固体分散体中药物分散状态测定方法的研究进展
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摘要
固体分散体将难溶性药物以分子、无定形或微晶等形式分散在载体材料中,是改善难溶性药物溶解度、溶出速率和生物利用度的有效途径,但其中药物重结晶等稳定性问题已成为制约以该技术为基础的给药系统市场化瓶颈之一,因此,研究固体分散体中的药物状态及药物状态随着贮存时间延长的变化情况,对其性质评价和稳定性研究意义重大。本文综述了近年来测定固体分散体中药物分散状态的光谱分析、热分析、显微分析等方法的原理、优势及不足的研究进展,为该制剂中药物分散状态的测定提供指导。
引文
[1] Swati S,George M,Lincy J. Improvement in solubility of poor water-soluble drugs by solid dispersion[J]. Int J Pharm Investig,2012,2(1):12-17.
[2]陈超,周福军,刘时乔,等.固体分散技术在中药制剂中的应用[J].药物评价研究,2011,34(4):279-282.
[3]何晨,田茜,贺敬霞,等.柿叶总黄酮固体分散体的制备[J].中成药,2017,39(2):417-420.
[4] Jiang Y R,Zhang Z H,Huang S Y,et al. Enhanced dissolution and stability of TanshinoneⅡA base by solid dispersion system with nano-hydroxyapatite[J]. Pharm Mag,2014,10(39):332-337.
[5]单冬媛,裴英,孟晴,等.穿心莲内酯固体分散体的制备[J].中成药,2017,39(4):719-723.
[6] Tian B,Zhang L,Pan Z D,et al. A comparison of the effect of temperature and moisture on the solid dispersions:Aging and crystallization[J]. Int J Pharm,2014,475(1-2):385-392.
[7] Kanaujia P,Lau G,Ng W K,et al. Investigating the effect of moisture protection on solid-state stability and dissolution of fenofibrate and ketoconazole solid dispersions using PXRD,HSDSC and Raman microscopy[J]. Drug Dev Ind Pharm,2011,37(9):1026-1035.
[8] Ozaki S,Kushida I,Yamashita T,et al. Evaluation of drug supersaturation by thermodynamic and kinetic approaches for the prediction of oral absorbability in amorphous pharmaceuticals[J]. J Pharm Sci,2012,101(11):4220-4230.
[9] Kawakami K. Modification of physicochemical characteristics of active pharmaceutical ingredients and application of supersaturatable dosage forms for improving bioavailability of poorly absorbed drugs[J]. Adv Drug Deliver Rev, 2012, 64(6):480-495.
[10] Karolewicz B,Górniak A,Owczarek A,et al. Solid dispersion in pharmaceutical technology. PartⅡ. The methods of analysis of solid dispersions and examples of their application[J]. Polim Med,2012,42(2):97-107
[11]唐婷,严航,周江,等.莲心碱固体分散体的表征及体外溶出度的测定[J].中成药,2015,37(8):1853-1855.
[12] Wang W,Cui C,Li M,et al. Study of a novel disintegrable oleanolic acid-polyvinylpolypyrrolidone solid dispersion[J].Drug Dev Ind Pharm,2017,43(7):1178-1185.
[13]徐耀,梁丽萍,吴东.小角X射线散射应用研究若干进展[J].物理,2007,36(7):524-527.
[14] Singh A,Bharati A,Frederiks P,et al. Effect of compression on the molecular arrangement of itraconazole-soluplus solid dispersions:induction of liquid crystals or exacerbation of phase separation?[J]. Mol Pharm,2016,13(6):1879-1893.
[15]刘明杰,王钊,孙素琴.傅里叶变换红外光谱法在药学研究中应用的最新进展[J].药物分析杂志,2001,21(5):373-377.
[16]田茜,何晨,贺敬霞,等.沙棘总黄酮-聚乙烯吡咯烷酮K30固体分散体的制备、表征及体外溶出研究[J].中国药房,2017,28(1):115-118.
[17] Zhang Q,Pu Y Q,Wang B,et al. Characterization,molecular docking,and in vitro dissolution studies of solid dispersions of20(S)-protopanaxadiol[J]. Molecules, 2017, 22(2):E274.
[18]张雅军,田颂九.衰减全反射傅里叶变换红外光谱法定量分析西咪替丁A晶型的含量[J].中国药学杂志,2005,40(20):1587-1589.
