正交法优选寒痹软膏的处方

目的 研究寒痹软膏的乳化成型工艺.方法 按L18(37)正交试验表[1],分别对单硬脂酸甘油酯等7种辅料的用量进行考察,以离心试验(4000r·min-1)与高温试验(60℃)的结果为指标,通过研究软量的稳定性优选软膏基质的最佳配比.结果 确定的处方最佳基质配比为:单硬脂酸甘油酯100g、硬脂酸80g、白凡士林50g、甘油60g、聚山梨酯(80)15g、十二烷基硫酸钠7g、三乙醇胺12g.结果 本制备工艺合理可行,稳定可控.     

白疙消软膏基质的工艺优选

目的：选择最佳白疙消软膏基质配比。方法：以伸展性、保湿性、粒度、耐热耐寒稳定性等主要指标综合评分为指标,用正交试验法进行优选试验。结果：白疤消软膏基质最佳配比为白凡士林25％、硅油5％、十六醇2％、单硬脂酸甘油酯3％、脱水山梨醇单硬脂酸酯司盘-60 3％、硬脂聚烃氧（40）酯9％、药液40％、甘油8％。结论：优选出的基质配比制备的软膏质量稳定。     

鞣酸软膏的处方和配制工艺的优化

目的：制定出新的鞣酸软膏的处方与配制工艺。方法：通过比较,筛选出一个最好的处方与配制工艺。结果：处方：鞣酸200g、甘油150g、乙醇50g、聚山梨酯-60 10g、凡士林550g。配制工艺：水相/将鞣酸与乙醇甘油混匀,水浴加热搅拌溶解,加入聚山梨酯-60融化,保持温度在90℃。油相/凡士林加热融化温度在90℃保持,最后将水相慢慢加入油相,边加边搅拌,流水冷却,搅拌至凝固。用这种处方和配制工艺配制鞣酸软膏快速简单,产品性状好,质量稳定,疗效确切,适合大量生产。     

水杨酸硫磺软膏配制方法的改进

目的：通过改进水杨酸硫磺软膏配制方法,提高该制剂的可操作性和制剂质量。方法：以二甲基亚砜为溶媒,溶解水杨酸,加入适量聚山梨酯-80可溶解硫磺。结果：新方法制成的软膏均匀细腻,质量可控。结论：水杨酸硫磺软膏新的配制方法比传统的制法优越得多,可替代传统方法。     

硝酸甘油软膏的无菌检查方法学验证

目的 建立硝酸甘油软膏的无菌检查方法,并对方法进行验证。方法取预热至45℃的供试品10支(15g/支),每支称取1g,加至含溶化的司盘80、聚山梨酯80无菌混合物和无菌玻璃珠的锥形瓶中,振摇混匀后,加入45℃的pH 7.0无菌氯化钠-蛋白胨水缓冲液至100ml,使供试品充分乳化。按薄膜过滤法,细菌、真菌每膜用300ml pH 7.0氯化钠-蛋白胨缓冲液冲洗,消除抑菌活性。结果 经方法验证,硝酸甘油软膏供试品组、阴性对照组均无菌生长,试验组各滤器中试验菌与相应对照组比较均生长良好,说明供试品在该检验量和检验条件下无抑菌作用或其抑菌作用可以忽略不计。结论薄膜过滤法有效可行,可用于硝酸甘油软膏的无菌检查。     

复方紫草油微生物限度检查法的建立

目的建立复方紫草油的微生物限度检查方法。方法采用无菌十四烷酸异丙酯、聚山梨酯80或混合中和剂溶解,制备供试液,按照中国药典2015年版第四部规定对复方紫草油进行微生物限度检查适用性实验。结果单独或混合无菌十四烷酸异丙酯和聚山梨酯80作为中和剂,无法得到稳定均一的供试液,使用无菌单硬脂酸甘油酯、聚山梨酯80和司盘80组成的混合中和剂可以得到性状稳定均一供试液,微生物回收率在0.5~2之间;控制菌检查中,各阳性试验菌均检出,阴性对照均无菌生长。结论复方紫草油的微生物限度检查方法可行。     

