UPLC-MS/MS法同时测定人血浆中卡马西平、拉莫三嗪、氯硝西泮、地西泮及其代谢物奥沙西泮浓度

目的 建立同时测定人血浆中卡马西平、拉莫三嗪、氯硝西泮、地西泮及其代谢物奥沙西泮浓度的方法。方法 采用超高效液相色谱-质谱联用法（UPLC-MS/MS）,以磺胺甲噁唑（SMZ）为内标,血浆经甲醇直接沉淀后进样分析。色谱柱为WatersACQUITYUPLCHSSPFP柱（2.1mm×100mm,1.8μm）,流动相为0.1%甲酸的5mmol·L1乙酸铵水溶液-0.1%甲酸的甲醇溶液（0~5min,35∶65→10∶90）,流速为0.2mL·min1。电喷雾离子源,正离子多反应监测扫描分析,卡马西平、拉莫三嗪、氯硝西泮、地西泮和奥沙西泮的离子对分别为m/z237.0→194.06、m/z255.98→144.95、m/z316.01→270.0、m/z285.04→193.07和m/z287.02→241;内标磺胺甲噁唑的离子对为m/z253.96→91.97。结果 卡马西平、拉莫三嗪、氯硝西泮、地西泮和奥沙西泮血药浓度分别在2.4~600ng·mL1（r=0.9997）,2.52~630ng·mL1（r=0.9920）,2.08~520ng·mL1（r=0.9979）,2.28~570ng·mL1（r=0.9982）,8.0~800ng·mL1（r=0.9992）线性关系良好;最低检出限分别为0.24,0.63,0.52,0.57,3.2ng·mL1。日内、日间精密度均〈15%;提取回收率均〉70%,且RSD〈15%。结论 该方法灵敏、快速、专属性强,可用于临床血药浓度测定及药动学研究。     

UPLC-MS/MS法测定人血浆中奥氮平、利培酮和帕潘立酮的浓度

目的:建立同时测定人血浆中奥氮平、利培酮和帕潘立酮浓度的方法。方法:血浆样品经液-液萃取后,以盐酸丁螺环酮为内标,采用超高效液相色谱-串联质谱法测定。色谱柱为ACQUITY UPLCTM BEH C_(18),流动相为甲醇-0.01 mol/L甲酸铵水溶液,梯度洗脱,流速为0.2 mL/min,柱温为45℃,进样量为5μL。采用电喷雾离子源,以多反应监测模式进行正离子扫描,用于定量分析的离子对分别为m/z 313.29→256.25(奥氮平)、m/z 411.42→191.19(利培酮)、m/z 427.45→207.18(帕潘立酮)和m/z 386.43→122.37(内标)。结果:奥氮平、利培酮、帕潘立酮血药浓度分别在0.426~108.954、0.213~54.476、0.213~54.476 ng/mL范围内线性关系良好;日内、日间RSD<20%,方法回收率分别为83.3%~112.9%,90.0%~109.8%和95.2%~114.9%,提取回收率分别为65.5%~95.0%、73.9%~98.5%和73.6%~99.4%,基质效应和稀释效应均不影响待测物血药浓度的测定。采用该法测得100例精神分裂症患者奥氮平、利培酮和帕潘立酮的血药浓度分别为(103.3±73.6)、(13.1±13.1)和(23.2±20.0)ng/mL。结论:该方法简单、快速、灵敏、特异性高,可用于奥氮平、利培酮和帕潘立酮血药浓度测定及药动学研究。     

LC-MS/MS法同时测定人血清中卡马西平和拉莫三嗪浓度

目的:建立同时测定人血清中卡马西平和拉莫三嗪浓度的方法。方法:采用液-质联用法,以伐地那非和红地那非为内标,血清经乙腈直接沉淀后进样分析。色谱柱为XbridgeTMPhenyl,流动相为含0.02%甲酸的水溶液-含0.02%甲酸的乙腈溶液(60∶40),流速为0.3mL·min-1。电喷雾离子源,正离子多反应监测扫描分析,卡马西平和内标伐地那非的离子对分别为m/z237→194和m/z489→72;拉莫三嗪和内标红地那非的离子对分别为m/z256→43和m/z467→111。结果:卡马西平和拉莫三嗪血药浓度分别在5～500μg·L-1(r=0.9988)和100～10000μg·L-1(r=0.9964)范围内线性关系良好,定量下限分别为5、100μg·L-1。日内、日间RSD均<8%;平均提取回收率分别在88.9%～100.9%和89.5%～100.3%范围内。结论:本方法样品处理简便,适用于临床血药浓度监测及药动学研究。     

