the associated improvement in endothelial function. Combi- nation treatment with a transdermal patch exhibited a synergistic therapeutic effect. Such favorable

关键词： transdermal patch Hypertension Isosorbide dinitrate Bisoprolol Cardiovascular protection

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Mechanistic insights of the controlled release capacity of polar functional group in transdermal drug delivery system:the relationship of hydrogen bonding strength and controlled release capacity

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Acta Pharmaceutica Sinica B 2020年第5期10卷 928-945页

作者： Zheng Luo Chao Liu Peng Quan Degong Yang Hanqing Zhao Xiaocao Wan Liang Fang Department of Pharmaceutical Sciences School of PharmacyShenyang Pharmaceutical Universityshenyang 110016China

Background:Hydrogen bonding interaction was considered to play a critical role in controlling drug release from transdermal ***,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 *** present study shed light on this ***:Acrylate PSAs with amide group were synthesized by a free radical-initiated solution *** drugs,i.e.,etodolac,ketoprofen,gemfibrozil,zolmitriptan,propranolol and lidocaine,were selected as model *** vitro drug release and skin permeation experiments and in vivo pharmacokinetic experiment were *** correlation analysis,fourier-transform infrared spectroscopy and molecular simulation were conducted to provide molecular details of drug-PSA *** test,rheology study,and modulated differential scanning calorimetry study were performed to scrutinize the free volume and molecular mobility of ***: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 *** was found that drug release was controlled by amide group through hydrogen bonding,and controlled release extent was positively correlated with hydrogen bonding ***: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.

关键词： Controlled release Polar functional group Hydrogen bonding strength Pharmacokinetics Pressure sensitive adhesive Hydrogen bonding interaction transdermal patch Stratum corneum

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