高效液相色谱法测定盐酸奈福泮萘普生胶囊中萘普生含量

目的建立高效液相色谱法测定盐酸奈福泮萘普生胶囊中萘普生含量。方法采用Krom Tek C18色谱柱（250mm×4.6mm，5μm），流动相为甲醇-用磷酸调节pH=3.0的0.01mol／L磷酸二氢钾溶液（75：25），流速为0，9mL／min，检测波长为262nm。结果萘普生质量浓度在50.02～600.24μg／mL范围内与峰面积有良好的线性关系，平均回收率为99.68％，RSD为0．86％（n=9）。结论该方法简便、准确，可用于控制盐酸奈福泮萘普生胶囊的质量。     

HPLC法同时测定盐酸奈福泮萘普生胶囊中2种成分的含量

目的 建立同时测定盐酸奈福泮萘普生胶囊中盐酸奈福泮和萘普生含量的高效液相色谱方法.方法 采用Apollo C18色谱柱,以庚烷磺酸钠溶液-乙腈(53:47)为流动相,流速为1.0 mL·min-1,检测波长为215 nm.结果 盐酸奈福泮浓度在15.8～47.5 μg·mL-1范围内与峰面积线性关系良好(r=0.9997),平均回收率为99.43％,RSD为1.31％(n=3);萘普生在54.7～164.2 μg·mL-1范围内线性关系良好(r=0.9999),平均回收率为99.72％,RSD为0.80％(n=3).结论 该方法操作简便,结果准确,精密度高,可用于控制盐酸奈福泮萘普生胶囊的质量.     

高效液相色谱法测定萘普生缓释片中萘普生的含量

目的:建立测定萘普生缓释片中萘普生含量的高效液相色谱法.方法:分析柱为HiQ sil C18柱(4.6 mm×250 mm,5 μm),流动相为0.02 mol/L磷酸二氢钾溶液(pH=3.5)-甲醇-乙腈(3:4:3),流速为1.0 mL/min,检测波长为275 nm.结果:萘普生线性范围是26～156μg/mL,平均回收率为98.8%,RSD=1.47%(n=9).结论:高效液相色谱法简便快速、准确可靠,可用于萘普生缓释片中萘普生的含量测定.     

高效液相色谱法测定盐酸奈福泮萘普生胶囊中盐酸奈福泮含量

目的 建立测定盐酸奈福泮萘普生胶囊中盐酸奈福泮萘含量的高效液相色谱法.方法 色谱柱为AgilentC18柱(250 mm×4.6mm,5 μm),以庚烷磺酸钠溶液(取庚烷磺酸钠2.02g,加水900mL使溶解,加三乙胺2mL,用稀磷酸调节pH=3.0,加水至1 000mL)-乙腈(60:40)为流动相,流速为1.0 mL/min,检测波长为215 nm.结果 盐酸奈福泮萘质量浓度在10.16 ～ 101.60 μg/mL范围内与峰面积线性关系良好(r=0.9999),平均回收率为100.23％,RSD为0.83％(n=6).结论 该方法简便、准确,可用于控制盐酸奈福泮萘普生胶囊的质量.     

紫外分光光度法测定萘普生-β-环糊精包合物中萘普生的含量

目的:建立测定萘普生-β-环糊精包合物中萘普生含量的方法。方法:采用紫外分光光度法,测定波长为330nm。结果:萘普生检测浓度在2·0~80·0mg/L范围内线性关系良好(r=0·9995,n=5),平均加样回收率为99·22%(RSD=1·03%)。结论:该方法简便、可靠,适用于萘普生-β-环糊精包合物中萘普生含量的测定。     

萘普西诺及其对映异构体的HPLC法测定

建立了高效液相色谱法测定萘普西诺及其对映异构体.采用ChiralpakAD-H色谱柱,以正己烷∶异丙醇(95∶5)为流动相,检测波长232 nm.萘普西诺在0.015～20μg/ml范围内线性关系良好.萘普西诺与其R-异构体分离良好,回收率为99.4％和96.2％,RSD为0.61％和8.1％.     

