克疱乳膏和酞丁安搽剂治疗单纯疱疹的疗效

目的：观察克疱乳膏治疗单纯疱疹的疗效和安全性。方法：选择了４２例单纯疱疹患者，分别接受克疱乳膏（ｎ＝２５）和酞丁安搽剂（ｎ＝１７）局部治疗，ｑｉｄ，疗程１￣２周。结果：克疱乳膏治疗组和酞丁安搽剂治疗组的有效率分别为１００％和６４．７％（Ｐ〈０．０１），两组均未见明显的不良反应。结论：克疱乳膏治疗口唇疱疹和生殖器疱疹有很好的疗效。     

酞丁安滴眼液的制备及其稳定性试验

本文提供了酞丁安滴眼液的改良配方和制备方法并经８批样品质量量检验和稳定性考察。结果表明，按本文方法生产的酞丁安滴眼液质量稳定，贮存２年各项检测指标仍符合药典标准，解决了本品放置易变色，结块等质量质量问题。     

维A酸乳膏联合重组人干扰素α-2b乳膏与酞丁安乳膏治疗面部扁平疣疗效观察

目的 观察维A酸乳膏联合重组人干扰素α-2b乳膏与酞丁安乳膏治疗面部扁平疣临床效果。方法 扁平疣患者116例随机分为治疗组58例、对照组58例,治疗组使用0.1%维A酸乳膏联合干扰素乳膏与酞丁安乳膏外涂,对照组使用维A酸乳膏联合干扰素乳膏外涂。结果 经过6周的临床观察,治疗组痊愈率91.38%,对照组痊愈率63.79%,两组痊愈率对照差异统计学意义(P<0.05),在治疗过程中有部分患者出现局部刺激反应,停药或隔日用药后症状消失。结论 维A酸乳膏联合重组人干扰素α-2b乳膏与酞丁安乳膏治疗面部扁平疣有较好的疗效。     

酞丁安霜剂的研制

本文通过用二甲基酰胺作助溶剂制成了２％酞丁安霜剂用于临床，并制定了含量测定方法，进行了回收率和稳定性实验，均获得满意结果。     

高效液相色谱法测定酞丁安搽剂的含量

目的 :建立高效液相色谱法内标法测定酞丁安搽剂中酞丁安含量的方法。方法 :采用KF -C18柱 ,以布美他尼为内标物 ,甲醇 水 (75∶2 5 )为流动相 ,流速 1.0mL·min-1,检测波长为 347nm。结果 :酞丁安浓度在 4～ 36mg·L-1范围内呈良好线性关系 (r =0 .9999)。结论 :本法简便 ,快速 ,结果准确 ,适用于该制剂的质量分析检验。     

酞丁安对实验性单疱角膜炎的作用

酞丁安(Tai-Ding-An,TDA)系我国自己设计合成的一个缩氨基硫脲类化合物。实验及临床研究证明具有抗沙眼衣原体与抗疱疹病毒作用。本文报道酞丁安对兔实验性单疱角膜炎的治疗作用。     

酞丁安对实验性单疱角膜炎的作用

The antiherpes virus effects of Tai-Ding-An (TDA) were studied in experimental herpetic keratitis in rabbits. Topical treatment With 1% or 2% TDA ointment 4 times daily was initiated 48h after virus inoculation in rabbits. Significant efficacy was obtained with herpetic epithelial keratitis. Responses to treatment with 2% TDA ointment were similar to those with 0.1% CC ointment. But 0.5% TDA ointment showed no significant effect. 1% TDA ointment was also not efficacious in the topical treatment of herpetic stromal keratitis in rabbits.     

酞丁安含量及色谱纯度的HPLC测定

建立了HPLC法检测酞丁安含量和色谱纯度.采用ODS-3色谱柱,流动相为乙腈-0.75%甲酸溶液（30：70）,检测波长280nm与347nm.酞丁安在0.5～400μg/ml范围内线性关系良好（r=0.9999）.检测限为1.0ng.     

高效液相色谱法测定酞丁安滴眼液的含量

目的建立高效液相色谱法测定酞丁安滴眼液中酞丁安含量的方法。方法采用Phenom enex C18柱,以甲醇:0.01m ol.L-1磷酸二氢钠溶液溶液(60∶40)为流动相,流速为1.0mL.m i-n 1,柱温为30℃,检测波长为347nm。结果酞丁安在4~36μg.mL-1范围内峰面积与进样量呈良好线性关系(r=0.9999),回归方程为y=0.0127x 0.3882,平均回收率为100.59%,RSD=0.91%,日内稳定性RSD=1.3%。结论本法简单,准确,快捷,可作为酞丁安滴眼液中酞丁安的含量测定方法。     

复方莪术油乳膏外用对大鼠长期毒性实验研究

目的:研究外用制剂复方莪术油乳膏对实验大鼠长期连续经皮给药的毒性反应,为其临床使用安全提供实验依据。方法:将60只SD大鼠按随机数表法分为空白对照(乳膏基质)组和完整皮肤及破损皮肤的复方莪术油乳膏低、高剂量(5%、10%)组,共5组,每组12只,♀♂各半。每日涂抹药2次,连续给药92 d后分别观察各组大鼠的一般状况,检测体质量、血常规(白细胞、红细胞、血红蛋白、淋巴细胞比值等)及血液生化各项指标(天门冬氨酸转氨酶、丙氨酸转氨酶、血清前白蛋白等),并对大鼠脏器进行系统观察、脏器系数的计算、组织病理学检查。结果:与空白对照组比较,复方莪术油乳膏各组中除完整皮肤低剂量组的血红蛋白降低,破损皮肤高剂量组的血红蛋白降低、淋巴细胞比值及血清前白蛋白水平均升高外(P<0.05),其余指标差异均无统计学意义(P>0.05);病理观察结果表明,其对主要脏器未见明显毒性。结论:复方莪术油乳膏对实验大鼠无明显的长期毒性。     

