甲硝唑片溶出度影响因素的探讨

目的考察影响甲硝唑片溶出度的因素。方法压片前分别按5种不同比例加羧甲基淀粉钠(CMS-Na)及硬脂酸镁,混匀,压片,测其溶出度;分别以87℃与50℃的淀粉浆作粘合剂制软材,压片,测其溶出度;分别以不同大小、不同硬度的颗粒压片,测其溶出度;同批颗粒分别制成直径8,9,10mm三种规格的片剂,测其溶出度。结果CMS-Na能显著提高甲硝唑片溶出度;淀粉浆温度为87℃与50℃时制成的甲硝唑片溶出度分别为94.55±1.67(n＝5)和84.32±2.60(n＝5);颗粒大、硬度大时溶出度较低,反之,则溶出度较高;直径8,9,10mm的甲硝唑片30min累积溶出度分别为98.85%、99.64%、99.51%。结论崩解剂对甲硝唑片溶出度影响较大;颗粒的大小、硬度及淀粉浆的温度对甲硝唑片溶出度亦有影响;片剂直径大小对甲硝唑片溶出度影响不大。     

高速剪切湿法制粒工艺制备氯沙坦钾片

目的通过优化高速剪切湿法制粒工艺参数制备氯沙坦钾片。方法采用高速剪切湿法制粒工艺制备氯沙坦钾片,通过对制备工艺参数优化:搅拌桨转速(X_1,r·min~(-1))、加水量(X_2,%)和制粒时间(X_3,s)为考察对象,以颗粒粒径大小(D50,Y_1,μm)、片剂硬度(Y_2,N)、15min药物溶出度(Y_3,%)为评价指标,利用Box-Behnken效应面法优化高速剪切湿法制粒工艺参数。结果方差分析结果显示:搅拌桨转速、加水量和制粒时间对颗粒粒径影响较显著(P<0.05);加水量、制粒时间对片剂的硬度影响较显著(P<0.05);加水量、制粒时间对药物的溶出度影响较显著(P<0.05)。结论通过Box-Behnken实验设计法优化高速剪切湿法制粒工艺,可以提高工艺过程的稳健性和灵活性。     

提高盐酸吡格列酮片溶出度的工艺研究

目的研究提高盐酸吡格列酮片溶出度的工艺。方法采用单因素试验法优化制剂工艺,包括黏合剂的加入量、搅拌速度、剪切速度、压片机主压力等项目,测定颗粒粒度分布、片剂硬度、崩解时间、溶出度等指标。结果调整工艺参数后,控制黏合剂用量为26．26％,制粒时搅拌速度为280r·min^-1,制得的盐酸吡格列酮片的质量指标符合要求且溶出度明显提高,符合药典以及企业内控标准。结论该方法处方合理,工艺简单,适合于产业化生产的要求。     

缬沙坦片的辊压干法制粒工艺研究

摘 要 目的：制备缬沙坦片并优化辊压干法制粒工艺参数。方法: 采用辊压干法制粒工艺制备缬沙坦片。以颗粒粒径大小（D50, Y1/μm）、片剂硬度（Y2/N）、30 min药物溶出度（Y3/%）为评价指标,首先利用Plackett Burman实验设计筛选出对缬沙坦片质量性质影响显著的关键性工艺变量,最终利用Box Behnken效应面法优化辊压干法制粒工艺参数。结果:Plackett Burman实验设计筛选结果显示：辊压压力和筛网孔径对颗粒大小影响较显著（P<0.05）;辊压压力、辊压辊隙和筛网孔径对片剂的硬度影响较显著（P<0.05）;经Box Behnken效应面法优化得到辊压干法制粒的最佳工艺参数为：辊压压力为30 bar、辊压辊隙为3.0 mm、筛网孔径为2.0 mm,制备的缬沙坦片可压性良好,药物溶出度高,与市售参比制剂相比体外溶出相似。结论:通过Plackett Burman联用Box Behnken效应面法优化缬沙坦片的辊压干法制粒工艺,可以提高产品质量的可控性。     

影响甲硝唑片溶出度的因素

目的：考察影响甲硝唑片溶出度的因素。方法：压片前分别按5种不同比例加羧甲基淀粉钠(CMS—Na)及硬脂酸镁，混匀，压片，测其溶出度：分别以87℃与50’C的淀粉作粘合剂制软材，压片，测其溶出度；分别以不同大小、不同硬度的颗粒压片，测其溶出度：同批颗粒分别制成直径8，9，10mm三种规格的片剂，测其溶出度。结果：CMS—Na能显著提高甲硝唑片溶出度。     

