含油中药浸膏片赋形剂的筛选

目的筛选含油中药浸膏片赋形剂。方法以外观、硬度、崩解度、脆碎度等为指标评价赋形剂对片剂成型性的影响。结果稀释剂选用糖粉，吸收剂选用辅料X，粘合剂选用微晶纤维素，崩解剂选用低取代羟丙基纤维素片剂成型性好。结论以上赋形剂适合于该片剂。     

正交试验法优化消旋山莨菪碱片生产工艺

目的优化消旋山莨菪碱片工艺。方法采用正交试验设计，考察淀粉、糊精、微晶纤维素、蔗糖的比例对消旋山莨菪碱片的硬度、崩解时限等质量指标的影响。结果当微晶纤维素、糊精、蔗糖、淀粉的比例为12：5：36：37时，消旋山莨菪碱片的崩解时限、脆碎度可满足产品质量标准要求。结论新处方辅料比例恰当，产品质量稳定，适合批量生产。     

呋喃妥因HPMCP包衣片质量及人体生物利用度研究

本文采用新研制开发的肠溶辅料羟丙基甲基纤维素酞酸酯（ＨＰＭＣＰ）将呋喃妥因制成肠溶薄膜衣片，实验考察了包衣片剂质量及用尿药法测定了其了其人体生物利用度，并与呋喃妥因市售片及丙烯酸树肠溶衣片进行了比较。体外质量考察结果表明，ＨＰＭＣＰ包衣片硬度及脆碎度与二种对照片相当；ＨＰＭＣＰ包衣片及丙烯酸树脂包衣片的崩解时限分别为２．４９±０．２１）ｍｉｎ和（７．４９±１．１７）ｍｉｎ，其溶出度参数Ｔ５０则分别     

盐酸氨溴索口腔崩解片的研制

目的:设计制备氨溴索口腔崩解片.方法:采用正交设计,根据口腔崩解片的特点选用不同辅料,考察各处方制备崩解片的溶出度和崩解时限.结果:最佳处方为:甘露醇10克,微晶纤维素 30 g,羟丙纤维素 8 g 和碳酸氢钠 1 g.结论:制备的氨溴索口腔崩解片崩解时限符合规定,口感良好,溶出速度明显优于普通片.     

布南色林分散片的处方研究

目的:采用正交试验筛选布南色林分散片的处方。方法:以内崩解剂微晶纤维素的用量、填充剂乳糖的用量、外崩解剂羧甲基淀粉钠的用量、黏合剂羟丙基甲基纤维素溶液的浓度为考查因素,以分散片的崩解时间、脆碎度和分散均匀性为评价指标进行正交试验,确定最佳处方;并对优化的处方进行工艺验证及质量评价。结果:优选处方为含微晶纤维素30%、乳糖50%、羧甲基淀粉钠0.5%,羟丙基甲基纤维素溶液浓度为2%;所制样品平均崩解时间为10.8s,脆碎度为0.29%,分散均匀性合格,30min药物累积溶出百分率超过75%。结论:布南色林分散片处方设计较为合理。     

替硝唑片粘合剂的筛选

目的筛选替硝唑片的粘合剂。方法分别采用8%聚乙烯吡咯烷酮(PVP-K30)、10%淀粉浆、40%糖浆和2.0%羟丙基甲基纤维素K4(HPMC-K4),50%乙醇作为替硝唑片的粘合剂,制成不同粘合剂配方的药片,观察素片的外观以及包衣后外观的变化,测定其硬度、脆碎度、崩解时限和溶出度。结果PVP-K30制成的片有光泽,测定脆碎度后有少许崩边缺角现象,包衣后片表面粗糙;淀粉浆制成的片有光泽,测定脆碎度后无崩边缺角现象,包衣后药片完整;糖浆制成的片较脆,测定脆碎度后有崩边、顶裂现象,包衣后片表面粗糙且有顶裂倾向;羟丙基甲基纤维素制成的片有光泽,振摇无崩边缺角现象,包衣后完整,外观好。结论用2.0%HPMC-K4、50%乙醇为粘合剂制备的药片外观好,在包薄膜衣过程中,不易出现崩边、缺角现象,包衣后片面美观,硬度、崩解度和溶出度也优于用其它粘合剂制成的片子。     

