肺部给药系统的研究进展

介绍了呼吸道的特殊生理特征和功能以及药物的吸收过程,综述了近年来国内外肺部给药系统的进展,包括定量吸入剂、喷雾剂、干粉吸入剂、微球和脂质体的肺部给药。     

肺部吸入给药装置的研究进展

目的介绍肺部吸入给药装置的使用情况及最新进展。方法参阅国内外代表性文献资料,以其中的36篇为依据对其进行分析、归纳和整理。结果阐明了肺部吸入治疗的优越性及原理,并对肺部给药的喷雾器、定量吸入器和干粉吸入器的种类、作用机制、优缺点以及发展方向加以综述。结论肺部吸入给药具有广阔的发展和应用前景。     

肺吸入给药剂型的研究进展

肺吸入给药可以将治疗药物直接输送到病灶区，减少了药物在其他组织的分布。因此，对于肺部疾病的治疗，吸人给药比口服给药治疗指数高、副作用小。支气管扩张剂、β2受体激动剂、皮质激素等药物以吸入疗法为首选给药方式。随着医药界对肺功能和肺疾病的深入了解，肺部给药以其吸收表面积大、吸收部位血流丰富、可避免肝脏首过效应以及上皮屏障薄、膜通透性高等优点，治疗范围正在扩大。如治疗糖尿病的胰岛素气雾剂和用于骨质疏松、变形性骨炎治疗的鲑降钙素粉雾剂。近年来对以蛋白质、多肽为主的大分子药物的吸人给药的研究也日益增多。     

老慢支哮喘吸入药物有讲究

慢性阻塞性肺病（俗称老慢支）治疗以长效抗胆碱药为主。可联合应用吸入糖皮质激素和长效β2受体激动剂。哮喘治疗以吸入糖皮质激素和长效β2受体激动剂为主。抗胆碱药为辅。     

万托林雾化吸入治疗支气管哮喘不良反应

我科1999年12月~2003年12月期间利用空气压缩泵或氧气作动力,雾化吸入β2受体激动剂万托林治疗哮喘急性发作629例次,其中55例在首次雾化吸入时出现明显不良反应,现总结如下:1对象与方法1.1对象1999年12月~2003年12月就诊于我科的急性哮喘发作患者629例次,其中男性340例,女性289     

肺部吸入给药系统的研究进展

肺部给药系统具有起效快、疗效好、同时减少不良反应等优点,已成为一种倍受关注的给药方式.在全球新型给药系统药物市场中,肺部吸入给药系统占有极为重要的地位,特别是在慢性阻塞性肺病和哮喘等与呼吸道相关疾病的治疗方面具有广泛的临床应用价值.本文将从吸入制剂的最新分类、美国FDA已上市产品情况和创新性产品研究进展等方面入手,对目...     

β2受体激动剂雾化吸入治疗哮喘不良反应的观察

目的 观察β２受体激动剂雾化吸入不良反应及处理，以达到最好的治疗作用。方法 １９９９年喘乐宁雾吸入。结果 治疗哮喘急性发作４４２９人次，其中２４例在首次雾化吸入时出现明显不良反应。     

药物对慢性阻塞性肺疾病临床进程的干预作用

慢性阻塞件肺疾病(COPD)是可预防及治疗的疾病,COPD患者接受适宜的药物长期治疗,可有效缓解或逆转临床进程.本文就β2受体激动剂、抗胆碱约物、吸入型糖皮质激素,以及COPD的联合治疗作一综述.     

吸入型糖皮质激素和长效β2受体激动剂在哮喘治疗中的作用和相互影响

尽管作用机制不同，吸入型糖皮质激素和长效β2受体激动剂仍是目前最常用的哮喘控制药物。 由于二者在作用机制上的互补性，使它们的联合治疗较单独使用具有更佳的临床效果，且较其它联合用药方案更为优越。本文主要就近年来联合吸入型糖皮质激素和长效β2受体激动剂在哮喘治疗中的作用及其相互影响方面的研究作一综述。     

脂质体肺部给药在抗菌药物中的应用

脂质体肺部给药作为一种非侵入性给药形式,给药方式和处方组成与一般制剂有明显区别,具有定位靶向、无首过效应、缓释性等优点,目前成为肺部疾病治疗的重要手段。该文就脂质体肺部给药的优势、给药方式和在抗菌药物中的应用进行综述,为今后脂质体肺部给药的研发创新提供启发和思路。     

脂质体肺部给药的研究

由于脂质体肺部给药具有刺激性小、吸收迅速、生物利用度高、安全性好、可实现持续缓慢释药等独特优势而成为近年来制剂领域的研究热点之一。本文论述脂质体肺部给药的特点、稳定性以及在药代动力学、药效学和安全性等方面的最新研究进展。     

Efficacy,safety, and tolerability of mometasone furoate in adult Japanese patients with mild asthma: open-label clinical trial findings

Abstract

Objective:

To evaluate the clinical efficacy and safety of mometasone furoate administered via a dry powder inhaler (MF-DPI) in Japanese patients with intermittent or mild persistent asthma who were not previously receiving inhaled corticosteroids.     

