均匀设计优化新白斑乳膏基质处方

目的:研究新白斑乳膏的最佳基质处方组成。方法:采用均匀设计,通过考察新白斑乳膏的外观性状、粒度、均匀性、稳定性、pH值确定最佳基质处方组成。结果:新白斑乳膏的最佳基质处方组成为:每100 g成品含白凡士林10g,十八醇10 g,单硬脂酸甘油酯6 g,OP乳化剂1 g,平平加O2 g,二甲基亚砜5 g。结论:按此处方组成制备的新白斑乳膏具有外观细腻均匀、易涂抹、稳定性好的特点。     

肝素钠肌醇烟酸酯乳膏处方筛选及稳定性研究

目的筛选肝素钠肌醇烟酸酯乳膏处方并考察其稳定性。方法以外观性状和稳定性等为评价指标,筛选不同基质组成的8个处方,确定优化处方;再采用加速试验和长期试验考察其稳定性。结果以白凡士林、单硬脂酸甘油酯、十六醇和司盘80等基质组成的8号处方外观性状及稳定性较好,3批中试乳膏质地均匀细腻,黏稠度适宜,易于涂布,含量均匀,质量稳定。结论筛选所得肝素钠肌醇烟酸酯乳膏处方合理稳定,生产工艺简便,质量稳定,适合工业化生产。     

聚桂醇尿素乳膏的处方工艺考察

目的:采用正交设计考察聚桂醇尿素乳膏的处方工艺。方法:采用正交试验表L₁₈(3⁷)考察不同的辅料组成比例(二甲硅油、苯基聚二甲基硅氧烷、液状石蜡、鲸蜡醇棕榈酸酯、硬脂酸、聚山梨酯40、卡波姆)对处方的影响，建立高效液相色谱法测定聚桂醇体外释放曲线、尿素体外释放曲线，外观性状，乳膏稳定性，乳膏黏度等为考察指标，对乳膏处方的辅料组成比例进行筛选，分步确定各辅料含量。结果:通过实验结果分析，得出聚桂醇尿素乳膏的处方工艺。每100g乳膏中聚桂醇3g,尿素5g,二甲硅油2g,苯基聚二甲基硅氧烷5g,液状石蜡1.5g,鲸蜡醇棕榈酸酯0.5g,硬脂酸1.5g,聚山梨酯40 3g,辛基十二醇10g,甘油1.7g,苯甲醇1g,卡波姆1.3g,氨丁三醇1.2g,纯化水，调整乳膏总量至100g。结论:正交设计试验法可用于聚桂醇尿素乳膏的处方工艺考察，优选处方稳定可行，为后期聚桂醇尿素乳膏的新药开发奠定良好的基础。     

正交设计法优选白斑乳膏Ⅱ号的基质处方

目的优选白斑乳膏Ⅱ号的基质处方。方法针对影响乳膏剂外观性状和稳定性的因素,用正交设计法,以油相、乳化剂和乳化温度为可变因素,选用L9(34)表进行实验。结果最佳的基质处方是:100 g白斑乳膏Ⅱ号中含液状石蜡9 g,白凡士林10 g,十八醇3 g,平平加O 1 g,十二烷基硫酸钠0.6 g,单硬脂酸甘油酯4 g,乳化温度80℃。结论正交设计法优选出的基质处方所配制的乳膏外观性状好,质量稳定,符合《中国药典》2010年版软膏项下有关规定。     

康肤霜处方改良及稳定性考察

目的:改进康肤霜乳膏处方,以提高其稳定性。方法:针对康肤霜中氧化锌的破乳及乳膏稳定性差的问题,以油相比例(硬脂酸-白凡士林-单硬脂酸甘油酯)和聚山梨酯80、三乙醇胺、聚氧乙烯(10)硬脂酸酯(SG-10)的用量为因素,以乳膏的光泽度、细腻度、稠度、涂布性、分层现象的综合评分(满分10分)为指标,用正交试验优化乳膏处方,验证并考察其配伍、耐热、耐寒、光照等稳定性。结果:最优处方为每100 g乳膏中含硬脂酸8 g、白凡士林8 g、单硬脂酸甘油酯6 g、聚山梨酯80 4 g、三乙醇胺3 g、SG-10 2 g和水适量;所制乳膏的综合评分>9.5分(n=3)。与原处方成品比较,改良后新品外观无明显变化,未见破乳、分层现象,无颜色变化。结论:成功制得稳定性优于原处方的康肤霜乳膏。     

