纤维素肠溶包衣材料的应用

纤维素类聚合物是非常重要的药用辅料。本文介绍了近年来纤维素类肠溶包衣材料的研究概况,包括其结构、理化性质、合成策略以及在包衣中的简单和特殊应用,并介绍了一种新的包衣方法－干法包衣。     

肠溶包衣材料在药物制剂中的应用

肠溶包衣材料在国内外发展很快,应用广泛,常见的有：虫胶,苯二甲酸醛酸纤维素,海藻胶,聚乙烯醇醋酸苯二甲酸酯,丙烯酸树脂,羟丙基甲基纤维素酞酸酯等,其中,甲基丙烯酸甲酯（MMA）,甲基丙烯酸（MAA）和丙烯酸丁醋（BA）的三元共聚物及一种新型包衣材料欧巴代在药物剂中展示了广阔的前景。     

乙基纤维素水性包衣技术I.水分散体与有机溶液包衣方法的比较

考察了乙基纤维素水分散体的基础性质,测定ＰＨ值、粘度、最低成膜温度、玻璃化转变温度,进行了处方相容性试验。以盐酸苯丙酸胺为模型工物,在流化床中蛊缓释微丸,考察在纤维素水分菜体的包衣应用特点,并与有机溶液包衣方法在缓释效果,增塑剂用量、包衣喷液方式的影响三方面进行比较。考察了水分菜体包衣微丸的稳定性,采用相似因子法评价微丸的体外释放度变化。     

几种包衣材料在红霉素肠溶片包衣中的应用

本文对邻苯二甲酸醋酸纤维素(CAP)、丙烯酸树脂、羟丙基甲基纤维素酞酸酯(HPMCP)等几种常见肠溶包衣材料在红霉素肠溶片包衣中的应用进行了综述,提出采用水性HPMCP纳米微粒进行片剂肠溶包衣,具有广阔的应用前景.     

肠溶包衣材料丙烯酸树脂水分散体的制备

目的:制备肠溶包衣材料甲基丙烯酸-丙烯酸乙酯水分散体.方法:通过单因素考察法确定最佳制备工艺.结果:最佳工艺为:聚合温度为75～80℃,在聚合过程中缓慢滴加单体的加料方式,使用复配乳化剂SDS及吐温80,0.3％的引发剂过硫酸铵,0.65％的分子量调节剂十二烷基硫醇.结论:根据最佳工艺制备的丙烯酸树脂符合药典规定,性能...     

乙基纤维素水性包衣技术的研究

水性包衣技术具有许多优点,它克服了有机溶媒包衣的诸多缺陷,而乙基纤维素是广泛用于固体制剂包衣的水学溶性聚合物之一。本文以市售乙基纤维素水性我衣产品－－Ａｑｕａｃｏａｔ及Ｓｕｒｅｌｅａｓｅ为例,综述了水性包衣的制备、组成、特点,应用以及成膜机理。     

用正交设计法研究肠溶衣片的包衣工艺条件

本文用正交设计法研究了温度、材料用量及包衣速度三因素,对肠溶衣片崩解时限的影响。在本实验条件下(一次包衣数量为20万片,平均片重为0.2g)制备的肠溶衣片其最佳工艺条件为:热风温度20℃、包衣材料用量135ml/万片、包衣速度100ml/min。     

美进行薄荷油肠溶包衣胶囊治疗儿童过敏性肠综合征的首次临床研究

美国医生 Kline 等去年用薄荷油肠溶包衣胶囊(Colpermin~(TM),含薄荷油0.1 mL,约187 mg;瑞士 Tillotts Pharma 制造)对42名8～17岁的过敏性肠综合征(IBS)患儿进行了随机、双盲、安慰剂对照的临床研究,疗程2周。体重45 kg 以上者每次2粒,每日3次;体重30～45 kg 者每次1粒,每日3次。治疗结果用胃肠道症状等级量表(GSRS,有15     

羟丙基甲基纤维素酞酸酯假胶乳的制备及应用于消炎痛肠溶包衣片的质量评价

实验制备了肠溶辅料羟丙基甲基纤维素酞酸酯（ＨＰＭＣＰ）假胶乳水性分散液，并以消炎痛片为底物，分别采用ＨＰＭＣＰ假胶乳及ＨＰＭＣＰ有机溶媒包衣液制备其肠溶薄膜包衣片。考察并比较了两种包衣系统的消炎痛包衣片的崩解时限、抗胃液性能及在人工肠液中的释药动力学。实验结果表明：两种包衣系统均能使包衣片产生良好的肠溶性；包衣片在人工胃液中的药物泄漏率均符合ＵＳＰⅩⅫ要求；经统计学检验两种包衣系统的不同包衣水平间的体外累积释药Ｔｄ值，均无显著性差异（Ｐ＞０．５），说明在一定包衣增重范围内，衣膜对包衣片释药速度影响不大。     