UPLC-MS/MS法同时测定人血浆中氯吡格雷及其代谢物的浓度

目的:建立同时测定人血浆中氯吡格雷(CLO)及其活性代谢产物(CATM)、非活性代谢产物(CCAM)浓度的方法,并用于药动学研究。方法:取烷化剂2-溴-3′-甲氧基苯乙酮(MPB)保护的血浆样品,经乙腈沉淀蛋白后,以卡马西平为内标,采用超高效液相色谱-串联质谱(UPLC-MS/MS)法测定。色谱柱为Waters ACQUITY UPLC HSS T3,流动相为水(含0.1%甲酸)-乙腈(含0.1%甲酸),梯度洗脱,流速为0.50 ml/min。采用电喷雾电离源(ESI),多反应监测(MRM)方式进行正离子监测,用于定量分析的离子对分别为m/z 322.1→211.8(CLO)、m/z 504.1→155.0(CATM烷化衍生物,CATMD)、m/z 308.3→198.0(CCAM)、m/z 273.2→194.3(内标)。结果:CLO、CATMD、CCAM血药浓度分别在0.03~20.00、0.30~200.00、10.00~10 000.00 ng/ml范围内线性关系良好;日内、日间RSD<15%,相对误差(RE)为-3.5%~5.7。5名健康受试者单剂量口服CLO 300 mg后,CLO、CATM、CCAM的cmax分别为(7.89±5.46)、(15.58±8.08)、(8 023.33±1 047.39)ng/ml,tmax分别为(1.25±0.43)、(1.25±0.43)、(1.67±0.29)h,t1/2分别为(2.31±0.61)、(0.64±0.08)、(6.53±2.55)h,AUC0-t分别为(17.19±14.59)、(21.39±9.58)、(30 648.85±8 026.63)ng·h/ml。结论:该方法操作简便、灵敏度高、分析时间短,适用于CLO及其代谢物血药浓度测定及药动学研究。     

LC-MS/MS法测定人血浆中卡马西平的浓度

目的建立LC-MS/MS法测定人血浆中卡马西平的浓度。方法以卡马西平-d2作为内标,血浆经甲醇直接蛋白沉淀后进样分析,色谱柱为CAPCELL PAK C18(100 mm×2.0 mm,5μm),流动相为甲醇-0.1 mmol·L-1乙酸铵水溶液(含0.02%乙酸)(70∶30),流速0.3 m L·min-1。电喷雾离子源,正离子多反应监测扫描分析。卡马西平和内标卡马西平-d2的离子对分别为m/z 237.1→194.1和m/z 239.1→196.1。结果卡马西平在质量浓度3.077 9~1 231.2μg·L-1内线性良好(r=0.999 3,n=10);批内和批间精密度良好(RSD均<7.0%);提取回收率为98.94%~108.84%,RSD<15%;基质效应为92.76%~98.54%,RSD<5%。结论本方法灵敏度、重复性以及专属性均较好,样品处理简便易行,可用于卡马西平的血药浓度测定及药动学研究。     

高效液相色谱-质谱串联法同时测定人血清中拉莫三嗪及卡马西平的含量

目的:建立高效液相色谱-质谱串联(LC-MS/MS)法测定人血清中拉莫三嗪及卡马西平的含量。方法:取人血清经乙腈直接沉淀后进样分析,色谱柱为Diamonsil C18(150 mm×4.6 mm,5μm),流动相为甲醇∶0.2%甲酸水溶液,流速为0.4 mL.min-1;流动相采用梯度洗脱。质谱采用ESI离子源,正离子多反应监测扫描分析,拉莫三嗪离子对为m/z 256→145,卡马西平离子对为m/z 237→194。结果:卡马西平和拉莫三嗪血药浓度分别在5～500μg.L-1(r=0.998 9)和5～500μg.L-1(r=0.997 2)范围内线性关系良好,定量下限分别为5μg.L-1。日内、日间RSD均<7.0%;提取回收率均>85%。结论:本方法处理样品简便,适用于临床血药浓度监测及为联合用药的药动学研究奠定基础。     