复方利多卡因乳膏的处方优选

目的:优选复方利多卡因乳膏处方。方法:采用正交试验设计法进行处方中各成分的用量筛选,以镇痛实验的小鼠痛阈提高百分率和抗炎实验的小鼠耳肿胀抑制率为考察指标,确定乳膏的最佳处方并进行验证试验。结果:优选的复方利多卡因乳膏的最佳处方为1000g乳膏中含盐酸利多卡因20g、马来酸氯苯那敏5g、薄荷脑20g、莫匹罗星20g;验证试验中小鼠痛阈提高百分率和耳肿胀抑制率均>60%,考察指标结果达到要求。结论:优选的复方利多卡因乳膏处方合理,可为临床应用提供实验依据。     

正交试验优选抗敏止痒乳膏的配方

目的:筛选抗敏止痒乳膏处方中最佳药物用量.方法:采用正交试验法考察不同处方制备的抗敏止痒乳膏治疗瘙痒性皮肤病的疗效,考察数据设计最佳处方.结果:抗敏止痒乳膏的处方为每 1000 g乳膏中含盐酸利多卡因 20 g,马来酸氯苯那敏 5 g,冰片 20 g,氯霉素 10 g.结论:该处方设计合理,制备的抗敏止痒乳膏治疗瘙痒性皮肤病临床疗效良好.     

硝酸咪康唑乳膏处方筛选及工艺

根据基质的HLB值,设计适合工业化生产的O/W型硝酸咪康唑乳膏处方,采用离心、耐热、耐寒等试验对处方进行筛选,又经中试放大,最终确定处方6为生产工艺处方。产品符合《中国药典》2010版二部有关规定。     

正交设计法优选复方咪康唑乳膏处方

目的：筛选复方咪康唑乳膏处方中最佳药物用量。方法：采用正交试验设计法，考察不同处方的复方咪康唑乳膏治疗豚鼠皮肤石膏样毛癣菌感染模型的作用和体外抑菌效果，根据考察数据设计最佳处方。结果：复方咪康唑乳膏的最佳处方为每1000g乳膏中含氯霉素10g，薄荷脑20g，硝酸咪康唑20g，月桂氮革酮30g。结论：正交试验设计法优选复方咪康唑乳膏的配方，方法可行，收效满意。     

复方润燥止痒乳膏的制备及皮肤刺激性评价

目的：探讨复方润燥止痒乳膏的制备,并对制剂的皮肤刺激性进行评价。方法：采用正交试验法,选取3个不同剂量的乳膏剂基质制成水包油（O/W）型乳膏剂,以制剂的外观性状、稳定性和保湿性为主要考察指标,优选出最佳处方;利用兔子完整皮肤评价乳膏剂对皮肤的刺激性。结果：优选出的最佳处方外观均匀细腻、有光泽、稠度适宜、稳定性和保湿性好,对完整皮肤无刺激性。最佳处方为1000 g乳膏中含维生素E 20 g、盐酸利多卡因20 g、马来酸氯苯那敏5 g、冰片20 g、荷荷巴油60 g、葡萄籽油60 g、甜杏仁油60 g、人参提取液100 g、甘草提取物10 g、苦参提取物10 g、马齿苋提取物10 g、甘油50 g、硬脂酸55 g、三乙醇胺25 g、聚山梨酯－80 30 g、蒸馏水450 mL、95%酒精15 mL。结论：优选的复方润燥止痒乳膏处方合理,所得制剂的外观性状、稳定性、保湿性良好,符合临床应用要求。     