对乙酰氨基酚片脆碎度的研究

目的研究解决对乙酰氨基酚片的脆碎度问题。方法以脆碎度、崩解度、溶出度为指标,通过处方筛选确定优化的生产工艺。结果预胶化淀粉对对乙酰氨基酚片脆碎度的改善明显优于微晶纤维素、麦芽糊精。结论优化处方的预胶化淀粉能保证对乙酰氨基酚片的脆碎度等相关质量要求。     

预胶化淀粉在片剂产品中的应用

目的为了提高片剂产品的质量。方法采用国产预胶化淀粉作辅料制备红霉素片、地巴唑片 。结果其片的硬度、脆碎度、崩解时限、溶出度等均优于原处方制成的成品。结论预胶化淀粉是一种可广泛应用的片剂传统辅料的替代品。     

基于预混辅料的拉莫三嗪口腔崩解片的制备

目的由预混辅料入手,制备拉莫三嗪口腔崩解片。方法以异麦芽酮糖醇、微晶纤维素和交联聚维酮为主要辅料,使用湿法制粒的方法制备预混辅料,并测定了预混辅料产品的粉体学性质。选用拉莫三嗪为主药,与预混辅料及少量崩解剂、润滑剂和矫味剂,通过粉末直压的方法制备拉莫三嗪口腔崩解片,并对拉莫三嗪口腔崩解片进行基本的体外评价。结果通过单因素考察和正交试验,预混辅料的最终处方组成为:异麦芽酮糖醇与微晶纤维素的比例为3∶4,加入8%交联聚维酮。拉莫三嗪口腔崩解片的最优处方组成(按1 000片计)为:25 g拉莫三嗪,137 g预混辅料,14.4 g低取代羟丙基纤维素,1.8 g硬脂酸镁,1.8 g矫味剂。拉莫三嗪口腔崩解片的崩解时限为35 s,且在5 min内溶出完全。结论根据试验,制备的预混辅料的性质优良,口腔崩解片的崩解时限、口感和溶出度等均符合规定。     

呋喃妥因HPMCP包衣片质量及人体生物利用度研究

本文采用新研制开发的肠溶辅料羟丙基甲基纤维素酞酸酯（ＨＰＭＣＰ）将呋喃妥因制成肠溶薄膜衣片。实验考察了包衣片剂质量及用尿药法测定了其人体生物利用度，并与呋喃妥因市售片及丙烯酸树脂肠溶衣片进行了比较。体外质量考察结果表明，ＨＰＭＣＰ包衣片硬度及脆碎度与二种对照片相当；ＨＰＭＣＰ包衣片及丙烯酸树脂包衣片的崩解时限分别为（２．４９±０．２ｌ）ｍｉｎ和（７．４９±ｌ．１７）ｍｉｎ，其溶出度参数Ｔ５０则分别为１２ｍｉｎ和５２．８ｍｉｎ．体内尿药浓度测定结果，ＨＰＭＣＰ包衣片、市售片及丙烯酸树脂肠溶衣片尿药累积排泄百分数分别为３３．９％，２４．Ｏ％及２０．９％，说明前者生物利用度明显高于后二者。     

海仙灵胃片崩解时限研究

目的制备海仙灵胃片,缩短崩解时限,确保产品质量。方法采用正交试验,考察崩解剂、崩解剂用量（％）、干燥温度、干颗粒水份这四个因素对崩解时限影响,从而确定最后工艺。结果通过处方工艺优化,选用4％羧甲淀粉钠（CMS）,60℃干燥温度,3％～5％干颗粒水份时,崩解时限最佳。结论正交试验为缩短海仙灵胃片的崩解时限提供依据。     

Design, development, and optimization of orally disintegrating tablets of etoricoxib using vacuum-drying approach

