Dissertation > Medicine, health > Pharmacy > Pharmacy > Pharmaceutics

Preparation and Evaluation of ROP Transdermal Patch

Author WenHuiYing
Tutor YuZuo
School Chongqing Medical University
Course Biopharmaceutical and biomedical materials
Keywords ROP Transdermal SMD Transdermal delivery system In vitro and in vivo evaluation
CLC R943
Type Master's thesis
Year 2010
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used alone significantly reduced early tremor palsy symptoms, significantly reduced the incidence of dyskinesia, can better control the symptoms of Parkinson's disease (PD) stage. The main indication for the treatment of PD syndrome and restless legs syndrome [2] [3]. Its mechanism of action and Luo rotigotine (Rotigoetine), pergolide the Pergolide similar [4]. ROP as a substitute for levodopa treatment of early disease has been first-line drugs in the \ROP oral formulations, in 1996 for the first time in the UK market, the trade name Requip; approved for marketing by the U.S. FDA in September 1997. Bioavailability appears by the from Global Clinical Application ROP oral preparation is not high, the obvious gastrointestinal adverse for other dosage forms of drugs to ROP also constantly developing, ROP sustained-release tablets in the United States FDA has just approved The purpose of this paper, the ROP low oral bioavailability and gastrointestinal side effects obvious major problem, hope the new transdermal patch developed by the ROP, in order to improve bioavailability, get rid of the purpose of the gastrointestinal side effects. To provide a basis for the development of ROP transdermal drug delivery system and its clinical application. Method 1. 2-room level diffusion cell, the horizontal diffusion cell rat skin transdermal experimental methods to study the percutaneous penetration of the drug substance. (2) the use of Franz diffusion cell, Franz diffusion transdermal drug delivery (SD rats leather) model to study the cumulative amount of transdermal ROP transdermal patch transdermal rate and steady-state percutaneous permeation rate. 3 phase high performance liquid chromatography, ROP transdermal patch main ingredients measured by reversed-phase high-performance liquid chromatography analysis. 4 using the differential scanning calorimetry analysis (DSC) method, to examine the presence status of the ROP in the transdermal patch. Using single factor method, study the mixed plastic DT4098/BP4202 ratio, and promote infiltration dosage, drug loading and other factors, of its preparations for transdermal factors influencing prescription and prescription transdermal patch preparation Filter optimization. 6 using HPLC-MS/MS method HPLC-MS/MS method for the determination of the method of analysis of the content of the plasma ROP. ROP medication in the form of identification: on physicochemical properties and permeability of the the ROP free base (ROP.base), and its hydrochloride (ROP.HCl) comparative study to determine to ROP.base as a transdermal patch main drugs. ROP exists in the form of study: a differential scanning calorimetric analysis (DSC) studies have shown that, ROP in the transdermal patch in the presence of molecular or amorphous form. The determination of the main ingredients in the ROP transdermal patch reversed-phase high performance liquid chromatography study shows ROP.base in the concentration range of 0.71 to 70.66μg/mL a good linear relationship (r = 0.9999), RSD is less than 0.5 % The method is rapid, accurate and reproducible. ROP content determination in plasma HPLC-MS/MS method: test showed the ROP concentration within the range of 0.02 to 416.72ng/mL a good linear relationship (r = 0.9998), RSD less than 6.0%, the method can to achieve the requirements of the detection method of the biological sample. Prescription Investigation and optimization of: the the cumulative transdermal amount transdermal rate and steady-state percutaneous permeation rate as a patch the percutaneous (SD rat) penetration indicators examine the ratio of mixed plastic DT4098 / BP4202 , the penetration dose and drug loading formulations transdermal test to determine the best prescription for ROP transdermal patch, ie the mixed plastic DT4098/BP4202 ratio of 1/4, penetration enhancers Azone 1%, 4% drug loading. 6 Study on the Preparation: The test showed the coating thickness of the, ROP transdermal patch for 0.2 mm, the drying temperature is 60 ° C, the skin adhesion of the drug-containing layer, the layer integrity, uniformity and patch appearance were good. Stability studies: accelerated 3-month results show that the stability of ROP transdermal patch, transdermal patch requirements are in line with its content and related substances. 8 local irritation studies: the display of the the rabbit abdominal and back skin irritation study, the ROP transdermal patch affixed to the back of the rabbit 3 days, non-irritating to the skin. 9 pharmacokinetic studies: displayed by rabbits pharmacokinetics experimental study, rabbits three days to achieve a stable transdermal rate and stable plasma concentration, the body steady-state plasma concentration of 25.0 ng / mL, which showed that the ROP transdermal patch having a certain sustained release characteristics. Conclusion In this paper, the physical and chemical properties of the ROP Select ROP.base as a model drug, developed ROP transdermal patch. In vivo experimental studies have shown that the transdermal patch without stimulation, the biocompatible good; rabbits steady-state plasma concentration of 25.0 ng / mL, the plasma concentration of homeostasis the transdermal rate and stable to maintain days, which indicates that the ROP transdermal patch having a sustained release characteristics. The results of these studies laid the foundation for the development and clinical application of the ROP transdermal drug delivery system has a certain theoretical and practical value.

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