化学药品对照品的吸湿性、溶解性与比表面积相关性研究

目的 初步研究药物(化学药品对照品)吸湿性溶解性与其比表面积的相关性,为药物制备工艺和防潮技术提供参考。方法 分析《化学药品对照品图谱集—动态水分吸附》中631种药物的水分吸附动力学图,把图中RH80%放180 min的最大吸湿率(质量变化率)、比表面积、水溶性、乙醇溶解性输入excel表,分析平均吸湿率、平均比表面积、水溶性、乙醇溶解性、水和乙醇中相同溶解性的相关性;分析极具引湿性药物的吸湿官能团及放湿情况;初步比较不同吸湿官能团的吸湿性强弱。结果 631种药物比表面积为0.00~396.11 m_².g_^-1、吸湿率为0.02%~81.00%。药物平均吸湿率与平均比表面积、水溶性、吸湿官能团均正相关,与乙醇溶解性、水和乙醇相同溶解性的相关性较复杂。吸湿官能团可能包括氨基、羟基、羧基、钠盐、钾盐、铵盐、硅酸铝、寡糖等20种,药物吸湿后在低相对湿度环境中会发生不放湿、部分放湿、完全放湿等现象。药物溶解性与平均比表面积关系：水中略溶以上负相关,以下正相关;乙醇中微溶以上不相关,以下负相关。结论 化学药品对照品的吸湿性溶解性与比表面积具有相关性,为药物防潮工艺和难溶性药物溶出度提高技术提供参考。     

Budesonide for the treatment of ulcerative colitis

Introduction: Budesonide is a synthetic corticosteroid characterized by enhanced topical potency and limited systemic bioavailability. Its use in ulcerative colitis (UC) was limited to rectal preparations until recently when the new oral budesonide formulation incorporating the multi-matrix system technology was introduced. The purpose of this review is to evaluate the current role of oral and rectal budesonide in managing UC patients

Areas covered: In this paper, we described the chemical structure and pharmacologic characteristics of the different oral and rectal budesonide preparations, provided a summary of the published trials that evaluated the efficacy and safety of budesonide in UC, and discussed the current status of its use in this population

Expert opinion: Budesonide is effective in inducing remission in a subset of patients with mild-moderate UC. Nevertheless, the current evidence suggests inferiority of oral budesonide to 5-aminosalisylates (5-ASA) and systemic steroids, whereas rectal applications are comparable to other rectal steroid preparations, but still inferior to rectal 5-ASA. In clinical practice, several issues need clarification including, its exact position in the line of induction agents; the role of combining budesonide and 5-ASAs; the role of combining oral and rectal budesonide; and the role of budesonide in maintenance therapy.     

布地奈德吸入联合氨溴索静脉点滴辅治毛细支气管炎疗效分析

目的探讨布地奈德雾化吸入联合盐酸氨溴索静脉点滴辅治毛细支气管炎的临床疗效。方法将112例毛细支气管炎患儿随机分人对照组与观察组,给予52例对照组患儿抗感染、平喘等常规治疗,60例观察组患者接受布地奈德雾化吸人联合盐酸氨溴索静脉点滴治疗。比较两组临床疗效、临床症状体征消失时间、缺氧症状评分的差别。结果观察组与对照组治疗总有效率分别为98．3％和78．9％,差别具有统计学意义（P〈0．I）5）;观察组咳嗽、气促、肺部体征及X线征象消失时间均显著早于对照组（P〈0．05）;观察组治疗1d、3d和5d缺氧症状评分显著低于对照组（P〈0．05）。结论布地奈德雾化吸人联合盐酸氨溴索静脉点滴辅治毛细支气管炎临床疗效更为理想,更有利于患儿病情恢复。     

沙美特罗联合布地奈德治疗哮喘37例

目的 观察沙美特罗联合布地奈德治疗哮喘的疗效.方法 将74例哮喘患者随机均分成治疗组和对照组,治疗组在常规治疗基础上加用布地奈德联合沙美特罗(舒利迭)干粉剂(50 μg/250μg)吸入,每日2次;对照组在常规治疗基础上加用布地奈德吸入,200 μg/次,每日2次.两组疗程均为15 d,并采用哮喘症状评分、肺功能及治疗后3个月进行哮喘测试控制量表(ACT)评分.结果 两组在哮喘症状评分、肺功能和哮喘测试控制量表评分上均有改善,而治疗组较对照组改善更明显(P＜0.01).结论 沙美特罗联合布地奈德治疗哮喘具有较好控制效果,且疗效好、经济、方便,值得临床推广应用.     

