Muco-Adhesive Liquid Ophthalmic Vehicles - Evaluation of Macromolecular Ionic Complexes of Pilocarpine

Abstract

Pilocarpine (Pi), a widely used anti-glaucoma drug, is characterized by a very low bioavailability, due to poor corneal penetration and extensive precorneal loss. Purpose of the present study was the preparation and “in vivo” evaluation of a series of liquid formulations containing salts (or ionic complexes) of Pi with soluble polyanionic polymers of natural, synthetic or semi-synthetic origin. It was speculated that since to some of the polymers have been attributed muco-adhesive properties, they might favour the preocular retention of the ionically bound drug, and enhance its bioavailability. The polymers submitted to investigation were a) hyaluronic acid (HA); b) poly-(galacturonic acid) (PGA); c) Mesoglycan (MG, a complex mixture of mucopolysaccharides); d) Carboxymethylchitin (CMCh) and d) two poly(acrylic acids) of different molecular weight (PAA1 and PAA2). Aqueous solutions of the Pi polymer salts, each containing 1.53% w/w Pi base (equivalent to 2.0% Pi nitrate) were tested for miotic activity in albino rabbits, using as reference an aqueous, 2% solution of Pi nitrate, either as such or viscosized with 1.5 and 5.0% poly(vinyl alcohol), (PVA). All polymeric solutions enhanced, in some cases to a statistically significant extent, the bioavailability of the drug with respect to the reference solutions. The relevance of viscosity effects, and of possible muco-adhesive phenomena to the bioavailability of Pi from the salt-vehicles are discussed     

Stability of Pilocarpine Ophthalmic Solutions

The stability of pilocarpine and pilocarpine-timolol eyedrop preparations available on the Argentine market was studied. A high-performance liquid chromatographic method that allows the estimation of pilocarpine in the presence of degradation products was used for the study according to the preestablished design. It was found that pilocarpine solutions are stable, while pilocarpine in association with timolol shows significant degradation.     

Stability of Pilocarpine Ophthalmic Solutions

The stability of pilocarpine and pilocarpine-timolol eyedrop preparations available on the Argentine market was studied. A high-performance liquid chromatographic method that allows the estimation of pilocarpine in the presence of degradation products was used for the study according to the preestablished design. It was found that pilocarpine solutions are stable, while pilocarpine in association with timolol shows significant degradation.     

磷酸酯基离子液体对木质素的溶解性能

合成表征了5种磷酸酯类离子液体,并将其用于溶解木质素。结果表明,离子液体1,3-二甲基咪唑磷酸甲酯盐[Mmim]DMP对木质素的溶解性能最佳,在70℃搅拌120 min,木质素溶解度可达45%。扫描电镜(SEM)、X射线衍射(XRD)和红外光谱(FT-IR)表征结果显示离子液体在木质素溶解过程中并未使木质素发生衍生化反应,但经离子液体溶解再生后,木质素的形貌均发生了显著变化,离子液体溶解性能越强,所得再生木质素颗粒越均匀、分散性越好且弥散衍射特征越强烈。此外,回收所得离子液体重复使用5次后,对木质素仍有较好的溶解性能。     

离子液体对酶原位降解微晶纤维素的促进作用

构建离子液体1-乙基-3-甲基咪唑醋酸盐[EMIM]OAc与纤维素的均相体系,采用酶原位降解法,以3,5-二硝基水杨酸法表征降解效果,考察各因素的影响确定最佳工艺条件:6.6 g 3%(质量分数)原溶液与4 mL pH4.6柠檬酸钠缓冲溶液组成均相体系、6 mg酶、50℃、26 h,酶解率迭78.5%,比非均相下提高了...     

