四元胶乳互穿聚合物网络的组成对其性能的影响

用分步乳液聚合法合成了具有核壳结构的胶乳互穿聚合物网络ＬＩＰＮ（ＰＭＭＡ－ＰＳ）／（Ｐｎ－ＢＡ－ＰＡＡ）；讨论了ＬＩＰＮ组成对乳液与膜性能的影响，提出了四元ＬＩＰＮ核壳结构的基本轮廓，探讨了软硬单体最佳配比及丙烯酸单体用量。     

聚乳酸酮洛芬微球的制备及其体外释放度

制备了生物可降解的材料聚乳酸,用粘度法测定其分子量,并选用Ａ、Ｂ、Ｃ三种不同分子量的聚乳酸为药物的载体,制备了酮洛芬微球（ＡＳ,ＢＳ,ＣＳ）,测定其粒径和体外溶出速率。结果表明催化剂四苯基锡用量增加,所得的聚乳酸分子量增加,而制备酮洛芬微球的聚乳酸分子量越大,其微球粒径越大,溶出速率越小。     

Effect of diet on the single- and multiple-dose pharmacokinetics of sustained-release ketoprofen

The indirect effect of diet on the single-and multiple-dose pharmacokinetics of sustained-release ketoprofen was studied in 16 healthy male volunteers. In an open, cross-over design, 200 mg ketoprofen was administered as a gastric-juice-resistant, sustained-release tablet once daily during two periods of 5 days. A low-calorie/low-fat diet (LCFD) was given in the first period and a high-calorie/high-fat diet (HCFD) in the second period. The first meal on each day was given 4 h after drug intake. Ketoprofen plasma concentrations were measured over 24 h after the first dose on day 1 and over 36 h after the final dose on day 5 of each period.On average, plasma concentrations of ketoprofen were higher with the LCFD than with the HCFD. With the HCFD there was a tendency to longer absorption-lag times on day 5. The maximum concentration and the area under the curve over one 24-h dosage period (AUC_0–24) were significantly higher with the LCFD, both on day 1 and on day 5. For AUC_0–24 the differences were on average 15% (day 1) and 24% (day 5). The same tendency was observed for the amount excreted in urine over 24 h (A_e), but the difference was only significant on day 1 (14%). The elimination rate constant (K) and the mean residence time were similar for the two diets, both on day 1 and on day 5.From these results, we conclude that there was an acute indirect effect of diet when a meal was had 4 h after intake of the medication. This resulted in a greater extent of ketoprofen absorption with the LCFD than with the HCFD. The absorption rate was apparently not influenced by this acute effect. The longer gastric residence time of ketoprofen with the HCFD may be the result of a long-term indirect effect on gastric emptying rate. If the extreme difference between the diets in this study is taken into account, it seems unlikely that the observed indirect effects have implications for clinical practice.     

口腔溃复平膜剂的研究

目的：优选口腔溃复平膜剂（黄柏，龙胆草，青黛等）最佳处方。建立膜剂中盐酸小檗碱含量的测定方法。方法：以膜剂外观和融化时间为指标。采用L9（3^4)正交试验筛选处方，反相液相色谱法测定膜剂中盐酸小檗碱的含量。结果：膜剂最佳处方为：中药提取液40mL,PVA0.588:PVA1788为4：1.5，甘油含量8%，CMC-Na0.25g；测定方法中盐酸小檗碱的平均回收率为97.7%。结论：膜剂的外观（包括可塑性，粘附性及抗拉强度）和融化时间等指标均符合质量标准的要求，采用反相液相色谱法可有效控制溃复平膜剂中盐酸小檗碱的含量。     

An Investigation into the Changes in Airway Dimension and the Efficacy of Mandibular Advancement Appliances in Subjects with Obstructive Sleep Apnoea

Abstract

This prospective clinical study evaluates a group of 37 male Caucasians with obstructive sleep apnoea for changes in airway dimension and the efficacy associated with the use of mandibular advancement splints. Lateral skull radiographs were obtained with the subjects—upright in occlusion, supine in occlusion, and supine in protrusion. Each radiograph was traced and digitized, and changes in mandibular position, airway dimensions, and hyoid were examined. Subjects were invited to complete pre- and post-treatment questionnaires, and interviewed following fitting of a removable Herbst mandibular advancement splint.