布地奈德气雾剂中布地奈德和R-异构体的HPLC测定

采用HPLC法测定了布地奈德气雾剂中布地奈德总量、每揿含量、有效部位药物沉积量及R-异构体的含量。采用ODSC18柱，检测波长244nm。其中气雾剂总量、每揿含量、药物有效部位沉积量的测定采用乙腈-水(60：40)为流动相；R-异构体的含量测定采用乙腈-水(40：60)为流动相。在0．01～0．15mg／ml范围内，布地奈德具良好的线性关系，平均回收率为100．2％，RSD为0．3％。     

布地奈德联合噻托溴铵治疗支气管哮喘的临床研究

目的 观察布地奈德联合噻托溴铵对支气管哮喘的肺功能影响.方法 将92例患者依据随机数字的方法分为对照组46例与试验组46例.对照组在常规治疗基础上使用布地奈德混悬液:布地奈德混悬液,2 mL,bid,吸入.试验组在常规治疗基础上使用布地奈德混悬液+噻托溴铵粉雾剂:噻托溴铵粉雾剂,18μg,qd,吸入.布地奈德混悬液使用...     

布地奈德联合雾化吸入治疗慢性支气管炎的效果观察

目的探讨布地奈德联合雾化吸入治疗慢性支气管炎的临床效果。方法回顾性分析我院收治的106例慢性支气管炎患者的临床资料,随机分为治疗组和对照组各53例。对照组患者给予常规治疗,治疗组在常规治疗基础上给予1.0mL布地奈德雾化吸入治疗,比较两组患者的临床疗效。结果治疗结束后,治疗组的总有效率高达90.57%,对照组的总有效率77.36%,两组具有显著性差异,P<0.05;治疗组的呼吸困难、喘气、咳嗽、痰鸣音等消失时间均短于对照组,差异具有显著性,P<0.05。结论采用布地奈德联合雾化吸入治疗慢性支气管炎,迅速改善临床症状,临床疗效显著。     

雾化吸入布地奈德治疗婴儿支气管肺发育不良的临床疗效

[摘要]目的：探讨雾化吸入布地奈德治疗婴儿支气管肺发育不良（BPD）的临床疗效。方法：收集2015年1月至2018年5月成都市妇女儿童医院儿童呼吸科住院部及呼吸专科门诊收治的28例支气管肺发育不良患儿及30例健康婴儿的病例资料,比较BDP患儿与健康婴儿肺功能指标及BDP患儿雾化吸入布地奈德治疗前后的临床疗效。结果：BDP患儿的潮气肺功能达峰时间比、达峰容积比、小气道功能指标（TEF75、TEF50）明显低于健康婴儿,且差异有统计学意义。雾化吸入布地奈德治疗后,BDP患儿呼吸道感染次数、喘息次数改善不明显,但住院次数明显下降（P<0.01）,潮气肺功能主要参数潮气量（VT/kg）、呼吸时间比（Ti/Te）、达峰时间比（TPTEF/TE）、呼出75%潮气容积时呼气流量（TEF25）、呼出75%潮气容积时呼气流量（TEF50）、呼出75%潮气容积时呼气流量（TEF75）改善不明显,达峰容积比（VPTEF/VE）明显改善（P<0.01）。结论：雾化吸入布地奈德治疗支气管肺发育不良在减少住院次数、改善患儿潮气肺功能方面有一定临床效果。     