氨基酸离子液体对壳聚糖溶解性能的影响

合成了一系列氨基酸类离子液体,从中筛选出对溶解壳聚糖具有良好性能的离子液体——甘氨酸盐酸盐离子液体。在常温常压下考察了该离子液体1%～10%水溶液对壳聚糖的溶解能力,溶解壳聚糖能力最大能达到6.32%(质量分数,下同)。对离子液体重复使用5次后,溶解能力没有明显下降。采用X射线衍射(XRD)和红外光谱(FT-IR)对再生的壳聚糖进行表征,结果表明,壳聚糖在溶解过程中没有发生衍生化。甘氨酸盐酸盐离子液体水溶液是壳聚糖的良溶剂。     

咪唑基离子液体对聚丙烯抗静电性能的影响

以咪唑基离子液体(im i-IL)为抗静电剂与聚丙烯(PP)熔融共混制备出PP/im i-IL共混复合材料,并对材料的抗静电性能、抗静电耐擦洗性能和力学性能进行了测试。结果表明,咪唑基离子液体在显著提高PP的抗静电性能和抗静电剂耐擦洗性能的同时,材料的冲击强度虽略有下降,但拉伸强度提高。     

离子液体法制备铜的纳米粒子

利用化学还原方法，加入不同量的离子液体1-甲基-3-乙基咪唑硫酸乙酯盐，制备了不同大小的金属铜的纳米摘要粒子。采用X射线衍射和透射电子显微镜对所制备的样品进行了结构表征。结果表明，两个样品中的粒子都具有五边形和六边形结构，粒径约为200～300nm，离子液体不但作为分散剂影响粒子的大小，而且有一定的防氧化作用。     

Preparation and Evaluation of Sustained Ophthalmic Gel of Enoxacin

ABSTRACT

The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of a gel system. The present work describes the formulation and evaluation of an ophthalmic delivery system containing an antibacterial agent, enoxacin, based on the concept of ophthalmic sustained gel, in which 2-hydroxypropyl-beta-cyclo-dextrin (HP-β-CD) was used as a penetration enhancer in combination with hydroxypropylmethylcellulose (Methocel F4M) which acted as a vehicle. The developed formulation was therapeutically efficacious, nonirritant, and provided sustained release of the drug over 8 h period in vitro and 7 h period in vivo. The developed system is a viable alternative to conventional eye drops.     

钴锌合金在氯化胆碱-尿素离子液体中的电沉积行为

为探索新型的Co-Zn合金电镀工艺,在氯化胆碱-尿素离子液体中电沉积了钴锌合金镀层,探讨了阴极电位、Co(Ⅱ)/Zn(Ⅱ)浓度比、温度及时间等工艺参数对电沉积的影响,并对合金镀层性能进行了测试.结果表明:在氯化胆碱-尿素离子液体中,控制体系的组成和沉积条件,可得到表面均匀、附着力强、有金属光泽的非晶态Co-Zn合金镀层,其中Co的质量分数可达90%.     

离子液体在电化学沉积中的研究进展

室温离子液体是由有机阳离子和有机或无机阴离子组成的一类新型液体,利用离子液体电沉积金属、半导体金属等有着重大意义.介绍了离子液体的性能,综述了离子液体在单质金属、合金、半导体电化学沉积中的应用.并展望了离子液体用于金属沉积的发展前景.     

[BMIM]ClO4离子液体的热力学性质

在273.15～353.15K范围内测定了[BMIM]ClO4离子液体的密度和表面张力。根据Glasser理论讨论了该离子液体的热力学性质,估算出其晶格能和标准熵。根据离子液体的空隙模型计算了离子液体的恒压热膨胀系数α=6.27×10-4 K-1,与实验值α=5.46×10-4 K-1基本一致。     

室温离子液体中电沉积金工艺研究

为探索新型镀金工艺,研究了在氯化胆碱/尿素离子液体系中采用牺牲阳极法电沉积单质金n+工艺.采用扫描电镜(SEM)、X射线衍射(XRD)等手段考察了电流密度、主盐浓度、温度及时间等工艺参数对沉积速率的影响,并对镀层性能进行了测试.结果表明,在电流密度0.2～0.5 A/dm2,3～7 g/L主盐AuP-Ph3Cl,温度70～80℃,电镀时间30～40 min条件下,制得的金镀层光亮、细致,性能良好.XRD结果表明镀层为面心立方晶系.     

