痛立消涂膜剂的透皮吸收研究

对痛立消涂膜剂透皮吸收进行了研究,采用薄层扫描仪对其东莨菪碱进行测定。     

创伤涂膜剂的体外透皮吸收

目的:通过大鼠离体皮肤的体外透皮试验,考察创伤涂膜剂中的3种药物成分在皮肤内的渗透过程,明确药物的释放机制,为临床确定用药剂量和用药时间提供实验依据。方法:采用Franz扩散池法,以SD大鼠背部皮肤作为渗透屏障,采用高效液相色谱法测定3种药物的含量,以单位面积累积渗透量对时间拟合,分别考察:3种药物在大鼠背部完整皮肤和破损皮肤的透皮吸收特性。结果:替硝唑、盐酸达克罗宁、醋酸氯己定完整皮肤24 h累积渗透率分别为35.3%,18.0%,0%,破损皮肤24 h累积渗透率分别为78.6%,63.8%,5.2%。药物成分的释放特征不同,替硝唑和盐酸达克罗宁对破损皮肤的释放曲线符合Higuchi模型,对完整皮肤的释放曲线符合零级模型,醋酸氯己定的累积渗透量较低。结论:替硝唑和盐酸达克罗宁在完整皮肤和破损皮肤均可不同程度透过,醋酸氯己定的累积渗透量较低,仅发挥局部抗菌作用。     

中药冰片—水杨酸低共熔物透皮吸收研究

某些固体有机药物有和水杨酸类生成低共熔物的特点。本文利用冰片(borneol简称BO)和水杨酸(salicylic acid简称SA)生成低共熔物性质,探讨了BO-SA低共熔物透过大白鼠离体皮肤的效果。实验结果表明BO-SA低共熔物比BO的透皮吸收有明显的增加,为研制冰片透皮吸收制剂提供了方法。     

复方苯甲酸醑中水杨酸透皮吸收实验研究

采用简单扩散小室装置,研究水溶性氮酮（Ａｚｏｎｅ）对复方苯甲酸醑中水杨酸透皮吸收的影响。结果表明：水溶性氮酮能明显地促进水杨酸的透皮吸收,用抛物线拟合法求得氮酮对水杨酸以吸收促进作用的最佳浓度０．６４±０．１％。     

薄荷醇和氮酮对水杨酸体外透皮吸收的促进作用

目的 研究薄荷醇和氮酮单独使用及合用时对水杨酸的促透作用。方法采用离体鼠皮作透皮吸收试验。结果 薄荷醇对水杨酸的促透作用强干氮酮。而两药合用时的促透作用并不比分别使用时的促进效果好，在合用浓度较高时，甚至表现促透作用降低。     

混合促透剂对肤康涂膜剂中水杨酸和酮康唑透皮效果的影响

目的:考察混合促透剂月桂氮(廾卓)酮和薄荷脑对肤康涂膜剂中水杨酸和酮康唑透皮促进作用的影响.方法:采用简单小室法,以离体雄性大鼠皮肤为透皮屏障,用高效液相色谱法测定体外接受液中水杨酸和酮康唑的含量,计算各时间点的累积透皮率.结果:含2%月桂氮(廾卓)酮和2%薄荷脑的涂膜剂与不含月桂氮(廾卓)酮的涂膜剂相比较,其透皮促进作用在6 h后则呈显著性差异(P＜0.01).结论:不同浓度的混合促透剂均可不同程度地提高水杨酸和酮康唑的透皮促进作用,其中以2%月桂氮(廾卓)酮和2%薄荷脑组成的混合促透剂作用最显著.     

雷公藤涂膜剂中阿魏酸体外透皮吸收特性

目的研究复方雷公藤涂膜剂中阿魏酸的体外透皮吸收特性,为阐明复方雷公藤涂膜剂的作用机制提供实验依据.方法采用静态扩散装置,用HPLC测定扩散池中不同时间阿魏酸的含量,计算其渗透系数和累积透皮吸收百分率.结果阿魏酸的渗透系数为0.25*h-1,7h内阿魏酸的累积透皮吸收百分率为15.4%.结论雷公藤涂膜剂中阿魏酸的透皮吸收符合Fick扩散定律,其渗透系数为0.25*h-1;提示阿魏酸可从雷公藤涂膜剂中溶解出来并透过皮肤发挥作用.     

