Symptoms of Depression and Smoking Behaviors Following Treatment with Transdermal Nicotine Patch

Subscales from the Center for Epidemiologic Studies Depression Scale (CESD), assessed prior to treatment, were examined as predictors of withdrawal, craving, and affect during the first week of abstinence, as well as smoking abstinence during the first week of abstinence and at the end of treatment. The negative affect and somatic features CESD subscales were related to higher levels of nicotine withdrawal. The relationship between the interpersonal disturbance CESD subscale and nicotine withdrawal approached significance. This study suggests the need to examine novel psychological mechanisms that may account for the relationship between depression symptoms and smoking cessation.     

反相高效液相色谱法测定复方戒烟贴片中尼古丁和可乐定的含量

目的 :建立反相高效液相色谱法检测复方戒烟贴片中尼古丁和可乐定的含量。方法 :用LichrosorbC8柱 ,甲醇 -磷酸盐缓冲液 (0 0 0 2 2mol·L- 1 磷酸二氢钾 - 0 0 16mol·L- 1 磷酸氢二钠溶液 ) (5 2∶48)为流动相 ,检测波长 2 6 8nm。结果 :该方法回收率尼古丁为 95 4% ,RSD为 3 8% (n =5 ) ;可乐定为 98 9% ,RSD为 4 8% (n =5 )。结论 :本法较简便 ,准确可靠 ,可作为复方戒烟贴片的质量控制方法。     

骨质增生透皮贴剂的制备

目的将传统的骨质增生膏改进为骨质增生透皮贴剂。方法利用挥发油提取方法提取药材中的有效成分,将其制成贴剂;以君药细辛中的主要成分甲基丁香酚作为药物经皮渗透的评价指标,进行体外经皮渗透实验以筛选贴剂中干姜挥发油的用量与透皮促进剂月桂氮卓酮的用量。结果贴剂处方中含2倍量干姜挥发油和2%氮酮时具有最佳的药物渗透量和渗透速度。结论筛选制得骨质增生透皮吸收贴剂的透皮效果较好,具有广阔的应用前景。     

骨质增生透皮贴剂的制备

目的 将传统的骨质增生膏改进为骨质增生透皮贴剂。方法利用挥发油提取方法提取药材中的有效成分,将其制成贴剂;以君药细辛中的主要成分甲基丁香酚作为药物经皮渗透的评价指标,进行体外经皮渗透实验以筛选贴剂中干姜挥发油的用量与透皮促进剂月桂氮卓酮的用量。结果贴剂处方中含2倍量干姜挥发油和2％氮酮时具有最佳的药物渗透量和渗透速度。...     

HST贴剂的透皮特性

目的研究HST贴剂的透皮特性。方法采用V-C水平扩散池,以透皮速率为指标,研究HST贴剂在离体人皮中的透过性。结果本品在透皮速率以及稳态透皮维持时间两方面均已达到设计要求。结论本文为后续研究提供了实验依据。     

妥洛特罗透皮贴剂的释放度测定及不同测定方法结果比较

目的 建立妥洛特罗透皮贴剂的释放度测定方法,并对不同装置测定的释放曲线进行比较。方法 采用中国药典2015年版收载的2种透皮贴剂释放度测定新方法,即桨碟法和转筒法,规定时间点取样后采用HPLC测定,色谱柱为Agilent C₁₈（250 mm×4.6 mm,5 μm）,流动相为乙腈-0.02 mol·L^-1磷酸盐缓冲液（pH 3.0）（32：68）,流速为1.0 mL·min^-1,柱温为35℃,检测波长为215 nm。分别考察妥洛特罗透皮贴剂在500 mL水中24 h的释放曲线,并对2种方法的释放曲线进行拟合,比较二者的相似性。结果 妥洛特罗在0.103~4.135 μg·mL^-1内线性关系良好（r=0.999 9）,回收率为99.8%（n=9）,样品溶液在24 h内稳定。将2种方法测定的释放度结果经Weibull方程拟合后得到的参数进行方差分析,2组数据间无显著性差异。结论 中国药典2015年版透皮贴剂释放度测定桨碟法（方法2）和转筒法均可用于妥洛特罗透皮贴剂的释放度测定,两者的测定结果不存在差异。     

盐酸多西环素透皮贴剂的制备

采用膜控透皮技术制备贮库型盐酸多西环素透皮贴剂,进行了透裸鼠离体皮肤试验和大鼠透皮给药的药动学初步研究.结果表明,盐酸多西环素能透过孔径5μm的聚乙烯微孔膜,且5%月桂氮革酮能显著提高其透皮量.     