Significant changes were recorded in the airway dimensions in response to both a change in position, from upright to supine, and in response to mandibular advancement. A compliance rate of 76 per cent was achieved with no reported serious complications associated with the use of mandibular advancement devices.     

RP-HPLC法测定酮洛芬凝胶中药物含量

目的建立酮洛芬凝胶中药物含量测定的方法,并明确光照对含量测定的影响。方法采用Diamonsil ODS柱(4.6 mm×200 mm,5μm);流动相为0.01 mol/L磷酸二氢钾溶液(用磷酸调pH值至3.0)-乙腈(50∶50),流速1.0 mL/min,检测波长为255 nm,柱温为室温。结果在本试验条件下,酮洛芬凝胶中与辅料及有关物质分离度均符合要求,酮洛芬进样量在0.525¹.575μg范围内线性关系良好(r=0.999 9,n=5),平均回收率为98.41%,RSD为1.35%(n=3)。经光照,酮洛芬含量明显降低,杂质A明显增加,杂质A为酮洛芬的光照降解产物。结论本方法简单、快捷,可用于酮洛芬凝胶中药物含量的测定。     

酮洛芬生产场所多组分有机溶剂同时测定

[目的]建立毛细管气相色谱法,对酮洛芬生产场所空气中多组分有机溶剂进行同时测定。[方法]采用CBP20毛细管柱分离,在程序升温条件下,同时测定混合溶剂。[结果]该法分离效果好,检出限在1.7～17.8μg/ml之间,相关系数在0.9990～0.999 9之间,变异系数在1.9%～5.7%之间。[结论]方法有较好的灵敏度和准确度,提高了项目的采样和检测效率。     

酮洛芬巴布剂的制备及其经皮体外渗透试验

目的:研究酮洛芬巴布剂的最优处方并考察其影响因素。方法:采用正交试验法设计处方,拉力机测定粘着强度,利用Franz扩散池考察体外经皮渗透性。结果:筛选出最优处方,其粘着强度为40N,稳态流量为9·72μg/(cm2·h)。结论:建立的巴布剂制备工艺合理、稳定,粘着强度和透皮效果为其主要质量影响因素。     

Microspheres for colonic delivery of ketoprofen-hydroxypropyl-β-cyclodextrin complex

A new multiparticulate system, with the potential for site-specific delivery to the colon, has been developed using ketoprofen as model drug. The system simultaneously exploits cyclodextrin complexation, to improve drug solubility, and vectorization in microspheres (MS) based on Ca-pectinate and chitosan. The effect of complexation with hydroxypropyl-β-cyclodextrin (HPβCyd) and of chitosan presence on drug entrapment efficiency and release properties, as well on the drug permeation rate across Caco-2 cells has been investigated. Solid-state interactions between the components have been investigated by FTIR spectroscopy, differential scanning calorimetry and X-ray powder diffractometry. The morphology of MS was examined by scanning electron microscopy. Release studies revealed a different behaviour for MS containing drug alone or as complex: drug alone was released faster than in the presence of cyclodextrin from MS without chitosan, due to a reservoir effect. The opposite was found for MS containing chitosan, due to a competition effect between polymer and drug for the cyclodextrin. Cytotoxicity tests demonstrated the safety of these formulations. Permeation studies showed an increased permeation of the drug formulated as MS, particularly marked when it was used as complex, thus revealing an enhancing power of both cyclodextrin and chitosan with a synergistic effect in improving drug permeation.