Evaluation of efficacy and safety of budesonide delivered via two dry powder inhalers

ABSTRACT

Background: The dry powder inhaler (DPI) device for budesonide inhalation powder 200?μg (DPI?A^*) was redesigned to improve dosing consistency and provide new features (budesonide inhalation powder 90?μg and 180?μg; DPI?B^?).

Objective: Two multicenter, parallel-group, double-blind, randomized, 12-week studies compared the efficacy and safety of budesonide delivered via each DPI versus placebo, and the systemic exposure of budesonide from each device.

Methods: Asthmatic adults with mild-to-moderate asthma (N?=?621) and patients 6–17 years with mild asthma (N?=?516) received budesonide DPI?B 360?μg or DPI?A 400 μg twice-daily (total daily dose 720?μg or 800?μg), budesonide DPI?B 180?μg or DPI?A 200?μg once daily (total daily dose 180?μg or 200?μg), or matching placebo. Change in forced expiratory volume in 1 second (FEV₁) and secondary variables (asthma symptoms, β₂-adrenergic agonist use, peak expiratory flow [PEF], and withdrawals due to worsening asthma) versus placebo were measured.

Results: In both studies, FEV₁ significantly (?p < 0.05) improved for all active treatments versus placebo except once-daily budesonide DPI?B 180?μg in adults. In the adult study, significantly (?p?<?0.05) greater improvements in all secondary variables occurred with all active treatments versus placebo. In the pediatric/adolescent study, improvements in AM/PM PEF were significantly (p?≤?0.011) greater with twice-daily budesonide DPI?B 360?μg versus placebo. Numerically fewer patients in all active-treatment groups withdrew due to worsening asthma versus placebo.

Adverse event profiles were similar among groups. In the pediatric/adolescent study, no significant differences in mean 24-h urine cortisol or cortisol?:?creatinine ratio assessments were observed between the active treatment groups and the placebo group. Although pharmacokinetic variables were generally similar across subgroups in the adult (n?=?77) and pediatric/adolescent (n?=?32) studies, pairwise treatment comparisons of twice-daily budesonide DPI?B 360 μg versus DPI?A 400?μg and once-daily budesonide DPI?B 180?μg versus DPI?A 200?μg showed large variability for the area under the drug plasma concentration–time curve over the dosing interval and the maximum detected drug plasma concentration.

Conclusions: The efficacy and safety of budesonide DPI?A and DPI?B versus placebo were demonstrated across the low to medium inhaled corticosteroid dose range in children?≥?6 years with very mild asthma and adolescents and adults with mild-to-moderate asthma. The study is limited by the evaluation of only two doses for each product in both studies. Additionally, the studies were not designed to test equivalence or noninferiority between the active products. Pharmacokinetic characterization was limited because of the small sample sizes.     

肺部给药微粒研究近况

综述近年来肺部给药微粒的研究进展，包括微粒肺内沉积的影响因素、微粒的类型及其制备特性以及肺吸人微粒的优越性。     

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。     

口服脉冲控释给药系统的释药机制及其应用

口服脉冲控释给药系统因具有定时或定位释放的特点而成为当前药剂研究领域的热点.本文介绍了其释药机制,包括有机酸诱导、渗透压调节、pH依赖、时间依赖、酶依赖、pH-时间依赖及各释药机制应用实例.提出了该给药系统在应用中,尤其是对中药复方制剂所存在的一些问题,期望为口服中药脉冲控释给药系统的研究提供思路.     

Liposomes in Pulmonary Applications: Physicochemical Considerations,Pulmonary Distribution and Antioxidant Delivery

Abstract

The application of liposomes for improved drug delivery to the lung is promising. Liposome-mediated pulmonary drug delivery promotes an increase in drug retention-time in the lung and more importantly, a reduction in extrapulmonary side-effects, invariably resulting in enhanced therapeutic efficacies. The engineering of an effective liposomal drug formulation for inhalation therapy must take into consideration the leakage problem associated with the nebulization process; vesicle stability and release kinetics within the pulmonary milieu; and, the altered pharmacokinetics of the entrapped drug. The delivery of liposome-entrapped antioxidants via the tracheobronchial route has been found to be very useful in increasing the half-times of the administered agents, thus providing a sustained release effect for prolonged drug action. The entrapment in liposomes of a-tocopherol, an extremely insoluble but highly effective antioxidant, has been shown to be very effective in ameliorating oxidant-induced injuries in the lung. The use of bifunctional liposomes containing two antioxidants have been determined to provide excellent resistance to an oxidative challenge and appears to hold promise for improved clinical applications in antioxidant therapy.     

金纳米粒及其在药物传递系统中的应用研究进展

近年来,随着纳米材料科学的蓬勃发展,金纳米粒由于具有独特的光学和物理性质以及毒性小、比表面积大、表面可功能化修饰、易与药物分子结合等特点,其作为载体在药物传递系统中的应用已引起广泛关注。综述金纳米粒的特性、合成方法、体内分布与毒性以及在不同药物传递系统中的应用研究。