直肠给药系统的研究进展
摘要
直肠给药可减少肝首过效应,避免胃肠道反应,具有起效快、安全性高等优势,逐渐受到重视,特别是对成分复杂而味道苦涩的中药、易被酶解的蛋白质类药物、不适合口服给药的群体、直肠疾病等情况,该方式具有重要意义。本文综述了目前直肠给药特点、适用范围、常用剂型,并分析了其研究方向和发展前景,以期为相关探索和应用提供参考。
引文
[1] 孟庆岩,张庆祥,高思华.从“津液相关”探讨肺与大肠相表里[J].北京中医药大学学报,2013,36(11):729-731.
[2] Seo Y G,Kim D W,Yeo W H,et al.Docetaxel-loaded thermosensitive and bioadhesive nanomicelles as a rectal drug delivery system for enhanced chemotherapeutic effect[J].Pharm Res,2013,30(7):1860-1870.
[3] Kamel R,Basha M,Abd EI-Alim S H.Development of a novel vesicular system using a binary mixture of sorbitan monostearate and polyethylene glycol fatty acid esters for rectal delivery of rutin[J].J Liposome Res,2013,23(1):28-36.
[4] Nunes R,Sarmento B,das Neves J.Formulation and delivery of anti-HIV rectal microbicides:advances and challenges[J].J Controlled Release,2014,194:278-294.
[5] Abou El Ela Ael S,Allam A A,Ibrahim E H.Pharmacokinetics and anti-hypertensive effect of metoprolol tartrate rectal delivery system[J].Drug Deliv,2016,23(1):69-78.
[6] Moawad F A,Ali A A,Salem H F.Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl:preparation,in vitro and in vivo performance[J].Drug Deliv,2017,24(1):252-260.
[7] Chiang L M,Wang H S,Shen H H,et al.Rectal diazepam solution is as good as rectal administration of intravenous diazepam in the first-aid cessation of seizures in children with intractable epilepsy[J].Pediatr Neonatol,2011,52(1):30-33.
[8] Yung A,Thung A,Tobias J D.Acetaminophen for analgesia following pyloromyotomy:does the route of administration make a difference?[J].J Pain Res,2016,9:123-127.
[9] 龚海峰.复方半边莲注射液保留灌肠佐治小儿急性支气管肺炎200例临床分析[J].中国实用内科杂志,2014,34(S1):109-110.
[10] 赵军宁.中药复方适度调节原理与中药复方新药转化中的药理学问题[J].中国中药杂志,2017,42(5):836-843.
[11] Ibraheem D,Elaissari A,Fessi H.Administration strategies for proteins and peptides[J].Int J Pharm,2014,477(1-2):578-589.
[12] Uchida T,Toida Y,Sakakibara S,et al.Preparation and characterization of insulin-loaded acrylic hydrogels containing absorption enhancers[J].Chem Pharm Bull (Tokyo),2001,49(10):1261-1266.
[13] Sakai M,Hobara N,Hokama N,et al.Increased bioavailability of tacrolimus after rectal administration in rats[J].Biol Pharm Bull,2004,27(9):1480-1482.
[14] Stifft F,Vanmolkot F,Scheffers I,et al.Rectal and sublingual administration of tacrolimus:a single-dose pharmacokinetic study in healthy volunteers[J].Br J Clin Pharmacol,2014,78(5):996-1004.
[15] Kauss T,Gaubert A,Boyer C,et al.Pharmaceutical development and optimization of azithromycin suppository for paediatric use[J].Int J Pharm,2013,441(1-2):218-226.
[16] Taki H,Ogawa K,Nikai T.Pharmaceutical study of suppository formulations for improved in vivo kinetics of rifampicin[J].Kekkaku,2008,83(6):451-456.
[17] Cohen R D,Dalal S R.Systematic review:rectal therapies for the treatment of distal forms of ulcerative colitis[J].Inflamm Bowel Dis,2015,21(7):1719-1736.