Etoricoxib is a cyclooxygenase 2 (COX-2) inhibitor that selectively inhibits the COX-2 enzyme and decreases the incidences of side effects associated with these agents. It is commonly prescribed for acute pain, gouty arthritis, and rheumatoid arthritis. Conventional tablets of etoricoxib are not capable of rapid action, which is required for faster drug effect onset and immediate relief from pain. Thus, the aim of the present investigation is to formulate orally disintegrating tablets (ODTs) of etoricoxib. A combination of the superdisintegrants with a sublimation technique was used to prepare the tablets. Tablets were prepared using a direct compression method employing superdisintegrants such as low substituted hydroxylpropyl methyl cellulose (L-HPMC), low substituted hydroxyl-propyl cellulose (L-HPC), crospovidone, croscarmellose sodium, and sodium starch glycolate. Tablets of etoricoxib prepared using L-HPC exhibited the least friability and disintegration time (approximately 65 s). To decrease the disintegration time further, a sublimation technique was used along with the superdisintegrants for the preparation of ODTs. The use of sublimating agents including camphor, menthol, and thymol was explored. The addition of camphor lowered the disintegration time (approximately 30 s) further, but the percent friability was increased. A 3(2) full factorial design was employed to study the joint influence of the amount of superdisintegrant (L-HPC) and the amount of sublimating agent (camphor) on the percent of friability and the disintegration time. The results of multiple linear regression analysis revealed that for obtaining an effective ODT of etoricoxib, higher percentages of L-HPC and camphor should be used. Checkpoint batches were prepared to validate the evolved mathematical model. A response surface plot is also presented to graphically represent the effect of the independent variables on the percent of friability and the disintegration time. The approach using the optimization technique helped to produce a detailed understanding of the effects of formulation parameters.     

Formulation and evaluation of mouth dissolving tablets of cinnarizine

The purpose of this research was to develop mouth dissolve tablets of cinnarizine by effervescent, superdisintegrant addition and sublimation methods. All the three formulations were evaluated for disintegration time, hardness and friability, among these superdisintegrant addition method showed lowest disintegration time; hence it was selected for further studies. Further nine batches (B1-B9) were prepared by using crospovidone, croscarmellose sodium and L-HPC in different concentrations such as 5, 7.5 and 10%. All the formulations were evaluated for weight variation, hardness, friability, drug content, in vitro disintegration time, wetting time, in vitro dissolution. Formulation with 10% L-HPC showed the less disintegration time (25.3 s) and less wetting time (29.1 s). In vitro dissolution studies showed total drug release at the end of 6 min.     

Exploration of melt granulation technique for the development of coprocessed directly compressible adjuvant containing lactose and microcrystalline cellulose

The objective of the present investigation was to prepare and evaluate lactose and microcrystalline cellulose based, directly compressible adjuvant using melt granulation technique. The percentage of polymer blend (PVP K 30 and PEG 4000; 5, 10, or 15%) and the polymer blend ratio (9:1, 1:1, or 1:9) were selected as independent variables in a 3(2) full factorial design. The lactose and microcrystalline cellulose blend (3:1) was mixed with the meltable binder on a water bath at 90 degrees C. The agglomerates were cooled to 35 degrees C and subsequently passed through 30 mesh. A batch containing 12.5% of the polymer blend containing 1:9 ratio of PVP:PEG was used for further studies. In an another 3(2) full factorial design, disintegrant (crospovidone, croscarmellose sodium, or sodium starch glycolate) and mode of addition of disintegrant (intragranular, extragranular, or combination of intragranular and extragranular) were used as independent variables. The agglomerates were evaluated for percentage fines and Carr's index. Tablets were prepared on a single-punch tablet machine, and they were evaluated for tensile strength, friability, and disintegration time. Regression analysis was carried out to evolve full and refined models. Contour plots are presented for graphical expression of the results. The use of composite index is demonstrated for the selection of an appropriate batch. The disintegration time of tablets reduced from 18 min to 6 min when 6% crospovidone was included in the product. The optimized adjuvant was characterized for particle size distribution, granular friability, Kawakita's and Kuno's equation, and dilution potential study. Turmeric, glycyrrhiza, acetaminophen, and metformin HCl were used as model drugs for the preparation of tablets. The present study underlines the fact that melt granulation technique may be adopted for the development of multifunctional directly compressible adjuvant for use in pharmaceuticals. The advantages of melt granulation technique over the classical wet granulation and spray-drying are presented.     

