RP-HPLC法测定复方双嘧达莫缓释片中双嘧达莫与阿司匹林的含量

目的　建立高效液相色谱法测定复方双嘧达莫缓释片的含量测定方法。方法　用ODS C18柱 ;流动相以 0 0 2mol/LNa2 HPO4缓冲液 (2 0 %H3 PO4调节pH3 2 ) 乙腈 甲醇 (6 7∶2 8∶5 ) ;检测波长 2 2 7nm ;流量 1 0ml/min。结果　双嘧达莫的线性范围 :2 0 0 6～ 4 0 1 2 μg/ml(r=0 9995 ) ,平均回收率 10 0 8% ,RSD为 0 7% ;阿司匹林的线性范围 :2 892～ 5 7 84 μg/ml(r =0 9995 ) ,平均回收率 99 94 % ,RSD为 0 3%。结论　本法简便、灵敏、准确。     

反相高效液相色谱法分别测定银杏达莫注射液中双嘧达莫与银杏总黄酮的含量

目的建立反相高效液相色谱测定银杏达莫注射液中的双嘧达莫和银杏总黄酮含量的方法。方法双嘧达莫采用Chromasil—C18（250mm×4．6mm，5μm）柱；流动相：0．1％磷酸二氢钠溶液．甲醇（25：75），检测波长为290nm，银杏总黄酮采用Shimpack-CLCODS（250mm×4．6mm，5μm）柱；流动相：0．4％磷酸溶液-甲醇（50：50），检测波长为360nm，流速为1．2ml／min。结果双嘧达莫进样浓度在6．12～24．48μg／ml范围内线性关系良好，平均回收率为99．82％，相对标准差（RSD）为0．85％；银杏总黄酮进样浓度在0．0476～0．1904mg／ml范围内线性关系良好，平均回收率为99．53％，RSD为0．69％。结论该法简便、快速、准确，可用于银杏达莫注射液的含量测定。     

氯霉素滴耳液及其相关物质二醇物的毛细管区带电泳分析法

建立适合氮霉素滴耳液含量测定及其杂质二醇物检测的高效毛细管电泳定量检测方法。采用区带电泳法，以水杨酸为内标，运行电压25kV，运行缓冲液为25mmol/L磷酸盐缓冲液(pH＝6．0)，检测波长214nm。氮霉素滴耳波及二醇物线性范围分别为50—250μg／ml(r＝0．9992)和4．0—20．0μg／ml(r＝0．9988)。平均回收率分别为99．8％和101．5％，RSD分别为0．8％和2．0％(n＝5)。     

复方双嘧达莫缓释片中阿司匹林和双嘧达莫的含量测定

目的建立同时测定复方双嘧达莫缓释片中阿司匹林和双嘧达莫含量的方法。方法采用反相高效液相色谱法，色谱柱：Alltech C18(4.6 mm×150 mm，5 μm)；流动相：甲醇-0.3%二乙胺水溶液-冰醋酸(45∶55∶4)；检测波长：235 nm；流速：1.2 mL·min^-1；柱温：30℃。 结果阿司匹林在635～101.60 μg·mL^-1范围内，峰面积与其浓度呈良好线性关系(r＝0.999 9，n＝6)，平均回收率为99.87%，RSD＝0.61%；双嘧达莫在18.7～299.2 μg·mL^-1范围内，峰面积与其浓度呈良好线性关系(r＝0.999 9， n＝6)，平均回收率为100.29%，RSD＝0.40%。3批自制复方双嘧达莫缓释片中阿司匹林和双嘧达莫相当于标示量的百分含量分别为：100.5%，100.4%，99.5%和100.9%，99.34%，100.3%。结论该法具有准确、简便、快速、灵敏且重现性好的特点，可用于复方双嘧达莫缓释片中阿司匹林和双嘧达莫含量的同时测定。     