非洛地平-美托洛尔复方透皮贴剂的基础处方优化

以贴剂外观和黏性为指标，通过正交设计考察非洛地平和美托洛尔的投料量、复合压敏胶材料Eudragit E PO和Eudragit RL PO重量比、增塑剂（PEG 400）和交联剂（琥珀酸）用量等因素对贴剂质量的影响。优选的基础处方为：非洛地平和美托洛尔投料量分别为2％和20％、Eudragit E PO-Eudragit RL PO为5：5（w／w）、PEG 400和琥珀酸用量分别为10％和12％。结果表明，该处方制备的贴剂外观良好，黏性适宜，药物体外释放速率和稳态透皮速率较高。     

Transdermal penetration of UV filters

A penetration study of 2-ethylhexyl-4-methoxycinnamate (EHMC), 4-methyl benzylidenecamphor (MBC), butyl methoxydibenzoylmethane (BMBM), 2-ethylhexyl-2,4,5-trimethoxycinnamate (EHTMC) and di(2-ethylhexyl)-2,4,5-trimethoxybenzalmalonate (TMB) through baby mouse skin (Mus musculus Linn.) was carried out using a vertical Franz diffusion cell. At 4.4 mg/cm(2) coverage of UV filter on the skin, 2.98 +/- 0.38, 1.15 +/- 0.14 and 0.80 +/- 0.28% of the applied EHMC, MBC and BMBM were detected in the receptor fluid at 24 h after application. Penetrations of UV filter in an ethanolic solution and lotion forms were comparable. EHTMC and TMB showed insignificant penetration across the baby mouse skins. Baby mouse skins kept at 4, -20 and -80 degrees C gave similar EHMC penetration results. Penetrations of EHMC, BMBM, EHTMC and TMB across human epidermis were carried out upon 5 volunteers using the suction blister technique. The results also confirmed the significant penetrations of EHMC and BMBM and the insignificant penetrations of EHTMC and TMB.     

丁螺环酮贴剂透皮吸收的药物动力学研究

目的:研究丁螺环酮透皮贴剂给药的药物动力学及生物利用度。方法:以丁螺环酮片剂为对照,采用HPLC法测定家兔随机交叉使用丁螺环酮贴剂和片剂在相同单剂量给药后的血药浓度,采用3p97软件处理数据,进行药物动力学及生物利用度的研究。结果:与片剂比较,贴剂达峰时间较长,但可维持较长时间平稳的血药浓度,在1.5～8 h内血药浓度保持在34.190±3.382 ng·ml~(-1)左右;贴剂和片剂的AUC_(0→∞)分别为(40.741±108.828)和(102.031±39.570)h·ng·ml~(-1),二者有极显著性盖异(P<0.01),贴剂相对生物利用度是片剂生物利用度的3.96倍。结论:外用贴剂相对口服片剂而言,有较高的生物利用度。     

非洛地平-美托洛尔复方透皮贴剂的处方与工艺研究

目的:考察并筛选非洛地平-美托洛尔(FEL-MET)复方透皮贴剂的基础处方与制备工艺。方法:以聚丙烯酸树脂Eu-dragit E PO和Eudragit RL PO为复合压敏胶,采用流涎法制备非洛地平-美托洛尔复方透皮贴剂。通过单因素试验考察处方与制备工艺对贴剂外观、物理黏性、药物体外释放和经皮渗透性等指标的影响,初步确定贴剂处方和工艺条件。结果:较佳的处方构成和工艺条件:FEL和MET载药量分别为2%~3%和20%~30%,Eudragit E PO∶Eudragit RL PO为4∶6~6∶4,贴剂厚度为(1·0±0·1)~(2·0±0·1)mm,固化条件为70℃干燥30min。上述各因素对贴剂质量考察指标影响显著。结论:筛选处方合理,工艺稳定可行,制备的贴剂质量符合相关要求。     

透皮贴剂市场研究及其新进展

目的：对透皮贴剂进行市场研究及分析，并介绍国内透皮给药研究的最新进展，为透皮贴荆的销售市场及其新药研究提供参考。结论；透皮给药系统具有广阔的市场和开发前景。     

Reservoir Based Fentanyl Transdermal Drug Delivery Systems: Effect of Patch Age on Drug Release and Skin Permeation

Purpose  To understand and evaluate the stability and skin permeation profiles of fentanyl reservoir systems as a function of patch age. Methods  Drug release and skin permeation studies were performed using a modified USP apparatus 5 with a novel sample preparation technique. Results  The amount of fentanyl present in the EVA/adhesive layer (EAL) increased from about 17% of label claim (LC) at 5 months to 25% LC at 22 months. The increase in the drug concentration was mainly observed in the peripheral EAL. Simultaneously, the alcohol content of the patch decreased as a function of patch age. A significant effect of patch age on the drug content in the EAL and the drug release from the system was observed; however, skin permeation studies did not indicate an increase in drug delivery rate. Conclusions  Novel sample preparation technique with USP Apparatus 5 allowed determination of in vitro skin permeation rates for fentanyl transdermal patches with different designs. Permeation rates with cadaver skin as substrate were found not to change with patch age despite changing drug concentration in the EAL.     