主压力数量化在优化对乙酰氨基酚片处方中的应用初探

运用RIMEK桌面感应压片系统考察主压力对不同处方对乙酰氨基酚片各项质量指标的影响,筛选粘合剂并优化其用量。结果表明,以2%PVPK29/32为黏合剂的处方最佳,在较宽的主压力范围内片剂硬度合格,脆碎度最小,崩解时间最短,溶出最完全。     

利用均匀设计筛选阿司匹林分散片处方

采用国产药用辅料，运用均匀设计方法对阿司匹林分散片处方进行筛选，给出三种崩解剂或溶胀性辅料占处方的比例分别为５％，７％，５％．经过对优选处方的实验表明：崩解时间小于３ｍｉｎ，分散均匀性试验能通过７１０μｍ筛网，均达到英国药典（１９９３年版）要求；体外溶出试验表明：Ｔ５０＝１．１６１ｍｉｎ，Ｔｄ＝２．１０９ｍｉｎ，与阿司匹林普通片溶出参数比较有显著差异，分散片溶出速度快，３０ｍｉｎ内几乎全部溶出．     

胃溶型银杏叶薄膜包衣片处方和质量研究

目的制备胃溶型银杏叶薄膜包衣片并考察处方与质量。方法以性状、重量差异、崩解时限、硬度、脆碎度、含量为指标因素,根据辅料相容性结果,采用正交设计试验,筛选最优处方,并进行质量考察。结果根据选定的优化处方和工艺制备的胃溶型银杏叶薄膜包衣片及片芯问题得到改善,质量符合药典规定要求。结论优选的胃溶型银杏叶薄膜包衣片处方工艺合理,成品质量符合要求。     

甲苯磺酸妥舒沙星分散片的研制和质量控制

目的探讨甲苯磺酸妥舒沙星分散片的制备工艺及其质量控制方法。方法以颗粒流动性以及分散片的外观光洁度、崩解时限为综合指标,选择L9（3^4）进行正交试验筛选出甲苯磺酸妥舒沙星分散片的最佳处方．同时对制备工艺中原辅料微粉化、崩解剂的加入方法、硬度等进行了研究。结果确定优选处方和制备工艺;所制备的分散片脆碎度、分散均匀性、溶出度均符合要求。结论本分散片制备工艺合理。具有溶散快、分散均匀、有效成分溶出量高的特性。     

Cyclodextrin polymer, a new tablet disintegrating agent

Cyclodextrin (CD) polymer, a type of crosslinked cyclodextrin, has been evaluated as a new tablet disintegrating agent in comparison with four common disintegrants (crosslinked polyvinylpyrrolidone, crosslinked carboxymethyl cellulose, formaldehyde casein and corn starch). Physical properties of the disintegrants have been studied. Tablets made by direct compression using microcrystalline cellulose as binder, magnesium stearate as lubricant and talc as antiadherent have been compared. The parameters evaluated were disintegration time, hardness and friability. CD polymer performs well as a tablet disintegrating agent with results paralleling those of crosslinked carboxymethyl cellulose (Ac-Di-Sol) and superior to the other three.     

Influence of disintegrant type and proportion on the properties of tablets produced from mixtures of pellets

The influence of the composition and properties of pellets on the properties of the tablets prepared from their mixtures has been evaluated. Three types of pellets were prepared, (a) those containing a model drug readily identifiable by colour, to evaluate tablet consistency; (b) those containing a deformable material, glyceryl monostearate, to provide pressure absorbing and binding properties, and (c) those containing an inorganic disintegrating agent. Tablets from various mixtures of these pellets, in a statistical designed manner, were prepared at a known compression force and their weight uniformity, friability, diametral breaking load and disintegration times were measured. The uniformity of composition of selected tablets was also determined. Analysis of variance established that the disintegrant type, the proportion of drug pellets and the proportion of disintegrant pellets influenced the breaking load and the disintegration time of the tablets. The proportion of drug and disintegrant pellets influenced the tablet friability whereas the type of disintegrant did not. Canonical analysis failed to establish an exact relationship between pellet properties and tablet properties. However some conclusions can be drawn from this analysis. First, an increase in either the amount of drug pellets or disintegrant pellets decreases the tablet breaking load, and the disintegration times are reduced. Secondly, disintegration times are increased with disintegrants of a high density. Thirdly, larger amounts of drug and disintegrant pellets increase the tablet friability.