直肠给药后卡马西平的吸收

对卡马西平直肠给药的生物利用度已经进行了研究。八名受试者参加,给他们经过全夜禁食后,每人分别口服卡马西平合剂(20mg/mL卡马西平和300mg/mL山梨醇)10mL或直肠给药10mL。随后采集血样并对卡马西平及其代谢产物酰胺咪嗪-10,11-环氧化物进行检测。直肠给药后较口服给药后的吸收情况要慢些,平均血浆水平峰值分别出现在5.2小时和2.8小时。口服后的达峰血浆浓度为13.8μmol/L和直肠给药后10μmol/L。正如     

抗痉挛药物卡马西平

卡马西平（Carbamazepine，商品名Carbatrol）为一种抗痉挛药和治疗三叉神经痛的专属性镇痛剂，美国药典中有200mg和300mg卡马西平缓释胶囊口服制剂。     

口服结肠定位给药系统的研究进展

<正>口服结肠定位给药系统(oral colon-specific drug delivery system,OCDDS)是通过口服给药,在结肠定位释放药物的一类制剂,是近年来发展起来的。结肠输送药物缓慢,缺     

喃氟啶制剂在家兔体内的生物利用度研究

本文介绍了喃氟啶(FT-207)九种制剂通过不同给药途径的生物利用度,有非常显著性的差异(P<0.01),吸收速度和吸收程度的顺序是栓剂>胶囊>片剂。五种栓剂直肠给药后,达峰时间约比口服制剂快一倍,血药浓度的峰值比口服制剂高一倍左右,栓剂的吸收速度常数也比口服制剂大1～2倍。栓剂的生物利用度与静脉注射的相近,比口服制剂大。说明FT-207栓剂直肠吸收比口服制剂吸收为优。     

胃滞留型控释给药系统研究进展

口服给药是最方便且被应用最广的一种给药方式 ,目前市场上５０ %以上的药物是口服给药。口服控释剂型首先必须在胃肠维持长时间零级动力学过程释药 ,且释放的药物能被胃肠道有效吸收。一般口服药物吸收部位是在小肠上部和中部 ,更主要的是在小肠中１８０ｃｍ～３５０ｃｍ无菌部位 ,若药物需在胃中发挥作用或在小场上段吸收 ,则制成普通的控缓释制剂就不能提供比常规速释制剂更大的优势。胃滞留型制剂是近几年迅速发展起来的一种剂型 ,它通过驻留制剂在胃中长时间释放药物 ,药物一部分被胃吸收或在胃内发挥作用 ,另一部分通过幽门喷入小肠再…     

口服结肠释药系统的研究进展

目的:综述近年来口服结肠释药系统临床和药学研究动态,为今后在此领域的研究和临床应用提供参考。方法:通过对国内外相关文献资料的整理,对比和分析,总结口服结肠释药系统制剂进展和临床应用的发展方向。结果结论:口服结肠释药系统是通过口服给药,在结肠处定位释放药物的靶向制剂。此类制剂以其靶向释药方式和独特的临床使用价值,越来越广泛地引起了临床医生的关注,同时也成为药学研究领域的一大热点。     

对常用给药途径的体会

药物应用后所产生的治疗效果，常与药物的剂量、制剂、给药途径、联合应用以及病人的心理状态等有一定的关系。同一药物的不同制剂和不同给药途径，会引起不同的药物效应＿般注射药物比口服吸收快，水溶性制剂比油溶液或混悬剂吸收快，在口限制剂中，溶液剂比片剂、胶囊容易吸收。1口服给药口服给药，在临床上应用最为广泛，常用于慢性病或病情较轻的患者。口服给药种类多、次数颗、疗程长，对胃粘膜有刺激。因此，不易做到定时、定量服药，甚至个别病人擅自停药，影响药物的有效浓度，降低疗效，加重甚至延误病情。护士在执行医嘱时，应向…     

固体制剂吸湿性研究进展(上)

固体制剂包括片剂、胶囊剂、颗粒剂、散剂、丸剂等,其中除少数用于注射给药、皮肤用药、吸入给药、粘膜给药等而外,主要用于口服给药。固体制剂的吸湿性包括吸湿速率和临界相对湿度两方面。吸湿速率属于动力学范畴,系指固体制剂在一定温度下露置于空气或一定湿度环境中,由     

口服控制释放给药体系

口服给药是最普通的治疗途径,然而,某些药物的常规口服制剂给药后,在消化道内的局部高浓度引致严重的刺激性;一些治疗指数小的药物快速吸收后的高血药浓度产生毒副作用;还有的由于体内消除很快,常频繁给药;这些都给临床治疗带来     