Preparation and Evaluation of A Sustained-Release Ophthalmic Vehicle for Dapiprazole

Abstract

The present investigation is concerned with the development and “in vivo” evaluation of a long-acting ocular vehicle for the α-adrenergic blocking drug dapiprazole (DAP). The approaches tested for prolonging the activity were a) salification of the drug base with polygalacturonic acid (PGA), and b) formulation as a highly viscous hydrogel. The vehicles prepared by applying (singly or in combination) these techniques, and two reference aqueous vehicles containing DAP-HCl were submitted to a series of biological tests on rabbits (miosis and reversion of mydriasis). When compared with an aqueous solution an aqueous solution, reconstituted prior to use from a freeze-dried formulation (marketed in Italy as Glamidolo^R, Angelini)

The topical administration of ophthalmic drugs from aqueous solutions (collyria) is characterized by a poor bioavailability and a short duration of action, as a result of a series of concomitant physiological factors (induced lacrimation, tear turnover, solution drainage etc.) which concur in removing the solution from the eye. These factors have been widely investigated and detailed in the relevant literature, and several approaches to extend the ocular residence time of topically applied medications have been reported (4). In the present study two such approaches, namely, a) salification of the basic drug with a polyanionic polymer and b) increased vehicle viscosity, were applied to the development of a long-acting ocular formulation for DAP. The effect of the said manipulations on the biological activity of a series of DAP vehicles was submitted to a preliminary verification “in vivo”, by performing miosis and reversion of tropicamide-induced mydriasis tests in rabbits     

Tissue Irritation Evaluation of Potential Parenteral Vehicles

Abstract

Twenty-three potential nonaqueous parenteral vehicles were evaluated for tissue irritation in chicken pectoral muscle. Benzyl benzoate, 1,3-butylene glycol, ethyl oleate, glyceryl triacetate, sesame oil and sesame oil: benzyl benzoate (1:1) were found to cause minimal tissue irritation.     

DMSO对纤维素在咪唑型离子液体中溶解性能的影响

本文通过向传统离子液体中添加助溶剂DMSO来增强离子液体对纤维素的溶解效果。系统研究了DMSO添加量对纤维素溶解性能的影响,结果表明50℃下随着DMSO添加量的增大,纤维素的溶解程度增加,当DMSO添加量为50%时溶解效果最佳。采用电导率测试研究了DMSO与离子液体的作用机理,并通过FT-IR、XRD、TGA、SEM以及力学性能测试等方法对添加不同量DMSO溶剂溶解再生后的纤维素膜进行了分析,结果表明添加DMSO后溶剂仍为纤维素的直接溶剂,溶解再生后纤维素晶型由Ⅰ转变为Ⅱ型,并且随着DMSO添加量的增加,溶剂对纤维素分子链及结晶区的破坏能力增大,从而导致再生纤维素结晶度、抗拉强度及聚合度相对纯离子液体再生的有所降低。     

离子液体在可逆加成-断裂链转移聚合中的应用

离子液体具有优良的物理化学性能,受到研究者的广泛关注.近年来,有关离子液体在可逆加成-断裂链转移(RAFT)聚合反应中的应用有大量的研究报道.作为溶剂,离子液体能溶解一些较难溶解的聚合物,如纤维素和壳聚糖等,可以为聚合反应提供较好的反应环境;作为单体,通过RAFT聚合可制备出聚合离子液体均聚物或带有聚合离子液体链段的嵌段聚合物,可以应用于燃料电池电解质膜、太阳能电池、催化、分离及吸附剂等领域;离子液体还可以作为表面活性剂,应用于RAFT的乳液聚合或细乳液聚合,有效地稳定和控制聚合物颗粒大小.从溶剂、单体和表面活性剂方面出发,简单总结了离子液体在RAFT聚合反应中的应用.     

Ionic Interactions in Molecular and Liquid States of Polyvalent Metal Halides

1.BackgroundandOutlineThebindingenergy0fac0mpoundsuchasNaClcanberegardedt0alargeextentasarisingfro111trans-ferofanelectr0nfromthehalogent0themetalatom.InanearlyseminalpaperB0rnandNIa3er[']prop0sedam0delwhichattributesthec0hesion0fanalkalihalidecrystalt0theCoul0mbinteractionsbetweenionscarryingintegerchargesandascribestheequilib-riumstateatgiventemperatureandpressuret0aba1-ancebetweenthenetCoul0mbattactionsandquan-talcl0sed-shelloverlaprepulsions.Thelattershowexp0nentialdecaywithincreasingin…