孟鲁司特钠片处方工艺研究

目的：研究孟鲁司特钠片的处方工艺。方法：对处方工艺进行筛选,通过相关试验考察工艺的稳定性。结果：采用所选处方工艺制备的孟鲁司特钠片外观光亮,硬度适中,溶出度好。结论：按照所设计的处方制备的鲁司特钠片外观美观,质量稳定,其处方合理,适用于工业化生产。     

安立生坦片处方和制备工艺研究

目的 筛选安立生坦片的最佳处方。方法 通过原料辅料的相容性试验筛选辅料,采用正交试验考察不同处方对颗粒流动性、外观、溶出度的影响,确定最优处方,与市售安立生坦片在4种溶出介质中进行累积溶出曲线对比研究,并考察制剂的加速稳定性。结果 开发出最优处方,产品与市售安立生坦片在4种溶出介质中溶出曲线相似,6个月的加速试验结果与0个月时比较无明显变化。结论 该处方设计合理、制备工艺可靠。     

盐酸加巴喷丁缓释片的研制

目的:研制盐酸加巴喷丁缓释片。方法:利用单因素优化设计法优化处方制备工艺,建立HPLC法测定释放度。结果:最佳处方为盐酸加巴喷丁180 mg,K15M型HPMC 150 mg,CMC·Na 50 mg,可压性淀粉20 mg,5%PVP(K25)95%的乙醇溶液适量,0.5%硬脂酸镁作润滑剂。结论:该优选条件制备的加巴喷丁缓释片工艺简单,体外释药具有明显的12 h缓释作用。     

加巴喷丁片剂的溶出度研究

目的建立测定加巴喷丁片剂溶出度的方法。方法以茚三酮光度法测定加巴喷丁片剂含量,测定波长为570 nm;采用转篮法,以900 mL水为溶出介质,转速为100 r/min,温度(37±0.5)℃,对5批加巴喷丁片剂在8,10,12,15,30 min内进行溶出度均一性和批间重现性试验。结果与结论样品溶出均一性良好,溶出度均大于90%,茚三酮光度法可用于测定该产品的溶出度。     

Formulation and Processing Strategies which Underpin Susceptibility to Matrix Crystallization in Amorphous Solid Dispersions

Through matrix crystallization, an amorphous solid may transform directly into its more stable crystalline state, reducing the driving force for dissolution. Herein, the mechanism of matrix crystallization in an amorphous solid dispersion (ASD) was probed. ASDs of bicalutamide/copovidone were prepared by solvent evaporation and hot melt extrusion, and sized by mortar and pestle or cryomilling techniques, modulating the level of mechanical activation experienced by the sample. Drug loading (DL) of the binary ASD was varied from 5-50%, and ternary systems were formulated at 30% DL with two surfactants (sodium dodecyl sulfate, Vitamin E TPGS). Imaging of partially dissolved or crystallized compacts by scanning electron microscopy with energy-dispersive X-ray analysis and confocal fluorescence microscopy was performed to investigate pathways of hydration, phase separation, and crystallization. Monitoring drug and polymer release of ASD powder under non-sink conditions provided insight into supersaturation and desupersaturation profiles. Systems at the greatest risk of matrix crystallization had high DLs, underwent mechanical activation, and/or contained surfactant. Systems having greatest resistance to matrix crystallization had rapid and congruent drug and polymer release. This study has implications for formulation and process design of ASDs and risk assessment of matrix crystallization.     

急性冠脉综合征合并心房颤动患者的抗栓治疗策略

目的:探讨急性冠脉综合征合并心房颤动患者的抗栓治疗有效策略。方法:选择2013年5月~2014年5月65例患者,随机分为对照组(n=32例)和观察组(n=33例),对照组给予氯吡格雷联合华法林抗凝治疗,观察组给予氯吡格雷联合阿司匹林抗栓治疗,均给予冠心病二级预防处理。比较两组1年内不良事件及不良反应发生率。结果:两组均未出现血栓栓塞事件、死亡事件,白细胞和血小板计数未出现异常,两组心绞痛、心功能恶化等心血管事件发生率比较差异无统计学意义(P>0.05);观察组出血不良反应发生率明显低于对照组(P<0.05)。结论:相较于氯吡格雷联合华法林抗凝治疗,氯吡格雷联合阿司匹林抗栓治疗急性冠脉综合征合并心房颤动患者安全性更强。     