Body Surface Area as a Determinant of Pharmacokinetics and Drug Dosing

Body surface area (BSA) was introduced intomedical oncology in order to derive a safestarting dose for phase I studies ofanticancer drugs from preclinical animaltoxicology data. It is not clear however,as to why dosing by BSA was extended to theroutine dosing of antineoplastic agents.Several formulas exist to estimate BSA, butthe formula derived by DuBois and DuBois isthe one used in adult medical oncology. This formula was derived based on data fromonly nine patients; subsequent attempts tovalidate the formula have found the DuBoisformula to either over or underestimate theactual determined BSA. While cardiacoutput does correlate with BSA, therelationship between BSA and otherphysiologic measures relevant for drugmetabolism and disposition, such as, renaland hepatic function, is weak ornonexistent. Further only epirubicin,etoposide, and carboplatin have beenstudied to determine if dosing by BSA wouldreduce interpatient variability, and noneof these drugs were found to havesignificant relationships between theirpharmacokinetics and BSA. Future clinicaltrials of new agents should not presumethat dosing based on BSA reducesinterpatient variability. Studies shouldexamine the role, if any, BSA has in dosingnew chemotherapeutic agents in initialphase I studies.     

布地奈德对哮喘急性发作且伴有感染患儿的临床疗效

目的:分析布地奈德对支气管哮喘急性发作且伴有感染患儿的疗效及对肺功能指标的影响。方法:将本院收治的96例支气管哮喘急性发作且伴有感染的患儿作为研究对象,随机分为对照组和观察组各48例,两组患儿均给予常规抗感染治疗,对照组给予地塞米松雾化吸入,观察组给予布地奈德雾化吸入,比较两组患儿临床疗效和治疗前、治疗后1周第1秒用力呼气容积(FEV1)、FEV1占预计值百分比(FEV1%)、肺活量(VC)、用力肺活量(FVC)等肺功能指标的改善状况及不良反应的发生情况。结果:观察组治疗总有效率为95.83%,高于对照组的72.92%(P<0.05)。两组患儿治疗后1周肺功能指标FEV1、FEV1%、VC、FVC水平较治疗前均升高,且观察组各指标水平均显著高于对照组(P均<0.01)。观察组患儿不良反应发生率(4.17%)低于对照组(18.75%)(P<0.05)。结论:布地奈德联合常规抗感染对治疗支气管哮喘急性发作且伴有感染的患儿具有良好的临床疗效,可有效改善FEV1、FEV1%等肺功能指标,且不良反应发生率较低,具有较高的安全性,因此具有良好的临床应用价值。     

Budesonide/formoterol for the treatment of asthma

Budesonide/formoterol (Symbicort^®, AstraZeneca plc) is a novel treatment for asthma, combining an inhaled corticosteroid – budesonide, and a long-acting β₂-agonist – formoterol, in a single inhaler, the Turbuhaler^®. Randomised, clinical studies in patients with asthma have demonstrated that budesonide/formoterol is more effective than the inhaled corticosteroids, budes-onide and fluticasone alone, and at least as effective as both monocomponents in separate inhalers. Results from clinical studies suggest a synergistic effect when both drugs are administered via one inhaler, although the mechanisms for this are not fully understood. Budesonide/formoterol has a rapid onset of effect, apparent within 1 min of treatment, which is largely because of the properties of formoterol. Once- and twice-daily dosing with budesonide/formoterol are effective treatment options for patients with mild or moderate asthma. Studies have also shown that the beneficial safety profiles and dose relationships of both budesonide and formoterol allow dose adjustments of budesonide/formoterol in response to variations in the patient’s asthma. Findings from the budesonide/formoterol adjustable maintenance dosing programme, comparing fixed and adjustable, symptom-guided dosing regimens, demonstrate that patients achieve equally good asthma control with adjustable dosing (from one inhalation twice-daily to more than four inhalations twice-daily), but at a significantly lower overall drug load. Adverse events, mainly expected inhaled corticosteroid and long-acting β₂agonist class effects, have been few in number and mild in nature. In addition, there is growing evidence that budesonide/formoterol is also effective in patients with chronic obstructive pulmonary disease. The future for treatment with budesonide/formoterol may include as-needed administration in addition to maintenance therapy.     