强力苷口服液中甘草酸铵和肌苷的高效液相测定法

建立反相高效该相色谱法（HPLC）同时测定强力苷口服液中甘草酸铵和肌苷含量。HPLC条件为．岛津ShimpackCLG－ODS（150×4．6mm）柱，流动相为甲醇－水（70：30），紫外检测波长252nm。结果甘草酸铵浓度线性范围10～100μg／ml（r＝0．9990），平均口收率为98．25％，RSD＝0．5％；肌苷浓度线性范围50～500μg／ml（r＝0．9999），平均回收率为99．87％，RSD＝0．4％．     

双波长分光光度法测定复方氨酰心安片含量

本文采用双波长分光光度法测定复方氨酰心安片中氨酰心安与氯噻酮的含量。氨酰心安的线性范围为48～112μg／ml，r=0．9999，平均回收率为100．4％，RSD为0.7％；氯噻酮的线性范围为12-28μg／ml，r=1．000，平均回收率为101．8％，RSD为1．0％。     

高效液相色谱法测定氯霉素氢化可的松滴耳液中氯霉素和氢化可的松的含量

目的 建立高效液相色谱法测定氯霉素氢化可的松滴耳液中氯霉素和氢化可的松的含量。方法 采用反相μBondpak C18色谱柱；甲醇-水(70：30)为流动相；检测波长为242nm，外标法定量。结果 氯霉素和氢化可的松的线性范围分别为5～301μg／mL(r=0．9995)，1-6μg／mL(r=0．9997)；平均加样回收率分别为：100．2％(RSD=0．75％)，99．53％(RSD=0．97％，n=5)；日内RSD分别为0．67％和0．66％(n=5)，日间RSD分别为0．74％和1．07％(n=4)。结论 该方法简便、准确，适合该制剂质量检验分析。     

HPLC法测定无极膏中丙酸倍氯米松的含量

目的建立HPLC法测定无极膏中丙酸倍氯米松的含量，并确定其含量限度。方法Diamonsil C18柱（4．6mm×250mm，5μm）；流动相：甲醇-水（70：30）；流速：1．0ml／min；检测波长为240nm。结果丙酸倍氯米松的线性范围为2．14～19．24μg／ml，r=0．9995。样品平均回收率为100．2％，RSD为1．1％。结论本法简单，快速，结果准确，可有效控制该制剂中丙酸倍氯米松的含量。     

复方双嘧达莫片的HPLC测定

建立高效液相色谱法测定复方双嘧达莫片中双嘧达莫及阿司匹林的含量.采用Ci8色谱柱,流动相为甲醇-水-磷酸-二乙胺(275:225:0.3:0.1),检测波长225nm.阿司匹林和双嘧达莫分别在6～14μg/mi和48～112ug/ml浓度范围内线性关系良好(r＞0.9995).平均回收率分别为98.0%(RSD=1.91%)和100.6%(RSD=1.50%).     

毛细管色谱法测定洛美沙星中的有机溶剂残留量

目的：建立毛细管气相色谱法测定洛美沙星中的有机溶剂残留量。方法：用INNOWAX毛细管气相色谱柱，FID检测器，以2-戊酮为内标进行测定。结果：乙酸乙酯、四氢呋喃、乙醇、乙腈的线性范围分别为0～80μg／ml(r=0．9997)、0～11．52μg／ml(r=0．9996)、0～80μg／ml(r=0．9997)，0～6．56μg／ml(r=0．9996)；平均回收率分别为100．5％、100．1％、101．2％、100．1％；RSD分别为1．30％、0．9％、1．18％和1．23％(n=9)。结论：本方法简单、准确、灵敏度高、重现性好，适用于洛美沙星中有机溶剂残留量的测定。     

