美洲大蠊提取物胃漂浮缓释片制备研究

以假酸浆子胶质为片剂辅料制备美洲大蠊提取物胃漂浮缓释片。在单因素试验的基础上,以美洲大蠊提取物胃漂浮缓释片中尿嘧啶体外释放百分率为评价指标进行正交试验优化美洲大蠊提取物胃漂浮缓释片处方。优化处方为美洲大蠊提取物10 g,羟丙甲基纤维素K100M 22 g,假酸浆子胶质冻干品4 g,十八醇12 g,乙基纤维素12 g, 1%硬脂酸镁。应用假酸浆子胶质制备的美洲大蠊提取物胃漂浮缓释片制备方法简单可行。     

壳聚糖接枝共聚物的应用研究

以壳聚糖与甲基丙烯酸接枝共聚物为载体,采用直接压片法制得药物非诺落芬钙的缓释片剂.测定了缓释片剂中的非诺落芬钙的体外溶出速率,用红外光谱(FT-IR)表征了缓释片剂中非诺落芬钙与接枝共聚物形成的分子间氢键.     

壳聚糖辐射接枝MAA共聚物的制备及应用

利用辐射源^60Co辐照壳聚糖(chitosan)与甲基丙烯酸(MAA)接枝聚合反应,合成的共聚物可以作为药物非诺洛芬钙缓释制剂的载体。本文研究了壳聚糖与甲基丙烯酸不同配比、不同辐照剂量对接枝聚合产物性能的影响。用红外光谱仪(FTIR)表征了接枝聚合产物,并以接枝聚合物为载体制备了药物非诺洛芬钙缓释片剂。通过测定药物片剂的非诺洛芬钙在人工肠液的缓释速率,表明药物片剂的非诺洛芬钙有缓释作用。     

壳降糖接枝共聚物的应用研究

以壳聚糖与甲基丙烯酸接枝共聚物为载体，采用直接压片法制得药物非诺落芬钙的缓释片剂。测定了绥释片剂中的非诺落芬钙的上溶出速率，用红外光谱（ＦＴ－ＩＲ）表征了缓释片剂中非诺落芬钙与接枝共聚物形成的分子同氢链。     

头孢克洛缓释片处方开发及释放度一致性研究

头孢克洛属于第二代口服头孢类抗生素,1976年由美国礼来公司研制开发,目前国内外已开发出本品的片剂、胶囊剂、颗粒剂、干混悬剂以及缓释、复方等多种规格和给药形式,根据市场调研及问卷分析,本文选择开发服用次数少,临床反映良好的头孢克洛缓释片进行研究。以原研单位的希刻劳头孢克洛缓释片Ⅱ为参比,本文进行了系统的处方工艺研究,对处方进行重新开发,检测释放度,进行体外释药相似性评价,旨在提升产品质量,达到与参比制剂的质量和疗效的一致性。     

酸化凹凸棒石/海藻酸复合材料的制备及其缓释性能

以海藻酸钠 (SA) 和酸化凹凸棒石 (H⁺-ATP) 为原料,运用溶液共混法制备了一种具有优良缓释性能的复合材料,并以其为基质材料制备了双氯芬酸钠 (DS) 缓释片.利用SEM、FTIR和XRD对复合材料形貌和结构进行了表征,考察了酸改性剂浓度、H⁺-ATP用量和复合时间对复合材料缓释性能的影响,以获得最佳复合工艺.结果表明,当用12 mol·L^-1盐酸酸化的ATP量占复合物总量60%时,复合缓释片在体外模拟肠液中缓释性能最佳.与单一海藻酸缓释片相比,复合缓释片2 h的累积释放率由42.6%下降到23.7%,有效改善了"突释"效应.释放动力学研究表明,复合缓释片的释药行为可以用Ritger-Peppas方程很好地拟合,释药速率受骨架溶蚀和药物扩散双重控制.H⁺-ATP的加入显著改善了海藻酸的缓释性能.     

壳聚糖缓释体系研究进展

综述了壳聚糖在缓释系统方面的最新研究进展。包括壳聚糖衍生物缓释体系的研究、壳聚糖缓释体系在医药系统的应用和吸附-控释复合体系的研究,重点介绍了壳聚糖衍生物缓释体系的研究,壳聚糖衍生物缓释体系分为壳聚糖衍生物缓释微球、壳聚糖纳米粒、壳聚糖缓释片、壳聚糖缓释微囊、壳聚糖缓释膜和壳聚糖水凝胶缓释体的研究等六个部分。壳聚糖缓释体系作为一项新技术在医药体系具有广泛的应用前景。     

