添加季铵盐离子液体润滑脂的摩擦学性能

以布洛芬为阴离子、季铵盐为阳离子制备了2种环境友好的季铵盐离子液体——三辛基十四烷基铵布洛芬(N88814-Ibu)和三辛基丁基铵布洛芬(N8884-Ibu),然后将其添加到PAO10复合锂基润滑脂(G)中,用四球摩擦试验机考察其摩擦学性能。结果表明,上述季铵盐离子液体添加到PAO10复合锂基润滑脂中表现出优异的减摩抗磨性能。N88814-Ibu-G的减摩抗磨性能优于N8884-Ibu-G,加入的质量分数为3%时,N8884-Ibu-G和N88814-Ibu-G的减摩抗磨性能最佳。EDS谱分析表明,季铵盐离子液体能够显著地降低摩擦磨损是因为在摩擦副表面形成了含N元素的化学反应膜。     

硅铁合金催化臭氧氧化水中布洛芬

近几年,在各地的饮用水中不断检测到微量布洛芬,其环境毒性引起了广泛关注。选用工业硅铁作为催化剂,催化臭氧氧化去除水中的布洛芬,并通过单因素试验,确定了反应体系的最佳条件。结果表明,在硅铁的作用下,催化臭氧氧化可以明显提高布洛芬的去除率。在硅铁投加量为1 g/L、水溶液初始pH值为8、臭氧浓度9.0 mg/L、布洛芬初始浓度为10 mg/L时,经过80 min,水样总有机碳(TOC)的去除率可达75.5%,较单独臭氧氧化提高了38.0%。将碳酸氢钠作为自由基抑制剂加入反应体系,可明显降低TOC的去除率,间接证明了催化臭氧氧化布洛芬的反应遵循自由基机理。     

可注射CS/PLLA-SA复合水凝胶的制备及载药性能

摘要：采用先核后臂法以及丁二酸酐(SA)羧基化修饰合成了末端为羧基的四臂星型聚乳酸（PLLA-SA），将其加入丙酮中得到PLLA-SA纳米分散液。壳聚糖（CS）与分散液通过静电作用自组装形成可注射CS/PLLA-SA复合水凝胶，并采用Zeta电位及激光粒度仪、FTIR和SEM等对PLLA-SA、分散液及水凝胶的组成、结构和性能进行表征与测定。PLLA-SA的最大Zeta电位值为-21.89 mV，分散液的平均粒径约为200 nm。在温度为15 ℃，PLLA-SA质量浓度为5 g/L，布洛芬（IBU）与PLLA-SA质量比为1:2，650 r/min搅拌1 h，550 r/min搅拌5 h的条件下，制备出载IBU的PLLA-SA分散液。将分散液与质量浓度为10 g/L的壳聚糖盐酸盐（CS-HCl）按体积比为7:3混合，快速自组装形成载药CS/PLLA-SA复合水凝胶，包封率和载药量分别达到85.34%和28.46%。体外药物释放结果表明，可注射载药水凝胶对IBU具有明显的缓释作用，30 h内药物的累积释放率可达到95.81%。     

Evaluation of the Structural Modification of Ibuprofen on the Penetration Release of Ibuprofen from a Drug-in-Adhesive Matrix Type Transdermal Patch