氧化苦参碱肠溶包衣微丸的制备

目的:制备氧化苦参碱肠溶包衣微丸。方法:采用单因素试验考察包衣锅转速、包衣锅温度和喷枪压力对包衣条件的影响,并比较各种树脂包衣液的性质,选出适宜的包衣材料;采用包衣锅法制备微丸;以体外释放度评价包衣效果。结果:包衣条件为包衣锅转速50r.min-1、包衣温度30℃、喷枪压力0.10MPa;包衣材料为湖州Ⅲ号聚丙烯酸树脂;制备的微丸体外释放度符合2005年版《中国药典》(二部)要求。结论:所选方法可制备出体外释放良好的氧化苦参碱肠溶包衣微丸。     

Development and in vitro Evaluation of Enteric Coated Multiparticulate System for Resistant Tuberculosis

The multiparticulate formulation of sodium para aminosalicylate for oral administration was developed by extrusion spheronization technique. Microcrystalline cellulose was used as filler in concentration of 14.4% w/w. Pellets were coated with Eudragit L 30 D-55 using fluidized bed processor. Different weight gains of acrylic polymer were applied onto the pellets and evaluated for in vitro dissolution behavior in 0.1 N HCl for two hours and then media was changed to phosphate buffer pH 6.8. A 60% w/w coating level of Eudragit L30 D 55 has produced the most acceptable results against the gastric attack. 3% Seal coat of HPMC E5 was also applied in order to protect the drug from migration into the Eudragit coat and film coat was applied in order to prevent aggregation of pellets in the dissolution media. Morphological characteristics of developed pellets were also investigated by scanning electron microscopy and found to be smooth and spherical. Developed system was found to be suitable for the delivery of Sod PAS in to intestinal region.     

Thiolated Polymers: Development and Evaluation of Transdermal Delivery Systems for Progesterone

Purpose. To evaluate the possible use of polycarbophil-cysteine (PCP-Cys) as polymeric matrix for transdermal progesterone application. Methods. Thiolated polycarbophil was synthesised by the covalent attachment of cysteine to the basis polymer. The adhesive properties of PCP-Cys in comparison to polyvinylpyrrolidone/hydroxypropyl- methylcellulose (PVP/HPMC) and polyvinylpyrrolidone/polyvinyl- alcohol (PVP/PVA) were investigated by testing the total work of adhesion (TWA) on porcine skin. Release studies in Franz diffusion cells and standard in vitro permeation experiments with porcine skin were performed analysing the progesterone content by high-per- formance liquid chromatography.Results. Films based on PCP-Cys displayed very high cohesive properties due to the formation of interchain disulfide bonds. The TWA of the thiolated polymer on porcine skin was significantly (P <0.05) the highest. In addition progesterone permeation was also the highest from PCP-Cys compared with PVP/HPMC and PVP/PVA within 24 hours. Conclusion. PCP-Cys—a partly thiolated polymer—might be a novel polymer matrix for transdermal progesterone delivery with excellent adhesiveness on porcine skin.     

Moisture Sorption by Polymeric Excipients Commonly Used in Amorphous Solid Dispersions and its Effect on Glass Transition Temperature: II. Cellulosic Polymers

Moisture sorption by polymeric carriers used for the development of amorphous solid dispersions (ASDs) plays a critical role in the physical stability of dispersed drugs since moisture may decrease glass transition temperature (T_g) and thereby increase molecular mobility of drugs leading to their crystallization. To assist the selection of appropriate polymers for ASDs, we conducted moisture sorption by five types of cellulosic polymers, namely, hydroxypropyl cellulose (HPC), hydroxypropyl methyl cellulose (HPMC), hydroxypropyl methyl cellulose acetate succinate (HPMCAS), hydroxypropyl methyl cellulose phthalate (HPMCP), and ethyl cellulose (EC), as functions of relative humidity (10 to 90% RH) and temperature (25 and 40 °C). The moisture sorption was in the order of HPC>HPMC>HPMCP>HPMCAS>EC, and there was no significant effect of the molecular weights of polymers on moisture uptake. There was also less moisture sorption at 40 °C than that at 25 °C. Glass transition temperatures (T_g) of the polymers decreased with the increase in moisture content. However, the plasticizing effect by moisture on HPC could not be determined fully since, despite being amorphous, there were very little baseline shifts in DSC scans. There was also very shallow baseline shift for HPMC at >1% moisture content. In contrast, T_g of HPMCAS and HPMCP decreased in general agreement with the Gordon-Taylor/Kelley-Bueche equation, and EC was semicrystalline having both T_g and melting endotherm, with only minor effect of moisture on T_g. The results of the present investigation would lead to a systematic selection of polymeric carriers for ASDs.     