优选精制蛇毒酶乳膏剂制备工艺的实验分析

目的优化精制蛇毒酶乳膏制备工艺。方法以乳膏剂的稳定性及外观性状为考察指标,采用正交实验设计法,以油相、水相、乳化温度和乳化时间为可变因素,选用L9(34)表进行实验。结果最优的基质组成工艺是:硬脂酸20.0 g、植物油10.0 g、液体石蜡8.0 g、丙三醇5.0 g、三乙醇胺1.0 g;混合乳化机搅拌60min;乳化温度85℃。结论按此法制备的乳膏剂符合中国药典软膏剂的规定。     

正交设计试验法优选痤疮乳剂的基质及工艺

目的:优选痤疮乳剂的基质及工艺。方法:用正交设计法,以油相、乳化剂和乳化温度为可变因素,选用L9(34)进行试验。结果:最优的基质组成及工艺为硬脂酸15g,液体石蜡13g,凡士林20g,三乙醇胺3g,乳化温度85℃。结论:该法制备的乳剂符合《中国药典》的规定     

D-最优混料设计优化复方醋酸曲安奈德乳膏

目的 优化乳膏基质的组成,以期得到外观、使用性和稳定性俱佳的复方醋酸曲安奈德乳膏。方法 以离心稳定性、耐寒稳定性、耐热稳定性、粒度、延展性、外观以及清洗性等作为指标,采用D-最优混料设计法确定乳膏基质的组成。结果 最佳复方醋酸曲安奈德乳膏的基质组成：硬脂酸8.3 g,单甘脂7.6 g,白凡士林9.5 g,液体石蜡8.1 g,十二烷基硫酸钠1.1 g,甘油7.5 g,水57 g。结论 按此处方制备的复方醋酸曲安奈德乳膏稳定性好、易涂布、易清洗,外观洁白有光泽。     

Physicochemical stability of solid dispersions of enantiomeric or racemic ibuprofen in stearic acid

The aim of this study was to investigate the solid dispersion phase behavior of s- or rs-ibuprofen in stearic acid. By means of thermal analysis, we have demonstrated the total immiscibility, in solid state, of the corresponding binary mixtures. This indicates that no specific interactions exist between the chosen excipient and active pharmaceutical ingredient (API) that lead to eutectic systems. Furthermore, based on calorimetric and X-ray diffraction experiments, we have showed that upon cooling of the molten state, only stearic acid recrystallizes in the presence of s-ibuprofen, whereas a quaternary phase mixture is obtained for the racemic ibuprofen/stearic acid preparation. The solubility of stearic acid in s-ibuprofen liquid in all proportions was also determined. Overall, the results presented here offer an approach for the study of API/excipient interactions.     

Factors influencing drug release from stearic acid based compacts

Fatty acids are potentially suitable carriers for use in the design of drug delivery systems, being biocompatible, biodegradable inexpensive and of low toxicity. The release of the model compound benzoic acid from fatty acid compacts of stearic acid was evaluated using the USP Apparatus 2 dissolution assembly in phosphate buffer pH 7.4. Matrix controlled drug release was expected. Release profiles were approximated by square root of time kinetics. Release rate was independent of stirring speed in the rpm range 50-150, however, at 200 rpm a significant increase in release rate was observed particularly at later times, the amount released versus square root of time plots becoming non-linear. Release was independent of compression pressure in the range 1-7 tons. The particle size of the benzoic acid and stearic acid used had a significant influence on release. The use of particles in the range 250-500 microm gave release rate constants (k, g/cm(2) per min(0.5)) approximately 1.5 greater than those of smaller particle size (63-125 microm). The formation factor (F) tended to increase exponentially with drug loading, the increase being steeper for compacts prepared from the larger particle sizes. At 80% drug loading for large sized systems the matrix appeared to offer little resistance to drug release and F approached one.     