高效液相色谱测定萘普待因片中萘普生及磷酸可待因含量

目的：建立高效液相色谱法测定萘普待因片中萘普生及磷酸可待因的含量。方法：色谱柱：Kromasil C18（4.6mm×250mm,5μm）；流动相：A液为0.01M辛烷磺酸钠∶冰醋酸（50∶1）,B液为甲醇,萘普生测定流动相为A液∶B液（30∶70）,磷酸可待因测定流动相为A液B液梯度洗脱,流速均为1.0mL/min；紫外检测波长：萘普生262nm,磷酸可待因284nm。结果：萘普生的进样量线性范围为0.256～1.28μg,r=0.9999,平均模拟回收率为100.1%,RSD为0.42%（n=9）；磷酸可待因的进样量线性范围为0.993～4.965μg,r=0.9999,平均模拟回收率为99.5%,RSD为0.35%（n=9）。结论：本法准确、重现性好、精密度高。     

超临界流体色谱法拆分萘普生对映体

目的:建立拆分萘普生对映体的方法。方法:采用超临界流体色谱法。以萘普生对映体的分离时间、容量因子、分离因子、分离度为考察指标,优选手性色谱柱、流动相中极性添加剂种类及占比、背压和柱温的条件。结果:优选条件为手性色谱柱采用CHIRALPAK®AD-H,极性添加剂为异丙醇(占比为20%),背压170 bar,柱温20℃,检测波长283 nm。在此条件下萘普生对映体能够达到基线分离,分离度为4.31,分离因子为1.90,且精密度、稳定性和重复性试验中相关指标的RSD均≤2.65%(n=5)。结论:建立的拆分方法简单、重现性好、拆分效果好,可用于萘普生对映体的手性分离。     

萘普生海藻酸钙凝胶微丸中萘普生的含量测定

目的:建立萘普生海藻酸钙凝胶微丸中萘普生的含量测定方法。方法:使用0．1 mol·L-1的枸橼酸钠水溶液为溶剂,在330 nm波长处紫外测定。结果:萘普生线性范围是40．3～100．8μg·ml-1,r=0．999 9,平均回收率100．3％,RSD=0．45％(n=9)。结论:本法准确可靠,简便快速,重复性好,可用于萘普生海藻酸钙凝胶微丸中萘普生的含量测定。     

萘普生涂膜剂的质量标准研究

目的建立萘普生涂膜剂的质量控制标准。方法采用分光光度法测量萘普生的含量,并进行稳定性研究。结果萘普生含量测定方法的回收率为100.13%,RSD为0.33%(n=5)。结论本文建立的质量标准可以控制萘普生涂膜剂的质量。     

HPLC法测定人血浆中萘普生的浓度

目的建立高效液相色谱法测定萘普生血药浓度的方法。方法采用HPLC法测定普生缓释片中萘普生的血浆药物浓度。大连依利特Hypersil ODS（5μm，4．6mm×250mm）柱，柱温40℃；流动相为甲醇-磷酸二氢钠缓冲液（50mmoL／L磷酸二氢钠水溶液，含0．3％三乙胺，用磷酸调pH值为3．7）=68．9：31．1；流速1．0mL／min。紫外检测波长为230nm。结果萘普生在0．93～93．20μg／ml线性关系良好，r^2=0．9999，最低检测浓度为0．10μg／ml。结论本法快速、灵敏，适用于萘普生血药浓度的监测。     

萘普生微丸的制备工艺研究

目的：研究萘普生微丸的制备工艺。方法：采用层积式制丸法制备萘普生微丸，对制备工艺和微丸质量进行了评价。结果：液相层积法和粉末层积法的上药率和微丸收率均达到90％以上，制备的微丸质量良好。结论：采用层积式制丸法制备萘普生微丸工艺可行。     

DOSE DEPENDENT PHARMACOKINETICS OF NAPROXEN IN MAN

The pharmacokinetics of one of the most widely used non-steroidal antiinflammatory drugs, naproxen, were studied in 28 healthy human volunteers at the two most commonly used dose levels, viz., 250 mg and 500 mg, in a cross-over design. The plasma levels of naproxen were analysed by a modified high-pressure liquid chromatography method. The plasma concentrations at higher doses were not proportional to dose, indicating a non-linearity in the pharmacokinetics at the dose levels studied; this finding is new since earlier studies had studied only higher doses and assumed that at lower doses the pharmacokinetics would be linear. There was, however, no significant difference in the elimination half-life (rate constant), time to reach peak concentration (C_max ), mean residence time (MRT), or area under first moment curve (AUMC). The clearance and distribution volume of naproxen were substantially increased at higher dose resulting in statistically lower proportional concentration and the total area under the curve (AUC). These observations are explained on the basis of a change in the plasma protein binding resulting in more free naproxen available for quicker clearance and wider penetration into tissues. These findings have several important clinical implications for the long-term use of naproxen as an antiarthritic drug. It is proposed that the clinical efficacy of naproxen can be increased and side-effects reduced by giving it in small divided doses instead of large doses.     