Pharmacokinetics of Dipyridamole

Abstract Dipyridamole, though originally introduced as a coronary vasodilator, has lately been increasingly investigated in the treatment of thromboembolic diseases because of its inhibitory influence upon blood platelet function. The compound is eliminated from the organism by hepatic biotransformation to the monoglucuronide, which almost exclusively is subjected to biliary and faecal excretion with simultaneous partial enterohepatic circulation taking place. Only minute amounts are excreted through the kidneys. In experiments on four normal human volunteers it was found that the serum concentration curve after intravenous administration of dipyridamole rather closely fits the pharmacokinetics of an open two-compartment model with first order, linear disposition kinetics and elimination taking place from the central compartment. Experiments with oral ingestion of the compound could be described by the use of a corresponding pharmacokinetic model with two consecutive first order input steps, representing the dissolution and absorption processes. The disposition rate constants (β) were within the range of 0.0051-0.0083 min.^-1 corresponding to biological half-lives of 84-145 min. The absorption rate constant was about 0.07 min.^-1, and the systemic availability of an oral dose of 100 mg dipyridamole in tablets varied from 37 to 66%.     

Dipyridamole monotherapy in schizophrenia

Background  

Emerging data indicate the neuromodulator adenosine may play a role in the therapeutics of schizophrenia. Adenosine A_2A receptor stimulation exerts a functional antagonism at postsynaptic D₂ receptors. Data from animal models relevant to schizophrenia support a therapeutic effect of modulating adenosinergic transmission in the ventral striatum. One previous clinical trial showed superiority of adjunctive dipyridamole, an adenosine reuptake inhibitor, compared to placebo in ameliorating positive symptoms in schizophrenia patients.     

Dipyridamole increases red cell deformability

The effects of dipyridamole on red cell filterability both in vitro and ex vivo were measured. In a balanced, randomised and double-blind trial, six healthy male and female volunteers (22-37 years) were given dipyridamole 400 mg/day or matching placebo in four divided doses for 3 days, and heparinised venous blood samples were taken 1 h after the ingestion of the last dose. Filterability of red cells was increased significantly (P less than 0.05 paired t-test) when the subjects were on dipyridamole compared with placebo. In separate experiments, 15 min incubation with 2 or 20 micrograms/ml dipyridamole in vitro was found to have no effect on the filterability of freshly prepared red cell suspensions. After 24 h storage at 4 degrees C, the filterability of red cells was significantly decreased (P less than 0.01) and this could be partially prevented by adding dipyridamole to the stored cells (P less than 0.05). These results suggest that dipyridamole has an effect on the behaviour of the red cell membrane to increase the deformability of the cells. This may contribute to its therapeutic effect.     

Dipyridamole: a critical evaluation

Dipyridamol is a vasodilator that is used primarily in clinical practice as an antiplatelet agent. It increases coronary blood flow and was originally introduced as an antianginal agent. An ability to prolong a shortened platelet survival has been used to justify its value in preventing thromboembolic complications. Conditions characterized by a reduction in platelet survival and where dipyridamole has been used include heart valve replacement, arterial grafting, cerebrovascular disorders, and disorders of peripheral circulation. The in vivo effect of dipyridamole on platelet aggregation has not been well defined and may depend on additional factors. Prostaglandins appear to have important roles in platelet homeostasis; their relationships to the action of dipyridamole are discussed. Dipyridamole usually is combined with aspirin for synergistic anti-aggregatory purposes. However, the nature of the interaction has not been elucidated and benefit from the addition of dipyridamole has not been demonstrated in clinical studies. A review of clinical studies using dipyridamole indicates that it currently has limited value.     