芪苈强心胶囊中芥子碱硫氰酸盐、槲皮素和山柰酚在大鼠体内的药动学研究

目的:建立测定大鼠血浆中芥子碱硫氰酸盐、槲皮素和山柰酚含量的方法,并研究大鼠体内芪苈强心胶囊的药动学。方法:采用高效液相色谱-串联质谱(HPLC-MS/MS)法。色谱柱为ZOBRAX XDB-C18,流动相为0.1%甲酸水溶液-含0.1%甲酸的乙腈溶液(梯度洗脱),流速为0.45 mL/min,进样量为10μL,定量离子为芥子碱硫氰酸盐质荷比(m/z)310.2→251.2,槲皮素m/z301.1→150.7,山柰酚m/z 286.2→242.0,内标氯霉素m/z 320.9→151.9。6只大鼠灌胃给予芪苈强心胶囊1.3 g/kg后0.083、0.167、0.333、0.667、1、1.5、2、3、4、6、8、12、24 h经目内眦静脉丛取血,并测定芥子碱硫氰酸盐、槲皮素和山柰酚的血药浓度。采用DAS3.0软件拟合计算各药动学参数。结果:芥子碱硫氰酸盐、槲皮素和山柰酚的检测质量浓度线性范围分别为0.05～100、0.1～200、0.1～200 ng/mL(r=0.999 4、0.999 7、0.999 9),精密度试验及基质效应RSD均≤11.55%(n=6),稳定性试验RE≤14.69%(n=3)。芥子碱硫氰酸盐、榭皮素和山柰酚在大鼠体内的cmax分别为(1.35±0.62)、(3.23±1.26)、(5.27±1.66)ng/mL,t_(max)分别为(1.50±0.00)、(0.67±0.00)、(0.67±0.00)h,t_(1/2)分别为(3.98±0.99)、(3.33±0.41)、(4.54±0.85)h,CL分别为(3 683.82±987.96)、(2 852.33±695.88)和(1 611.85±129.59)mL/(h·kg),AUC_(0-24h)分别为(3.98±1.21)、(10.96±3.42)和(13.59±5.35)h·ng/mL。结论:该检测方法灵敏度高、专属性强、重复性好,适用于芪苈强心胶囊中芥子碱硫氰酸盐、槲皮素和山柰酚在大鼠体内的药动学研究。     

LC-MS/MS法测定癫痫患者血清中卡马西平的浓度

目的:建立以高效液相色谱-电喷雾串联质谱(LC-MS/MS)法测定癫痫患者血清中卡马西平浓度的方法。方法:色谱柱为Zorbax Extend-C18,流动相为甲醇-0.01mmol.L-1乙酸铵溶液(80:20),流速为0.3mL.min-1,进样量为10μL;离子源为电喷雾离子化源,正离子方式检测,扫描方式为正离子监测,卡马西平的碰撞诱导解离电压为30V,用于定量分析的离子反应为m/z237.2→m/z194.2。结果:卡马西平血药浓度在2.0～40.0ng.mL-1范围内线性关系良好(r=0.9974);平均提取回收率为101.1%,日内、日间RSD分别为3.39%、4.11%。10名患者血清中卡马西平的平均浓度为5.69ng.mL-1(RSD=4.75%),比荧光偏振免疫法测定结果的RSD小。结论:本方法专属性强,灵敏度和准确度、重现性好,易于操作,可用于癫痫患者血清中卡马西平浓度的测定。     