左卡尼汀片的处方及制备工艺研究

目的：优化左卡尼汀片的处方及制备工艺。方法：通过处方设计与筛选,以进口制剂在不同介质中的溶出曲线为指标,确定优化处方及制备工艺。结果：采用优化处方和工艺制备的左卡尼汀片在常用介质中的溶出行为与进口制剂基本一致。结论：自制制剂的处方合理,工艺可行,适合工业生产。     

左卡尼汀片处方及制备工艺研究

左卡尼汀,即左旋内碱,作为一种能量补充剂,主要生理功能是促进脂肪代谢,以供人体组织能量需要,临床上用于治疗心血管疾病、糖尿病、肝病以及原发或继发性肉碱缺乏症等,并可用于肾病透析[1]。目前市售剂型有注射剂和口服液。根据临床需要,我院研制了左卡尼汀片剂,本文对其处方与     

格列喹酮缓释片的处方设计

目的：对格列喹酮缓释片进行处方研究。方法：以药物的累积释放度为标准,同时结合相似因子,首先进行单因素试验,确定影响药物释放的主要因素,在此基础上,以HPMC（K4M）及乳糖的含量为变量,进行比较试验,采用综合评分法确定最优处方。并且对最优处方进行验证。结果：最优处方为格列喹酮、HPMC（K4M）、乳糖用量分别为60mg、30mg、55mg,70％乙醇为粘合剂,所制得的格列喹酮缓释片在2,6,12h的体外累积释放度分别为（19．82±0．92）％,（51．07±0．95）％和（83．48±0．71）％。结论：格列喹酮缓释片体外显示出缓释行为,释放度符合规定,可进一步研究开发。     

地拉罗司分散片的处方筛选研究

目的：筛选和优化地拉罗司分散片的处方。方法：以崩解时限和30min累积溶出度为考察指标,以稀释剂微晶纤维素（MCC）和乳糖用量、崩解剂交联聚维酮（PVPP）内加质量比、助溶剂十二烷基硫酸钠（SDS）用量为因素,以L（3。）正交试验表对试验方案进行设计,对地拉罗司分散片处方进行筛选,并进行处方验证。结果：优化处方为MCC用量为12．5％、乳糖用量为27．5％、PVPP添加比例为18％（内加）、SDS用量为1．0％;验证试验中地拉罗司分散片在120S内完全崩解,平均30min累积溶出度为86．O％,与普通片相比具有较大优势。结论：按该处方制备的地拉罗司分散片溶出度、崩解时限等各项指标均符合要求。     

普罗布考片剂溶出度及稳定性考察

利用紫外法和高效液相色谱法对普罗布考片剂的溶出度及稳定性进行考察，结果表明：溶出４５ｍｉｎ时，溶出度达７０％以上；高温８０℃放置１０天，含量下降２％，降解产物＞１％；高湿（ＲＨ９２５％）条件下溶出度略有下降，其它条件各项指标均未发生明显改变；加速实验及室温留样２年，其各项指标均未发生明显改变，可暂定有效期为２年．普罗布考片剂应于低温、密闭、干燥处保存．     

琥珀酸索利那新片的制备及处方优化

目的 对琥珀酸索利那新片处方与工艺进行优化.方法 通过设计不同处方,对粘合剂、填克剂、润滑剂的用量及包衣工艺进行考察,确定了最终处方,并测定在4种溶出介质中的溶出曲线.结果 以琥珀酸索利那新为主药,以乳糖、淀粉为填充剂,以羟丙基甲基纤维素为粘合剂,以硬脂酸镁为润滑剂,以胃溶型薄膜包表预混剂为包表材料,制得琥珀酸索利那新片.结论 该制剂工艺稳定,制得琥珀酸索利那新片(5mg)与原研市售品溶出行为相似,质量符合规定.     

