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1.
新型凝胶给药系统研究进展   总被引:3,自引:0,他引:3  
周红义  杨今祥 《中国药师》1999,2(3):121-123
凝胶在现代药学中应用广泛,以凝胶为基质的缓释控释剂型,如胃滞留控释系统、凝胶骨架片等,得到了全面的研究。适用于凝胶给药系统的药物甚多,亲水性药物、疏水性药物、酸性药物、阳离子药物、大分子药物、细胞组织等均可作为它的模型药物。而且可以从口腔、鼻腔、眼粘膜、消化道粘膜、阴道、直肠、皮肤等途径给药。  相似文献   

2.
目的了解米索前列醇新剂型—凝胶剂,对大鼠在体子宫平滑肌的收缩频率、幅度的影响,为制药企业开发和临床应用米索前列醇凝胶剂提供客观依据。方法采用抗早孕的动物研究方法,将米索前列醇凝胶剂通过大鼠阴道给药,进行药物作用实验。结果米索前列醇通过阴道给药可明显增强大鼠子宫收缩力,并且较口服给药起效时间缩短。结论米索前列醇凝胶剂是抗早孕的一种较好的剂型。  相似文献   

3.
目的介绍传统剂型,新技术,新方法在黏膜给药系统上的研究进展。方法综述了凝胶剂、喷雾剂、气雾剂、粉雾剂等传统剂型;微球、脂质体、纳米粒、乳剂、原位凝胶等新技术以及吸收促进剂、生物黏附剂、前体药物、酶抑制剂等方法在促进药物黏膜吸收方面的进展。结果国内外对这些剂型、方法、技术等已经进行了广泛和深入的研究,取得了较大的进展。结论黏膜给药系统已成为目前研究的热点,它是传统给药方式的补充,具有广阔的应用前景。同时,为了进一步促进黏膜给药系统的发展,对安全、低毒、有效的吸收促进剂和新型载药体系的开发仍将是今后研究的主要方向。  相似文献   

4.
《中国药房》2015,(1):132-135
目的:为温敏凝胶的研发及临床应用提供相关理论参考。方法:以"温敏凝胶""作用机制""辅料""给药途径""Temperature-sensitive gel""Mechanism""Accessories""Route of administration"等为关键词,组合检索2009-2014年Pub Med、中国知网、万方等数据库,对温敏凝胶的作用机制、释药模式、给药途径及应用情况等作简要综述。结果与结论:温敏凝胶通过改变分子间的作用力,使聚合物之间的相互作用发生改变,随着温度升高而形成凝胶。其中常用的是丙烯酰胺类,主要释药模式包括挤压式、正反"开-关"式、压力作用式等。采用注射、口腔、耳内、鼻腔、眼内、皮肤等多种给药方式,使药物在人体内发挥很好的缓释作用,降低药物毒性,防止药物外渗,提高药物的稳定性,比同类药物的其他剂型更有优势。随着温敏凝胶研究和应用的不断深入,其作为一种新型剂型,有望在肿瘤、中药新剂型等方面得到更好的应用。  相似文献   

5.
中药的传统剂型有膏、丹、丸、散等。明代李时珍编著的《本草纲目》总结了16世纪以前我国的用药经验,收载了药物剂型近4 0种[1] ,除现代剂型中的注射剂与片剂外几乎都有。但相对于西药制剂而言,中药因其固有的粗、大、黑和显效缓慢等缺陷,故不易被国外所广泛理解、接受,妨碍了中药制剂走向国际医药市场。近年来,我国医药工作者对新型中药给药系统进行了卓有成效的探索,发展了中药结肠定位制剂、中药透皮贴剂以及涂膜剂、膜剂、凝胶剂、巴布剂、穴位贴敷剂等新剂型。清华大学等还推出了口服渗透泵控释制剂、基质型经皮给药系统和胃肠定位系统…  相似文献   