[19] Iqbal W S,Chan K L. FTIR spectroscopic study of poly(ethylene glycol)-nifedipine dispersion stability in different relative humidities[J]. J Pharm Sci,2015,104(1):280-284.
[20]杨伟,渠荣遴.固体核磁共振在高分子材料分析中的研究进展[J].高分子通报,2006(12):69-74.
[21] Yang F Y,Su Y C,Zhu L,et al. Rheological and solid-state NMR assessments of copovidone/clotrimazole model solid dispersions[J]. Int J Pharm,2016,500(1-2):20-31.
[22]胡成龙,陈韶云,陈建,等.拉曼光谱技术在聚合物研究中的应用进展[J].高分子通报,2014(3):30-45.
[23] Cuzzucoli Crucitti V,Migneco L M,Piozzi A,et al. Intermolecular interaction and solid state characterization of abietic acid/chitosan solid dispersions possessing antimicrobial and antioxidant properties[J]. Eur J Pharm Biopharm,2018,125:114-123.
[24] PuncochováK,Vukosavljevic B,Hanu2 J,et al. Non-invasive insight into the release mechanisms of a poorly soluble drug from amorphous solid dispersions by confocal Raman microscopy[J].Eur J Pharm Biopharm,2016,101:119-125.
[25]张兴宁,陈稷,周泽魁.太赫兹时域光谱技术[J].激光与光电子学进展,2005,42(7):35-38.
[26] Takeuchi I,Shimakura K,Kuroda H,et al. Estimation of crystallinity of nifedipine-polyvinylpyrrolidone solid dispersion by usage of terahertz time-domain spectroscopy and of X-ray powder diffractometer[J]. J Pharm Sci,2015,104(12):4307-4313.
[27]王杰晶,李银峰,李佩,等.差示扫描量热法在药物定性分析中的应用[J].现代药物与临床,2013,28(5):815-818.
[28]崔锋,候佳威,孙文霞,等.高乌甲素固体分散体的表征及其体外溶出度测定[J].中药材,2016,39(9):2072-2074.
[29] Saunders M,Podluii K,Shergill S,et al. The potential of high speed DSC(hyper-DSC)for the detection and quantification of small amounts of amorphous content in predominantly crystalline samples[J]. Int J Pharm,2004,274(1-2):35-40.
[30] Mc Gregor C, Bines E. The use of high-speed differential scanning calorimetry(Hyper-DSC)in the study of pharmaceutical polymorphs[J]. Int J Pharm,2007,350(1-2):48-52.
[31]王艳色,魏志勇,申凯华,等.调制差示扫描量热法在高分子材料中的应用[J].高分子通报,2016(3):16-22.
[32] Nair R,Lamare I,Tiwari N K,et al. In situ salification in polar solvents:a paradigm for enabling drug delivery of weakly ionic drugs as amorphous solid dispersion[J]. AAPS Pharm Sci Tech,2018,19(1):326-337.
[33]赵俊霞,尹蓉莉,孙彩霞,等.广金钱草总黄酮-PVP-K30固体分散体的制备和体外特征[J].中成药,2014,36(10):2070-2074.
[34]陈洁,邱利焱,胡敏新,等.多烯紫杉醇固体分散体的制备和体内外研究[J].中国药学杂志,2007,42(22):1717-1722.
[35]叶为标,何小维,黄强,等.透射电子显微镜在淀粉及其衍生物中的应用[J].粮油加工,2008(5):102-105.
[36] Jin X,Zhang Z H,Zhu J,et al. Response surface method optimize of nano-silica solid dispersion technology assistant enzymatic hydrolysis preparation genistein[J]. Acta Pharm Sin,2012,47(4):522-528.
[37] Singh G, Sharma S,Gupta G D. Extensive diminution of particle size and amorphization of a crystalline drug attained by eminent technology of solid dispersion:a comparative study[J].AAPS Pharm SciTech,2017,18(5):1770-1784.
[38]张泸,刘新湘,余红,等.丹皮酚固体分散体的制备和表征[J].中国医药工业杂志,2015,46(3):261-264.
[39] Meng F,Liu T Z,Schneider E,et al. Self-association of rafoxanide in aqueous media and its application in preparing amorphous solid dispersions[J]. Mol Pharm, 2017, 14(5):1790-1799.
[40] Zijlstra G S,Rijkeboer M,Jan van Drooge D,et al. Characterization of a cyclosporine solid dispersion for inhalation[J].AAPS J,2007,9(2):E190-E199.