缓释胸腺肽口服片剂的制备及免疫调节作用

目的制备缓释胸腺肽口服片剂,并探讨其生物学活性及对小鼠免疫功能的影响。方法采用常规方法制备缓释胸腺肽片剂。以E-玫瑰花环试验及淋巴细胞转化试验,评价其生物学活性;免疫小鼠,以乳酸脱氢酶释放法检测小鼠NK细胞活性;巨噬细胞吞噬功能试验检测小鼠腹腔巨噬细胞的吞噬率;流式细胞仪检测T淋巴细胞亚群。结果所制备的缓释胸腺肽口服片剂,各项质量检测指标均达到《中国药典》三部(2005版)要求,其释药过程无突释和释药峰。缓释片剂组的E-玫瑰花结形成率及淋巴细胞转化率明显高于空白基质片组,且差异有显著意义;NK细胞活性、巨噬细胞吞噬率及CD3~+、CD4~+、CD4~+/CD8~+比值与空白基质片组相比,差异均有显著意义。结论缓释胸腺肽口服片剂具有良好的生物学活性,并对小鼠免疫调节功能有明显的增强作用。     

吡虫啉片剂壁材对缓释速率的影响及其防治白粉虱效果分析

[目的]探讨囊化壁材对吡虫啉缓释片剂缓释速率的影响。[方法]经机械搅拌、化学交联、烘干、造粒、压片等工艺措施,分别以淀粉和β-环糊精为壁材制备了2种缓释剂片剂CS(淀粉为壁材)和CD(β-环糊精为壁材)。采用温室防效、模拟土壤pH值以及片剂对番茄植株生长的影响等试验。[结果]明确了最佳施用方式为在定植时用在植株根部正下方6 cm深度范围,最适土壤pH值为7;片剂CS和CD在第90天对白粉虱防效分别为90%和64%,对煤污病防效在107 d分别为96.8%和92.7%;在相应剂量内对植株生长有明显促进作用。[结论]CS片剂较CD片剂持效期长且缓释速率慢而均匀,以淀粉作为缓释壁材较好。     

固体分散体法制备氢溴酸右美沙芬缓释片及体外释放度研究

目的:应用固体分散体技术制备氢溴酸右美沙芬缓释粉末,与适合辅料混合、压片,并对其性质进行考察。方法:用固体分散技术制备了氢溴酸右美沙芬缓释粉末,采用单因素考察筛选最优处方和工艺条件,再与适合辅料混合压片,考察了缓释粉末的粉体学性质及压片后的体外释放情况。结果:制得的氢溴酸右美沙芬缓释片外观整洁,片面光滑,收率较高,体外释放较理想。结论:该法制备工艺简单易行,重复性好,采用适当的工艺,制得的氢溴酸右美沙芬缓释片具备较理想的缓释特征。     

The Preparation of Capsaicin-Chitosan Microspheres (CCMS) Enteric Coated Tablets

This study aimed to research the preparation and content determination of capsaicin-chitosan microspheres (CCMS) enteric coated tablets. The core tablets were prepared with the method of wet granulation. Nine formulae were designed to determine the optimal formula of the core tablet. Eudragit L100 was used to prepare the CCMS enteric-coated tablets. The effect of enteric coated formulation variables such as content of talc (10%, 25% and 40%), plasticisers (TEC and DBS), dosage of plasticiser (10%, 20% and 30%) and coating weight (2%, 3% and 5%) were evaluated for drug release characteristics. The in vitro release was studied using 0.1 N HCl and pH 6.8 phosphate buffer. Enteric coated tablets without ruptures or swelling behaviour over 2 h in 0.1 N HCl indicated that these tablets showed acid resistance. The accumulated release rate in phosphate buffer (pH 6.8) revealed that the prepared tablets were able to sustain drug release into the intestine and a first-order release was obtained for capsaicin. This research is the first report of the preparation and content determination of CCMS enteric coated tablets. The sustained release behavior of enteric coated formulations in pH 6.8 phosphate buffer demonstrated that it would be a potential drug delivery platform for sustained delivery of gastric irritant drugs.     

盐酸二甲双胍胃漂浮缓释制剂的制备与释药过程研究

采用湿法制粒压片制备了盐酸二甲双胍胃漂浮缓释片。片剂具有良好的漂浮特性 ,药物释放可延长至 8h以上。片剂的漂浮迟滞时间随羟丙甲基纤维素质量分数的增加而降低 ,片剂密度与十八醇质量分数的关系为 :ρ =1 1 4 6 - 1 2 1 2w。采用单层桨网法对片剂的体外释放实验结果表明 ,药物的体外释放动力学符合 :Q =S[DPCP(2C0 -CP)t] 1 / 2,药物通过扩散和骨架溶蚀共同作用进行释放     

Effect of Polymer Concentration on the Dissolution Rates of Pioglitazone Hydrochloride

An emulsion of pioglitazone hydrochloride (drug) was prepared by mixing drug:polymer (gelatin) in different ratios of 1:0.5, 1:1, and 1:1.5 (wt/wt), respectively. These emulsions were used for the preparation of tablets of different composition. Tablet hardness increased with a decrease in concentration of polymer, while the percentage friability increased with an increase in polymer concentration in the tablet. The encapsulated tablet showed better sustained release than conventional tablets. The effect of concentration of polymer on dissolution rates of these tablets was studied using the Hixson-Crowell cube root law equation. The data obtained prove that the formulations are useful for a sustained release of pioglitazone hydrochloride, since the percentage released after 24 h was nearly 76%. The release of pioglitazone hydrochloride was influenced by the presence of polymer and different compositions of lactose. The tablet containing an emulsion of ratio 1:0.5 showed an excellent result of rate constant, better than conventional and other compositions.     