生化药物鼻腔给药的研究进展

鼻腔给药系统 (nasaldraydeliverysystem ,NDDS)是指在鼻腔内使用 ,经鼻粘膜吸收而发挥局部或全身治疗作用的制剂。鼻腔给药是传统的给药方式 ,在耳鼻喉科应用极为广泛 ,一般用来治疗各种鼻腔和鼻窦疾病。随着新辅料和治疗新技术的应用 ,发挥全身治疗作用的鼻腔给药制剂的研究越来越受到人们的广泛关注。研究发现许多药物的鼻腔给药生物利用度高于口服给药 ,尤其是随着生物技术的发展 ,越来越多的生化药物 (蛋白质和多肽 )用于治疗各种疾病 ,而这些药物一般不能口服给药 ,因此越来越多的制剂专家把注意力转向鼻腔给药系统。1 鼻腔给药的…     

Comparative bioavailability and steady state fluctuations of Tegretol commercial and carbamazepine OROS tablets in adult and pediatric epileptic patients.

The comparative bioavailability and steady state fluctuations resulting from the administration of Tegretol 200 mg commercial tablets and carbamazepine OROS controlled delivery tablets were investigated in 22 adult and 12 pediatric epileptic patients. Tegretol commercial tablets were dosed according to previously established clinical regimens of 400 to 2000 mg daily doses divided into four equal or unequal intervals. Carbamazepine OROS was dosed every 12 h at the same corresponding daily dose. Comparisons of the pharmacokinetic parameters AUC, Cmax, Cmin, and tmax at steady state for the two dosage forms demonstrated definitively the bioequivalence of carbamazepine OROS with Tegretol commercial tablet over a 24-h treatment interval.     

卡马西平大鼠在体肠吸收动力学

目的研究卡马西平在大鼠各肠段的吸收动力学特征。方法采用大鼠在体肠灌流方法,研究卡马西平大鼠肠吸收动力学。结果卡马西平在整个肠道均吸收良好,吸收速度按十二指肠、结肠、回肠、空肠的顺序依次下降,吸收速度常数依次为0.230、0.182、0.178、0.165 h-1。药物在肠道的吸收呈现一级吸收动力学,吸收机制为被动吸收。结论卡马西平的吸收窗比较长,适合于制备日服一次的缓释给药系统。     

Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Carbamazepine

Literature relevant to assessing whether BCS-based biowaivers can be applied to immediate release (IR) solid oral dosage forms containing carbamazepine as the single active pharmaceutical ingredient are reviewed. Carbamazepine, which is used for the prophylactic therapy of epilepsy, is a non-ionizable drug that cannot be considered “highly soluble” across the range of pH values usually encountered in the upper gastrointestinal tract. Furthermore, evidence in the open literature suggests that carbamazepine is a BCS Class 2 drug. Nevertheless, the oral absolute bioavailability of carbamazepine lies between 70 and 78% and both in vivo and in vitro data support the classification of carbamazepine as a highly permeable drug. Since the therapeutic and toxic plasma level ranges overlap, carbamazepine is considered to have a narrow therapeutic index. For these reasons, a BCS based biowaiver for IR tablets of carbamazepine cannot be recommended. Interestingly, in nine out of ten studies, USP dissolution conditions (900 mL water with 1% SLS, paddle, 75 rpm) appropriately discriminated among bioinequivalent products and this may be a way forward to predicting whether a given formulation will be bioequivalent to the comparator product.     

卡马西平治疗儿童癫痫的血药浓度监测与合理用药

目的:研究儿童癫痫患者服用卡马西平后,其血药浓度、给药剂量及给药时间的关系。方法:对服用卡马西平及联合用其他抗癫痫药物的51例癫痫患儿,用荧光偏振免疫法(FPIA)监测其血药浓度,并结合疗效进行统计分析。结果:稳态血药浓度与给药剂量、给药时间、是否联合用药等有着密切的关系。结论:儿童癫痫患者服用卡马西平后的血药浓度个体差异大,及时监测血药浓度、调整给药剂量及给药时间,对控制儿童癫痫发作有重要意义。     

癫痫患儿卡马西平血药浓度监测结果分析

目的:探讨癫痫患儿卡马西平血药浓度与临床疗效、给药剂量、性别、年龄和体质量的相关性。方法:回顾性查阅我院临床药学室158例/次癫痫患儿卡马西平血药浓度监测记录,将浓度值、性别、年龄等资料录入数据库,利用SPSS13.0软件进行分析处理。结果:癫痫患儿卡马西平血药浓度值与性别不存在明显的相关性,但与临床疗效、给药剂量、年龄和体质量密切相关。结论:卡马西平在患儿体内的代谢差异与年龄和体质量相关,应根据每位患儿自身的具体情况并结合血药浓度监测结果来制订个体化给药方案。     