尿素乳膏的配制改进与临床应用

手足皲裂是常见病，病程长，治疗比较困难、自1993年以来，我院配制尿素乳育用于治疗手足皲裂，经临床使用，疗效较满意，现介绍如下：1．处方：尿素200g，甘油80g，OP乳化剂5g，依地酸二钠0．1g，凡士林50g，液体石蜡350g，单硬脂酸甘油酯120g，尼泊金乙酯1．0g，司盘-803．0g，蒸馏水200ml，共制1000g。2制法：水相取甘油、OP与适量蒸馏水混合加热至约70～80C，加人尼泊金乙酯溶解。油相取单甘脂、白凡士林、液体石腊、司盘一80，加热熔化．埃温度70～80℃。乳化将水相缓缓加入油相中，依同一方向搅拌，候温度70C许加入尿素，边加边揽…     

卡波姆基质硫软膏的研制

硫软膏为医院常用制剂，具有杀疥虫及霉菌的作用，用于治疗疥疮，体癣、脂溢性皮炎等，地方和军队制剂规范均用升华硫，凡士林基质，研和法配制[1，2]。按该法制备的硫软骨质地粗糙，费时费力，影响含量测定的准确度，难以达到软膏剂的质量要求。我们选用国产新型药用辅料一卡波姆（Carbomer）为基质配制硫软膏，产品均匀细腻、稠度适宜、制备方便、质量稳定。1处方与制备1．l处方升华硫100g，甘油1009，卡波姆sg，王乙醇胺sg，蒸馏水适量，全量10009。1．2制备取甘油1009置容器中，加卡波姆sg使润湿，研匀，加蒸馏水约400ml浸泡，使其充分…     

紫外分光光度法测定苯酚软膏的含量

目的研究用紫外分光光度法测定苯酚软膏的含量。方法用水作溶剂,50℃水浴溶解软膏,冰浴析出基质,使基质与苯酚分离,在270nm波长处,用外标一点法测定含量。结果苯酚浓度在7.48~59.84μg.mL-1范围内线性关系良好,方法回收率为98.76%,基质对苯酚的测定无干扰。结论本方法操作简便、快速,结果准确,可用于该制剂的含量测定。     

聚山梨酯80在微生物限度检查中的应用

目的：对有抑菌性或非水溶性的药品提供适宜的供试液制备方法,建立方便有效的微生物限度检查方法。方法：应用聚山梨酯80的中和、乳化、增溶及保护微生物等作用,对本院配制的11种制剂进行供试液的制备及微生物限度检查验证。结果：加菌回收率及控制菌检查结果符合《中国药典》的要求。结论：聚山梨酯80可用于上述药品微生物限度检查时供试液的制备。     

非水溶性软膏供试液制备方法的探讨

目的：探讨简便,快速制备非水溶性软膏供试验液的方法。方法：采用十四烷酸异丙酯溶介非水溶性基质,再以吐温－80为乳化剂制备供试液。结果：上述方法所制备的[溶液乳化均匀,与药典法比较,其结果一致。结论：本法简便,快速,可靠,不失为一种较为理想且实用的方法。     

Oral bioavailability of the antioxidant astaxanthin in humans is enhanced by incorporation of lipid based formulations.

Astaxanthin is a carotenoid with antioxidant properties, synthesised by plants and algae, and distributed in marine seafood. Astaxanthin is also available as a food supplement, but, like other carotenoids, is a very lipophilic compound and has low oral bioavailability. However, bioavailability can be enhanced in the presence of fat. There is not much information in the literature about the pharmacokinetics of oral astaxanthin in humans. In this open parallel study, healthy male volunteers received a single dose of 40 mg astaxanthin, as lipid based formulations or as a commercially available food supplement, followed by blood sampling for further analysis of plasma concentrations. Pharmacokinetic parameters were calculated to evaluate the extent and rate of absorption from each formulation. The elimination half-life was 15.9+/-5.3 h (n=32), and showed a mono-phasic curve. Three lipid based formulations: long-chain triglyceride (palm oil) and polysorbate 80 (formulation A), glycerol mono- and dioleate and polysorbate 80 (formulation B), and glycerol mono- and dioleate, polysorbate 80 and sorbitan monooleate (formulation C), all showed enhanced bioavailability, ranging from 1.7 to 3.7 times that of the reference formulation. The highest bioavailability was observed with formulation B, containing a high content of the hydrophilic synthetic surfactant polysorbate 80.     