HPLC法测定双嘧达莫分散片中双嘧达莫的含量及其均匀度

目的:建立双嘧达莫分散片中双嘧达莫含量及其均匀度的测定方法。方法:采用高效液相色谱法。色谱柱为Shimpack C18柱,流动相为磷酸氢二钠溶液-甲醇(25:75),流速为1.0mL·min-1,检测波长为288nm,进样量为20μL,柱温为25℃。结果:双嘧达莫检测浓度在16.07～80.35μg·mL-1(r=0.9999)范围内与峰面积积分值线性关系良好;低、中、高浓度的平均加样回收率分别为99.63%、98.82%、100.03%,RSD=1.0%(n=9)。结论:该法灵敏度高、重复性好、结果准确,可用于双嘧达莫分散片的质量控制。     

Perivascular Tissue Pharmacokinetics of Dipyridamole

Purpose The tissue diffusivity (D_g) and partitioning (K) for dipyridamole were determined and a model was developed to examine the relationship between perivascular dose and local dipyridamole tissue concentrations. Methods Experiments were performed using an in vitro perfusion apparatus that recirculated buffer through different graft samples or normal porcine femoral arteries and veins. The grafts or blood vessels were immersed in a compartment containing Krebs–Henseleit (KH) buffer and dipyridamole (30 μg/mL). The recirculating buffer was sampled at multiple time points and dipyridamole was assayed. Estimates of the effective diffusivity (D_g) and partition coefficient (K) of the drug in the vessel wall were determined and used to simulate dipyridamole tissue concentration after perivascular delivery. Results Dipyridamole diffusivity within native femoral veins (D_g = 3.87 ± 0.93 × 10⁻⁶ cm²/s) was approximately twice that within femoral arteries (D_g = 2.06 ± 0.79 × 10⁻⁶ cm²/s, p < 0.01). Explanted grafts showed the lowest diffusivity. Partition coefficients of femoral arteries (K = 4.11 ± 0.99) were higher than those of femoral veins (K = 2.05 ± 0.85, p < 0.01) and explanted graft (K = 0.89 ± 0.56, p<0.01). Discussion The results demonstrate that local drug kinetics vary greatly for different types of blood vessels and grafts. The pharmacokinetic parameters and resulting computational simulations are helpful in exploring perivascular drug delivery strategies.     

Dipyridamole and vascular prostacyclin production

The action of dipyridamole on the vascular production of prostacyclin (PGI2) has been investigated. Dipyridamole (1-100 microM) did not induce a significant stimulation of PGI2 release in any of the following experimental models: rings of rabbit aorta, cultured endothelial cells from bovine aorta or human umbilical vein, cultured explants of bovine aortic smooth muscle. The activity of known stimuli of PGI2 release (ADP, suloctidil, serotonin) and the capacity of dipyridamole to inhibit adenosine uptake into endothelial cells were carefully checked. Pretreatment of the rabbit aorta with dipyridamole (10-100 microM) prolonged the transient stimulation of PGI2 release induced by mechanical deendothelialization: this effect was probably due to a partial protection of the cyclooxygenase against oxidative self-inactivation. Our largely negative results are consistent with the current theory that the antiplatelet action of dipyridamole is mediated by adenosine and not by PGI2.     

双嘧达莫缓释滴丸的研制

采用正交设计优化了药液温度、滴速、冷凝液上部温度梯度和冷凝管高度等制备非pH依赖型双嘧达莫缓释滴丸，并初步研究其成型工艺。结果表明，所得缓释滴丸在pH1．2盐酸和pH6．8磷酸盐缓冲液中的体外释药行为相似，不受pH变化影响。     

双嘧达莫凝胶剂的制备与质量控制

目的 制备双嘧迭莫新型凝胶剂,并建立其质量控制方法.方法 以卡波姆-940为基质,以双嘧达莫为主药,以薄荷脑为透皮促进剂.辅以1,3-丙二醇、羟苯乙酯、吐温-80,制成凝胶剂,用紫外分光光度法测定凝胶剂的主药双嘧达莫含量,测定波长为(283±1)nm.结果 双嘧达莫质量浓度在2～12μg/mL范围内与峰面积线性关系良好,回归方程A=0.060 8 C-0.0016(r=1).回收率为99.78%,RSD为0.70%.结论 双嘧达莫凝胶剂制备工艺简单,具有良好黏合性、成膜性和稳定性;质量控制方法 简便且准确,可在临床推广使用.