葛根汤颗粒喷雾干燥工艺条件试验研究

目的：优选葛根汤颗粒啧雾干燥的最佳工艺条件。方法：应用正交设计法，以每小时药粉产率及有效成分含量为考察指标，对影响葛根汤喷雾干燥过程的因素进行考察。结果：正交试验法设计的三个因素中，浸膏的相对密度影响显著，入塔风温影响较显著。结论：颗粒最佳工艺条件为：入塔风温：170℃，气流量：700L／h，浸膏相对密度：1．22，在此条件下，葛根汤颗粒有效成分中葛根素及芍药苷的含量明显高于原湿法制粒制剂。     

病毒唑雾化吸入治疗上呼吸道感染临床疗效观察

选择89年2月至90年2月175例上呼吸道感染患儿,分为病毒唑雾化吸入组(61例).病毒唑全身给药组(53例)和对照组(61例).平均退热时间分别为30.01±.11,31.89±9.28,40.57±16.94小时.病毒唑组与对照组有非常显著性差异(p<0.01)但两病毒唑治疗组之间无显著性差异,并发现发病时间在一天内接受治疗者,退热时间明显短于超过一天之病例,且发病两天后治疗者与对照组已无显著差异(p<0.05).病毒唑全身用药组和对照组共有4例发展为支气管炎和肺炎,而雾化吸入组无,说明该治疗方法可以阻止病毒感染蔓延至下呼吸道.     

Haarkrankheit oder hitze-(brand)-einwirkung?

Zusammenfassung Ein 4 Tage nach einem offensichtlich durch Brandstiftung erfolgten Dachstuhlbrand einer Kirche untersuchter Tatverdächtiger wies in einem umschriebenen Bezirk stumpfe Haarenden auf. Typische Haarspitzenveränderungen durch Hitzeeinwirkung waren makroskopisch und lupenmikroskopisch nicht sicher erkennbar. Mikroskopisch konnte jedoch die Diagnose eindeutig gestellt werden. Auffällige spindelförmige Haarveränderungen, die zunächst ebenfalls als hitzebedingt oder durch krankhafte Haarveränderungen hervorgerufen angesehen wurden, erwiesen sich als Artefakte durch Aufsprühen eines Haarfestigers.Auszugsweise auf der Tagung der Deutschen Gesellschaft für Rechtsmedizin in St. Gallen im September 1986 vorgetragen     

药氧雾化吸入治疗慢性阻塞性肺病的临床研究

目的:以中医药疗法治疗慢性阻塞性肺病(COPD).方法:中药制剂经氧气超声雾化吸入,按照疗程观察.结果:随机分为治疗组和对照组,治疗组有效率为87.00%,对照组有效率为75.00%,治疗组疗效优于与对照组(P《0.05).结论:中药经氧气雾化吸入治疗慢性阻塞性肺病有效,值得推广运用.     

An overview on in situ micronization technique – An emerging novel concept in advanced drug delivery

The use of drug powders containing micronized drug particles has been increasing in several pharmaceutical dosage forms to overcome the dissolution and bioavailability problems. Most of the newly developed drugs are poorly water soluble which limits dissolution rate and bioavailability. The dissolution rate can be enhanced by micronization of the drug particles. The properties of the micronized drug substance such as particle size, size distribution, shape, surface properties, and agglomeration behaviour and powder flow are affected by the type of micronization technique used. Mechanical communition, spray drying and supercritical fluid (SCF) technology are the most commonly employed techniques for production of micronized drug particles but the characteristics of the resulting drug product cannot be controlled using these techniques. Hence, a newer technique called in situ micronization is developed in order to overcome the limitations associated with the other techniques. This review summarizes the existing knowledge on in situ micronization techniques. The properties of the resulting drug substance obtained by in situ micronization were also compared.     