[41] van Drooge D J,Hinrichs W L J,Visser M R,et al. Characterization of the molecular distribution of drugs in glassy solid dispersions at the nano-meter scale,using differential scanning calorimetry and gravimetric water vapour sorption techniques[J].Int J Pharm,2006,310(1-2):220-229.
[42] Yang Z Y,Nollenberger K,Albers J,et al. The effect of processing on the surface physical stability of amorphous solid dispersions[J]. Eur J Pharm Biopharm,2014,88(3):897-908.
[2]陈超,周福军,刘时乔,等.固体分散技术在中药制剂中的应用[J].药物评价研究,2011,34(4):279-282.
[3]何晨,田茜,贺敬霞,等.柿叶总黄酮固体分散体的制备[J].中成药,2017,39(2):417-420.
[4] Jiang Y R,Zhang Z H,Huang S Y,et al. Enhanced dissolution and stability of TanshinoneⅡA base by solid dispersion system with nano-hydroxyapatite[J]. Pharm Mag,2014,10(39):332-337.
[5]单冬媛,裴英,孟晴,等.穿心莲内酯固体分散体的制备[J].中成药,2017,39(4):719-723.
[6] Tian B,Zhang L,Pan Z D,et al. A comparison of the effect of temperature and moisture on the solid dispersions:Aging and crystallization[J]. Int J Pharm,2014,475(1-2):385-392.
[7] Kanaujia P,Lau G,Ng W K,et al. Investigating the effect of moisture protection on solid-state stability and dissolution of fenofibrate and ketoconazole solid dispersions using PXRD,HSDSC and Raman microscopy[J]. Drug Dev Ind Pharm,2011,37(9):1026-1035.
[8] Ozaki S,Kushida I,Yamashita T,et al. Evaluation of drug supersaturation by thermodynamic and kinetic approaches for the prediction of oral absorbability in amorphous pharmaceuticals[J]. J Pharm Sci,2012,101(11):4220-4230.
[9] Kawakami K. Modification of physicochemical characteristics of active pharmaceutical ingredients and application of supersaturatable dosage forms for improving bioavailability of poorly absorbed drugs[J]. Adv Drug Deliver Rev, 2012, 64(6):480-495.
[10] Karolewicz B,Górniak A,Owczarek A,et al. Solid dispersion in pharmaceutical technology. PartⅡ. The methods of analysis of solid dispersions and examples of their application[J]. Polim Med,2012,42(2):97-107
[11]唐婷,严航,周江,等.莲心碱固体分散体的表征及体外溶出度的测定[J].中成药,2015,37(8):1853-1855.
[12] Wang W,Cui C,Li M,et al. Study of a novel disintegrable oleanolic acid-polyvinylpolypyrrolidone solid dispersion[J].Drug Dev Ind Pharm,2017,43(7):1178-1185.
[13]徐耀,梁丽萍,吴东.小角X射线散射应用研究若干进展[J].物理,2007,36(7):524-527.
[14] Singh A,Bharati A,Frederiks P,et al. Effect of compression on the molecular arrangement of itraconazole-soluplus solid dispersions:induction of liquid crystals or exacerbation of phase separation?[J]. Mol Pharm,2016,13(6):1879-1893.
[15]刘明杰,王钊,孙素琴.傅里叶变换红外光谱法在药学研究中应用的最新进展[J].药物分析杂志,2001,21(5):373-377.
[16]田茜,何晨,贺敬霞,等.沙棘总黄酮-聚乙烯吡咯烷酮K30固体分散体的制备、表征及体外溶出研究[J].中国药房,2017,28(1):115-118.
[17] Zhang Q,Pu Y Q,Wang B,et al. Characterization,molecular docking,and in vitro dissolution studies of solid dispersions of20(S)-protopanaxadiol[J]. Molecules, 2017, 22(2):E274.
[18]张雅军,田颂九.衰减全反射傅里叶变换红外光谱法定量分析西咪替丁A晶型的含量[J].中国药学杂志,2005,40(20):1587-1589.
[19] Iqbal W S,Chan K L. FTIR spectroscopic study of poly(ethylene glycol)-nifedipine dispersion stability in different relative humidities[J]. J Pharm Sci,2015,104(1):280-284.
[20]杨伟,渠荣遴.固体核磁共振在高分子材料分析中的研究进展[J].高分子通报,2006(12):69-74.
[21] Yang F Y,Su Y C,Zhu L,et al. Rheological and solid-state NMR assessments of copovidone/clotrimazole model solid dispersions[J]. Int J Pharm,2016,500(1-2):20-31.