阿昔洛韦眼膏的制备及质量控制

目的:制备阿昔洛韦眼膏并建立质量控制方法。方法:以凡士林,羊毛脂,液体石蜡为基质制备阿昔洛韦眼膏,用反相高效液相色谱法测定阿昔洛韦的含量。结果:测定阿昔洛韦的平均回收率为98.47％,RSD为1.20％(n=5);制剂无刺激,稳定性好。结论:本制剂工艺简单,质量稳定、可控,能适应临床需要,以反相高效液相色谱法测定阿昔洛韦的含量准确、快速。     

新目安眼膏制备工艺及含量测定方法的研究

目的 建立制备新目安眼膏的最佳工艺,并建立测定新目安眼膏中更昔洛韦含量的方法.方法 采用正交实验法,以成型性、涂展性和均匀性为考察指标对新目安眼膏的制备工艺进行了优化,且采用高效液相法对更昔洛韦的含量进行测定.结果 正交实验表明,基质配比最优用量为PEG-4000 1.0 g、PEG-400 4.0 g、聚山梨酯-80为1.5 g.建立了高效液相法测定更昔洛韦的方法:Phenomenex C18( 250 mm×4.6 mm,5μm)柱,流动相为甲醇-水(10∶90),流速:1.0mL·min-1,测定波长252 nm,柱温30℃,进样量20 μL.结论 新目安眼膏的制备工艺简单,符合质量要求.定量方法操作简单、灵敏度高、结果准确,可用于测定新目安眼膏中阿昔洛韦的含量.     

Investigation of the absorption of hypericin into the skin of hairless mice

The skin absorption of hypericin was evaluated in hairless mice to develop an optimised hypericin topical formulation that could be used in the clinical study of psoriasis. Hypericin (0.01-1.0%) in Beeler basis, polyethylene glycol ointment, carbopol gel, cetomacrogol cream, petrolatum or emulsifying ointment, with and without skin-absorption enhancers (isopropylidene glycerol and diethylene glycol monoethyl ether), was tested in-vivo on hairless mice skin. Using a skin-stripping technique and the intrinsic fluorescence of hypericin under standardised UV365 irradiation, it was demonstrated that the absorption of hypericin very much depended on the vehicle used. The concentrations of hypericin in the skin were then estimated by HPLC analysis. For this purpose, two vehicles were employed, with which hypericin penetrated the skin of hairless mice well (emulsifying ointment with isopropylidene glycerol) or very poorly (polyethylene glycol ointment). In the case of emulsifying ointment with isopropylidene glycerol (0.05% hypericin), a substantial concentration of hypericin (8.6+/-3.2 microg g(-1)) (mean +/- s.d., n = 5) was found in the skin. With polyethylene glycol ointment, however, only a limited hypericin skin concentration (0.38+/-0-34 microg g(-1), n = 5) was achieved. These results show that emulsifying ointment with polyethylene glycol holds promise as an effective topical vehicle for the treatment of skin diseases, such as psoriasis, with hypericin.     

The oral administration of Polysorbate 80 to the immature female rat does not increase uterine weight

Some xenobiotics display estrogenic activity in in vitro and/or in vivo systems. Previous studies by Gajdova et al. have shown that polysorbate 80 (also known as Tween 80) administered by intraperitoneal injection to neonatal female rats on days 4–7 after birth produced estrogenic effects including earlier vaginal opening, prolongation of the estrus cycle and persistent vaginal estrus [1]. Some of these effects were evident many weeks after cessation of administration of polysorbate 80. The present study has evaluated the estrogenic properties of polysorbate 80 following oral administration, a route of exposure which is more relevant for the consideration of human health hazard. The effects of polysorbate 80 at oral gavage doses of up to 5 g/kg/day for 3 consecutive days on uterine growth of immature female rats, a commonly used in vivo mammalian assay for estrogenic activity, have been determined. Estradiol benzoate administered subcutaneously was used as a positive control and significantly increased uterine weight in this age and strain of female rat (21–23 days, Alpk:APfSD Wistar derived) by up to 4.5-fold above vehicle control values. Polysorbate 80 administered orally to rats had no effect on uterine weight. Thus, intrinsic estrogenic effects of polysorbate 80 reported following its intraperitoneal injection to neonatal 4-day-old female rats are not manifest when it is administered by oral gavage to immature 20- to 22-day-old female rats. This latter route of exposure is of more relevance to human exposure scenarios and these data are, therefore, important in assessing hazard/risk of polysorbate 80 to man.     