[18] Zaghloul A A,Lila A,Abd-Allah F,et al.Preparation and in vitro/in vivo evaluation of metformin hydrochloride rectal dosage forms for treatment of patients with type Ⅱ diabetes[J].J Drug Target,2017,25(5):463-470.
[19] Zaporowska-Stachowiak I,Kowalski G,?uczak J,et al.Bupivacaine administered intrathecally versus rectally in the management of intractable rectal cancer pain in palliative care[J].Onco Targets Ther,2014,7:1541-1550.
[20] Jannin V,Lemagnen G,Gueroult P,et al.Rectal route in the 21st century to treat children[J].Adv Drug Deliv Rev,2014,73:34-49.
[21] Lo Y L,Lin Y,Lin H R.Evaluation of epirubicin in thermogelling and bioadhesive liquid and solid suppository formulations for rectal administration[J].Int J Mol Sci,2013,15(1):342-360.
[22] Patil B S,Mahajan H S,Surana S J.Development of suppositories containing flutamide-loaded alginate-tamarind microparticles for rectal administration:in vitro and in vivo studies[J].Chem Pharm Bull,2015,63(11):851-857.
[23] He C L,Kim S W,Lee D S.In situ gelling stimuli-sensitive block copolymer hydrogels for drug delivery[J].J Controlled Release,2008,127(3):189-207.
[24] Ozgüney I,Kardhiqi A.Properties of bioadhesive ketoprofen liquid suppositories:preparation,determination of gelation temperature,viscosity studies and evaluation of mechanical properties using texture analyzer by 4×4 factorial design[J].Pharm Dev Technol,2014,19(8):968-975.
[25] Ramadass S K,Perumal S,Jabaris S L,et al.Preparation and evaluation of mesalamine collagen in situ rectal gel:a novel therapeutic approach for treating ulcerative colitis[J].Eur J Pharm Sci,2013,48(1-2):104-110.
[26] 刘健.白虎汤加减灌肠治疗温病气分热证的研究[D].广州:广州中医药大学,2006.
[27] Loew B J,Siegel C A.Foam preparations for the treatment of ulcerative colitis[J].Curr Drug Deliv,2012,9(4):338-344.
[28] Kealy T,Abram A,Hunt B,et al.The rheological properties of pharmaceutical foam:implications for use[J].Int J Pharm,2008,355(1-2):67-80.
[29] Wellauer J,Del Buono M,Ory A M,et al.Gelatin rectal capsules,a new drug form for rectal use[J].Pharm Acta Helv,1960,35:619-630.
[30] Gomez L E A,Jurado M H,Cambon N.Randomised efficacy and safety study of two 3-day artesunate rectal capsule/mefloquine regimens versus artesunate alone for uncomplicated malaria in Ecuadorian children[J].Acta Trop,2003,89(1):47-53.
[31] Beubler E,Dittrich P.About the therapy of laryngotracheitis (croup):significance of rectal dosage forms[J].Pharmacology,2015,95(5-6):300-302.
[32] Bounoure F,Lahiani Skiba M,Besnard M,et al.Effect of iontophoresis and penetration enhancers on transdermal absorption of metopimazine[J].J Dermatol Sci,2008,52(3):170-177.
[33] Miyake M,Minami T,Oka Y,et al.Optimization of suppository preparation containing sodium laurate and taurine that can safely improve rectal absorption of rebamipide[J].Biol Pharm Bull,2006,29(2):330-335.
[34] Koffi A A,Aqnelv F,Besnard M,et al.In vitro and in vivo characteristics of a thermogelling and bioadhesive delivery system intended for rectal administration of quinine in children[J].Eur J Pharm Biopharm,2008,69(1):167-175.
[35] Yong C S,Oh Y K,Jung S H,et al.Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol[J].Eur J Pharm Sci,2004,23(4-5):347-353.
[36] Kim J Y,Ku Y S.Enhanced absorption of indomethacin after oral or rectal administration of a self-emulsifying system containing indomethacin to rats[J].Int J Pharm,2000,194(1):81-89.
