缓控释非胃肠道给药系统的体外加速释放方法综述
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摘要
近年来,长效缓控释非胃肠道给药系统由于具有减少给药频率、提高药效、降低药物副作用和增加患者的顺应性等传统给药系统不能比拟的优势,在科学研究和临床应用中引起广泛关注和应用。对于缓控释非胃肠道给药系统的研发生产和质量控制来说,监测其体外的实时释放需要耗费数周乃至数月的时间,因此建立适当的体外加速释药方法是保证其质量、特性以及各批次间稳定性的关键步骤。文章对缓控释非胃肠道给药系统的体外加速释放的不同方法,如温度、pH值、添加有机溶剂或表面活性剂等进行了综述。
In recent years,long-term controlled release parenteral drug delivery system has attracted considerable attention in clinical and research fields because of its advantages compared with traditional drug delivery systems,including reducing dosing frequency,increasing drug efficacy,decreasing adverse side effects,and enhancing patient compliance. In the process of product development and quality control,real-time in vitro release tests for these dosage forms are often run over periods of weeks and months which are time consuming. Hence,the establishment of appropriate accelerated in vitro release methods is the key step to guarantee the quality,features and stability of each batch. In this paper,various of methods related to acceleration in vitro release studies include temperature,pH value,addictive of organic solvent or surfactant etc. are reviewed.
In recent years,long-term controlled release parenteral drug delivery system has attracted considerable attention in clinical and research fields because of its advantages compared with traditional drug delivery systems,including reducing dosing frequency,increasing drug efficacy,decreasing adverse side effects,and enhancing patient compliance. In the process of product development and quality control,real-time in vitro release tests for these dosage forms are often run over periods of weeks and months which are time consuming. Hence,the establishment of appropriate accelerated in vitro release methods is the key step to guarantee the quality,features and stability of each batch. In this paper,various of methods related to acceleration in vitro release studies include temperature,pH value,addictive of organic solvent or surfactant etc. are reviewed.
引文
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[3] Shameem M,Lee H,Deluca PP. A short-term(accele-rated release)approach to evaluate peptide release from PLGA depot formulations[J]. Aaps Pharmsci,1999,1(3):1-6.
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[13] Zolnik BS,Burgess DJ. Effect of acidic pH on PLGA microsphere degradation and release[J]. J Contr Rel,2007,122(3):338-344.
[14] Rawat A,Stippler E,Shah VP,et al. Validation of USP apparatus4 method for microsphere in vitro release testing using Risperdal Consta[J]. Interna J Pharmac,2011,420(2):198-205.
[15] Guse C,Koennings S,Kreye F,et al. Drug release from lipidbased implants:Elucidation of the underlying mass transport mechanisms[J]. Intern J Pharm,2006,314(2):137.
[16]刘承,梅乐,胡小琴,等.醋酸曲普瑞林缓释微球体外加速释放及体内外相关性研究[J].国际药学研究杂志,2017,44(6):622-628.
[17] Koennings S,BeriéA,Tessmar J,et al. Influence of wettability and surface activity on release behavior of hydrophilic substances from lipid matrices[J]. J Contr Rel Official J Contr Rel Society,2007,119(2):173.
[18] Xie XY,Yang Y,Zhang H,et al. An in vitro accelerated approach based on in vivo release to assess thymopentin release from PLGA microspheres[C].中国药学大会暨中国药师周,2014:672-679.
[19] Zolnik BS,Raton JL,Burgess DJ. Application of USP apparatus 4and in situ fiber optic analysis to microsphere release testing[J]. Dissol Technol,2005,12(2).
[20] Larsen SW,Jessen MNB,?stergaard J,et al. Assessment of drug release from oil depot formulations using an in vitro modelpotential applicability in accelerated release testing[J]. Drug Develop Indust Pharm,2008,34(3):297-304.
[21] Shameem M,Lee H,Deluca PP. A short-term(accelerated release)approach to evaluate peptide release from PLGA depot formulations[J]. Aaps Pharmsci,1999,1(3):1-6.
[22] Siewert M,Dressman J,Brown CK,et al. FIP/AAPS guidelines to dissolution/in vitro release testing of novel/special dosage forms[J]. Aaps Pharmscitech,2003,4(1):43-52.
[23] D'souza SS,Faraj JA,Deluca PP. A model-dependent approach to correlate accelerated with real-time release from biodegradable microspheres[J]. AAPS Pharm Sci Tech,2005,6(4):E553-564.