6.
国内外药物凝胶剂研究进展   总被引:18,自引:5,他引:13  
高正华 《中国药房》2001,12(11):691-692
药剂学研究中的剂型设计 ,主要目的是为了方便临床用药并使药物发挥最佳疗效。随着药物新剂型研究的不断深入 ,一种新型的外用药物制剂———凝胶剂开始引起药剂研究人员的重视。由于凝胶剂具有水溶性特点 ,局部给药后 ,患处表面皮肤吸收良好 ,不仅避免了口服给药存在的胃肠道首过效应 ,而且使副作用大大减小 ;同时 ,水溶性凝胶剂给药后皮肤表面的药膜不粘衣物 ,也使患者乐于接受。凝胶剂有单相和双相凝胶之分 [1]。《中国药典》2000年版在 (二部 )凡例中界定了凝胶剂 :“凝胶剂是指药物与能形成凝胶的辅料制成的均一、混悬或乳剂型…  相似文献   

7.
黄体酮是目前临床上治疗、预防先兆流产和习惯性流产的一线药物。随着我国生育政策的逐渐放开,高龄产妇显著增加,市场对黄体酮的需求量及个性化要求不断提高。临床研究发现,黄体酮的适应症并不局限于妇科疾病,还可用于肾绞痛、创伤性脑损伤等疾病的治疗。现有黄体酮上市制剂有口服胶囊、肌肉注射剂和阴道凝胶剂等,但其已无法满足市场的需求及适应症的增多。开发新型制剂、开拓新的给药途径已成为黄体酮药物研究的方向之一。本文将黄体酮现有给药途径中的新剂型、给药新途径及其相关制备方法研究做一综述。  相似文献   

8.
眼部给药剂型的研究进展   总被引:1,自引:0,他引:1  
目的介绍眼部给药剂型的特点与发展。方法根据文献综述了眼部给药剂型及给药系统的特点和应用。结果目前滴眼剂、眼膏、眼用膜剂广泛应用于治疗眼病,眼部给药系统如原位凝胶给药系统、胶体给药系统、微球、植入剂等可以明显地提高药物的生物利用度。结论眼用给药系统在药学领域中有着广阔的发展前景。  相似文献   

9.
凝胶剂是指药物与能形成凝胶的辅料制成的均一、混悬或乳剂型的半透明半固体制剂。临床上应用较多的是水性凝胶基质,还有乳剂性凝胶。乳剂性凝胶基质兼有乳剂和凝胶的一些特性,洁白、细腻、富有光泽,极易涂布和洗除,无刺激且稳定,比单纯凝胶剂润滑性好,可作为外用药物的良好基质。 凝胶剂目前在临床上主要应用于局部和透皮给  相似文献   

10.
适用于中药外用的剂型--凝胶剂   总被引:7,自引:0,他引:7  
方和桂 《中国药业》2002,11(8):25-26
目的:介绍一种适用于中药外用的剂型--凝胶剂。方法:通过对凝胶剂的含义、特点、质量要求,以及凝胶剂的发展概况的阐述,提出了凝胶剂在中药制剂中应用的思路。结果与结论:凝胶剂是一种适用于皮肤、粘膜及腔道给药的外用剂型,有减轻药物的毒副作用,符合中医“内病外治”的理念,适应中药复方制剂的生产现状,是中药传统外用药剂较为理想的剂型。  相似文献   

11.
复方盐酸林可霉素凝胶的研制   总被引:1,自引:0,他引:1  
复方盐酸林可霉素凝胶是以卡波姆940为基质的水溶性透明凝胶,主要成分为盐酸林可霉素、成纤维细胞生和工因子,可用于治疗皮肤科各种化脓性感染、溃疡等。  相似文献   

12.
复方盐酸林可霉素凝胶的研制   总被引:1,自引:0,他引:1  
复方盐酸林可霉素凝胶是以卡波姆940为基质的水溶性透明凝胶,主要成分为盐酸林可霉素、成纤维细胞生长因子,可用于治疗皮肤科各种化脓性感染、溃疡等。本文介绍了复方盐酸林可霉素凝胶的处方组成、制备方法、含量测定和质量标准。凝胶中盐酸林可霉素的含量采用抗生素微生物检定法进行测定,操作简单,无需特殊设备。  相似文献   