布地奈德联合肺表面活性物质治疗新生儿呼吸窘迫综合征疗效观察

目的:探讨布地奈德联合肺表面活性物质(PS)治疗新生儿呼吸窘迫综合征(NRDS)的临床疗效。方法:将我院新生儿科2016年1月至2017年1月收治的96例NRDS患儿,采用随机数字表法分为观察组和对照组各48例。对照组给予PS制剂猪肺磷脂注射液200 mg/kg气管内滴入治疗,观察组给予布地奈德混悬液(0.25 mg/kg)与猪肺磷脂注射液(200 mg/kg)混合后气管内滴入,比较两组患儿在治疗后48 h的临床疗效。结果:观察组总有效率87.5%,对照组总有效率75.0%,两组比较差异有统计学意义(P<0.05)。结论:布地奈德混悬液联合猪肺磷脂注射液治疗NRDS较单用猪肺磷脂注射液疗效更为显著。     

Surface Denaturation at Solid-Void Interface—A Possible Pathway by Which Opalescent Participates Form During the Storage of Lyophilized Tissue-Type Plasminogen Activator at High Temperatures

During protein lyophilization, it is common practice to complete the freezing step as fast as possible in order to avoid protein denaturation, as well as to obtain a final product of uniform quality. We report a contradictory observation made during lyophilization of recombinant tissue-type plasminogen activator (t-PA) formulated in arginine. Fast cooling during lyophilization resulted in a lyophilized product that yielded more opalescent particulates upon long term storage at 50 °C, under a 150 mTorr nitrogen seal gas environment. Fast cooling also resulted in a lyophilized cake with a large internal surface area. Studies on lyophilized products containing 1% (w/w) residual moisture and varying cake surface areas (0.22 - 1.78 m²/gm) revealed that all lyophilized cakes were in an amorphous state with similar glass transition temperatures (103 - 105 °C). However, during storage the rate of opalescent particulate formation in the lyophilized product (as determined by UV optical density measurement in the 360 to 340 nm range for the reconstituted solution) was proportional to the cake surface area. We suggest that this is a surface-related phenomenon in which the protein at the solid-void interface of the lyophilized cake denatures during storage at elevated temperatures. Irreversible denaturation at the ice-liquid interface during freezing in lyophilization is unlikely to occur, since repeated freezing/thawing did not show any adverse effect on the protein. Infrared spectroscopic analysis could not determine whether protein, upon lyophilization, at the solid-void interface would still be in a native form.     

布地奈德雾化吸入治疗新生儿肺炎63例

目的 探讨布地奈德雾化吸入治疗新生儿肺炎的临床治疗效果及安全性.方法 选择医院新生儿肺炎患者126例,随机分为观察组和对照组.在西医常规治疗基础上,对照组给予0.9％氯化钠注射液雾化吸入,观察组给予布地奈德雾化吸入,观察两组的临床治疗效果及安全性.结果 观察组总有效率为95.24％,明显高于对照组的82.54％(P＜0.05).观察组患儿鼻阻消失时间、呼吸困难好转时间及肺部罗音消失时间均短于对照组(P＜0.05).不良反应发生率观察组为6.35％,对照组为4.76％,两组比较差异无统计学意义(P＞0.05).结论 在新生儿肺炎的治疗中采用雾化吸入布地奈德辅助西医常规治疗的疗效肯定,应用安全.     

不同剂量布地奈德长期雾化吸入对儿童哮喘的临床效果观察

目的:探讨不同剂量布地奈德长期雾化吸入对小儿哮喘的临床效果。方法:选取2016 年我院儿科收治的哮喘急性发作患儿100 例,采用随机数表法分为高剂量组和低剂量组各50 例,在常规治疗基础上,分别给予每次1.0 mg 和每次0.5 mg 的布地奈德雾化吸入,每隔8 h 一次,连续治疗7 d;急性期后,分别以400 µg/ d 和200 µg/ d 的小剂量布地奈德混悬液雾化吸入维持治疗3 个月,症状控制后剂量减半,总疗程1 年。另选同期来我院免疫接种的健康儿童30 例作为对照组。比较两组患儿的总有效率、症状改善情况及不良反应,及治疗前、治疗3 个月、12 个月时的血清IL-4、IL-5、TNF-α、VEGF、IgE 水平。结果:高剂量组治疗总有效率96.00%,高于低剂量组的82.00%(P<0.05)。高剂量组患儿的喘息、咳嗽、哮鸣音、呼吸困难缓解时间及住院时间均短于低剂量组(P 均<0.01)。治疗前两组患儿的IL-4、IL-5、TNF-α、VEGF、IgE 水平均高于对照组(P 均<0.05);治疗后两组患儿各指标水平均逐步下降,且治疗3 个月时高剂量组均低于低剂量组(P 均<0.05)。两组患儿治疗期间均无明显不良反应发生。结论:高剂量布地奈德雾化吸入能更有效地缓解哮喘患儿的症状,降低气道高反应性,无明显不良反应,值得临床推广应用。     