[2] Martinez MN,Rathbone MJ,Burgess D,et al. Breakout session summary from AAPS/CRS joint workshop on critical variables in the in vitro and in vivo performance of parenteral sustained release products[J]. J Contr Rel,2010,142(1):2-7.
[3] Shameem M,Lee H,Deluca PP. A short-term(accele-rated release)approach to evaluate peptide release from PLGA depot formulations[J]. Aaps Pharmsci,1999,1(3):1-6.
[4] Shen J,Burgess DJ. Accelerated in-vitro release testing methods for extended-release parenteral dosage forms[J]. J Pharmacy Pharmacol,2012,64(7):986-996.
[5] Zolnik BS,Leary PE,Burgess DJ. Elevated temperature accelerated release testing of PLGA microspheres[J]. J Contr Rel Official J Contr Rel Society,2006,112(3):293-300.
[6] Burgess DJ,Hussain AS,Ingallinera TS,et al. Assuring quality and performance of sustained and controlled release parenterals:AAPS workshop report,co-sponsored by FDA and USP[J].Pharm Res,2004,21(5):679-690.
[7]张芳,杨志强,王杏林.长效注射剂释药技术研究进展[J].中国新药杂志,2013,22(5):547-555.
[8] Jelonek K,Kasperczyk J,Dobrzyński P,et al. Comparison of accelerated and real-time cyclosporine A release testing from poly(l-lactide-co-trimethylene carbonate)matrices[J]. Acta Poloniae Pharmaceutica,2010,67(6):722.
[9] Shen J,Burgess DJ. Accelerated in vitro release testing of implantable PLGA microsphere/PVA hydrogel composite coatings[J].Int J Pharm,2012,422(1):341-348.
[10] Shen J,Lee K,Choi S,et al. A reproducible accelerated in vitro release testing method for PLGA microspheres[J]. Int J Pharm,2016,498(1-2):274-282.
[11] Burgess DJ,Hussain AS,Ingallinera TS,et al. Assuring quality and performance of sustained and controlled release parenterals:AAPS workshop report,co-sponsored by FDA and USP[J].Pharmac Res,2004,21(5):679-90.
[12] D'souza SS,Faraj JA,Deluca PP. A model-dependent approach to correlate accelerated with real-time release from biodegradable microspheres[J]. AAPS Pharm Sci Tech,2005,6(4):E553-564.
[13] Zolnik BS,Burgess DJ. Effect of acidic pH on PLGA microsphere degradation and release[J]. J Contr Rel,2007,122(3):338-344.
[14] Rawat A,Stippler E,Shah VP,et al. Validation of USP apparatus4 method for microsphere in vitro release testing using Risperdal Consta[J]. Interna J Pharmac,2011,420(2):198-205.
[15] Guse C,Koennings S,Kreye F,et al. Drug release from lipidbased implants:Elucidation of the underlying mass transport mechanisms[J]. Intern J Pharm,2006,314(2):137.
[16]刘承,梅乐,胡小琴,等.醋酸曲普瑞林缓释微球体外加速释放及体内外相关性研究[J].国际药学研究杂志,2017,44(6):622-628.
[17] Koennings S,BeriéA,Tessmar J,et al. Influence of wettability and surface activity on release behavior of hydrophilic substances from lipid matrices[J]. J Contr Rel Official J Contr Rel Society,2007,119(2):173.
[18] Xie XY,Yang Y,Zhang H,et al. An in vitro accelerated approach based on in vivo release to assess thymopentin release from PLGA microspheres[C].中国药学大会暨中国药师周,2014:672-679.
[19] Zolnik BS,Raton JL,Burgess DJ. Application of USP apparatus 4and in situ fiber optic analysis to microsphere release testing[J]. Dissol Technol,2005,12(2).
[20] Larsen SW,Jessen MNB,?stergaard J,et al. Assessment of drug release from oil depot formulations using an in vitro modelpotential applicability in accelerated release testing[J]. Drug Develop Indust Pharm,2008,34(3):297-304.
[21] Shameem M,Lee H,Deluca PP. A short-term(accelerated release)approach to evaluate peptide release from PLGA depot formulations[J]. Aaps Pharmsci,1999,1(3):1-6.
[22] Siewert M,Dressman J,Brown CK,et al. FIP/AAPS guidelines to dissolution/in vitro release testing of novel/special dosage forms[J]. Aaps Pharmscitech,2003,4(1):43-52.
[23] D'souza SS,Faraj JA,Deluca PP. A model-dependent approach to correlate accelerated with real-time release from biodegradable microspheres[J]. AAPS Pharm Sci Tech,2005,6(4):E553-564.