摘要
枸橼酸西地那非(SC)是一种5型磷酸二酯酶抑制药,临床用于治疗男性勃起功能障碍与肺动脉高压。近年来在文献中报道了SC在治疗女性不孕及伤口愈合等方面也有一定的药理作用。但由于SC口服生物利用度低而限制了应用,故开发新的剂型用来提高药物的生物利用度已经成为当前研究的热点。因此,本文检索文献对国内外SC新剂型的研究概况进行综述,为其新剂型的开发提供参考。
Sildenafil citrate (SC) is a 5-type phosphodiesterase inhibitor,which has been used in the treatment of male erectile dysfunction and pulmonary hypertension. In recent years,it was found that the pharmacological activity of SC could be applied in the treatment of female infertility and wound healing. However,the low bioavailability of SC limits its application,and the development of new dosage forms to improve its bioavailability has become the focus of current research. Therefore,the research progress in the new dosage forms of SC at home and abroad was reviewed through searching literatures in order to provide reference for the development of the new dosage forms of SC.
引文
1 Badr-Eldin SM,Ahmed OA.Optimized nano-transfersomal films for enhanced sildenafil citrate transdermal delivery:ex vivo and in vivo evaluation[J].Drug Design,Development and Therapy,2016,10:1323-1233
2 Kirby M,Creanga DL,Stecher VJ.Erectile function,erection hardness and tolerability in men treated with sildenafil 100 mg vs.50 mg for erectile dysfunction.[J].International Journal of Clinical Practice,2013,67(10):1034-1039
3 Unegbu C,Noje C,Coulson JD,et al.Pulmonary hypertension therapy and a systematic review of efficacy and safety of PDE-5 inhibitors[J].Pediatrics,2017,139(3):2016-2039
4 Simiele M,Pensi D,Pasero D,et al.Development and validation of an ultra performance liquid chromatography tandem mass method for sildenafil and N-desmethyl sildenafil plasma determination and quantification.[J].J Chromatogr B Analyt Technol Biomed Life Sci,2015,1001:35-40
5 Shah V,Sharma M,Parmar V,et al.Formulation of sildenafil citrate loaded nasal microsphers:An in vitro,ex vivo characterization[J].International Journal of Drug Delivery,2011,2(3):213-220
6 Fraisse A,Butrous G,Taylor MB,et al.Intravenous sildenafil for postoperative pulmonary hypertension in children with congenital heart disease[J].Intensive Care Medicine,2011,37(3):502-509
7 Sae YA,Sawatdee S,Woradechakul C,et al.Physicochemical and microbio-logical stability of the extemporaneous sildenafil citrate oral suspension[J].Scientia Pharmaceutica,2015,83(4):659-670
8 Degim IT,Tugcu-Demiroz F,Tamer-Ilbasmis S,et al.Development of controlled release sildenafil formulations for vaginal administration[J].Drug Delivery,2008,15(4):259-265
9 Melnikov P,Corbi PP,Cuin A,et al.Physicochemical properties of sildenafil citrate(Viagra)and sildenafil base[J].Journal of Pharmaceutical Sciences,2003,92(10):2140-2143
10黄学荪,王志强,张虎祥.枸橼酸西地那非阴道栓对雌性日本大白兔子宫内膜的影响[J].中国临床药学杂志,2008,17(6):357-358
11 Ring A,Morris T,Wozniak M,et al.A Phase I study to determine the pharmacokinetic profile,safety and tolerability of sildenafil(Revatio(R))in cardiac surgery:the REVAKI-1 study[J].British Journal of Clinical Pharmacology,2017,83(4):709-720
12 Aizawa N,Ito H,Sugiyama R,et al.Effects of Sildenafil,a Phosphodiesterase type 5 inhibitor,on the primary single afferent activity of the rat bladder[J].Lower Urinary Tract Symptoms,2017,9(1):57-61
13 Wang S,Zhang J,Ge W,et al.Efficacy and safety of oral sildenafil in treatment of pediatric head and neck lymphatic malformations[J].Acta Oto-Laryngologica 2017,137(6):674-678
14 Cakmak E,Yesilada AK,Sevim KZ,et al.Effect of sildenafil citrate on secondary healing in full thickness skin defects in experiment[J].Bratislava Medical Journal,2014,115(5):267-271