Spray freeze drying for dry powder inhalation of nanoparticles

Formulating nanoparticles for delivery to the deep lung is complex and many techniques fail in terms of nanoparticle stability. Spray freeze drying (SFD) is suggested here for the production of inhalable nanocomposite microcarriers (NCM). Different nanostructures were prepared and characterized including polymeric and lipid nanoparticles. Nanoparticle suspensions were co-sprayed with a suitable cryoprotectant into a cooled, stainless steel spray tower, followed by freeze drying to form a dry powder while equivalent compositions were spray dried (SD) as controls. SFD-NCM possess larger specific surface areas (67–77 m²/g) and lower densities (0.02 g/cm³) than their corresponding SD-NCM. With the exception of NCM of lipid based nanocarriers, SFD produced NCM with a mass median aerodynamic diameter (MMAD) of 3.0 ± 0.5 μm and fine particle fraction (FPF ⩽ 5.2 μm) of 45 ± 1.6% with aerodynamic performances similar to SD-NCM. However, SFD was superior to SD in terms of maintaining the particle size of all the investigated polymeric and lipid nanocarriers following reconstitution (S_f/S_i ratio for SFD ≈ 1 versus >1.5 for SD). The SFD into cooled air proved to be an efficient technique to prepare NCM for pulmonary delivery while maintaining the stability of the nanoparticles.     

Effects of fabrication conditions on the characteristics of etanidazole spray-dried microspheres

Etanidazole, a hypoxic radiosensitizer, has potential applications in radiotherapy. Due to its high solubility in water, common methods to encapsulate etanidazole into microspheres are not feasible. In this study, a spray-drying technique was employed to encapsulate etanidazole into the biodegradeable polymer, PLGA65:35. Different fabrication conditions, such as polymer concentration, inlet temperature, feed rate, compressed air flow rate, aspirator ratio, as well as drug-loading were investigated to understand their effects on the particle size and distribution, encapsulation efficiency, and release behaviour. The effect on the morphologies of microspheres were also observed by scanning electron microscopy (SEM) and atomic force microscopy (AFM). It was demonstrated that most of these fabrication conditions influence either the droplet formation process or its subsequent evaporation and particle shrinking process, thereby determining the properties of the microspheres obtained. In many cases, temperature seems to be more important among all the factors considered. The present study demonstrates good fabrication conditions for producing the etanidazole-PLGA65:35-microspheres by using DCM as a solvent. The release of etanidazole from the spray dried PLGA65:35 microspheres was very fast, with an initial burst of 47% within the first 30 min and a cumulative release of over 80% within the first 5.5 h. The encapsulation efficiency of the drug in the microspheres varied with operating conditions from 69-96%.     

Investigation of the effects of process variables on derived properties of spray dried solid-dispersions using polymer based response surface model and ensemble artificial neural network models

The objective of this study was to use different statistical tools to understand and optimize the spray drying process to prepare solid dispersions. In this study we investigated the relationship between input variables (inlet temperature, feed concentration, flow rate, solvent and atomization parameters) and quality attributes (yield, outlet temperature and mean particle size) of spray dried solid dispersions (SSDs) using response surface model and ensemble artificial neural network. The Box Behnken design was developed to investigate the effect of various input variables on quality attributes of final products. Moreover, Pearson correlation analysis, self organizing map, contour plots and response surface plot were used to illustrate the relationship between input variables and quality attributes. The influence of different physicochemical properties of solvent on the quality attributes of spray dried products was also investigated. Final validation of prepared models was done using binary SSDs of six model drugs with PVP. Results demonstrated the effectiveness of proposed PVP based model which can help scientists to gain detailed understanding of spray drying process of solid dispersion using minimal resources and time during early formulation development stage. It will also help them to ensure consistent quality of SSDs using broad range of input variables.     

Drug/polymer nanoparticles prepared using unique spray nozzles and recent progress of inhaled formulation

Inhaled formulations are promising for pulmonary and systemic non-pulmonary diseases. Functional engineered particles including drugs and drug-loaded nanocarriers have been anticipated because they can improve drug delivery efficacy against target sites in the lungs or blood. In this review, unique spray nozzles (e.g., four-fluid spray nozzle and two-solution mixing type nozzle) for the preparation of nanocomposite particles which mean microparticles containing drug nanoparticles are described. These nozzles can produce nanocomposite particles in one-step and their spray drying system is suitable for scaling-up. Nanocomposite particles are useful in improving drug absorption and delivery efficacy against alveolar macrophages. In addition, recent studies on several pulmonary diseases (tuberculosis, lung cancer, cystic fibrosis, pneumonia, vaccine and others) and related inhaled formulations were also reviewed.