盐酸美金刚缓释胶囊在比格犬体内的药动学研究

目的建立LC-MS/MS法研究盐酸美金刚缓释胶囊在比格犬体内的药动学特征。方法采用Agilent Extend-C18色谱柱(30 mm×4.6 mm,1.8μm);流动相A为0.1%甲酸,流动相B为甲醇,流动相B比例为65%,等度洗脱2.5 min;体积流量为1 mL/min,柱温40℃;进样量5μL。采用电喷雾离子源(ESI),多级反应监测(MRM)模式,以正离子化方式进行检测,用于定量分析的离子反应分别为m/z 180.0→107.0(盐酸美金刚)、m/z 268.0→116.0(内标琥珀酸美托洛尔)。将6只比格犬随机分为两组,采用两种制剂双周期交叉给药方法,分别ig盐酸美金刚缓释胶囊受试制剂或参比制剂1粒。采用LC-MS/MS法测定比格犬体内盐酸美金刚血药浓度。采用DAS ver 2.1.1软件进行数据分析并计算出相关药动学参数。结果盐酸美金刚的线性范围为1.25～125 ng/mL,定量下限为1.25 ng/mL,日内、日间精密度RSD值均小于6.5%。单次ig受试制剂和参比制剂后,比格犬血浆中盐酸美金刚的Cmax分别为(59.99±14.78)、(64.79±16.26)ng/mL,tmax分别为(7.83±2.64)、(7.33±3.5)h,t1/2分别为(10.84±2.04)、(11.39±1.31)h,AUC0-t分别为(9.99±3.3)、(11.02±2)μg·h/mL,AUC0-∞分别为(10.63±3.42)、(11.72±2.13)μg·h/mL。结论采用LC-MS/MS方法操作简单、准确度、专属性高,可用于盐酸美金刚缓释胶囊的药动学研究,盐酸美金刚受试制剂在比格犬体内药动学行为与参比制剂相似。     

液相色谱串联质谱法测定人血浆中文拉法辛及其代谢物的浓度

目的建立测定血浆中文拉法辛及其代谢物O-去甲基文拉法辛的液相色谱串联质谱(LC-MS/MS)方法。方法血浆样品中加入内标(氘6-文拉法辛和氘6-O-去甲基文拉法辛),直接沉淀法处理样品。色谱柱为CAPCELL PAK C18 MGⅢ分析柱(100 mm×2.0 mm,5μm),流动相为含0.3%甲酸的水溶液-含0.3%甲酸的乙腈溶液(78∶22,V/V),流速为0.3 mL.min-1。正离子多离子反应监测(MRM)扫描分析,离子通道分别为m/z 278→58(文拉法辛)、m/z 264→58(O-去甲基文拉法辛)、m/z 284→58(氘6-文拉法辛)、m/z 270→58(氘6-O-去甲基文拉法辛)。结果文拉法辛和O-去甲基文拉法辛的线性范围均为2～1 000μg.L-1,定量下限均为2μg.L-1,提取回收率在90.14%～97.33%,批内、批间RSD均小于8%。结论本方法操作简便,特异性强,灵敏度高,可用于人血浆内文拉法辛和O-去甲基文拉法辛的含量测定研究。     

Safety assessment of poloxamers 101, 105, 108, 122, 123, 124, 181, 182, 183, 184, 185, 188, 212, 215, 217, 231, 234, 235, 237, 238, 282, 284, 288, 331, 333, 334, 335, 338, 401, 402, 403, and 407, poloxamer 105 benzoate, and poloxamer 182 dibenzoate as used in cosmetics