[37] Zidan A S,Emam S E,Shehata T M,et al.Pediatric suppositories of sulpiride solid dispersion for treatment of Tourette syndrome:in vitro and in vivo investigations[J].AAPS Pharm Sci Tech,2015,16(3):645-655.
[2] Seo Y G,Kim D W,Yeo W H,et al.Docetaxel-loaded thermosensitive and bioadhesive nanomicelles as a rectal drug delivery system for enhanced chemotherapeutic effect[J].Pharm Res,2013,30(7):1860-1870.
[3] Kamel R,Basha M,Abd EI-Alim S H.Development of a novel vesicular system using a binary mixture of sorbitan monostearate and polyethylene glycol fatty acid esters for rectal delivery of rutin[J].J Liposome Res,2013,23(1):28-36.
[4] Nunes R,Sarmento B,das Neves J.Formulation and delivery of anti-HIV rectal microbicides:advances and challenges[J].J Controlled Release,2014,194:278-294.
[5] Abou El Ela Ael S,Allam A A,Ibrahim E H.Pharmacokinetics and anti-hypertensive effect of metoprolol tartrate rectal delivery system[J].Drug Deliv,2016,23(1):69-78.
[6] Moawad F A,Ali A A,Salem H F.Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl:preparation,in vitro and in vivo performance[J].Drug Deliv,2017,24(1):252-260.
[7] Chiang L M,Wang H S,Shen H H,et al.Rectal diazepam solution is as good as rectal administration of intravenous diazepam in the first-aid cessation of seizures in children with intractable epilepsy[J].Pediatr Neonatol,2011,52(1):30-33.
[8] Yung A,Thung A,Tobias J D.Acetaminophen for analgesia following pyloromyotomy:does the route of administration make a difference?[J].J Pain Res,2016,9:123-127.
[9] 龚海峰.复方半边莲注射液保留灌肠佐治小儿急性支气管肺炎200例临床分析[J].中国实用内科杂志,2014,34(S1):109-110.
[10] 赵军宁.中药复方适度调节原理与中药复方新药转化中的药理学问题[J].中国中药杂志,2017,42(5):836-843.
[11] Ibraheem D,Elaissari A,Fessi H.Administration strategies for proteins and peptides[J].Int J Pharm,2014,477(1-2):578-589.
[12] Uchida T,Toida Y,Sakakibara S,et al.Preparation and characterization of insulin-loaded acrylic hydrogels containing absorption enhancers[J].Chem Pharm Bull (Tokyo),2001,49(10):1261-1266.
[13] Sakai M,Hobara N,Hokama N,et al.Increased bioavailability of tacrolimus after rectal administration in rats[J].Biol Pharm Bull,2004,27(9):1480-1482.
[14] Stifft F,Vanmolkot F,Scheffers I,et al.Rectal and sublingual administration of tacrolimus:a single-dose pharmacokinetic study in healthy volunteers[J].Br J Clin Pharmacol,2014,78(5):996-1004.
[15] Kauss T,Gaubert A,Boyer C,et al.Pharmaceutical development and optimization of azithromycin suppository for paediatric use[J].Int J Pharm,2013,441(1-2):218-226.
[16] Taki H,Ogawa K,Nikai T.Pharmaceutical study of suppository formulations for improved in vivo kinetics of rifampicin[J].Kekkaku,2008,83(6):451-456.
[17] Cohen R D,Dalal S R.Systematic review:rectal therapies for the treatment of distal forms of ulcerative colitis[J].Inflamm Bowel Dis,2015,21(7):1719-1736.
[18] Zaghloul A A,Lila A,Abd-Allah F,et al.Preparation and in vitro/in vivo evaluation of metformin hydrochloride rectal dosage forms for treatment of patients with type Ⅱ diabetes[J].J Drug Target,2017,25(5):463-470.