透皮促进剂在透皮释放给药系统中的应用

本文介绍了透皮释放给药系统的特点,阐明了透皮促进剂的作用及其机理;介绍了国内外常用的透皮促进剂,综述其在透皮释放给药系统中合理知科学的应用。同时展示了透皮促进剂的新发展和药物增加透皮吸收的新研究。     

多塞平透皮剂的初步体外透皮试验

以鼠皮为材料测定多塞平（Ｄｏｘｅｐｉｎ）透皮剂体外透皮释放率。结果表明累积释放率和释放量２４ｈ分别为６．１３±５．５７％及３．０７±２．７ｍｇ；４８ｈ分别为９．９４±６．７％及４．９７±３．３５ｍｇ。此结果提示用多塞平透皮剂治疗荨麻疹可达到多塞平有效血浓度。     

复方苯甲酸醑中水杨酸透皮吸收实验研究

采用简单扩散小室装置 ,研究水溶性氮酮 (Azone)对复方苯甲酸醑中水杨酸透皮吸收的影响。结果表明 :水溶性氮酮能明显地促进水杨酸的透皮吸收 ,用抛物线拟合法求得氮酮对水杨酸透皮吸收促进作用的最佳浓度为 0 64± 0 1 %。     

茶碱透皮贴片的制备及其体外渗透性研究

目的:制备茶碱透皮贴片,并考察其体外经皮渗透性。方法:以丙烯酸酯压敏胶为骨架材料,月桂氮酮和丙二醇为促渗剂,用离体人皮和Franz扩散池作为体外经皮释药模型,研究茶碱贴片体外渗透性。结果:茶碱贴片中的药物经皮渗透符合零级动力学,4%月桂氮酮和20%丙二醇有较好的促进渗透作用,其增渗倍数分别为不含促渗剂的茶碱对照贴片的2.30和2.04倍。结论:茶碱贴片体外经皮渗透作用较好。     

Preliminary evaluation of the correlation between in vitro release and in vivo bioavailability of two aminophylline slow-release tablets

An in vitro dissolution study has been carried out with a USP rotating paddle apparatus using the stepwise pH change method. The dissolution kinetics of two different matrix-type aminophylline slow-release (SR) tablets were compared. both aminophylline SR tablets show similar release rates and slow release behavior. The bioavailability of these two aminophylline SR tablets was also evaluated in eight healthy male Chinese volunteers and correlated with in vitro dissolution results by moment analysis. The preliminary results suggest that there is no evidence indicating that the two different matrix types of aminophylline SR tablets are not bioequivalent, and a good in vitro-in vivo correlation for these aminophylline SR tablets may therefore be presumed.     

氨甲环酸纳米乳膏的制备及体外透皮效果评价

目的设计制备氨甲环酸纳米乳膏(TA-NC),并观察其体外透皮效果。方法采用高压均质法制备氨甲环酸纳米乳,并进一步制得TA-NC,检测TA-NC粒径、微观结构及包封率。以裸鼠皮肤为模型,通过体外透皮吸收实验、离体皮肤组织滞留实验考察TA-NC的体外透皮效果;以尼罗红为荧光探针制备荧光标记TA-NC,共聚焦显微镜观察其促透进入真皮层的效果。并考察TA-NC的6个月加速稳定性。结果制备的TA-NC粒径为(109.9±7.4)nm,形态圆整,分布均匀;包封率为(90.13±2.90)%。体外透皮吸收实验中,TA-NC组给药6 h药物皮肤中的累积滞留量达饱和状态,24 h累积透过量达(163.9±7.4)μg·cm-2;TA水溶液组皮肤的滞留量在20μg·cm-2以下,24 h累积透过量为(15.9±0.8)μg·cm-2,组间差异非常显著(P<0.01)。共聚焦显微镜下,荧光素TA水溶液组仅表皮角质层有荧光,荧光标记的TA-NC经皮吸收后可透过角质层和表皮层到达真皮层,且TA-NC粒径越小透皮能力越强。6个月内TA-NC制剂外观性状、有关物质、含量、粒度等均未发生明显改变。结论 TA-NC制备简单,透皮效果显著,稳定性好。     

In vitro and in vivo evaluation of the transdermal iontophoretic delivery of sumatriptan succinate.