Poloxamers are polyoxyethlyene, polyoxypropylene block polymers. The impurities of commercial grade Poloxamer 188, as an example, include low-molecular-weight substances (aldehydes and both formic and acetic acids), as well as 1,4-dioxane and residual ethylene oxide and propylene oxide. Most Poloxamers function in cosmetics as surfactants, emulsifying agents, cleansing agents, and/or solubilizing agents, and are used in 141 cosmetic products at concentrations from 0.005% to 20%. Poloxamers injected intravenously in animals are rapidly excreted in the urine, with some accumulation in lung, liver, brain, and kidney tissue. In humans, the plasma concentration of Poloxamer 188 (given intravenously) reached a maximum at 1 h, then reached a steady state. Poloxamers generally were ineffective in wound healing, but were effective in reducing postsurgical adhesions in several test systems. Poloxamers can cause hypercholesterolemia and hypertriglyceridemia in animals, but overall, they are relatively nontoxic to animals, with LD(50) values reported from 5 to 34.6 g/kg. Short-term intravenous doses up to 4 g/kg of Poloxamer 108 produced no change in body weights, but did result in diffuse hepatocellular vacuolization, renal tubular dilation in kidneys, and dose-dependent vacuolization of epithelial cells in the proximal convoluted tubules. A short-term inhalation toxicity study of Poloxamer 101 at 97 mg/m(3) identified slight alveolitis after 2 weeks of exposure, which subsided in the 2-week postexposure observation period. A short-term dermal toxicity study of Poloxamer 184 in rabbits at doses up to 1000 mg/kg produced slight erythema and slight intradermal inflammatory response on histological examination, but no dose-dependent body weight, hematology, blood chemistry, or organ weight changes. A 6-month feeding study in rats and dogs of Poloxamer 188 at exposures up to 5% in the diet produced no adverse effects. Likewise, Poloxamer 331 (tested up to 0.5 g/kg day(-1)), Poloxamer 235 (tested up to 1.0 g/kg day(-1)), and Poloxamer 338 (at 0.2 or 1.0 g/kg day(-1)) produced no adverse effects in dogs. Poloxamer 338 (at 5.0 g/kg day(-1)) produced slight transient diarrhea in dogs. Poloxamer 188 at levels up to 7.5% in diet given to rats in a 2-year feeding study produced diarrhea at 5% and 7.5% levels, a small decrease in growth at the 7.5% level, but no change in survival. Doses up to 0.5 mg/kg day(-1) for 2 years using rats produced yellow discoloration of the serum, high serum alkaline phosphatase activity, and elevated serum glutamicpyruvic transaminase and glutamic-oxalacetic transaminase activities. Poloxamers are minimal ocular irritants, but are not dermal irritants or sensitizers in animals. Data on reproductive and developmental toxicity of Poloxamers were not found. An Ames test did not identify any mutagenic activity of Poloxamer 407, with or without metabolic activation. Several studies have suggested anticarcinogenic effects of Poloxamers. Poloxamers appear to increase the sensitivity to anticancer drugs of multidrug-resistant cancer cells. In clinical testing, Poloxamer 188 increased the hydration of feces when used in combination with a bulk laxative treatment. Compared to controls, one study of angioplasty patients receiving Poloxamer 188 found a reduced myocardial infarct size and a reduced incidence of reinfarction, with no evidence of toxicity, but two other studies found no effect. Poloxamer 188 given to patients suffering from sickle cell disease had decreased pain and decreased hospitilization, compared to controls. Clinical tests of dermal irritation and sensitization were uniformly negative. The Cosmetic Ingredient Review (CIR) Expert Panel stressed that the cosmetic industry should continue to use the necessary purification procedures to keep the levels below established limits for ethylene oxide, propylene oxide, and 1,4-dioxane. The Panel did note the absence of reproductive and developmental toxicity data, but, based on molecular weight and solubility, there should be little skin penetration and any penetration of the skin should be slow. Also, the available data demonstrate that Poloxamers that are introduced into the body via routes other than dermal exposure have a rapid clearance from the body, suggesting that there would be no risk of reproductive and/or developmental toxicity. Overall, the available data do not suggest any concern about carcinogenesis. Although there are gaps in knowledge about product use, the overall information available on the types of products in which these ingredients are used, and at what concentration, indicates a pattern of use. Based on these safety test data and the information that the manufacturing process can be controlled to limit unwanted impurities, the Panel concluded that these Poloxamers are safe as used.     

HPLC法测定抗妇炎胶囊中木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱

目的 采用高效液相色谱（HPLC）法同时测定抗妇炎胶囊中木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱10种活性成分。方法 采用InerSustain AQ-C₁₈色谱柱（250 mm×4.6 mm,5 μm）,流动相A：乙腈–无水乙醇（80∶20）,流动相B：0.1%磷酸溶液,梯度洗脱,检测波长220 nm,体积流量1.0 mL/min,柱温30℃,进样量10 μL。结果 木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱分别在2.69～134.50、1.95～97.50、0.63～31.50、0.86～43.00、11.95～597.50、0.59～29.50、6.08～304.00、4.85～242.50、1.66～83.00、19.79～989.50 μg/mL线性关系良好（r≥0.999 3）;平均回收率分别为99.11%、98.23%、96.95%、97.78%、100.02%、97.21%、99.66%、99.52%、98.81%、100.08%,RSD值分别为1.04%、1.23%、1.37%、1.65%、0.70%、1.28%、0.65%、0.81%、1.11%、0.63%。结论 建立的HPLC法可用于抗妇炎胶囊中10种活性成分的测定,作为抗妇炎胶囊质量控制方法。     

Arformoterol: (R,R)-eformoterol, (R,R)-formoterol, arformoterol tartrate, eformoterol-sepracor, formoterol-sepracor, R,R-eformoterol, R,R-formoterol