影响片剂溶出度的因素探讨

通过对辅料的选择,工艺的影响,测定方法来讨论影响片剂溶出度的因素,提出合适的条件,切实提高片剂的溶出度,从而控制片剂的质量,以利提高片剂的生物利用度。     

胶囊剂溶出度控制因素分析

目的：提高胶囊剂溶出度，从而提高该产品质量。方法：通过实验，研究各种参数对胶囊剂溶出度的影响，选择出最佳工艺条件，如改进处方、控制粒度、控制压力等工艺参数，用于指导大型生产，提高胶囊剂溶出度。结论：经大量生产实践，实验获得的工艺条件是最佳的溶出度控制条件，达到了提高溶出度的目的。     

影响片剂溶出度的因素探讨

通过对辅料的选择,工艺的影响,测定方法来讨论影响片剂溶出度的因素,提出合适的条件,切实提高片剂的溶出度,从而控制片剂的质量,以利提高片剂的生物利用度.     

影响片剂溶出度的因素探讨

通过对辅料的选择,工艺的影响,测定方法来讨论影响片剂溶出度的因素,提出合适的条件,切实提高片剂的溶出度,从而控制片剂的质量,以利提高片剂的生物利用度.     

淀粉-阿司匹林颗粒生产工艺的改进

目的改进淀粉-阿司匹林颗粒的处方工艺,提高片剂的溶出度。方法在处方中增加聚维酮K30,用等量递加混合法增加物料的均一性。结果及结论改进后的淀粉-阿司匹林颗粒压片后溶出度≥90%,溶出度稳定性良好。     

乙酰螺旋霉素片的制备工艺及对溶出度的影响

目的:寻求制备乙酰螺旋霉素片的最佳工艺。方法:考察L—HPC的用量和加入方法、粘合剂种类、乙酰螺旋霉素粉末粒度及润滑剂对乙酰螺旋霉素片溶出度的影响。结果:所选处方和工艺制备的乙酰螺旋霉素片,硬度较好,外观光洁,溶出度可达98％以上。结论:本法处方合理,工艺简单,适用于工业化生产。     

魔芋葡甘露聚糖在灰黄霉素片制备中的应用

目的:探讨魔芋葡甘露聚糖在灰黄霉素片制备中的应用.方法:以魔芋葡甘露聚糖作为黏合剂,采用湿法制粒压片法制备灰黄霉素片,并进行质量检验.结果:所得灰黄霉素片的硬度、脆碎度、崩解时限、溶出速度及溶出度各项指标均有明显的改善,质量检查合格.结论:以魔芋葡甘露聚糖为黏合剂制备的灰黄霉素片崩解完全,溶出度增大.     

克拉霉素缓释片释放度研究

目的:研究自制克拉霉素缓释片的体外释放度。方法:以紫外分光光度法测定自制克拉霉素体外释放度。结果:释放度曲线经Weibull分布拟合,自制缓释片为lnln 1/(1-F(t))=1.5 291 lnt-3.7 539(r=0.9 842);进口缓释片为lnln 1/(1-F(t))=1.5 216 lnt-3.6 759(r=0.9 830)。自制和进口克拉霉素缓释片的释放度基本一致。结论:自制克拉霉素缓释片有较好的释药性能。本文建立的释放度测定方法可作为该制剂的质控方法。     

氟康唑阴道缓释片的制备及体外释放的研究

目的：制备氟康唑阴道缓释片,选择最优缓释片处方,为下一步体内药动学实验和其它各项研究奠定基础。方法：以氟康唑为主药,采用三因素三水平,正交试验设计方法考察MCC,HPMC,Carbopol对氟康唑缓释片释放的影响。应用紫外分光光度法测定药物片剂的释放度和片剂中氟康唑的含量。结果：确定处方FCZ50mg Carbopol 100mg MCC 150mg。HPMC 90mg淀粉210mg为最佳处方,片重0.6g。HPMC为该片剂缓释作用的主要影响因素,卡波姆影响作用次之。结论：该制剂有望成为治疗阴道真菌感染的有效制剂。     

Effects of hardness on the disintegration time and the dissolution rate of uncoated caffeine tablets.