Enteric microsphere formulations of papain for oral delivery

Enteric microspheres formulations of papain were prepared by w/o/w emulsion solvent evaporation using hydroxypropyl methylcellulose phthalate (HPMCP), Eudragit L 100 and Eudragit S 100, to avoid gastric inactivation of papain. Smaller internal and external aqueous phase volume provided maximum encapsulation efficiency (74.49-79.76%), least particle size (52.4-60.2 μm) and 21-26% loss of enzyme activity. Release studies in 0.1 N HCl confirmed the gastro-resistance of formulations. The anionic microspheres, zeta potential between -18.21 and -20.06 mV, aggregated in 0.1 N HCl (i.e., gastric pH 1.2), due to protonation of carboxylic groups of enteric polymer and loss of surface charge with subsequent change in zeta potential. The aggregates being <500 μm size would not impede gastric emptying. However, at pH>5.0 (duodenal pH) the microspheres showed de-aggregation due to restoration of surface charge. HPMCP and Eudragit L 100 microspheres facilitated almost complete release of papain within an hour at pH 6.0 and 6.8, respectively while Eudragit S 100 microspheres released 84.56% papain at pH 7.4, following Higuchi kinetics. FTIR spectroscopy revealed entrapment of enzyme; PXRD & DSC indicated amorphous character and SEM showed spherical shape of microspheres. In simulated gastro-intestinal pH condition, HPMCP, Eudragit L 100 and Eudragit S 100 microspheres showed good digestion of paneer and milk protein. Thus, enteric microspheres formulations could serve as potential carrier for oral enzyme delivery. Stability studies indicated the formulations with around 5% overage would ensure 2 years shelf life at room temperature.     

聚丙烯酸树脂肠溶胶囊壳的制备

目的 寻找明胶替代材料作为囊材,制备肠溶胶囊壳,并对其做出制剂学评价.方法 考察Eudragit L100-55成膜性能,以其作为囊材,使用蘸胶-成膜法制备胶囊壳,采用对乙酰氨基酚作为模型药物,考察体外释放.结果 获得了制备胶囊壳的最佳处方,制备所得肠溶胶囊壳符合药典要求.结论 Eudragit L100-55可以作为明胶的替代囊材制备胶囊壳,其体外释放满足肠溶胶囊要求.     

Enteric diseases of homosexual men

Certain enteric ailments are particularly common among homosexual men. They are primarily infectious diseases and include not only such common venereal diseases as gonorrhea and syphilis but also infections not usually regarded as being sexually transmitted. Among the latter are shigellosis, salmonellosis, giardiasis, and amebiasis. Patients' symptoms are non-specific and seldom helpful in diagnosing particular diseases. The practitioner must be prepared to identify a number of infections with similar presentations that may occur singly or together in gay men. Gonorrhea is probably the most common bacterial infection in gay men. Carriage rates as high as 50% have been reported, and extra-genital carriage is common; this necessitates culturing the urethra, rectum, and pharynx. Procaine penicillin G is the treatment of choice for most patients; spectinomycin is probably the drug of choice in penicillin-sensitive patients. In contrast to other venereal diseases, syphilis may have a characteristic protoscopic presentation. Benzathine penicillin G is the treatment of choice for most patients. Lymphogranuloma venereum causes penile lesions and inguinal lymphadenitis in heterosexual men, whereas homosexual men are more prone to proctitis. The disease may mimic Crohn's disease. Recommended treatment includes tetracycline or sulfamethoxazole-trimethoprim. Shigellosis usually presents as an acute diarrheal illness. Patients generally require only supportive treatment with fluids. Herpes simplex viral infection is difficult to diagnose and has several different presentations, including lumbosacral radiculomyelopathy. Symptomatic treatment with sitz baths, anesthetic ointment, and analgesics is recommended. Venereal warts are believed to be caused by the same virus that causes verrucous warts; they are usually found in the anal canal or around the anal orifice. They are commonly treated with 25% podophyllin solution. Parasitic infections include giardiasis, amebiasis, and pinworm infections. Metronidazole may be used in the treatment of symptomatic giardiasis and amebiasis, but it is not approved for the former indication; quinacrine is approved for giardiasis. Pinworm infestation may be treated with pyrantel pamoate or mebendazole. Cure of enteric diseases in homosexual men must be documented.     

红霉素肠溶微丸制备工艺

采用挤出—滚圆技术制备红霉素微丸丸芯，并用正交设计筛选其制备工艺；以甲基丙烯酸共聚物水分散体为包衣材料，建立微丸包衣数学模型指导包衣工艺。