Sepracor in the US is developing arformoterol [R,R-formoterol], a single isomer form of the beta(2)-adrenoceptor agonist formoterol [eformoterol]. This isomer contains two chiral centres and is being developed as an inhaled preparation for the treatment of respiratory disorders. Sepracor believes that arformoterol has the potential to be a once-daily therapy with a rapid onset of action and a duration of effect exceeding 12 hours. In 1995, Sepracor acquired New England Pharmaceuticals, a manufacturer of metered-dose and dry powder inhalers, for the purpose of preparing formulations of levosalbutamol and arformoterol. Phase II dose-ranging clinical studies of arformoterol as a longer-acting, complementary bronchodilator were completed successfully in the fourth quarter of 2000. Phase III trials of arformoterol began in September 2001. The indications for the drug appeared to be asthma and chronic obstructive pulmonary disease (COPD). However, an update of the pharmaceutical product information on the Sepracor website in September 2003 listed COPD maintenance therapy as the only indication for arformoterol. In October 2002, Sepracor stated that two pivotal phase III studies were ongoing in 1600 patients. Sepracor estimates that its NDA submission for arformoterol, which is projected for the first half of 2004, will include approximately 3000 adult subjects. Sepracor stated in July 2003 that it had completed more than 100 preclinical studies and initiated or completed 15 clinical studies for arformoterol inhalation solution for the treatment of bronchospasm in patients with COPD. In addition, Sepracor stated that the two pivotal phase III studies in 1600 patients were still progressing. In 1995, European patents were granted to Sepracor for the use of arformoterol in the treatment of asthma, and the US patent application was pending.     

欧洲刺柏（Juniper）

活性成分与药理作用欧洲刺柏药用部位是其浆果，具有促水排泄、防腐、抗胃肠胀气和抗风湿作用，还可改善胃功能。用作促水排泄药可增加尿量（水丢失），但不增加钠排泄。成分萜品烯-4-醇可增加肾小球滤过率，但刺激肾。欧洲刺柏浆果对单纯疱疹病毒体外显示抗病毒活性，并具抗真菌活性。动物实验显示，欧洲刺柏浆果提取物具有堕胎、抗生育、抗炎、抗胚胎植入、降血压、升血压和降血糖作用。欧洲刺柏浆果油具有兴奋子宫的活性，以及利尿、胃肠道抗菌和刺激作用，该油对平滑肌有阻止解痉作用。     

Oral Presentations (LDD, LPES, LNM, LPAT, LNT, LPPT, LPM)

Probiotic microorganisms have been shown to provide specific health benefits when consumed as food supplements or as food components. The main problem of such products is the poor survival of the probiotic bacteria in the low pH of gastric fluid. However the use of synthetic excipients for enteric coating to prevent the exposure of microorganisms to gastric fluid is limited in food supplementary industry. Therefore the aim of this study was to develop an enteric coating formulation containing shellac as a natural polymer. Shellac possesses good resistance to gastric juice; the major disadvantage of this polymer is its low solubility in the intestinal fluid [1, 2]. Thus films containing different ratios of shellac and water-soluble polymers (sodium alginate, hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidon (PVP)) or plasticizers (glycerol and glyceryl triacetate (GTA)) were prepared in order to analyse the films’ melting temperatures (T_m), the changes in enthalpy (ΔH), their capability of taking up water, and their solubility in different media. The release characteristics of the films were studied by loading pellets with Enterococcus faecium M74 and coating them with formulations containing different amounts of shellac and polymer or plasticized shellac. Using dissolution tests, performed according to USP XXXI paddle method, the resistance of the coatings to simulated gastric fluid (SGF, pH 1.2) and the release of cells in simulated intestinal fluid (SIF, pH 6.8) was investigated.The trials showed that an increasing amount of plasticizer results in a decrease of T_m and ΔH of the films whereat glycerol had a superior plasticization effect to GTA. The compatibility of films made of water-soluble polymers and shellac was also concentration dependent. HPMC and PVP showed superior compatibility with shellac compared to sodium alginate, since films containing shellac and more than 10% [w/w] sodium alginate tended to separate into two phases. In the end five formulations containing shellac and either 5% [w/w] glycerol, 10% [w/w] PVP, 20% [w/w] PVP, 10% [w/w] HPMC, or 5% [w/w] sodium alginate emerged as feasible for enteric coating purposes.