13.
Purpose This study was aimed at formulating a hydrophilic non-aqueous gel for topical delivery of the model moisture-sensitive drug, minocycline hydrochloride (MH). Methods Stability study of MH dissolved in water and various hydrophilic non-aqueous solvents was performed over a period of four months in order to select a suitable non-aqueous solvent for MH gel. To improve MH stability, the effect of different cation additives on MH stability in the selected solvent was investigated. Non-aqueous gel matrices were prepared from three different types of hydrophilic polymers in glycerin-propylene glycol mixture with Mg2+ cation additive. Oscillatory shear rheometry was performed on the gel matrices using a cone-and-plate rheometer. Results MH stability was affected by the type of solvent employed and the duration of storage. Different cation additives affected the extent of MH stabilization through MH-cation complex formation. Rheological properties of the non-aqueous gel matrices were significantly affected by the type and concentration of polymer, and the vehicle ratios in the formulations. Conclusions MH stabilization could be achieved using the selected glycerin-propylene glycol mixture containing MgCl2. Gel matrix formulated using this solvent system and 3%w/w N-vinylacetamide/sodium acrylate copolymer had demonstrated the most favorable rheological properties as a gel for topical application.  相似文献   

14.
H Junginger 《Die Pharmazie》1984,39(9):610-614
O/W creams with crystalline gel structures are supposed to be four phase systems. Their dominant structural elements are the hydrophilic and lipophilic gel phases. The hydrophilic gel phases have - depending on the hydrophilic character of their polar groups - a very strong swelling capacity. Further, a dynamic equilibrium is maintained between the water interlamellarly inserted into the hydrophilic gel phase and the bulk water phase. The latter is mainly fixed mechanically by the hydrophilic gel phase. The lipophilic gel phases, however, which immobilize the dispersed phase, have no or only an extremely weak swelling capacity. By means of thermogravimetry (TG) a quantitative differentiation between water interlamellarly fixed in the hydrophilic gel phase and bulk water is possible. Using dynamic TG, the curves of water release and the results obtained are discussed. In the water-containing hydrophilic ointment DAB 8 and in the non-ionic hydrophilic ointment DAC the fractions of interlamellarly fixed water are substantially higher than those of the bulk water. In the investigated stearate creams, however, the fraction of the bulk water is much higher than the fraction of interlamellarly fixed water. Consequently the water release from these stearate creams is higher than that of the other O/W creams mentioned above. It is concluded that the ratio of interlamellarly fixed water and bulk water is an important criterion for the properties of such O/W creams and that TG can be suitably applied not only as in process control during product manufacturing but also as a useful tool in the development of O/W creams with a controlled water release.  相似文献   

15.
This study investigates the effect of the chemical heterogeneity of hydroxypropyl methylcellulose (HPMC) on the release of model drug substances from hydrophilic matrix tablets. The hypothesis was that the release of drug substances could be influenced by possible interactions with HPMC batches having different chemical heterogeneity. The cloud point of the most heterogeneous batch was more affected by the model drug substances, methylparaben and butylparaben, and most by butylparaben with the lowest solubility. The different clouding behaviour was explained by the heterogeneously substituted batches being more associative and the more lipophilic butylparaben being able to interact more efficiently with the hydrophobic HPMC transient crosslinks that formed. Interestingly, tablet compositions of the heterogeneously substituted HPMC batches released the more soluble methylparaben at lower rates than butylparaben. The explanation is that the hydrophobic HPMC interactions with butylparaben made the gel of the tablet less hydrated and more fragile and therefore more affected by erosional stresses. In contrast, drug release from compositions consisting of the more homogeneously substituted batches was affected to a minor extent by the drugs and was very robust within the experimental variations. The present study thus reveals that there can be variability in drug release depending on the lipophilicity of the drug and the substituent heterogeneity of the HPMC used.  相似文献   

16.
A microsphere–gel in situ forming implant (MS–Gel ISFI) dual-controlled drug delivery system was applied to a high water-soluble small-molecule compound Rasagiline mesylate (RM) for effective treatment of Parkinson’s disease. This injectable complex depot system combined an in situ phase transition gel with high drug-loading and encapsulation efficiency RM–MS prepared by a modified emulsion-phase separation method and optimized by Box–Behnken design. It was evaluated for in vitro drug release, in vivo pharmacokinetics, and in vivo pharmacodynamics. We found that the RM-MS-Gel ISFI system showed no initial burst release and had a long period of in vitro drug release (60?days). An in vivo pharmacokinetic study indicated a significant reduction (p?in situ gel systems after intramuscular injection to rats. A pharmacodynamic study demonstrated a significant reduction (p?p?in situ phase transition gel is superior for use as a biodegradable and injectable sustained drug delivery system with a low initial burst and long period of drug release for highly hydrophilic small molecule drugs.  相似文献   