浅谈现代农药剂型进展

本文简述了国内外现代农药剂型的研究进展,对悬浮剂、缓释剂、微乳剂、片剂、水分散粒刺等剂型的发展动态进行了初步讨论。     

Effect of Polymer Concentration on Sustained Release Microparticles of Metformin Hydrochloride Prepared by Using Spray Dryer

Metformin hydrochloride, polyacrylic acid and β-cyclodextrin were taken for the preparation of spray dried sustained released micro particles in a different ratios. These sustained release micro particles were used for the preparation of tablets. Hardness of tablet increases with increase in concentration of polymer while the percentage friability decreases with increase in polymer concentration in tablet. The encapsulated drug shows better sustained release than the conventional tablet. The kinetics of the dissolution process were studied by analyzing the dissolution data using three kinetic equations—the zero-order equation, the first-order equation and the Hixson–Crowell cube root law equation.     

The Manufacture and Characterization of Casein Films as Novel Tablet Coatings

The use of casein as a novel film-forming agent, capable of functioning as a pharmaceutical tablet coat, was assessed. Diltiazem HCl core tablets were coated with casein using a pan coater and the efficacy of four different plasticizing agents (glycerol, triethyl citrate, dibutyl sebacate and oleic acid) in producing a continuous tablet-coat were evaluated. Interestingly, only those films formed using oleic acid as a plasticizing agent were capable of producing a continuous, acceptable coat. Consequently, the drug dissolution properties of casein/oleic acid film-coated tablets in pH 1.2 and pH 6.8 media were further investigated. Post-coating thermal treatment (60, 80 and 100°C) was shown to have a significant effect on the properties of the casein-oleic acid films. Diltiazem HCl drug release at pH 1.2 was found to decrease with increasing post-coating heat treatment temperature. Additionally, only coated tablets that were subjected to post-coating heat treatment at 100°C showed sustained drug release properties at pH 6.8, which may be attributed to casein cross-linking.     

医药剂型在农药中的应用及发展趋向

医药剂型与农药剂犁有许多相通的地方,许多医药剂型已经渗入到农药领域并得到了成功的应用.综述了新剂型及新技术在医药和农药中的应用情况及发展趋向,主要介绍了医药缓控释制剂、片剂、水乳剂、微乳剂以及混悬剂(悬浮剂)在农药中的应用,并对医药新制剂中的分散片、速溶片及渗透泵片在农药领域的应用做了展望,同时指出需审慎对待微乳剂等农药纳米制剂的研发和审批.     

Investigation of the impact of insoluble diluents on the compression and release properties of matrix based sustained release tablets

In the present study the effect of insoluble diluents such as microcrystalline cellulose (MCC) and dibasic calcium phosphate (DCP) on the compression characteristics and release profile of sustained release tablets containing Hydroxypropylmethylcellulose (HPMC) matrices was investigated. The effect of diluents on the compression characteristics was studied using Heckel and Kawakita equations. The effect of compression forces on the release profile was also investigated. Diclofenac Sodium (DS) was used as a model drug. Tablets were prepared using wet granulation method. It was found that there is a decrease in the drug release as the concentration of these insoluble diluents is increased. From the Heckel and Kawakita analysis it was concluded that the compressed granules of formulations containing microcrystalline cellulose showed higher plastic deformation, densification and granule fragmentation as compared to DCP. Also a relationship was evaluated between the compression force and the release profile i.e. an increase in compression force causes decrease in the release rate of the drug from the formulation irrespective of change in the diluent.     

新型不饱和聚酯基亲水性药物缓释材料的制备

采用本体熔融聚合方法,以三羟甲基丙烷二烯丙基醚（TMPDE）对不饱和聚酯酰胺脲树脂进行封端,得到了一种药物缓释载体的亲水性预聚物,以盐酸环丙沙星为模型药物,制备了盐酸环丙沙星-不饱和聚酯酰胺脲树脂药片。研究了尿素含量和饱和二元酸对材料降解性能和亲水性的影响。体外降解和药物释放（37℃,pH 7.4 PBS缓冲溶液）结果表明,该空白材料的降解速率可通过改变尿素含量来调节;缓释药片释药平稳,持续释药时间可达30 d。