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作为一种非侵入给药方式,鼻腔给药具有快速起效、使用方便、依从性高、无首过效应、不良反应较小、黏膜免疫等诸多优点,且提供了鼻脑递送途径,鼻用制剂日益成为研发热点,以着力解决未被满足的临床需求。但是,因鼻腔结构和生理学上的特殊性,鼻用制剂的开发和评价还存在诸多挑战。 相似文献
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Drugs in nasal preparations, for local use as well as for systemic use, should not interfere with the self-cleaning capacity of the nose, effectuated by the ciliary epithelium. Many drugs and additives, however, have a negative effect on nasal ciliary function. Examples of ciliotoxic agents are lipophilic and mercuric preservatives, local anesthetics, antihistamines, propranolol, and absorption enhancers such as the bile salts. Cholinergic drugs and -adrenergic drugs exert a ciliostimulatory effect. It is the purpose of this review to summarize the present knowledge of ciliotoxicity of drugs and additives and to give recommendations for the use of ciliofriendly drugs in nasal preparations. 相似文献
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目的研究栀子环烯醚萜苷类成分鼻腔给药的吸收特性,为其鼻腔给药制剂设计提供依据。方法采用Franz扩散池,选用新鲜猪鼻黏膜为渗透屏障,以栀子苷为测定指标,HPLC测定含量,进行渗透试验;采用大鼠鼻腔循环灌流实验,以PBS溶液(pH7.4)作为鼻腔循环液,HPLC测定栀子苷,进行在体鼻黏膜吸收试验。结果栀子苷表观渗透系数Papp为(2.01±0.23)×10 5cm 2.s 1;药物稳态流量Jss为(1.61±0.18)×10 4μg.cm 2.s 1,透黏膜扩散属于以膜两侧浓度差为动力的被动扩散。栀子苷大鼠在体鼻黏膜吸收动力学方程lnC=1.165 7 0.001 6t,r=0.991 4,k=(1.6±0.021)×10 3min 1。结论栀子环烯醚萜苷可经鼻吸收,可制成经鼻给药的新制剂用于脑部疾病的防治。 相似文献
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Washington N McGlashan JA Jackson SJ Bush D Pitt KG Rawlins DA Gill DA 《Pharmaceutical research》2000,17(6):733-736
Purpose. The objective of this study was to investigate the effect ofnasal cavity patency on the penetration, deposition, and clearance ofan aqueous isotonic saline solution.
Methods. The study was carried out as a single center, open,randomized, 2-way cross-over in healthy volunteers. Nasal patency wasassessed using misting patterns on a cold metal surface at the beginningand end of study. 100 l of technetium-99m radiolabeled saline solutionwas introduced into either the most or least patent nasal cavity usinga purpose designed spray device. The distribution and residence timeof the radiolabel was followed for 2 hours using gamma scintigraphy.
Results. The mean times to 50% clearance were34 ± 7 and 28 ± 12minutes (±s.d.) for the side view of the least and most patent nasalcavity respectively. Total clearance of the radiolabelled saline from thenose was not affected by patency. Between 7 and 3% of theradiolabelled saline solution remained in the nasal cavity at the end of imaging.Using endoscopy to track the clearance of an aqueous solution of fooddye using the same delivery procedure, identified this region as hairin the nasal vestibule. The dye was seen to dry in this region alongwith the mucus.
Conclusions. Nasal patency affects the initial, but not total clearanceof solutions, however, the remaining solution may not be available fordrug delivery. 相似文献
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用于全身治疗的鼻腔给药系统研究概况 总被引:2,自引:0,他引:2
陈新梅 《中国现代应用药学》2007,24(1):23-27
目的介绍用于全身治疗的鼻腔给药系统研究概况。方法综述了鼻腔给药的特点、手段、制剂方法、要求、影响因素及研究状况。结果与讨论鼻腔给药可以产生全身作用,可以代替静脉给药,有广泛的应用前景。 相似文献
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Pharmaceutical Research - 相似文献
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《Expert opinion on drug delivery》2013,10(4):549-552
There were ~ 700 delegates who attended Respiratory Drug Delivery X (RDD-X) at the Boca Raton Resort and Club in Boca Raton, Florida, between the 24th and 27th April 2006. Participants from North America, Europe and many other parts of the world came together to hear a series of invited podium presentations covering the latest scientific developments in pulmonary and nasal drug delivery, along with regulatory and quality control issues. A total of 150 proffered posters were also presented, and a Technology Exhibition involved the products of 78 companies. The conference also provided unparalleled networking opportunities. The proceedings of RDD-X will prove to be an invaluable resource for years to come. 相似文献
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Nasal drug delivery has now been recognized as a promising route for drug delivery due to its capability of transporting a drug to systemic circulation and central nervous system. Though nasal mucosa offers improved bioavailability and quick onset of action of the drug, main disadvantage associated with nasal drug delivery is mucocilliary clearance due to which drug particles get cleared from the nose before complete absorption through nasal mucosa. Therefore, mucoadhesive polymeric approach can be successfully used to enhance the retention of the drug on nasal mucosal surface. Here, some of the aspects of the stimuli responsive polymers have been discussed which possess liquid state at the room temperature and in response to nasal temperature, pH and ions present in mucous, can undergo in situ gelation in nasal cavity. In this review, several temperature responsive, pH responsive and ion responsive polymers used in nasal delivery, their gelling mechanisms have been discussed. Smart polymers not only able to enhance the retention of the drug in nasal cavity but also provide controlled release, ease of administration, enhanced permeation of the drug and protection of the drug from mucosal enzymes. Thus smart polymeric approach can be effectively used for nasal delivery of peptide drugs, central nervous system dugs and hormones. 相似文献
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Ishikawa F Murano M Hiraishi M Yamaguchi T Tamai I Tsuji A 《Pharmaceutical research》2002,19(8):1097-1104
Purpose. To evaluate the utility of insoluble powder formulation for nasal systemic drug delivery.
