吸收促进剂对复方替硝唑单向缓释膜中药物渗透性的影响

目的:建立复方替硝唑单向缓释膜体外透膜吸收的实验方法。方法:以恒温双室卡口渗透池为实验装置,以羊的肠粘膜为透粘膜屏障,采用紫外分光光度法检测替硝唑经粘膜的渗透量及透保护膜层的扩散量。结果:吸收促进剂能增加替硝唑的透粘膜吸收,以3%月桂氮卓酮 5%丙二醇效果最好。结论:吸收促进荆在不影响保护膜层的情况下能够提高药膜中替硝唑的单向透粘膜吸收。     

复方替硝唑单向缓释膜的研制及其生物相容性的研究

药膜用于口腔疾病的治疗取得了较好的效果,但用于治疗口腔粘膜疾病的常用膜剂,在口腔内被唾液所包围,有相当一部分药物会随唾液流走,影响了病灶部位药物有效浓度的维持。为此,我们研制成复方替硝唑单向缓释药膜并对其生物相容性进行了研究。1 仪器与材料     

复方替硝唑单向缓释药膜的研制及其释放特性

本实验以保护膜和药物膜制备复方替硝唑单向缓释药膜（以下简称药膜），并通过双室恒温卡口渗透池研究药膜及药膜透过粘膜的药物释放情况，结果表明：药膜有良好的单向释放及单向透过粘膜释放药物的特性。药物透过粘膜的量随时间的延长而增加，5min及60min透过粘膜释放药物的累积百分率分别为（15．29±5．77）％，（6．25±2．96）％。     

双戊烯对替硝唑透皮吸收促进作用的研究

目的：研究双戊烯对替硝唑的促透效果,为透皮促进剂的选择提供参考。方法：通过离体小鼠皮肤渗稼透释药实验,测定含不同浓度双戊烯和氮酮对替硝唑溶液促透效果。结果：不同浓度促透剂对替硝唑的透皮吸收促进效果大小顺序为3％双戊烯＞2％双戊烯≈4％氮酮＞3％氮酮。结论：3％双戊烯对替硝唑溶液有显著的透皮促进作用,与其他浓度的双戊烯和氮酮相比具有显著差异（P＜0.05)。     

替硝唑缓释药膜的研制与应用

目的：制备替硝唑缓释药膜并进行临床应用观察;方法：以替硝唑为主药,以聚乙烯醇为缓释剂,将药膜用于牙周袋或冠周的牙龈盲袋中,并与口服片剂作对照,进行了200例的临床观察。结果：膜剂与片剂具有同样显著的序效。结论：制剂使用方便,几无不良反应。     

牙用替硝唑缓释药膜的制备

目的：探讨替硝唑缓释药膜的制备方法。方法：用ＰＶＡ１７５０和ＰＶＡ１２４及ＣＭＣＮａ为膜材制备缓释药膜。结果：以膜材ＰＶＡ１７５０∶ＰＶＡ１２４∶ＣＭＣＮａ为１∶１∶２,加主药替硝唑制缓释药膜;以ＰＶＡ１７５０∶ＰＶＡ１２４∶ＣＭＣＮａ为１∶１∶１,加主药替硝唑制凝胶具缓释作用。结论：本方法所制的膜剂为骨架型缓释膜剂。     

混合秀皮促进剂对替硝唑凝胶透皮吸收作用的研究

目的;考察混合促进剂用月桂氮Ｚｈｏｕ酮和薄离对替硝唑透皮吸收作用的影响。方法;采用改良Ｆｒａｎｚ直立式释放池,以离体小白鼠皮肤为透皮屏障,使用不同浓度的混合月桂氮Ｚｈｏｕ酮的薄荷脑,测量替硝唑的透皮吸收量。结果：含０．５％,１．５％,２％,２．５％月桂氮Ｚｈｏｕ酮和薄荷脑的替硝唑凝胶与不含月桂氮Ｚｈｏｕ酮和薄荷脑的替硝唑凝胶间,其透皮吸收在２４ｈ后有显著差异。     

牙用替硝唑缓释药膜的制备及临床应用

目的 利用羧甲基纤维素钠和聚乙烯醇－１２４为载体,替硝唑为主药制成一种可吸收性牙周炎级释药膜。方法 采用膜剂制备方法制备此药膜,并用紫外分光光度法测定主药含量。结果 经药膜可贴、口含和插入牙周袋内。结论 临床应用表明,本品具有给药方便、疗效高、疗程短、无任何不良反应等优点。     