Evaluation and preparation of controlled release lipid micropheres of sulphamethizole by a congealable disperse phase encapsulation method

A congealable disperse phase encapsulation method was used to prepare controlled release lipid microspheres of sulphamethizole as a model drug. Hydrogenated cotton seed oil (HCSO) and stearic acid were employed as the lipid matrix materials. Tween 60 was the droplet stabilizer used to form microspheres. In in vitro dissolution tests, the drug release was found to be affected by the type of lipid material depending on hydrophilicity. Generally, an initial rapid release followed by a slower release of the drug from the lipid microspheres was observed. Lipid microspheres were also compressed in the tablet form to prevent the initial rapid release of the drug. But the drug release drastically decreased. To achieve a controlled release of the drug. Eudragit L as a channeling agent was added internally to HCSO-microspheres. Although the drug release increased, the controlled release pattern was not achieved. The external addition of polyethyleneglycole 4000 to HCSO-microspheres before compressing tablets, did not produce an affirmative change in the release profile. The lipid microspheres prepared by stearic acid released all of the drug within 1 h. Upon compression, the drug release was very low. Therefore, stearic acid-microspheres were compressed in the tablet form adding disintegrating agents, sodium alginate and Ac-Di-Sol (cross-linked sodium carboxymethylcellulose). A pH-dependent drug release was obtained from the tablets containing sodium alginate. With the tablets of stearic acid-microspheres containing Ac-Di-Sol, the controlled release could be achieved due to gradual disintegration from the tablet to aggregates, and to individual microspheres. Furthermore, in vivo study on 6 healthy volunteers confirmed the controlled release pattern of this dosage form.     

正交试验优选复方苦芩软膏基质处方

目的：优选复方苦芩软膏的基质处方。方法：以十二烷基硫酸钠、硬脂酸、月桂氮酮用量为考察因素,以涂展性、家兔皮肤刺激性的综合评分为指标,采用正交试验优选基质处方。结果：基质处方最佳配比为十二烷基硫酸钠、硬脂酸、月桂氮酮用量分别占0.27%、3.28%、1.64%。结论：以优选的基质处方制备的复方苦芩软膏对家兔皮肤无刺激性,外观良好,有适当黏稠性,易于涂展。     

硝苯地平缓释液体填充硬胶囊的研制

目的优化硝苯地平缓释液体填充硬胶囊处方。方法通过单因素考察和处方筛选,确定影响硝苯地平释放度的3个因素分别为S-40、硬脂酸、淀粉含量。采用三因素三水平正交实验设计,对其影响因素的最佳配比进行筛选。结果优选后的最佳处方是每千个硝苯地平胶囊含量20 g、S-40含量320 g、硬脂酸含量20g,淀粉含量20 g。结论按优化处方制备500粒Nif液体缓释硬胶囊,测定其释放度,释放符合要求并较好地解决了Nif放置过程中的稳定性问题。     

Formulation of sustained-release verapamil HCl and diltiazem HCl semisolid matrix capsules

Semisolid matrix capsule formulations of verapamil HCl and diltiazem HCl prepared by hot-melt capsule filling are an especially appealing and simple way to make sustained-release formulations. Semisolid matrices of Gelucire 50/13 and stearic acid combination eroded and disintegrated at various rates, depending on the combination of waxes, and drug release rates were dependent on storage time (2.5 years) and temperature. Semisolid matrices of combinations of only Gelucire 50/13 and cetyl alcohol eroded at a rate much less than combinations of Gelucire 50/13 and stearic acid. The drug release mechanism from Gelucire 50/13: stearic acid matrices involved diffusion and erosion, whereas Gelucire 50/13 and cetyl alcohol matrices exhibited a diffusion mechanism only. A combination of Gelucire 50/13 with cetyl alcohol is more effective than stearic acid in appropriately extending verapamil HCl release from semisolid matrix capsules. The semisolid matrix formulations studied are sensitive to dissolution stirring speeds.     

挤出滚圆法制备氢溴酸右美沙芬骨架缓释微丸

目的以乙基纤维素和硬脂酸为骨架材料 ,采用挤出滚圆法制备氢溴酸右美沙芬骨架缓释微丸。方法以圆整度和释放度为评价指标 ,先对工艺因素 (挤出速度 ,滚圆速度 ,滚圆时间及热处理温度 )和处方因素 (乙基纤维素与硬脂酸的比例 ,微晶纤维素的用量 ,润湿剂的用量 )进行了单因素考察 ,然后进一步采用正交设计对其优化。结果优化条件所得缓释微丸外观圆整 ,粒子大小分布均匀 ,具有明显的缓释特性。结论通过以上处方和工艺可以制备具有 1 2h缓释的骨架微丸