The objective was to evaluate the transdermal delivery of the 5-HT(1B/1D) agonist, sumatriptan from an iontophoretic patch system, in vivo. Initial in vitro experiments were conducted to optimize formulation parameters prior to iontophoretic delivery in Yorkshire swine. It was found in vitro that increasing drug load in the patch from 9.7 to 39 mg had no statistically significant effect on cumulative delivery (cf. 305.6+/-172.4 vs. 389.4+/-80.4 microg cm(-2), respectively). However, for a given drug load (39 mg) increasing formulation pH from pH 4.7 to 6.8 significantly increased the cumulative amount of sumatriptan delivered across the skin (389.4+/-80.4 vs. 652.4+/-94.2 microg cm(-2)). A biphasic current profile comprising intensities of 1.8 mA from t=0 to t=180 min and 0.8 mA from t=181 min to t=360 min was used for the in vivo experiments. Drug levels in the blood were 13.7+/-4.5 and 53.6+/-10.2 ng ml(-1) at the 30 and 60 min time-points, rising to 90-100 ng ml(-1) during the 90-180 min time-period. The in vivo results show that the pharmacokinetics following transdermal iontophoretic delivery are comparable to those after oral, nasal or rectal administration, but do not match those upon subcutaneous injection.     

Salicylic acid and PEG-contained polyanhydrides: synthesis, characterization, and in vitro salicylic acid release

Poly[bi(o-carboxyphenyl)adipate-polyethylene glycol] anhydrides—P(BOCA-PEG)—polymeric drugs were synthesized and characterized by Fourier transformed infrared spectroscopy, NMR, DSC, gel permeation chromatography etc. Salicylic acid loading efficiency of these polymers ranged from 43.5% to 71.3%, which was much higher than that of other polymeric drugs with salicylic acid. The in vitro release of salicylic acid from the polymers was carried out in buffer solutions with different pH values and rat gastrointestinal contents. The results showed the release rate of salicylic acid increased with the increase of PEG content in the polymers and the increase of pH value of degradation buffer solution. The rat cecal contents also greatly promoted the release of salicylic acid. In 0.1M phosphate buffer solution at pH8.0, 37°C containing 5% rat cecal contents, P(BOCA-PEG200)(80:20) had 15% salicylic acid released in 21 hr, indicating its potential use in colon-specific salicylic acid delivery.     

Development and evaluation of dual controlled release microballoons containing riboflavin and citric acid: in vitro and in vivo evaluation

The objective of this work was to optimize the incorporation of citric acid (CA) in the gastroretentive microballoons containing riboflavin (RF) in order to achieve dual controlled release system and consequently enhance the bioavailability of RF. Microballoons of 739?±?1.9?µm containing RF–CA were prepared by modified emulsion solvent diffusion method and were evaluated both for in vitro and in vivo performance. RF–CA microballoons with 22.8% RF and 37.2% CA entrapped in the shell matrix composed of Eudragit® S 100 and HPMCK4M and in vitro buoyancy of 86.0?±?0.88% (RCM3) was selected for further studies. RCM3 exhibited biphasic, pH-dependent in vitro dual controlled release of RF (0.9933–0.9962) and CA (0.996–0.9984) beyond 1?h in both simulated fasted and fed state conditions. RCM3 was able to achieve higher mean plasma concentrations than reference formulation RM2 (RF microballoon) both in fed and fasted states in rabbits. The mean AUC_0–24 estimate of RCM3 was 55% higher in fasted state (p?<?0.01) and about 51% higher in fed state (p?<?0.05) relative to mean AUC_0–24 from RM2 formulation. Conclusively, enhancement in RF in the presence of CA along the entire plasma level curve suggests a possibility of reduction in dosing frequency. This controlled release drug delivery system of RF, where CA is incorporated in the microballoons can be easily encapsulated in capsule dosage form negating the need of CA solution as vehicle for administration of RF microballoons.     

Development and evaluation of dual controlled release microballoons containing riboflavin and citric acid: in vitro and in vivo evaluation

The objective of this work was to optimize the incorporation of citric acid (CA) in the gastroretentive microballoons containing riboflavin (RF) in order to achieve dual controlled release system and consequently enhance the bioavailability of RF. Microballoons of 739?±?1.9?μm containing RF-CA were prepared by modified emulsion solvent diffusion method and were evaluated both for in vitro and in vivo performance. RF-CA microballoons with 22.8% RF and 37.2% CA entrapped in the shell matrix composed of Eudragit? S 100 and HPMCK4M and in vitro buoyancy of 86.0?±?0.88% (RCM3) was selected for further studies. RCM3 exhibited biphasic, pH-dependent in vitro dual controlled release of RF (0.9933-0.9962) and CA (0.996-0.9984) beyond 1?h in both simulated fasted and fed state conditions. RCM3 was able to achieve higher mean plasma concentrations than reference formulation RM2 (RF microballoon) both in fed and fasted states in rabbits. The mean AUC(0-24) estimate of RCM3 was 55% higher in fasted state (p?相似文献