寡聚精氨酸壳聚糖对替硝唑透皮吸收促进作用的体内外研究

摘 要 目的： 考察寡聚精氨酸壳聚糖（CS-R9）的体内外透皮吸收促进作用。 方法: 以离体小鼠腹部全皮为皮肤屏障,采用Franz扩散池,以替硝唑（TNZ）溶液为阴性对照,氮酮TNZ溶液为阳性对照,考察CS-R9对TNZ溶液的体外透皮促进作用;以大鼠为实验动物,随机分为阴性组、氮酮组及实验组,分别给予TNZ溶液,氮酮TNZ溶液及CS-R9 TNZ溶液,于给药后不同时间点取血0.5 ml,用HPLC法测定其中TNZ的浓度,考察CS-R9对TNZ在体透皮吸收促进作用。结果:体外试验结果表明与阴性对照相比,CS-R9对TNZ具有显著的透皮吸收促进作用（P<0.05）,与同浓度氮酮作用差异无统计学意义（P>0.05）;体内透皮实验也表明CS-R9具有显著透皮吸收促进效果,与同浓度氮酮相比,差异无统计学意义（P>0.05）,且对药物具有一定的缓释作用。结论: CS-R9对TNZ的透皮吸收具有理想的促进作用,值得进一步研究。     

氮酮对替硝唑凝胶透皮吸收影响的实验研究

通过离体皮肤渗透释药实验,选择促替硝唑凝胶透皮吸收的最佳氮酮浓度。本实验证实,３％和５％氮酮对０．５％替硝唑凝胶有明显的促渗透作用,８～１０ｈ即可使替硝唑透皮释放率达到±１５％,可以认为３％和５％的氨酮是配制替硝唑外用制剂较为适宜的浓度。     

替硝喷口腔复合股的研制及质量控制

目的：建立替硝唑口腔复合膜的制备和质量控制方法。方法：采用聚乙烯醇17—88为成膜材料,制成由药膜层和覆盖层组成的替硝唑单向缓释复合膜。采用双波长紫外分光光度法检测替硝唑含量。结果：双波长紫外分光光度法有效消除辅料对替硝唑的干扰,在5．0-50．0μg／m1范围内具良好的线性(r＝0．9998);平均回收率为99．4％,RSD＝0．73％(n＝6);日内、日间RSD分别为1.01％和1.23％。结论：本制剂操作简单,质控方法准确、精密、稳定,适合医院制剂室生产。     

洛汀烟酸缓释片中洛伐他汀溶出度的测定

目的建立了洛汀烟酸缓释片中洛伐他汀溶出度测定方法。方法采用转蓝法,以2%十二烷基硫酸钠溶液1 000 m l(内含1.38 g磷酸二氢钠,并用1 mol.L-1氢氧化钠溶液调pH至7.0)为溶出介质,转速为75 r.m in-1,采用HPLC法检测。结果洛伐他汀在2.5~25 mg.L-1范围内峰面积与浓度呈良好的线性关系,r=0.9998,平均回收率为97.39%,RSD=1.68%(n=9),与国外同品种AdvicorTM中洛伐他汀溶出度一致。结论方法准确可靠,可用于洛汀烟酸缓释片的质量控制。     

Chitosans as absorption enhancers of poorly absorbable drugs: 3: Influence of mucus on absorption enhancement

Chitosans are potent nontoxic absorption enhancers after nasal administration but their effects on the intestinal epithelium in vivo has not been studied in detail. In this study, the effects of chitosans with varying molecular weights and degrees of acetylation on the absorption of a poorly absorbed model drug (atenolol) were studied in intestinal epithelial cell layers with or without a mucus layer and in an in situ perfusion model of rat ileum. The effects of the chitosans on epithelial morphology and release of lactate dehydrogenase (LDH) into the perfusate were investigated in the in situ model. The chitosans had pronounced effects on the permeability of mucus-free Caco-2 layers and enhanced the permeation of atenolol 10- to 15-fold, with different absorption kinetics for different chitosans, in accordance with previous results. In contrast, enhancement of atenolol absorption through rat ileum was modest. LDH release from the tissues perfused with chitosans did not increase, indicating that the chitosans were used at nontoxic concentrations. Morphological examination of the perfused ileal tissues revealed more mucus discharge from the tissues exposed to chitosans than from controls, which suggested that the discharged mucus may inhibit the binding of chitosan to the epithelial surface and hence decrease the absorption-enhancing effect. This hypothesis was supported by studies with intestinal epithelial HT29-H goblet cells covered with a mucus layer. The binding of chitosan to the epithelial cell surface and subsequent absorption-enhancing effects were significantly reduced in mucus-covered HT29-H cultures. When the mucus layer was removed prior to the addition of chitosan, the cell surface binding and absorption-enhancing effects of the chitosans were increased. We conclude that the modest absorption-enhancing effects of unformulated chitosan solutions in the perfused rat ileum are a result of the mucus barrier in this tissue. This effect may be overcome by increasing the local concentrations of both chitosan and drug, i.e,. through formulation of the chitosan into a particulate dosage form.     