The effects of hardness on disintegration and dissolution characteristics of uncoated caffeine tablets made at eight different pressure levels were studied. The disintegration times were determined using the J.P. VIII procedure with disks and the dissolution rate measurements were performed with the U.S.P.XVIII procedure (U.S.P. method) and the J.P. VIII disintegration test apparatus (J.P. method). A good correlation between the hardness and the disintegration times was obtained. The dissolution rate constants were determined from the equation of Noyes & Whitney (1897) and a good correlation between the hardness and the dissolution rate constants was obtained. The hardness governed the dissolution over all the stages from tablet to the smallest particles after the breakage by disintegration. The dissolution rates of the J.P. method were greater than those of the U.S.P. method.     

Formulation and optimization of potassium iodide tablets

The use of potassium iodide (KI) as a protective agent against accidental radioactive exposure is well established. In this study, we aimed to prepare a KI tablet formulation using a direct compression method. We utilized Design of Experiment (DoE)/mixture design to define the best formulation with predetermined physical qualities as to its dissolution, hardness, assay, disintegration, and angle of repose. Based on the results from the DoE, the formulation had the following components (%w/w): Avicel 48.70%, silicon dioxide 0.27%, stearic acid (1.00%), magnesium stearate 2.45%, and dicalcium phosphate 18.69%, in addition to potassium iodide 28.89% (130 mg/tablet). This formulation was scaled-up using two tablet presses, a single-punch press and a rotary mini tablet press. The final scaled-up formulation was subjected to a variety of quality control tests, including photo-stability testing. The results indicate that potassium iodide tablets prepared by a rotary mini tablet press had good pharmaceutical characteristics and a shelf-life of 25 days when stored at room temperature protected from light.     

The effect of tablet formulation and hardness on in vitro release of cephalexin from Eudragit L100 based extended release tablets

Eighteen batches of cephalexin extended release tablet were prepared by wet granulation method by using Eudragit L100. The effect of the concentration of Eudragit L100, microcrystalline cellulose and tablet hardness on cephalexin release was studied. The formulated tablets were also characterized for physical and chemical parameters. The dissolution results showed that a higher amount of Eudragit in tablet composition and higher tablet hardness resulted in reduced drug release. An increased amount of microcrystalline cellulose in tablet composition resulted in enhanced drug release. Tablet composition of 13.3% w/w Eudragit L100 and 6.6 to 8% w/w microcrystalline cellulose with hardness of 7-11 kg/cm2 gave predicted release for 6 h. The in vitro release was compared with a marketed tablet. Physical and chemical parameters of all formulated tablets were within acceptable limits. The effect of storage on in vitro release and physicochemical parameters of tablets was evaluated and two batches among formulated eighteen batches found to be in acceptable limits.     

Evaluation of Selected Micronized Poloxamers as Tablet Lubricants

The primary objective of this study was to compare the lubrication properties of micronized poloxamer 188 (Lμ trol micro 68®) and micronized poloxamer 407 (Lμ trol micro 127®) with certain conventional lubricants such as magnesium stearate and stearic acid. The secondary objective was to use these micronized poloxamers as water-soluble tablet lubricants in preparation of effervecsent tablets. The results showed that these micronized poloxamers have superior lubrication properties compared with stearic acid, with no negative effect on tablet hardness, friability, disintegration, or dissolution. Moreover, lubricant mixing time had no significant effect on tablet properties when poloxamers were used as lubricants. Effervescent tablets also were produced successfully using micronized poloxamers as lubricants. The micronized poloxamers had a better lubrication effect in compariason with that of water-soluble lubricant l-leucine.     

格列喹酮片的分剂量评价

目的 评价单面带刻痕的格列喹酮片的分剂量药学特性。方法 分别采用切药器和手工对自研品和参比制剂进行分割,以分割前后质量损失为评价指标,考察自研品和参比制剂的可分割性;取在硬度上限（8 kg）和下限（4 kg）处的自研格列喹酮片分别用切药器分割后,考察分割质量损失;按照《中国药典》2020年版片剂脆碎度检查法研究分割后的片剂脆碎度;参考《欧洲药典》,随机取30片,分割后检测单一半片占半片平均片质量百分比;高效液相色谱法测定格列喹酮整片、半片在pH 8.5磷酸盐缓冲液中的溶出曲线;参照《中国药典》含量均匀度检查法（通则0941）,对切药器分割后的30片自研品进行含量均匀度测定。结果 质量损失结果表明手工分割和切药器分割无显著性差异;硬度上限与下限时片剂分割后的脆碎度和质量损失均符合要求;分割后片剂质量差异、脆碎度和含量均匀度均符合药典要求;自研品与参比制剂的半片溶出行为一致;与整片溶出量相比,分割后的自研品60 min溶出量为51.46%,参比制剂为49.12%。结论 自研品和参比制剂分割后的药学特性相同。