【摘要】：埃索美拉唑鎂是治療酸相關(guān)疾病的藥物,是第一個(gè)單一光學(xué)異構(gòu)體的質(zhì)子泵抑制劑。2003年,埃索美拉唑鎂腸溶片在中國(guó)獲得上市批準(zhǔn)(商品名:耐信,Nexium),上市的埃索美拉唑鎂腸溶片有20 mg和40 mg兩種規(guī)格。本課題對(duì)方法學(xué)進(jìn)行了再驗(yàn)證并對(duì)埃索美拉唑鎂腸溶片進(jìn)行了質(zhì)量研究。通過實(shí)驗(yàn),主要得出以下幾個(gè)結(jié)論:本實(shí)驗(yàn)對(duì)埃索美拉唑鎂腸溶片進(jìn)行了質(zhì)量研究,分別采用高效液相色譜法對(duì)其含量、溶出曲線、有關(guān)物質(zhì)、異構(gòu)體等進(jìn)行了檢測(cè),結(jié)果均符合2015版《中國(guó)藥典》艾司奧美拉唑鎂腸溶片質(zhì)量標(biāo)準(zhǔn)。有關(guān)物質(zhì)測(cè)定色譜條件:色譜柱:Microspher C18(4.6 mm×100 mm,3μm);流動(dòng)相A:水-pH7.6磷酸鹽緩沖液(每1000 mL中含磷酸二氫鈉0.0052 mol、磷酸氫二鈉0.0135 mol)-乙腈(80:10:10),流動(dòng)相B:乙腈-pH7.6磷酸鹽緩沖液-水(80:1:19);進(jìn)樣體積:20μL;柱溫:35℃;檢測(cè)波長(zhǎng):302 nm。流速:1 mL/min。主藥與有關(guān)物質(zhì)D的分離度大于2.5�？瞻纵o料不干擾有關(guān)物質(zhì)的測(cè)定。埃索美拉唑鎂及有關(guān)物質(zhì)線性關(guān)系良好;該方法準(zhǔn)確,簡(jiǎn)便,重復(fù)性好,可用于埃索美拉唑鎂腸溶片的質(zhì)量控制。含量、溶出曲線測(cè)定色譜條件:色譜柱:Aglient Microspher C18,3.0μm,4.6mm×100 mm;流動(dòng)相:乙腈-pH7.3磷酸鹽緩沖液-水(35:50:15);檢測(cè)波長(zhǎng):302 nm;進(jìn)樣體積:20μL;流速:1 mL/min;柱溫:40℃。主峰保留時(shí)間大于3.5 min�？瞻纵o料不干擾含量、溶出樣品的測(cè)定,專屬性較好,回收率均在98%~102%之間,符合要求,該方法能夠準(zhǔn)確測(cè)定埃索美拉唑鎂腸溶片含量和溶出度。對(duì)映異構(gòu)體檢測(cè)色譜條件:流動(dòng)相:乙腈-磷酸鹽緩沖液(pH6.0)-水(150:85:765);色譜柱:CHIRALAPK?AGP(100×4 mm,5μm);檢測(cè)波長(zhǎng):302 nm;進(jìn)樣體積:20μL;流速:0.6 mL/min;柱溫:25℃。該方法簡(jiǎn)便,準(zhǔn)確,專屬性好,能夠準(zhǔn)確測(cè)定R-奧美拉唑的含量。最后,對(duì)埃索美拉唑腸溶片穩(wěn)定性進(jìn)行了考察。影響因素實(shí)驗(yàn)、六個(gè)月的加速實(shí)驗(yàn)分別以腸溶片的外觀性狀、溶出度、含量等為考察指標(biāo)。實(shí)驗(yàn)結(jié)果表明,埃索美拉唑鎂腸溶片在高溫、高濕條件下均不穩(wěn)定,應(yīng)采用防潮包裝并且避免接觸高溫環(huán)境。由加速實(shí)驗(yàn)數(shù)據(jù)的變化趨勢(shì)可知,自制片與參比制劑的含量、有關(guān)物質(zhì)、溶出度變化趨勢(shì)基本一致,均符合艾司奧美拉唑鎂腸溶片質(zhì)量標(biāo)準(zhǔn),具有較好的穩(wěn)定性。
[Abstract]:Esomeprazole magnesium is the first proton pump inhibitor of a single optical isomer to treat acid-related diseases. Esomeprazolium enteric-coated tablets were approved in China in 2003 (trade name:, Nexium),) Esomeprazole magnesium enteric-coated tablets are available in 20 mg and 40 mg specifications. The methodology was revalidated and the quality of esomeprazolium enteric-coated tablets was studied. The main conclusions are as follows: the quality of esomeprazole magnesium enteric-coated tablets was studied in this experiment. The contents, dissolution curves, related substances, isomers and so on were determined by HPLC. The results were in accordance with the quality standard of esomeprazole tablets in 2015 edition of Chinese Pharmacopoeia. Chromatographic conditions for the determination of related substances: Microspher C18 (4.6 mm 脳 100 mm,3 渭 m);) Mobile phase A: water pH7.6 phosphate buffer (containing 0.0052 mol, sodium dihydrogen phosphate 0.0135 mol per 1000 mL) -acetonitrile (80:10:10), Mobile phase B: acetonitrile-pH7.6 phosphate buffer solution-water (80:1:19); Injection volume: 20 渭 L; column temperature: 35 鈩，

本文編號(hào)：2421860