[19] Zaporowska-Stachowiak I,Kowalski G,?uczak J,et al.Bupivacaine administered intrathecally versus rectally in the management of intractable rectal cancer pain in palliative care[J].Onco Targets Ther,2014,7:1541-1550.
[20] Jannin V,Lemagnen G,Gueroult P,et al.Rectal route in the 21st century to treat children[J].Adv Drug Deliv Rev,2014,73:34-49.
[21] Lo Y L,Lin Y,Lin H R.Evaluation of epirubicin in thermogelling and bioadhesive liquid and solid suppository formulations for rectal administration[J].Int J Mol Sci,2013,15(1):342-360.
[22] Patil B S,Mahajan H S,Surana S J.Development of suppositories containing flutamide-loaded alginate-tamarind microparticles for rectal administration:in vitro and in vivo studies[J].Chem Pharm Bull,2015,63(11):851-857.
[23] He C L,Kim S W,Lee D S.In situ gelling stimuli-sensitive block copolymer hydrogels for drug delivery[J].J Controlled Release,2008,127(3):189-207.
[24] Ozgüney I,Kardhiqi A.Properties of bioadhesive ketoprofen liquid suppositories:preparation,determination of gelation temperature,viscosity studies and evaluation of mechanical properties using texture analyzer by 4×4 factorial design[J].Pharm Dev Technol,2014,19(8):968-975.
[25] Ramadass S K,Perumal S,Jabaris S L,et al.Preparation and evaluation of mesalamine collagen in situ rectal gel:a novel therapeutic approach for treating ulcerative colitis[J].Eur J Pharm Sci,2013,48(1-2):104-110.
[26] 刘健.白虎汤加减灌肠治疗温病气分热证的研究[D].广州:广州中医药大学,2006.
[27] Loew B J,Siegel C A.Foam preparations for the treatment of ulcerative colitis[J].Curr Drug Deliv,2012,9(4):338-344.
[28] Kealy T,Abram A,Hunt B,et al.The rheological properties of pharmaceutical foam:implications for use[J].Int J Pharm,2008,355(1-2):67-80.
[29] Wellauer J,Del Buono M,Ory A M,et al.Gelatin rectal capsules,a new drug form for rectal use[J].Pharm Acta Helv,1960,35:619-630.
[30] Gomez L E A,Jurado M H,Cambon N.Randomised efficacy and safety study of two 3-day artesunate rectal capsule/mefloquine regimens versus artesunate alone for uncomplicated malaria in Ecuadorian children[J].Acta Trop,2003,89(1):47-53.
[31] Beubler E,Dittrich P.About the therapy of laryngotracheitis (croup):significance of rectal dosage forms[J].Pharmacology,2015,95(5-6):300-302.
[32] Bounoure F,Lahiani Skiba M,Besnard M,et al.Effect of iontophoresis and penetration enhancers on transdermal absorption of metopimazine[J].J Dermatol Sci,2008,52(3):170-177.
[33] Miyake M,Minami T,Oka Y,et al.Optimization of suppository preparation containing sodium laurate and taurine that can safely improve rectal absorption of rebamipide[J].Biol Pharm Bull,2006,29(2):330-335.
[34] Koffi A A,Aqnelv F,Besnard M,et al.In vitro and in vivo characteristics of a thermogelling and bioadhesive delivery system intended for rectal administration of quinine in children[J].Eur J Pharm Biopharm,2008,69(1):167-175.
[35] Yong C S,Oh Y K,Jung S H,et al.Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol[J].Eur J Pharm Sci,2004,23(4-5):347-353.
[36] Kim J Y,Ku Y S.Enhanced absorption of indomethacin after oral or rectal administration of a self-emulsifying system containing indomethacin to rats[J].Int J Pharm,2000,194(1):81-89.
[37] Zidan A S,Emam S E,Shehata T M,et al.Pediatric suppositories of sulpiride solid dispersion for treatment of Tourette syndrome:in vitro and in vivo investigations[J].AAPS Pharm Sci Tech,2015,16(3):645-655.