HPLC测定阿司达莫缓释片的含量

目的 建立测定阿司达莫缓释片含量的方法.方法 采用HPLC法,色谱柱为Diamonsil C18(200 mm×4.6 mm,5μm),流动相为甲醇-0.05 mol·L-1磷酸二氢钾缓冲液(52:48),检测波长275 nm,柱温35℃,流速1.0 ml·min-1,以内标法计算阿司达莫缓释片的含量.结果 阿司匹林的线性范围为6～16μg·ml-1(r=0.9999),低、中、高3种浓度的平均回收率分别为101.4%±1.1%、97.1%±1.3%、94.2%±1.5%(n=3);双嘧达莫的线性范围为20～120 μg·ml-1(r=0.9998),低、中、高3种浓度的平均回收率分别为98.6%±2.3%、99.0%±1.6%、101.4%±2.3%(n=3).结论 所建方法简便、准确、专属性强,可用于阿司达莫缓释片的质量控制.     

盐酸氨溴索缓释片体内外相关性研究

目的考察盐酸氨溴索缓释片体外释放度与体内吸收的相关性。方法应用释放度测定法研究盐酸氨溴索缓释片体外释药行为 ,采用HPLC法测定盐酸氨溴索缓释制剂在家犬体内的血药浓度 ,按照Wagner Nelson公式计算药物的吸收分数。 结果 3种自制盐酸氨溴索缓释片与参比制剂生物等效 ,以药物累积吸收百分数 f(t)与相应时刻的体外累积释放百分数F(t)建立的一元线性回归方程 ,参比制剂与 3种自制制剂的体内外相关系数分别为 0 969、0 979、0 970和 0 983。结论盐酸氨溴索缓释片的体外释放度与体内吸收具有显著的相关性。     

Influence of some plant extracts on the transdermal absorption and penetration of marker penetrants

Context: Plant extracts are commonly used in a number of cosmetics and topical pharmaceuticals. The effects on such extracts on the subsequent dermal absorption and penetration of other cosmetic ingredients needs to be evaluated.

Objective: This study demonstrates the effect of some natural extracts routinely found in cosmetics on the dermal absorption and penetration of marker penetrants.

Methods: Aqueous ethanolic extracts of Gingko biloba, Lavendula angustifolia, Rosmarinus officinale, Mentha piperita, Matricaria recutita, Persea Americana, Avena sativa, Zingiber officinale were prepared. ¹⁴C-caffeine and ¹⁴C-salicylic acid were topically dosed with either 10% solutions of natural extracts or ethanol (control) using a flow through in vitro porcine skin diffusion system. Samples were analyzed with liquid scintillation counter. The parameters of flux, permeability, and percent dose absorbed/retained were calculated and compared.

Results: The dermal absorption of ¹⁴C-caffeine was significantly higher (p?≥?0.05) with avocado, chamomile, ginger and peppermint extract as compared to the control ethanol; while dermal absorption of ¹⁴C-salicylic acid was significantly greater with ginkgo and chamomile extract as compared to ethanol. Over four fold increase in flux and permeability of caffeine with avocado extract was observed while chamomile and peppermint extracts increased the flux and permeability of caffeine over three fold. Gingko and chamomile extracts increased salicylic acid’s flux and permeability by two fold. Sum of %dose skin residue?+?%absorption in receptor fluid for different extracts exhibited the similar trend as shown by flux and permeability. The other natural extracts tested did not produce statistically significant effects on dermal penetration parameters for both caffeine and salicylic acid (p?≥?0.05).

Conclusion: These results emphasize the influence of natural plant extracts on the transdermal penetration of hydrophilic (caffeine) and hydrophobic (salicylic acid) penetrants and thus warrants the consideration as to their safety in cosmetics and topical pharmaceuticals containing natural extracts.     

以玻璃酸钠为媒介对布洛芬体外释放及透皮吸收的影响

目的:研究以玻璃酸钠为媒介对布洛芬释放的影响因素和透皮吸收的影响。方法:配制不同的布洛芬溶液,采用改良的Franz扩散池,测定药物的体外渗透速率。结果:增加溶液的黏度能减慢布洛芬的释放速率,其释放速率随着玻璃酸钠浓度的增加而降低,随着布洛芬浓度的增加而提高。玻璃酸钠在水溶液中能抑制布洛芬的透皮吸收。结论:布洛芬的释放速率与溶液的黏度和药物浓度有关,玻璃酸钠是一种良好的外用药物媒介。     

复方广痛消水提物中3个成分的离体直肠吸收动力学研究

目的考察复方广痛消水提物中有效成分延胡索乙素(THP)、盐酸小檗碱(Ber)和芍药苷(Pae)在大鼠直肠段的吸收特性。方法采用大鼠离体非翻转肠囊模型,以LC-MS/MS对不同浓度的复方广痛消水提物中的THP、Ber和Pae进行检测,计算各成分的吸收速率常数(Ka),分析它们在直肠部位的吸收特征。结果不同浓度复方广痛消水提物中的THP、Ber和Pae在直肠段均为线性吸收,r2均>0.95。随着THP浓度的增高其Ka无显著变化(P>0.05);Ber和Pae的Ka随着浓度的增加而增大(P<0.01)。结论 THP在直肠的吸收呈现一级动力学特征,其吸收形式可能为被动扩散;而Ber和Pae的吸收形式并非简单的被动扩散,可能有转运载体的介导。