丙泊酚载药脂肪乳的处方及工艺研究

目的:考查处方和制备工艺对丙泊酚载药脂肪乳稳定性的影响。方法:以注射用大豆油为油相,大豆磷脂和泊洛沙姆为乳化剂,在单因素考查的基础上采用正交设计优化了大豆油、乳化剂和稳定剂的用量,并优化了制备工艺。结果:乳剂的最优处方为10%油相,1.2%乳化剂,1.0%稳定剂,最优工艺为水相和油相在55℃混合,10000 r/min均质5min,4.14×105Pa压力下通过微射流仪6次。结论:制得的丙泊酚乳剂物理稳定性良好,为进一步研究丙泊酚注射乳剂奠定了一定的基础。     

载药脂肪乳剂的研究进展

脂肪乳作为一种给药载体,不论处方组成还是制备工艺已经日益成熟.SolEmul技术给油水均难溶药物的制剂带来希望;自乳化给药系统可提高难溶性药物的生物利用度;阳离子脂肪乳不仅延长药物体内循环时间,还使肺部给药技术得到长足发展;同时脂肪乳在细胞靶向和中药制剂的研究中也呈现出独特的优势.随着载药脂肪乳各项研究的深入和发展,未...     

载药微球制备的研究进展

微球作为新型给药载体,在提高药物稳定性、生物利用度尤其在药物缓控释,靶向方面优势明显,而这些优势在很大程度上取决于所选载体材料。就根据制备微球的常用载体的特点及具体制备方法进行了综述。     

纳米载药系统的研究进展

纳米粒是现代药剂学研究的热点,其体积微小、结构特殊,在医药领域中显示出特殊的优势。该文根据近年来文献,对纳米粒的特点、制备、后处理以及应用等方面进行了介绍。     

水飞蓟宾脂肪乳的制备、性质及体外释药研究

目的：制备水飞蓟宾脂肪乳并对其体外释放进行考察。方法：在单因素试验的基础上,采用正交试验设计优化水飞蓟宾脂肪乳处方。采用高压均质法制备水飞蓟宾脂肪乳。结果：脂肪乳平均粒径为（74.42±14） nm,粒径分布系数（ PDI）为0.106,Zeta电位为（-30.2±2.13）mV,pH为6.48±0.04,包封率（91.45±0.0052）%,体外12 h内,累积释放原药的90%左右。结论：本试验获得了较理想的水飞蓟宾脂肪乳,其体外释放具有显著的缓释作用。     

羟基喜树碱脂肪乳与市售注射液在家兔肝脏中分布的比较

目的考察羟基喜树碱（HCPT）自制脂肪乳和市售注射液静脉推注给药后,药物在家兔肝脏的分布。方法采用2步乳化法制备HCPT脂肪乳,静脉推注自制脂肪乳和市售注射液,采用HPLC法测定家兔肝脏药物含量。结果与市售注射液相比,给药0.5、1、3、4h后自制脂肪乳在肝脏中药物的浓度分别提高了3.0、3.4、7.1、8.4倍。结论以脂肪乳作为药物载体大幅度提高了羟基喜树碱在肝脏中的分布。     

口服载药纳米粒的研究进展

综述近年来口服载药纳米粒的有关研究进展，着重从制备方法、表面修饰、药物释放及应用几个方面进行介绍。作为一种新型给药系统，纳米粒在口服给药方面具有广阔的开发及应用前景。     

载药金纳米粒的研究进展

近年来,作为一种新型药物递送系统,金纳米粒已引起了广泛关注。由于其特殊的物理化学性质,能与多种类型药物发生相互作用,如蛋白质、核酸、小分子药物等,从而可应用于肿瘤治疗和检测。笔者对载药金纳米粒的制备方法、载药方式和安全性等问题进行综述。     

药用静脉注射乳剂的研究进展

目的:介绍药用静脉注射乳剂的种类和主要作用,重点介绍药物的种类、作用特点及开发动态。方法:以国内外相关文献为基础进行分析和归纳。结果:药用静脉注射乳剂提高了药物的靶向性和缓释作用,增加了脂肪乳剂的应用范围。结论:药用静脉注射乳剂具有重要的实用价值和应用前景。     

对静脉注射脂肪乳剂质量影响因素的探讨

通过查阅国内外相关文献,对近几年静脉注射脂肪乳制剂学方面的研究进行分析综合,为静脉注射脂肪乳的工艺研究提供参考.结果表明静脉注射脂肪乳是一些水溶性差的药物的良好载体,用不同处方和方法制备而成的乳剂在制剂质量上有较大差别.影响其制剂质量的因素主要有处方组成和制备方法.     