HPLC法测定芬太尼透皮贴剂中芬太尼含量

目的：采用高效液相色谱法测定芬太尼透皮贴剂中芬太尼含量。方法：采用内标法,用甲醇混合液90min超声提取样品。色谱柱为Shim—pack CLC—ODS C18（250mm×4．6mm,5μm）,以甲醇溶液（取甲醇400ml,乙腈200ml,及冰醋酸0．6ml,混匀）-0．2％无水硫酸钠的醋酸胺（1—100）（7：3）并用冰醋酸调节pH（6．5±0．1）为流动相,流速1ml·min^-1,柱温25℃,检测波长为230nm。结果：芬太尼浓度在2．5～50μg·ml^-1。范围内线性关系良好（r=0．9999）,最低检测限0．1ng·ml^-1,样品24h稳定,平均回收率为100．9％,RSD为1．27％。结论：本方法简便快速,结果准确,重现性好,适用于芬太尼透皮贴中芬太尼含量的测定。     

硝酸甘油透皮给药系统体外释药速率测试方法的研究

随着透皮吸收研究的兴起,先后已有东茛菪碱、硝酸甘油、硝酸异山梨醇、可乐定和雌二醇等透皮给药系统进入市场。各生产单位对这些产品都有一定的质量控制项目,主要有药物含量、粘附力及药物释放速率,其中药物的释放速率是一个较重要的质量控制项目。虽然现在上市的透皮给药系统     

Pharmacokinetic Disposition of Multiple-Dose Transdermal Nicotine in Healthy Adult Smokers

The pharmacokinetics and cardiovascular effects of nicotine and its major metabolite, cotinine, were characterized during repeated once-daily application for 5 days of a 30-cm² nicotine transdermal system, Nicotine TTS (Habitrol), to nine healthy, black, adult, male smokers. Subjects abstained from smoking throughout the study. Pharmacokinetic analysis indicated that nicotine was delivered from Nicotine TTS for the 24-hr application period averaging 0.76 mg/ cm²/24 hr, and at a relatively constant rate compared to other modes of drug administration. The transdermal clearance of nicotine, 1351 ml/min, coincided with reported values following intravenous nicotine administration; however, the terminal-phase half-life, 5.0 hr, did not. An analysis of the components of variance contributing to the variability in nicotine delivery from repetitive application of Nicotine TTS indicated that the in vivo transdermal permeation of nicotine is rate limited by both the device and the intrinsic skin conductivity. Clinical cardiovascular side effects were negligible as an apparent result of subclinical vasopressive nicotine concentrations, although drug activity with regard to other effects was manifested.     

高效液相色谱法测定复方葛根透皮贴剂中葛根素的含量

目的:建立复方葛根透皮贴剂中葛根素的HPLC含量测定方法.方法:用Kromasil C<,18> column(4.60mm×150mm,5μm),流动相为甲醇-水-乙酸(25:75:0.01),检测波长为250nm.结果:线性范围在20～100μg/ml,葛根素的加样回收率为96.76%,RSD为0.95%(n=6)...     

芬太尼透皮贴剂治疗门诊癌痛患者53例

目的 观察中、重度门诊癌痛患者使用芬太尼透皮贴剂(多瑞吉)的镇痛效果及安全性.方法 选取53例伴有中、重度疼痛的恶性肿瘤惠者,按照WHO三阶梯癌痛治疗原则给予芬太尼透皮贴剂镇痛治疗,初始剂量为25～125 μg/h,最大剂量为350 μg/h.结果 疼痛程度评分均值治疗前为(7.23±1.28)分,治疗后为(1.75±1.26)分,治疗后疼痛程度显著减轻(P<0.01);总有效率为94.34%,其中中度缓解率22.64%,明显缓解率60.37%,完全缓解率11.32%,不良反应少且较轻微;治疗后患者的生活质量明显改善(P<0.05).结论 芬太尼透皮贴剂使用方便,疗效显著,不良反应少,能明显改善癌症惠者的生活质量,比较适合于门诊应用.