萘普生市场透析

目的 :了解我国萘普生的市场现状及发展趋势。方法 :介绍萘普生在生产和应用方面的最新进展 ,对其市场前景进行分析。结果与结论 :我国萘普生生产具有一定基础 ,生产企业尚需密切注意市场变化 ,完善自身条件 ,以求进一步发展     

紫外分光光度法测定萘普生片的含量

采用乙醇为溶剂的紫外分光光度法测定萘普生片的含量，不受辅料干扰，简单、快速、准确。萘普生乙醇溶液的吸收系数（Ｅ３３１ｎｍ）为８５．６，ＲＳＤ为０．９０％（ｎ＝２０）。平均回收率为１００．４％，ＲＳＤ为０．５１％（ｎ＝５）。本法与中和法作了比较，结果无明显差异（Ｐ＞０．０５）。     

Interaction of naproxen with cholestyramine

‘In vitro’ and ‘in vivo’ studies were used to determine the interaction of naproxen, an anti-inflammatory agent, and cholestyramine, a hypocholesterolemic substance. Cholestyramine shows a marked affinity for naproxen and the intensity of this is governed by the pH values. The maximum amount of naproxen adsorbed by the resin is close to 2·2 mMg^?1. The pharmacokinetics of naproxen was studied in eight healthy volunteers after concurrent oral administration in a single dose of 250 mg of naproxen and 4 g of cholestyramine. The resin causes an important delay in the incorporation of naproxen into the systemic circulation, though no significant modifications are seen to take place in any other pharmacokinetic parameters of the drug.     

Preparation of microparticles of naproxen with Eudragit RS and Talc by spherical crystallization technique

Microparticles of naproxen with Eudragit RS and talc were prepared by the spherical crystallization technique, i.e. quasi-emulsion solvent diffusion method. The obtained microparticles were evaluated by micromeritic properties, yield, encapsulation efficiency, drug physical state and dissolution rate of drug. The influence of formulation factors and preparation condition (drug: polymer ratio, talc: polymer ratio, SLS concentration, stirring speed) on the properties of the microparticles were also examined. The resultant microparticles were finely spherical and uniform with high incorporation efficiency and yield. Greater encapsulation efficiency was obtained by increasing the drug: polymer ratio and talc: polymer ratio and by reducing the SLS %. The dissolution rate of naproxen from microparticles was enhanced significantly with increasing the ratio of drug: polymer and stirring rate, and sustained by increasing SLS % in crystallization medium. The results of X-ray diffraction and differential scanning calorimeter analysis indicated that naproxen was highly dispersed in microparticles, so as amorphous state. Studies carried out to characterize the micromeritic properties of formulations, such as flowability and packability showed that microparticles were suitable for further pharmaceutical manipulation (e.g. capsule filling). Hence, the spherical crystallization technique can be successfully used for obtaining spherical microparticles, generating a heterogeneous matrix system and providing sustained drug release.     

Comparative in vitro and in vivo bioavailability of naproxen from tablet and caplet formulations

A 500 mg dose of naproxen in a caplet formulation (product A) or a tablet (Naprosyn 500, product B) was administered to 14 fasting healthy subjects on two separate occasions, separated by a 1–2 week washout period in an open, randomized crossover. Blood samples were drawn periodically and plasma naproxen concentrations measured by HPLC. The median time T_max to reach peak concentration for product A was shorter than that for product B (1·025 h versus 1·5 h) but A and B were similar with respect to median peak plasma concentration C_max (77·9 mg 1^?1 versus 71·4 mg 1^?1), and average area AUC_0–∞ under the plasma concentration—time curve (1210·2 mg 1^?1 h versus 1211·0 mg 1^?1 h). In vitro parameters (A versus B) of mean dissolution time MDT (5·03 min versus 15·0 min), and time for 70% dissolution T₇₀ (6·67 min versus 20·2 min), differed significantly.     

两种包衣方法制备萘普生肠溶微丸的比较研究

目的:考察萘普生肠溶微丸两种包衣工艺的可行性。方法:分别选用离心包衣法和流化床包衣法,对萘普生药丸进行肠溶包衣,评价和比较其制备工艺和产品质量。结果:两种方法制得的肠溶微丸质量评价指标均良好,无显著差异,但流化床包衣工艺更经济、更安全。结论:流化床包衣法更适用于萘普生肠溶微丸的制备。