[22]胡成龙,陈韶云,陈建,等.拉曼光谱技术在聚合物研究中的应用进展[J].高分子通报,2014(3):30-45.
[23] Cuzzucoli Crucitti V,Migneco L M,Piozzi A,et al. Intermolecular interaction and solid state characterization of abietic acid/chitosan solid dispersions possessing antimicrobial and antioxidant properties[J]. Eur J Pharm Biopharm,2018,125:114-123.
[24] PuncochováK,Vukosavljevic B,Hanu2 J,et al. Non-invasive insight into the release mechanisms of a poorly soluble drug from amorphous solid dispersions by confocal Raman microscopy[J].Eur J Pharm Biopharm,2016,101:119-125.
[25]张兴宁,陈稷,周泽魁.太赫兹时域光谱技术[J].激光与光电子学进展,2005,42(7):35-38.
[26] Takeuchi I,Shimakura K,Kuroda H,et al. Estimation of crystallinity of nifedipine-polyvinylpyrrolidone solid dispersion by usage of terahertz time-domain spectroscopy and of X-ray powder diffractometer[J]. J Pharm Sci,2015,104(12):4307-4313.
[27]王杰晶,李银峰,李佩,等.差示扫描量热法在药物定性分析中的应用[J].现代药物与临床,2013,28(5):815-818.
[28]崔锋,候佳威,孙文霞,等.高乌甲素固体分散体的表征及其体外溶出度测定[J].中药材,2016,39(9):2072-2074.
[29] Saunders M,Podluii K,Shergill S,et al. The potential of high speed DSC(hyper-DSC)for the detection and quantification of small amounts of amorphous content in predominantly crystalline samples[J]. Int J Pharm,2004,274(1-2):35-40.
[30] Mc Gregor C, Bines E. The use of high-speed differential scanning calorimetry(Hyper-DSC)in the study of pharmaceutical polymorphs[J]. Int J Pharm,2007,350(1-2):48-52.
[31]王艳色,魏志勇,申凯华,等.调制差示扫描量热法在高分子材料中的应用[J].高分子通报,2016(3):16-22.
[32] Nair R,Lamare I,Tiwari N K,et al. In situ salification in polar solvents:a paradigm for enabling drug delivery of weakly ionic drugs as amorphous solid dispersion[J]. AAPS Pharm Sci Tech,2018,19(1):326-337.
[33]赵俊霞,尹蓉莉,孙彩霞,等.广金钱草总黄酮-PVP-K30固体分散体的制备和体外特征[J].中成药,2014,36(10):2070-2074.
[34]陈洁,邱利焱,胡敏新,等.多烯紫杉醇固体分散体的制备和体内外研究[J].中国药学杂志,2007,42(22):1717-1722.
[35]叶为标,何小维,黄强,等.透射电子显微镜在淀粉及其衍生物中的应用[J].粮油加工,2008(5):102-105.
[36] Jin X,Zhang Z H,Zhu J,et al. Response surface method optimize of nano-silica solid dispersion technology assistant enzymatic hydrolysis preparation genistein[J]. Acta Pharm Sin,2012,47(4):522-528.
[37] Singh G, Sharma S,Gupta G D. Extensive diminution of particle size and amorphization of a crystalline drug attained by eminent technology of solid dispersion:a comparative study[J].AAPS Pharm SciTech,2017,18(5):1770-1784.
[38]张泸,刘新湘,余红,等.丹皮酚固体分散体的制备和表征[J].中国医药工业杂志,2015,46(3):261-264.
[39] Meng F,Liu T Z,Schneider E,et al. Self-association of rafoxanide in aqueous media and its application in preparing amorphous solid dispersions[J]. Mol Pharm, 2017, 14(5):1790-1799.
[40] Zijlstra G S,Rijkeboer M,Jan van Drooge D,et al. Characterization of a cyclosporine solid dispersion for inhalation[J].AAPS J,2007,9(2):E190-E199.
[41] van Drooge D J,Hinrichs W L J,Visser M R,et al. Characterization of the molecular distribution of drugs in glassy solid dispersions at the nano-meter scale,using differential scanning calorimetry and gravimetric water vapour sorption techniques[J].Int J Pharm,2006,310(1-2):220-229.
[42] Yang Z Y,Nollenberger K,Albers J,et al. The effect of processing on the surface physical stability of amorphous solid dispersions[J]. Eur J Pharm Biopharm,2014,88(3):897-908.