布地奈德联合多种营养素预防早产儿支气管肺发育不良的疗效观察

目的:观察布地奈德联合维生素A为主的多种营养素防治早产儿支气管肺发育不良(BPD)的临床疗效.方法:选取2018年3月至2019年5月新生儿科重症监护室的120例早产儿,采用随机数字表法分为对照组、布地奈德组和布地奈德+营养素组,对照组接受常规治疗,布地奈德组在常规治疗基础上加用布地奈德雾化吸入治疗,布地奈德+营养素组...     

盐酸氨溴索与布地奈德单用或联合雾化吸入辅助治疗小儿毛细支气管炎疗效比较

目的:比较盐酸氨溴索与布地奈德混悬液单用或联合雾化吸入辅助治疗小儿毛细支气管炎的疗效,优化治疗方案。方法:选取2012年12月至2014年12月在我院治疗的108例小儿毛细支气管炎患儿,随机分为盐酸氨溴索组、布地奈德组和联合用药组各36例。三组患儿均给予常规治疗(抗感染、止咳、镇静、吸痰等),同时给予相应的药物雾化吸入辅助治疗,观察三组患儿用药前后动脉血气指标变化情况、临床症状的改善情况及临床疗效。结果:联合用药组治疗后第3天SpO2、PaO2升高,PaCO2降低,与盐酸氨溴索组和布地奈德组比较差异均有统计学意义(P均<0.05);联合用药组咳嗽、气促、喘鸣音、湿啰音消失时间及住院时间均短于盐酸氨溴索组和布地奈德组(P均<0.05);联合用药组总有效率高于盐酸氨溴索组和布地奈德组(P均<0.01)。结论:盐酸氨溴索与布地奈德混悬液联合雾化吸入辅助治疗小儿毛细支气管炎,疗效优于单用一种药物,值得临床推广应用。     

硫酸特布他林联合布地耐德对支气管扩张合并支气管哮喘患者的临床反应性

OBJECTIVE To observe the clinical reactivity of Budesonide and Terbutaline in the treatment of bronchiectasis and bronchial asthma.METHODS 98 patients were divided into two groups randomly,who have reversible airway reactivity-bronchial asthma in clinic w     

硫酸特布他林联合布地耐德对支气管扩张合并支气管哮喘患者的临床反应性

目的观察硫酸特布他林联合布地耐德雾化吸入治疗对支气管扩张合并支气管哮喘的临床反应性。方法选择98例经HRCT明确诊断为支气管扩张,并且在临床同时有可逆性气道反应-支气管哮喘的患者随机分为两组。治疗组48例给予硫酸特布他林联合布地耐德雾化吸入;对照组50例给予常规治疗。观察用药后两组患者的症状改善、肺功能指标{第1秒最大呼气量(FEV1)、FEV1/FVC%、峰流速(PEF)}的变化。结果治疗组前后症状记分由12.13分下降至5.06分,对照组有11.26分下降至10.21分。治疗4个月后治疗组肺功能各指标(FEV1、FEV1/FVC%、PEF)明显改善(P<0.01)。结论支气管扩张合并支气管哮喘患者在常规治疗基础上,硫酸特布他林联合布地耐德雾化吸入治疗,能有效改善患者临床症状及通气功能,缩短病程。     

布地奈德鼻喷雾剂和地氯雷他定片联合治疗过敏性鼻炎

目的探讨布地奈德喷雾剂和地氯雷他定片联合应用治疗过敏性鼻炎的疗效。方法 150例确诊为过敏性鼻炎的患者分为3组,分别给予布地奈德鼻喷雾剂和地氯雷他定片(联合组)50例,布地奈德喷雾剂(单药A组)50例,地氯雷他定片(单药B组),观察2周,并对治疗前后的症状和体征记分比较。结果联合组的近期疗效总有效率达96%,单药A组为75%,单药B组为68%,联合组效果明显优于单药A组和单药B组,无明显的不良反应。结论布地奈德鼻喷雾剂和地氯雷他定片联合治疗过敏性鼻炎安全有效。