Effect of carbamazepine initiation and discontinuation on antithrombotic control in a patient receiving warfarin: case report and review of the literature

A 72-year-old Caucasian woman with paroxysmal atrial fibrillation had been taking warfarin therapy for 5 years with a stable international normalized ratio (INR). Her dentist then prescribed carbamazepine 200 mg/day to control facial nerve pain. At her next physician visit about 2 weeks after the start of the carbamazepine, the patient's INR had dropped from 3.3 to 1.3; she reported no contributing changes in her diet or warfarin dosage, nor had she taken other interacting drugs. Her warfarin dosage was increased, and the INR returned to the target range of 2.0-3.0 approximately 2 months later. The patient's INR remained stable for approximately 6 more months, until she had facial surgery. During that time, her warfarin was discontinued for 5 days, and the patient had stopped taking the carbamazepine because she had no pain. One month later, her INR increased from 2.2 to 3.6. She did not experience any thrombotic or hemorrhagic episodes. Warfarin undergoes hepatic metabolism through cytochrome P450 2C9, and carbamazepine induces this isoenzyme. Inducing warfarin metabolism necessitates an increase in the warfarin dosage to maintain the INR in the therapeutic target range. To our knowledge, this is the first report documenting the effect of the carbamazepine initiation and discontinuation in a patient receiving anticoagulation therapy with warfarin. In patients taking warfarin, clinicians should monitor the INR closely when carbamazepine is started or discontinued, or when either dosage is changed.     

Design and in vitro evaluation of floating drug delivery system for an antipsychotic agent: a technical report

Floating drug delivery systems are used to target drug release in the stomach or to the upper parts of the intestine. The oral delivery of the anti-psychotic agent carbamazepine was facilitated by preparing a non-disintegrating floating dosage form which can increase its absorption in the stomach by increasing the drug's gastric residence time. The polymers used were HPMC (low and high viscosity), guar gum, and carbopol, along with sodium bicarbonate as the gas-generating agent. The prepared tablets were evaluated for their physicochemical properties and drug release. In vitro release studies indicated that the carbamazepine release from the floating dosage forms was uniform and followed a zero-order release. It was observed that the devices containing higher proportions of HPMC (high viscosity) showed slower release than those containing lower proportions while also maintaining the integrity of the device (> or = 24 h). The incorporation of guar gum helps to maintain the device's integrity, and due to its viscolysing property also affects the drug's release profile. Sodium bicarbonate which was used as the gas-generating agent causes the tablet to float for the required time (> or = 24 h).     

Elevated serum carbamazepine concentrations following diltiazem initiation

A case of carbamazepine neurotoxicity following the addition of diltiazem is reported. A patient with previously stable carbamazepine serum concentrations was treated with diltiazem for atrial fibrillation and a rapid ventricular response. After three days on the combined regimen, the patient developed neurological symptoms resulting in hospitalization. After a review of the patient's medication usage and carbamazepine concentrations, an interaction between diltiazem and carbamazepine was suspected. Carbamazepine's elimination appears to have been decreased, resulting in neurotoxicity. The toxicity resolved when the carbamazepine dosage was decreased 62 percent.     

甲氧基红霉素对卡马西平药物动力学的影响

应用荧光偏振免疫法，测定６只家兔ｐｏ卡马西平及连续多次ｐｏ用搓甲氧基红霉素后ｐｏ卡马西平的血清卡马西平浓度，用３ｐ８７程序包按二室模型对数据进行处理并进行统计学分析。     

卡马西平重症药疹危险因素的临床分析

目的：探讨临床卡马西平重症药疹的危险因素，以减少药疹的发生。方法：收集1997年至2007年服用卡马西平出现药疹的住院患者55例的资料，其中非重症药疹28例，重症药疹27例。统计分析药疹与患者年龄、性别、药物过敏史、癫痫病、药物初始剂量、药疹潜伏期的关系，并对2组患者出现的其他不良反应进行比较。结果：药疹的严重程度与年龄、性别、药物过敏史、癫痫病无关（P〉0．05），与卡马西平的起始剂量和药疹潜伏期有关。而重症药疹组和非重症药疹组的卡马西平起始剂量及药疹潜伏期有差异，卡马西平起始剂量分别为（155．74±81．130）mg／d和（124．11±44．867）mg／d（P〈0．05），药疹潜伏期分别为（11．81±7．45）d和（6．14±5．30）d（P〈0．01）。重症药疹的肝损害较非重症者显著增多（P〈0．01），且早期均有发热表现，病情也较重。结论：卡马西平的起始剂量犬及药疹潜伏期长可能增加药疹的严重程度。