脂肪乳剂的临床应用进展

脂肪乳剂是肠外营养液中非蛋白能源之一,不仅能提供热能和必需脂肪酸,还能维持细胞结构和功能,影响机体免疫功能,有助于疾病康复。不同脂肪乳剂不同的代谢特点决定了其在临床的不同应用。本文对脂肪乳剂的临床应用进展作一综述。     

Sodium bicarbonate reverts electrophysiologic cardiotoxicity of ropivacaine faster than lipid emulsions in a porcine model

Ropivacaine has been described as a safer local anaesthetic (LA); however, serious cardiotoxic accidents have been reported. Intravenous-lipid-emulsion (ILE) therapy during LA intoxication seems to act as an antidote. Sodium bicarbonate is the standard treatment for sodium channel blocker drug toxicity. We compared both antidotes on the reversion of electrophysiologic toxicity induced by ropivacaine. Ropivacaine 5 mg kg⁻¹ was administered in 24 pigs, and 3 min later, the animals received ILE: 1.5 ml kg⁻¹ + 0.25 ml kg⁻¹ min⁻¹ (ILE group); sodium bicarbonate: 2 mEq kg⁻¹ + 1 mEq kg⁻¹ h⁻¹ (NaHCO₃ group); saline solution (CTL group). Electrophysiological parameters were evaluated for 30 min. The area under the curve (AUC) for the first 5 or 30 min was compared between groups. Ropivacaine induced a lengthening of the PR interval by 17% (P = 0.0001), His-ventricle-interval by 58% (P = 0.001), sinus QRS complex by 56% (P = 0.0001), paced QRS at 150 bpm by 257% (P = 0.0001), and at 120 bpm by 143% (P = 0.0001) in all groups. At 5 min after treatment, sinus QRS in the NaHCO₃ group was shorter than that in the CTL group (AUC_QRS5, P = 0.003) or ILE group (AUC_QRS5, P = 0.045). During the first minute, seven of the animals in the NaHCO₃ group vs. two in the ILE or 0 in the CTL group recovered more than 30% of the sinus QRS previously lengthened by ropivacaine (P = 0.003). Sodium bicarbonate reversed the electrophysiological toxicity of ropivacaine faster than ILE and control groups.     

Cationic lipid emulsions as potential bioadhesive carriers for ophthalmic delivery of palmatine

Palmatine (PM) is a potent anti-infective agent used to treat eye diseases. However, PM is less effective for ocular application due to short residence time within the eyes. This study aimed to develop a cationic lipid emulsions (CLEs) for ophthalmic delivery of PM and evaluate its suitability in infection treatment. PM-loaded CLEs (PM-CLEs) were prepared through emulsifying/high-pressure homogenisation and characterised by particle size, ζ potential and morphology. The resulting PM-CLEs possessed a particle size of 192?nm and ζ potential of 45?mV around. In vitro release illustrated that PM was released less from CLEs. Corneal bioadhesion test showed that PM-CLEs exhibited an enhanced ocular residence time. Improved anti-infective activity was achieved in the model of fungus-induced keratitis. Furthermore, PM-CLEs demonstrated predominant cellular uptake and internalisation in the corneal epithelial cells. These results provide proof of concept that CLEs are promising bioadhesive carriers for ophthalmic delivery of PM.     

人参皂苷C-K静脉乳剂的制备及理化性质考察

目的研究人参皂苷C K静脉乳剂的处方及制备工艺 ,并对其理化性质进行考察。方法以人参皂苷C K为原料 ,以精制豆磷脂为乳化剂 ,加入适量的辅助乳化剂、稳定剂 ,用正交实验法优化乳剂的处方及工艺 ;用加速实验法考察乳剂的理化性质。结果制备的乳剂符合《中华人民共和国药典》对静脉乳剂的要求 ,经过影响因素试验确定了乳剂的储存条件。结论制备的乳剂性质稳定 ,为乳剂的进一步开发奠定了基础     

聚α-氰基丙烯酸丁酯载药纳米微粒的研究进展

目的：对作为药物载体的聚α-氰基丙烯酸丁酯的研究进展进行综述，就其制备工艺、体外释药和体内分布、毒理学和稳定性等作一介绍。方法：查阅聚α-氰基丙烯酸丁酯作为载药毫微粒的国内外文献。结果：聚α-氰基丙烯酸丁酯作为药物载体具有生物利用度高、释药速率可控、靶向性，能够改变药物体内分布等优点。结论：聚α-氰基丙烯酸丁酯作为药物载体具有广阔的应用前景。     

Preparation of solid lipid nanoparticles from W/O/W emulsions: Preliminary studies on insulin encapsulation

Abstract

A method to produce solid lipid nanoparticles (SLN) from W/O/W multiple emulsions was developed applying the solvent-in-water emulsion-diffusion technique. Insulin was chosen as hydrophilic peptide drug to be dissolved in the acidic inner aqueous phase of multiple emulsions and to be consequently carried in SLN. Several partially water-miscible solvents with low toxicity were screened in order to optimize emulsions and SLN composition, after assessing that insulin did not undergo any chemical modification in the presence of the different solvents and under the production process conditions. SLN of spherical shape and with mean diameters in the 600–1200 nm range were obtained by simple water dilution of the W/O/W emulsion. Best results, in terms of SLN mean diameter and encapsulation efficiencies, were obtained using glyceryl monostearate as lipid matrix, butyl lactate as a solvent, and soy lecithin and Pluronic®F68 as surfactants. Encapsulation efficiencies up to 40% of the loaded amount were obtained, owing to the actual multiplicity of the system; the use of multiple emulsion-derived SLN can be considered a useful strategy to encapsulate a hydrophilic drug in a lipid matrix.     

脂肪乳剂用于亲脂类药物毒性救治的研究进展

长效局部麻醉药等亲脂类药物过量使用可导致心跳骤停,且肾上腺素等药物复苏成功率低。脂肪乳剂作为肠外营养在临床应用已有近50年的历史。近年发现脂肪乳剂还可用于治疗亲脂类局部麻醉药物所致的心脏毒性,但其确切机制尚不明确。今后应更深入地阐明其确切机制,并确立治疗标准。