This study aimed to evaluate the effect of chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU] from the acrylic pressure-sensitive adhesive used as a drug-in-adhesives matrix type transdermal patch. The active substances tested were ibuprofen salts obtained by pairing the ibuprofen anion with organic cations, such as amino acid isopropyl esters. The structural modification of ibuprofen tested were Ibuprofen sodium salt, [GlyOiPr][IBU], [AlaOiPr][IBU], [ValOiPr][IBU], [SerOiPr][IBU], [ThrOiPr][IBU], [(AspOiPr)₂][IBU], [LysOiPr][IBU], [LysOiPr][IBU]₂, [PheOiPr][IBU], and [ProOiPr][IBU]. For comparison, the penetration of unmodified ibuprofen and commercially available patches was also investigated. Thus, twelve transdermal patches with new drug modifications have been developed whose adhesive carrier is an acrylate copolymer. The obtained patches were characterized for their adhesive properties and tested for permeability of the active substance. Our results show that the obtained ibuprofen patches demonstrate similar permeability to commercial patches compared to those with structural modifications of ibuprofen. However, these modified patches show an increased drug permeability of 2.3 to even 6.4 times greater than unmodified ibuprofen. Increasing the permeability of the active substance and properties such as adhesion, cohesion, and tack make the obtained patches an excellent alternative to commercial patches containing ibuprofen.     

Investigation of the tableting behavior of Ibuprofen DC 85 W

The aim of the present study was to investigate the tableting behavior of Ibuprofen DC 85?W with special focus on the tablet disintegration time, the tablet crushing strength, and the sticking tendency to punch surfaces. To simulate production conditions, tableting was conducted on a rotary press, equipped with three compaction stations. An I-optimal design of experiments was used to analyze the influence of the pre-compaction, the intermediate compaction, and the main compaction force on the two responses: tablet disintegration time and crushing strength. It was shown that Ibuprofen DC 85?W showed a good tableting behavior with regard to both responses. The tablet disintegration was considerably affected by the maximum compaction force applied, but was also slightly affected by preceding compaction events. The tablet crushing strength was mainly affected by the maximum applied compaction force independent of the order of these forces. The sticking tendency of Ibuprofen DC 85?W was compared with that two other ibuprofen powder formulations in long-term tableting runs. Compared to the other two formulations, sticking was considerably lower with Ibuprofen DC 85?W. The sticking tendency was not influenced by the addition of an intermediate compaction force, but was remarkably reduced by the choice of the punch tip coating.     

Hybrid transdermal drug delivery patch made from poly(p‐phenylene vinylene)/natural rubber latex and controlled by an electric field

A flexible, natural rubber (NR) patch was developed for electrically controllable transdermal drug delivery. NR latex was crosslinked at various crosslinking ratios under the UV curing method. Ibuprofen (Ibu) was the model drug and was used as the dopant for poly(p‐phenylene vinylene) (PPV) acting as the drug encapsulating host. For the pristine Ibu‐loaded NR patch, the amount of Ibu permeation increased with decreasing crosslink density and increasing electrical potential. For the Ibu‐doped PPV/NR patch, the amount of Ibu release?permeation also increased with increasing electrical potential and was higher than that of the pristine NR matrices. Without an applied electric field, the drug remained attached to the PPV during an initial period of 6 h. Under an applied electric field, the oxidation state of the conductive polymer was altered, the iontophoretic effect, pore formation in the NR matrix, expansion of the pore size in hair follicles and PPV chain expansion combined to increase the Ibu release?permeation amount. Thus, the flexible PPV/NR transdermal drug delivery patch was demonstrated to be effective in drug release?permeation based on the strength of the electrical potential, the crosslinking density and the presence of PPV as the encapsulation host. © 2018 Society of Chemical Industry     

Influence of probe-sonication process on drug entrapment efficiency of liposomes loaded with a hydrophobic drug

Since probe-sonication is commonly used to homogenize liposomal formulations, it is necessary to investigate its influence on drug entrapment efficiency (EE) of liposomes. In this study, ibuprofen-loaded liposomes (IBU-Lip) dispersion was prepared from ibuprofen (IBU), soy phosphatidylcholine (SPC) and cholesterol (Chol) by thin film hydration and probe-sonication process. The influences of sonication time and power on EE were studied. Also, the effects of SPC-to-Chol ratio and drug-to-lipid ratio on EE were demonstrated. The results indicated that increasing sonication time or decreasing drug-to-lipid ratio could increase EE. Additionally, EE first increased then decreased as sonication power increased or SPC-to-Chol ratio decreased.     