双氯芬酸钠眼膏的研制

目的：制备双氯芬酸钠眼膏并建立质量控制方法。方法：以黄凡士林,羊毛脂,液体石蜡为基质制备双氯芬酸钠眼膏,用高效液相色变法测定含量,结果：含量测定平均回收率为99．30％,RSD为0．99％（n=5),制剂无刺激性,稳定性好。结论：本制剂工艺简单,质量稳定,以高效液相色谱法测定含量,准确,快速。     

GC-MS法测定盐酸金霉素眼膏中16种多环芳烃含量

目的 建立盐酸金霉素眼膏中16种多环芳烃(PAHs)的气相色谱-质谱含量测定方法。方法 盐酸金霉素眼膏经正己烷溶解后，用正己烷饱和乙腈多次萃取，浓缩后经GC-MS法检测，气相色谱采用DB-5MS毛细管柱，程序升温，进样口温度250℃，质谱采用电子轰击(EI)离子源，以选择反应监测(SIM)模式进行检测。同时从辅料来源及生产工艺上分析制剂中PAHs异常的主要原因。结果 16种PAHs在相应浓度范围内线性关系良好，定量限(LOQ)为0.3~20.0ng/mL，回收率为72%~118%，相对标准偏差(RSD)均小于2.5%，辅料凡士林的质量直接影响制剂的好坏。结论 本法准确度高、灵敏度强，适用于盐酸金霉素眼膏中PAHs的检测，可为眼膏剂的质量控制与安全性评估提供数据参考。     

Hypotensive action of commercial intravenous amiodarone and polysorbate 80 in dogs

Commercial intravenous amiodarone has been reported to have antiarrhythmic actions and to cause only mild hypotension in humans. In the dog, however, amiodarone was observed to cause severe hypotension. Since commercial intravenous amiodarone is amiodarone compound (50 mg/ml) dissolved in water with polysorbate 80 (Tween 80) (100 mg/kg), the effects of amiodarone in ethanol (5 mg/kg) and polysorbate 80 (10 mg/kg) were studied individually, and in combination in anesthetized dogs. Commercial intravenous amiodarone and polysorbate 80 caused at least a 60% drop in mean blood pressure and left ventricular maximum dP/dt for at least 30 min, whereas amiodarone in ethanol did not. The drop in blood pressure was not principally due to peripheral vasodilation. Therefore, in dogs the diluent polysorbate 80 is the major cause of severe hypotension resulting from commercial intravenous amiodarone. These studies show that commercial intravenous amiodarone produces results different in dogs than has been previously reported in humans. Therefore: (a) canine models for studying the antiarrhythmic actions of commercial intravenous amiodarone would produce results complicated by severe hypotension; and (b) polysorbate 80 is not an inert substance, but is a potent cardiac depressant.     

Apolipoprotein-mediated transport of nanoparticle-bound drugs across the blood-brain barrier

Recent studies have shown that drugs that are normally unable to cross the blood-brain barrier (BBB) following intravenous injection can be transported across this barrier by binding to poly(butyl cyanoacrylate) nanoparticles and coating with polysorbate 80. However, the mechanism of this transport so far was not known. In the present paper, the possible involvement of apolipoproteins in the transport of nanoparticle-bound drugs into the brain is investigated. Poly(butyl cyanoacrylate) nanoparticles loaded with the hexapeptide dalargin were coated with the apolipoproteins AII, B, CII, E, or J without or after precoating with polysorbate 80. In addition, loperamide-loaded nanoparticles were coated with apolipoprotein E alone or again after precoating with polysorbate 80. After intravenous injection to ICR mice the antinociceptive threshold was measured by the tail flick test. Furthermore, the antinociceptive threshold of polysorbate 80-coated dalargin-loaded nanoparticles was determined in ApoEtm1Unc and C57BL/6J mice. The results show that only dalargin or loperamide-loaded nanoparticles coated with polysorbate 80 and/or with apolipoprotein B or E were able to achieve an antinociceptive effect. This effect was significantly higher after polysorbate-precoating and apolipoprotein B or E-overcoating. With the apolipoprotein E-deficient ApoEtm1Unc mice the antinociceptive effect was considerably reduced in comparison to the C57BL/6J mice. These results suggest that apolipoproteins B and E are involved in the mediation of the transport of drugs bound to poly(butyl cyanoacrylate) nanoparticles across the BBB. Polysorbate 80-coated nanoparticles adsorb these apolipoproteins from the blood after injection and thus seem to mimic lipoprotein particles that could be taken up by the brain capillary endothelial cells via receptor-mediated endocytosis. Bound drugs then may be further transported into the brain by diffusion following release within the endothelial cells or, alternatively, by transcytosis.