15 Gürsoy K,Oru9 M,Kankaya Y,et al.Effect of topically applied sildenafil citrate on wound healing:experimental study[J].Bosnian Journal of Basic Medical Sciences,2014,14(3):125-131
16 De Rose RF,Cristiano MC,Celano M,et al.PDE5 inhibitors-loaded nanovesicles:physico-chemical properties and in vitro antiproliferative activity[J].Nanomaterials,2016,6(5):92-104
17 Leoni LA,Leite GS,Wichi RB,et al.Sildenafil:two decades of benefits or risks?[J].Aging Male,2013,16(3):85-91
18 Swetman GL,Berk DR,Vasanawala SS,et al.Sildenafil for severe lymphatic malformations[J].N Engl J Med,2012,366(4):384-386
19 Trapani A,Jr,Goncalves LF,Trapani TF,et al.Comparison between transdermal nitroglycerin and sildenafil citrate in intrauterine growth restriction:effects on uterine,umbilical and fetal middle cerebral artery pulsatility indices[J].Ultrasound in Obstetrics&Gynecology,2016,48(1):61-65
20 Karakhanova S,Yang Y,Link J,et al.Gender-specific immunological effects of the phosphodiesterase 5 inhibitor sildenafil in healthy mice[J].Molecular Immunology,2013,56(4):649-659
21 Tripathi AS,Timiri AK,Mazumder PM,et al.Does glimepiride alter the pharmacokinetics of sildenafil citrate in diabetic nephropathy animals:investigating mechanism of interaction by molecular modeling studies.[J].Journal of Molecular Modeling,2015,21(10):1-10
22马冬冬,孟庆丽,刘红梅,等.阴道黏膜给药系统的研究进展[J].中国药师,2015,18(4):649-651
23 Soliman GM,Fetih G,Abbas AM.Thermosensitive bioadhesive gels for the vaginal delivery of sildenafil citrate:in vitro characterization and clinical evaluation in women using clomiphene citrate for induction of ovulation[J].Drug Development and Industrial Pharmacy,2017,43(3):399-408
24 Piazzini V,Landucci E,Graverini G,et al.Stealth and cationic nanoliposomes as drug delivery systems to increase andrographolide BBB permeability[J].Pharmaceutics,2018,10(3):128-147
25 Refai H,Hassan D,Abdelmonem R.Development and characterization of polymer-coated liposomes for vaginal delivery of sildenafil citrate[J].Drug Delivery,2017,24(1):278-288
26王勉,朱家壁,汤玥.肺部给药传递系统的研究进展[J].中国新药杂志,2009,18(8):694-698
27 Kurmi BD,Kayat J,Gajbhiye V,et al.Micro-and nanocarrier-mediated lung targeting[J].Expert Opinion on Drug Delivery,2010,7(7):781-794
28 Ghasemian E,Vatanara A,Rouini MR,et al.Inhaled sildenafil nanocomposites:lung accumulation and pulmonary pharmacokinetics[J].Pharmaceutical Development and Technology,2016,21(8):961-971
29 Makled S,Nafee N,Boraie N.Nebulized solid lipid nanoparticles for the potential treatment of pulmonary hypertension via targeted delivery of phosphodiesterase-5-inhibitor[J].Int J Pharm,2017,517(1-2):312-321
30 Sawatdee S,Phetmung H,Srichana T.Sildenafil citrate monohydrate-cyclodextrin nanosuspension complexes for use in metered-dose inhalers[J].International Journal of Pharmaceutics,2013,455(1-2):248-258
31陈黎,高永良.舌下给药研究进展[J].中国药物应用与监测,2008,5(6):42-45
32 Sheu MT,Hsieh CM,Chen RN,et al.Rapid-onset sildenafil sublingual drug delivery systems:in vitro evaluation and in vivo pharmacokinetic studies in rabbits[J].Journal of Pharmaceutical Sciences,2016,105(9):2774-2781
33 Lenz E,Sprunk A,Kleinebudde P,et al.Impact of fillers on dissolution kinetic of fenofibrate dry foams[J].Pharmaceutical Development&Technology,2015,20(5):570-578
34 Sawatdee S,Atipairin A,Sae Yoon A,et al.Enhanced dissolution of sildenafil citrate as dry foam tablets[J].Pharmaceutical Development and Technology,2017,30(1):1-11