Degradation of the emerging contaminant ibuprofen in water by photo-Fenton

In this study the degradation of the worldwide Non-Steroidal Anti-Inflammatory Drug (NSAID) ibuprofen (IBP) by photo-Fenton reaction by use of solar artificial irradiation was carried out. Non-photocatalytic experiments (complex formation, photolysis and UV/Vis-H₂O₂ oxidation) were executed to evaluate the isolated effects and additional differentiated degradation pathways of IBP. The solar photolysis cleavage of H₂O₂ generates hydroxylated-IBP byproducts without mineralization. Fenton reaction, however promotes hydroxylation with a 10% contamination in form of a mineralization. In contrast photo-Fenton in addition promotes the decarboxylation of IBP and its total depletion is observed. In absence of H₂O₂ a decrease of IBP was observed in the Fe(II)/UV-Vis process due to the complex formation between iron and the IBP-carboxylic moiety. The degradation pathway can be described as an interconnected and successive principal decarboxylation and hydroxylation steps. TOC depletion of 40% was observed in photo-Fenton degradation. The iron-IBP binding was the key-point of the decarboxylation pathway. Both decarboxylation and hydroxylation mechanisms, as individual or parallel process are responsible for IBP removal in Fenton and photo-Fenton systems. An increase in the biodegradability of the final effluent after photo-Fenton treatment was observed. Final BOD₅ of 25 mg L⁻¹ was reached in contrast to the initial BOD₅ shown by the untreated IBP solution (BOD₅ < 1 mg L⁻¹). The increase in the biodegradability of the photo-Fenton degradation byproducts opens the possibility for a complete remediation with a final post-biological treatment.     

高选择性脂肪酶的筛选及其拆分布洛芬

为了实现脂肪酶在有机相中对外消旋布洛芬的高效拆分,筛选得到了一株具有高立体选择性的脂肪酶产生菌-扩展青霉TS414(Penicillium expansum TS414). 实验探讨了水分、温度、有机溶剂、酶浓度、醇结构和醇浓度对酶促拆分反应的影响,确立了酯化反应的最佳反应体系：布洛芬6.46 mmol/L,脂肪酶53.3 mg/mL,正丙醇40 mmol/L,异辛烷15 mL,水0.5%(j),60℃条件下反应50 h. 在此条件下,拆分反应的转化率和对映体选择率分别为42%和429.63. 结果表明,Penicillium expansum TS414脂肪酶是一种较为理想的用于外消旋布洛芬拆分的工具酶,在布洛芬手性拆分方面具有广阔的应用前景.     

手性溶剂萃取分离布洛芬对映体

研究了布洛芬对映体在含有疏水性L-酒石酸酯的1,2-二氯乙烷溶液及甲醇水溶液两相中的萃取分配行为,考察了不同烷基链长的L-酒石酸酯、D-酒石酸酯以及L-酒石酸酯的浓度、有机溶剂的种类和溶解布洛芬的甲醇水溶液浓度对分配系数K和分离因子α的影响。实验表明,L-酒石酸酯与布洛芬Ⅱ对映体形成的复合物稳定性比与布洛芬Ⅰ对映体形成的复合物稳定性要大,而D-酒石酸酯的萃取性能则与此相反,它与布洛芬Ⅰ对映体形成的复合物稳定性比与布洛芬Ⅱ对映体形成的复合物稳定性要大。有机溶剂的萃取性能为醇＞1,2-二氯乙烷＞烷烃,随着溶解布洛芬的甲醇水溶液中甲醇浓度的增大,分配系数K和分离因子α均降低,当甲醇的浓度为10%时,可以得到最佳的K和α。随着L-酒石酸酯浓度的提高,分配系数K和分离因子α先增大后减小,当L-酒石酸酯的浓度约为0.2 mol·L-1时,K和α达到最大值;L-酒石酸酯的碳链长度对分配系数K和分离因子α也有很大的影响。