a a, b a
a a, b a
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发表时间：
1999
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通讯作者：
Kouji Nakamura;Y. Maitani;A. Lowman;K. Takayama;N. Peppas;T. Nagai
中科院分区：
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作者：
Kouji Nakamura;Y. Maitani;A. Lowman;K. Takayama;N. Peppas;T. Nagai
制备了新型聚甲基丙烯酸-聚乙二醇接枝共聚物（P(MAA-g-EG)）的微颗粒，研究了布地奈德在黏附、ph敏感共聚物上的吸收和释放及其在鼻腔给药中的应用。本研究的目的是研究布地奈德在体外从P（MAA-g-EG）中吸收和释放的动力学以及含布地奈德聚合物经鼻给药后的药代动力学。用不同的乙醇溶液考察了布地奈德在ph敏感聚合物中的负载。药物增溶需要乙醇，但在pH 7.2时阻碍水凝胶膨胀。在使用25%乙醇溶液的情况下，聚合物中获得了药物的最大负载。布地奈德从25%乙醇溶液中膨胀的聚合物中释放符合经典的菲克释放行为。经鼻给药含布地奈德P（MAA-g-EG）时，布地奈德的血药浓度在给药后约45分钟达到峰值后保持不变。1. 该途径允许小分子量药物的高吸收率，疏水性药物，避免第一次，对药物递送通过效果和易于患者给药非常感兴趣。近年来通过非注射途径。非亲本-然而，仍然存在一些问题，如药物给药途径低和初始的外侧途径，包括鼻腔给药，药物的快速吸收。这些问题有口腔[2]，肺部[3]和透皮途径[4]。通过使用渗透增强剂来克服，特别是通过鼻腔途径[5]和/或生物粘合剂载体给药。特别是氢-已被许多研究者研究过，因为后者已使用凝胶来增加药物吸收。高度可膨胀的阴离子水凝胶
Uptake and release of budesonide from mucoadhesive, pH-sensitive copolymers and their application to nasal delivery a a , b a Abstract Microparticles of novel, bioadhesive graft copolymers of polymethacrylic acid and polyethylene glycol (P(MAA-g-EG)) were prepared. The aims of this study were to investigate the uptake and release kinetics of budesonide from P(MAA-g-EG) in vitro as well as the pharmacokinetics following nasal administration of the polymer contained budesonide. The loading of budesonide into the pH-sensitive polymers was examined using various ethanol solutions. Ethanol was required for drug solubilization but hindered hydrogel swelling at pH 7.2. Maximum loading of the drug in the polymer was obtained using 25% ethanol solutions. The release of budesonide from the polymer swollen in 25% ethanol solutions obeyed classical Fickian release behavior after an initial rapid drug burst. For nasal administration of budesonide-containing P(MAA-g-EG) the plasma concentration of budesonide was kept constant following a peak concentration of the drug approximately 45 min after administration. 1. Introduction this route allows for high absorption of small molecular weight, hydrophobic drugs, avoidance of first There has been significant interest in drug delivery pass effects and ease in administration by patients. via nonparenteral routes in recent years. Nonparen-However, problems still exist such as low and initial teral routes for drug delivery include nasal [1], rapid absorption of the drug. These problems have buccal [2], pulmonary [3] and transdermal routes [4]. been overcome by the use of permeation enhancers In particular, drug administration by the nasal route [5] and / or bioadhesive carriers. In particular, hydro-has been examined by many investigators because gels have been used for the latter to increase drug absorption [6]. Highly swellable, anionic hydrogels that exhibit