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排序方式: 共有234条查询结果,搜索用时 31 毫秒
1.
Recombinant human deoxyribonuclease I (rhDNase) is a new therapeutic agent developed to improve clearance of purulent sputum from the human airways. It is delivered by inhalation. Four jet nebulizers, T Up-Draft II (Hudson), Customized Respirgard II (Marquest), Acorn II (Marquest), and Airlife Misty (Baxter), were evaluated in vitro for their ability to deliver aerosols of rhDNase. The aerosols were generated from 2.5-mL aqueous solutions of rhDNase, at concentrations of either 1 or 4 mg/mL. In all experiments, the Pulmo-Aide Compressor (De Vilbiss) was used to supply the air to the nebulizers. Between 20 and 28% of the rhDNase dose initially placed in the nebulizers was delivered to the mouthpiece in the respirable range (1-6 µm). Evaluation of the rhDNase following nebulization in all four devices indicated that there was no loss in enzymatic activity and no increase in aggregation. Circular dichroism spectrophotometry indicated there was no change in either the secondary or the tertiary structure in rhDNase following nebulization. These results show that all four nebulizers are essentially equivalent in their ability to deliver respirable doses of rhDNase in an intact, fully active form. Changing the concentration of the solution in the nebulizer from 4 to 1 mg/mL rhDNase leads to a proportional reduction in the respirable dose delivered to the mouthpiece. 相似文献
2.
天然放射性气溶胶粒径分布的变化会引起氡及其子体所致肺剂量的较大涨落。由于我国对其报道甚少,在肺剂量估算中均引用UNSCEAR的推荐值。为验证这种引用的合理性和建立气溶胶粒径分布的测量方法,开展本项研究。方法采用金属丝网筛(165目)扩散法测量天然空气经不同数目网筛扩散前后的放射性浓度比(衰减比)来绘制衰减曲线,然后用池边模式计算出粒径分布曲线。衰减比、粒径分布的计算和曲线的绘制均采用计算机。结果室内外天然放射性气溶胶粒径呈几何正态分布,分布的峰值的平均值分别为(0.20±0.09)μm和(0.27±0.11)μm。粒径分布和氡浓度、气压、气温、湿度等未发现相关关系。结论本研究结果与UNSCEAR报告书(1988)的推荐值相比,室内值相同,室外值略高,与Jacobi的研究相近。由此可得出结论,福州地区引用UNSCEAR报告书的推荐值来估算氡及其子体所致肺剂量是合适的。此结论能否推广到其他地区,还需作进一步的研究。 相似文献
3.
色甘酸钠混悬气雾剂与茶碱缓释胶囊治疗中度哮喘的比较 总被引:1,自引:1,他引:0
84例中度哮喘病人分成2组。色甘酸钠组(男性23例,女性20例,年龄26±s8a)吸入色甘酸钠混悬气雾剂10.5mg,tid。茶碱缓释胶囊组(男性22例,女性19例,年龄27±8a)口服0.25g。bid。2组均连续观察3mo。结果:色甘酸钠在减轻病人慢性症状、改善肺功能和降低气道高反应性等方面优于茶碱缓释胶囊,(P<0.01)。而后药仅可缓解近期症状。 相似文献
4.
A series of multilamellar liposome dispersions was prepared from lipids of soy phosphatidylcholine or hydrogenated soy phosphatidylcholine containing from 0 to 30 mol% of either cholesterol, steary-lamine, or dipalmitoyl phosphatidylglycerol. The liposome dispersions were aerosolized with a Collison nebulizer for 80 min at an output flow rate of 4.7 liters of air/min. The effects of nebulization on the vesicles were determined by monitoring the release of encapsulated 5,6-carboxyfluorescein (CF) from dispersions containing 200 µg of total CF, of which 93.1 ± 2.4% (N = 18) was initially encapsulated. In all experiments CF was released from the liposomes while being aerosolized, and this ranged from a mean of 12.7 ± 3.8 to 60.9 ± 1.9% of the encapsulated CF, depending upon the lipid composition. The lipid concentration in the dispersions did not affect the rate or percentage release of CF over a range of 0.5 to 50 mg per nebulized dispersion. If liposomes are to be used as drug carriers in an inhalation aerosol a lipid composition should be employed which will minimize the release of encapsulated drug caused by nebulization. 相似文献
5.