氨酚待因片处方工艺的优化

采用正交试验设计，优化了氨酚待因片的处方工艺，使制粒周期由每批8h降至2h，产品质量符合中国药典2000年版要求。     

复方呋塞米螺内酯片的处方优化研究

目的优化复方呋塞米螺内酯片的处方。方法以溶出度为指标,采用单因素试验优选复方呋塞米螺内酯片的最佳处方影响因素。结果优选出最佳处方为:以3%十二烷基硫酸钠(SDS)为表面活性剂,10%微晶纤维素为填充剂,5%交联聚维酮(PVPP)为崩解剂以内3%外2%法加入的方式制备复方呋塞米螺内酯片。结论制备的复方呋塞米螺内酯片表面光洁,硬度适宜,溶出度较好,工艺简便可行。     

Extended-Release Tablets of Nitrofurantoin: An Old Antibiotic Carried in a New Formulation

Pharmaceutical Chemistry Journal - Nitrofurantoin is an old antibiotic currently prescribed to treat urinary tract infections. High dosing frequency causes fluctuations in the drug plasma...     

法莫替丁生物黏附片的处方筛选研究

目的:筛选和优化法莫替丁生物黏附片的处方.方法:采用3因素9水平的均匀设计,结合多元线性回归的方法,以溶出度为指标,对制剂处方进行筛选、优化.结果:多元线性回归结果表明,处方中生物黏附材料HPMC、卡波姆对药物释放起阻滞作用,方程较好地阐明了主要辅料对法莫替丁生物黏附片释放度的影响.结论:均匀设计优化法莫替丁生物黏附片处方结果良好,优化处方的释放速度达到设计要求.     

替米沙坦氢氯噻嗪双层片处方工艺研究

目的：研究替米沙坦氢氯噻嗪双层片的处方工艺。方法：采用单因素筛选方法获得双层片的处方组成和制备工艺。结果：本品的溶出曲线和各项质量指标均符合要求,处方工艺合理,质量可控。结论：替米沙坦氢氯噻嗪双层片的处方工艺可靠,质量稳定,适合于工业化生产。     

Succinate Buffer in Biologics Products: Real-world Formulation Considerations,Processing Risks and Mitigation Strategies

The succinic acid/succinate system has an excellent buffering capacity at acidic pH values (4.5-6.0), promising to be a buffer of choice for biologics having slightly acidic to basic isoelectric points (pI 6 – 9). However, its prevalence in drug products is limited due to the propensity (risk) of its components to crystallize during freezing and the consequent shift in the pH which might affect the product stability. Most of these previous assessments have been performed under operational conditions that do not simulate typical drug product processing conditions. In this work, we have characterized the physicochemical behavior of succinate formulations under representative pharmaceutical conditions. Our results indicate that the pH increases by ～ 1.2 units in 25 mM and 250 mM succinate buffers at pharmaceutically relevant freezing conditions. X-ray diffractometry studies revealed selective crystallization of monosodium succinate, which is posed as the causative mechanism. This salt crystallization was not observed in the presence of 2% w/v sucrose, suggesting that this pH shift can be mitigated by including sucrose in the formulation. Additionally, three monoclonal antibodies (mAbs) that represent different IgG subtypes and span a range of pIs (5.9 - 8.8) were formulated with succinate and sucrose and subjected to freeze-thaw, frozen storage and lyophilization. No detrimental impact on quality attributes (QA) such as high molecular weight (HMW) species, turbidity, alteration in protein concentration and sub-visible particles, was observed of any of the mAbs tested. Lastly, drug formulations lyophilized in succinate buffer with sucrose demonstrated acceptable QA profiles upon accelerated kinetic storage stability, supporting the use of succinate buffers in mAb drug products.     

氯波必利生物黏附缓释片的处方筛选

目的:优化氯波必利生物黏附缓释片的处方和制备工艺。方法:以累积释放度为指标,采用正交设计方法,对制剂辅料羟丙基甲基纤维素(HPMC)、卡波姆、淀粉及乳糖的用量进行考察,确定氯波必利生物黏附缓释片处方。结果:缓释片规格为每片0.1 g,以HPMC和卡波姆为生物黏附和骨架材料,乳糖为稀释剂,淀粉为填充剂和崩解剂,每100片用量分别为5.5、2.2、1.2、2.0g。与氯波必利普通片比较,缓释片具有显著缓释和黏附性能。结论:本制剂制备工艺简单,符合缓释、黏附要求。