Methods. To compare the efficacy of liquid and powder formulations, the nasal absorption of drugs was examined in rats using hydrophilic compounds with various molecular weights (MW) such as phenol red, cyanocobalamin, and fluorescein isothiocyanate (FITC)-Dextrans, and several kinds of powder. Intranasal residence time was also compared among the different formulations.
Results. All the drugs examined were absorbed through the nasal mucosa to varying extent; their systemic bioavailability decreased with increasing MW. Insoluble calcium carbonate (CaCO3) powder formulation provided increased absorption of drugs over the wide range of MW from 354 to 77,000 Da. In the case of phenol red, intranasal administration as a CaCO3 powder formulation resulted in a plasma concentration profile similar to that of an intravenous bolus dose due to its very rapid and complete absorption from the nasal cavity. Furthermore, improved bioavailability of FITC-Dextran (MW 4,400; FD-4) was also achieved with other insoluble powders as well as CaCO3, but not with soluble powders such as lactose, d-sorbitol, and d-mannitol. Insoluble powder formulation prolonged the residence time of FD-4 within the nasal cavity.
Conclusions. Insoluble powder formulations improve nasal bioavailability predominantly by retarding drug elimination from the absorption site and appear to be effective for nasal systemic drug delivery. 相似文献
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Phonophoresis is defined as the migration of drug molecules, contained in a contact agent, through the skin under the influence of ultrasound. Several drugs have been introduced into the body by this technique. The design of a phonophoretic drug delivery system is in developmental stages in various research laboratories. Parameters affecting the delivery of drugs by this technique and devices available for drug delivery purposes are discussed in this review. 相似文献
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Colonic Drug Delivery: Prodrug Approach 总被引:2,自引:0,他引:2
The colon is largely being investigated as a site for administration of protein and peptides, which are degraded by digestive enzymes in the upper GIT. Also for local diseases of the colon, drug administration to the site of action can not only reduce the dose to be administered, but also decrease the side effects. One of the approaches used for colon specific drug delivery is the formation of a prodrug which optimizes drug delivery and improves drug efficacy. Many prodrugs have been evaluated for colon drug delivery. These prodrugs are designed to pass intact and unabsorbed from the upper GIT and undergo biotransformation in the colon releasing the active drug molecule. This biotransformation is carried out by a variety of enzymes, mainly of bacterial origin present in the colon (e.g. azoreductase, glucuronidase, glycosidase, dextranase, esterase, nitroreductase, cyclodextranase, etc.). The present review includes varius prodrug approaches investigated for colon drug delivery and their site specificity. 相似文献
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On The Rate and Extent of Drug Delivery to the Brain 总被引:1,自引:0,他引:1
To define and differentiate relevant aspects of blood-brain barrier transport and distribution in order to aid research methodology in brain drug delivery. Pharmacokinetic parameters relative to the rate and extent of brain drug delivery are described and illustrated with relevant data, with special emphasis on the unbound, pharmacologically active drug molecule. Drug delivery to the brain can be comprehensively described using three parameters: Kp,uu (concentration ratio of unbound drug in brain to blood), CLin (permeability clearance into the brain), and Vu,brain (intra-brain distribution). The permeability of the blood-brain barrier is less relevant to drug action within the CNS than the extent of drug delivery, as most drugs are administered on a continuous (repeated) basis. Kp,uu can differ between CNS-active drugs by a factor of up to 150-fold. This range is much smaller than that for log BB ratios (Kp), which can differ by up to at least 2,000-fold, or for BBB permeabilities, which span an even larger range (up to at least 20,000-fold difference). Methods that measure the three parameters Kp,uu, CLin, and Vu,brain can give clinically valuable estimates of brain drug delivery in early drug discovery programmes. 相似文献
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Drug Delivery and Transport to Solid Tumors 总被引:3,自引:0,他引:3
Purpose. The purpose of this review is to provide an overview of the principles of and barriers to drug transport and delivery to solid tumors.
Methods. This review consists of four parts. Part I provides an overview of the differences in the vasculature in normal and tumor tissues, and the relationship between tumor vasculature and drug transport. Part II describes the determinants of transport of drugs and particles across tumor vasculature into surrounding tumor tissues. Part III discusses the determinants and barriers of drug transport, accumulation, and retention in tumors. Part IV summarizes the experimental approaches used to enhance drug delivery and transport in solid tumors.
Results. Drug delivery to solid tumors consists of multiple processes, including transport via blood vessels, transvascular transport, and transport through interstitial spaces. These processes are dynamic and change with time and tumor properties and are affected by multiple physicochemical factors of a drug, multiple tumor biologic factors, and as a consequence of drug treatments. The biologic factors, in turn, have opposing effects on one or more processes in the delivery of drugs to solid tumors.
Conclusion. The effectiveness of cancer therapy depends in part on adequate delivery of the therapeutic agents to tumor cells. A better understanding of the processes and contribution of these factors governing drug delivery may lead to new cancer therapeutic strategies. 相似文献