Byron Peter R. Sun Zhuang Katayama Hirokazu Rypacek Frantisek 《Pharmaceutical research》1994,11(2):221-225
The pulmonary absorption kinetics of a single molecular weight distribution (MWD) of fluorophore-labeled poly-,-[N(2-hydroxyethyl)-DL-aspartamide] (F-PHEA), a hydrophilic and biocompatible synthetic polypeptide, were studied in the isolated, perfused rat lung (iprl) as functions of administered polymer concentration, dose, vehicle, and presence and absence of fluorophore. The MWD was characterized before and after absorption by measurement of weight- and number-averaged molecular weights (M
wand M
n, respectively) using high-performance gel-permeation chromatography. Values for M
w and M
n were 8.6 and 5.3 kD before, and 6.7 and 4.7 kD after, absorption into the perfusate; there was no significant metabolism and the MWD of the absorbed polymer was independent of both dose and sampling time over a 3-hr period. F-PHEA failed to show any evidence of aggregation in solution or changes in dose distribution within the airways as functions of increasing polymer concentration and dose. A concentration ranging study indicated the presence of a saturable, carrier-mediated transport process for F-PHEA with a maximum absorption rate, V
max, of approximately 180 µg or 0.027 µmol/hr. Coadministration of fluorophore-free PHEA was capable of depressing the absorption of F-PHEA. The transport process for F-PHEA appeared to have a molecular weight limit of about 7 kD for this hydrophilic polymer. 相似文献
6.
Niven Ralph W. Whitcomb K. Lane Shaner Linda Ip Anna Y. Kinstler Olaf B. 《Pharmaceutical research》1995,12(9):1343-1349
Purpose. The objective of this study was to highlight differences in the pulmonary absorption of a monoPEGylated rhG-CSF and rhG-CSF after intratracheal instillation and aerosol delivery.
Methods. Male Sprague Dawley rats (250 g) were anesthetized and intratracheally instilled (IT) with protein solution or were endotracheally intubated and administered aerosol for 20 min via a Harvard small animal ventilator. A DeVilbiss Aerosonic nebulizer containing 5 ml of protein solution at 3 mg/ml was used to generate aerosol. The volume of protein solution deposited in the lung lobes was estimated to be 13 µl after delivery of Tc-99m HSA solutions. The PEGylated proteins consisted of a 6 kDa (P6) or 12 kDa PEG (PI2) linked to the N-terminus of rhG-CSF. rhG-CSF also was administered IT in buffers at pH 4 and pH 7 and in dosing volumes ranging from 100 to 400 µl. Blood samples were removed at intervals after dosing and the total white blood cell counts (WBC) were determined. Plasma was assayed for proteins by an enzyme immuno assay.
Results. The plasma protein concentration v. time profiles were strikingly different for aerosol v. IT delivery. The C
max values for rhG-CSF and P12 after aerosol delivery were greater than found after IT (Aerosol: 598 ± 135 (ng/ml) rhG-CSF; 182 ± 14 P12 v. IT: 105 ± 12 rhG-CSF; 65.9 ± 5 P12). Similarly, Tmax was reached much earlier after aerosol administration (Aerosol: 21.7 ± 4.8 (min) rhG-CSF; 168 ± 31 P12 v. IT: 100 ± 17 rhG-CSF; 310 ± 121 P12). Estimated bioavailabilities (Flung %) were significantly greater via aerosol delivery than those obtained after IT (Aerosol: 66 ± 14 rhG-CSF; 12.3 ± 1.9 P12 v. IT: 11.9 ± 1.5 rhG-CSF; 1.6 ± 0.1 P12). An increase in circulating WBC counts was induced by all proteins delivered to the lungs. The rate and extent of absorption of rhG-CSF was not influenced by the pH employed nor the instilled volume.
Conclusions. Estimates of bioavailability are dependent upon the technique employed to administer drug to the lungs. Aerosol administration provides a better estimate of the systemic absorption of macromolecules. 相似文献
7.
A series of carboxyfluorescein (CF)-containing multilamellar vesicle (MLV) dispersions was prepared and extruded through polycarbonate membranes ranging in size from 0.2 to 5 µm. Vesicle dispersions were nebulized for 80 min using a Collison nebulizer, and the release of CF was monitored during nebulization. Solute retention was dependent upon the size of the vesicles and leakage ranged from 7.9 ± 0.4% (N = 3) for vesicles extruded through 0.2-µm filters to 76.8 ± 5.9% (N = 3) for liposomes that were not filtered. Solute release profiles obtained over 420-min nebulization periods conformed to a two-compartment kinetic model and exhibited a fast initial phase (k
l = 0.052 ± 0.0043) followed by a slow terminal phase (k
2 = 0.0034 ± 0.00018). The results show that CF retention can be increased by nebulizing small vesicles and modeling suggests that the rate of CF leakage from the bilayers is faster than from the core of the liposomes. 相似文献
8.
9.
《Journal of biopharmaceutical statistics》2013,23(3):323-332
For locally acting drug products such as nasal aerosols and nasal sprays, therapeutic equivalence between two drug products may be established by in vitro bioequivalence studies based on measurements intended to reflect the rate and extent to which the active ingredient becomes available at the site of action. For cascade impaction or multistage liquid impinger for particle size distribution, profile analysis is required. However, we find that the analysis procedure described in the 1999 FDA guidance lacks statistical justification. In this article, we explain why FDA's approach is incorrect and propose a correct statistical method for profile analysis using the basic ideas in the FDA guidance. 相似文献
10.