17.
Studies on the effect of hydrophilic gel composition on pharmaceutical availability of prednisolone complexed with beta-cyklodextrin at P:beta-CD ratios 1:1 and 1:2 revealed that the half-release times were shortened and differentiated depending on the substances added hydrogel to propylene glycol, dimethylacetamide and polysorbate 20 in comparison to preparations containing non-complexed active substance.  相似文献   

18.
PURPOSE: This study reports the development of a method based on dynamic contact angle to investigate the wetting behavior of non-aqueous ethylcellulose (EC) gel matrices intended for topical drug delivery. METHODS: Non-aqueous gel matrices were prepared from the three fine particle grades of EC and propylene glycol dicaprylate/dicaprate. Dynamic contact angle measurements of sessile drops of water and isopropylmyristate (IPM) on EC gel matrices were performed using a dynamic contact angle analyzer equipped with axisymmetric drop shape analysis of the sessile drop images. Gel density was determined by weighing known volumes of gel samples. RESULTS: The EC gel matrices were wetted by both water and IPM, with much higher wettability by the latter. Increased EC concentration and polymeric chain length decreased the extent and rate of wetting. Linear correlation was observed between wetting parameters and rheological as well as mechanical properties of EC gel matrices. CONCLUSIONS: The EC gel matrices exhibited both hydrophilic and lipophilic properties, with predominance of the latter. The extent and rate of wetting was governed by a balance of chemical and physical characteristics of the gel. EC gel matrices showed desirable wetting behavior in their function as a moisture-barrier, bioadhesive and vehicle for topical drug delivery.  相似文献   

19.
UDPGT isoenzymes are products of multiple gene families as demonstrated by sequence analysis of purified proteins and by molecular cloning experiments. These isoenzymes are relatively specific for endogenous substrates but have broad substrate specificities for xenobiotic substrates. They are important metabolic enzymes capable of converting exogenous and endogenous substances to more hydrophilic metabolites. Each species has its own pattern of UDPGTs and it is not possible at this time to extrapolate information directly from one species to another.  相似文献   

20.
Aquatic toxicity tests were originally developed for water-soluble substances. However, many substances are hydrophobic and thus poorly water-soluble, resulting in at least two major implications. Firstly, toxicity may not be reached within the range of water solubility of the tested compound(s), which may result in the formation of solids or droplets of the tested substance and consequently an uneven exposure. Secondly, because of multi-phase distribution of the tested substance it may be complicated to keep exposure concentrations constant. To overcome such problems, we have introduced silica gel as a particulate carrier in a toxicity test with the benthic copepod Nitocra spinipes. The main objective of the current study was to evaluate whether a controlled exposure could be achieved with the help of silica gel for testing single poorly water-soluble substances. A secondary objective was to evaluate whether an equilibrium mass balance model could predict internal concentrations that were consistent with the toxicity data and measured internal concentrations of two model hydrophobic substances, i.e., the polybrominated diphenyl ethers BDE-47 and BDE-99. Larval N. spinipes were exposed for 6 days to BDE-47 and BDE-99, respectively, in the silica gel test system and, for comparative reasons, in a similar and more traditional semi-static water test system. Via single initial amounts of the model substances administered on the silica gel, effects on both larval development and mortality resulted in higher and more concentration-related toxicity than in the water test system. We conclude that the silica gel test system enables a more controlled exposure of poorly water-soluble substances than the traditional water test system since the concentration-response relationship becomes distinct and there is no carrier solvent present during testing. Also, the single amount of added substance given in the silica gel test system limits the artefacts (e.g., increased chemical load in test system) that a semi-static renewal may introduce when testing substances that partition to non-water phases. However, measured and modelled internal concentrations did not match toxicity, which may indicate that chemical equilibrium was not reached during the test. Further experiments are thus needed to explain the processes behind the observed positive effects of silica gel and a kinetic model would likely also be more appropriate to describe the concentrations and distributions in the two test systems.  相似文献   

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