他扎罗汀倍他米松乳膏对小型猪经皮给药后的系统吸收及其相互作用研究

目的：通过与已上市单方他扎罗汀凝胶（tazarotene gel）和二丙酸倍他米松乳膏（betamethasone dipropionate cream）比较，研究新的复方制剂他扎罗汀倍他米松乳膏（tazarotene and betamethasone dipropionate cream，简称"复方"）对小型猪经皮给药后的药物吸收以及药物组分间吸收的相互影响。方法：将18只小型猪随机分入复方组、他扎罗汀凝胶组和二丙酸倍他米松乳膏组，每组6只。小型猪按20%的体表面积2 mg·cm^-2给予相应组别的药物，并在给药后24 h清除药物。分别于给药前和给药后不同时间点采集血样。高效液相色谱-串联质谱（liquid chromatography-tandem mass spectrometry，LC-MS/MS）法测定血浆中他扎罗汀及其代谢物他扎罗汀酸和/或二丙酸倍他米松及其代谢物倍他米松的浓度。DAS 2.1.1软件进行药代动力学（pharmacokinetic，PK）参数计算并统计分析。结果：复方他扎罗汀倍他米松乳膏与单方他扎罗汀凝胶中的他扎罗汀均不易透过小型猪皮肤到达血液，系统吸收非常低，而复方组血浆中的他扎罗汀及其活性代谢产物他扎罗汀酸较单方组更低；复方他扎罗汀倍他米松乳膏和二丙酸倍他米松乳膏中的二丙酸倍他米松几乎不透过小型猪皮肤到达血液，系统吸收非常低，其中复方组与单方组中二丙酸倍他米松及其代谢产物倍他米松到达血液的量未见明显的差异。结论：复方制剂中他扎罗汀对二丙酸倍他米松的系统吸收未产生相互作用，而二丙酸倍他米松对他扎罗汀的系统吸收产生了有益的相互作用，有利于用药安全。     

黄芪甲苷乳膏对小鼠光老化皮肤的保护作用

目的 探讨皮肤外用黄芪甲苷对紫外线(UV)照射引起的小鼠光老化皮肤的影响.方法 BALB/c小鼠84只,随机分成6组:模型组(A组)、模型+基质组(B组)、模型+黄芪甲苷低剂量组(C组)、模型+黄苠甲苷中剂昔组(D组)、模型+黄芪甲苷高剂量组(E组)、正常对照组(F组),每组14只.模拟日光紫外线长期照射,形成皮肤光老化小鼠模型.C组、D组、E组照射同时外用黄芪甲苷乳膏.用组织切片HE染色、间苯二酚-碱性品红(Weigert)染色观察皮肤结构改变;以生化分析方法 测定羟脯氨酸(HYP)含量.结果 与F组比较,A组小鼠皮肤组织HYP含量明显降低(P<0.01),HE染色、Weigert染色病理切片呈现光老化状态;与A组比较,E组小鼠皮肤组织HYP含量升高明显(P<0.01),HE染色、Weigert染色病理切片显示抗光老化改变.结论 黄苠甲苷乳膏对紫外线照射引起的小鼠皮肤光老化具有保护作用.     

铁箍散乳膏对大鼠皮肤疮疡的药效学研究

目的研究铁箍散乳膏对大鼠皮肤疮疡的药效学评价。方法采用在皮肤缺损(人为切口)部位皮下注射金黄色葡萄球菌悬液建立大鼠皮肤疮疡模型,以莫匹罗星软膏为阳性对照药物,观察铁箍散乳膏对各项相关指标的影响。结果铁箍散乳膏可显著降低大鼠创面愈合积分值、增加分泌物中溶菌酶的含量和降低血清中白介素IL-2因子的含量,且与阳性对照药物比较,差异无统计学意义。结论铁箍散乳膏具有促进创面愈合、提高机体免疫力和抗感染能力的功效。     

Comedogenicity of squalene monohydroperoxide in the skin after topical application

The comedogenicity of squalene peroxides was examined on the rabbit ear skin after topical application of squalene-monohydroperoxide (Sq-OOH), the initial product when squalene was irradiated with UV-A. Since comedogenic products from UV-irradiated squalene were extracted with methanol solution, we isolated Sq-OOH by reverse-phased HPLC with a methanol mobile phase solvent. The degree of comedogenic reaction induced by Sq-OOH was higher than that of well-known comedogenic cosmetic ingredients. Unlike two other mono-peroxides, tert-butyl hydroperoxide and cumene-mono-hydroperoxide, Sq-OOH induced comedo-formation in the rabbit ear skin. However, the comedogenicity of reduced Sq-OOH, squalene-hydroxide (Sq-OH) and squalene itself was lower than that of Sq-OOH. These results indicate that Sq-OOH is a potent comedogenic mono-hydroperoxide chemical to rabbit skin.     

Metabolism of aldrin to dieldrin by rat skin following topical application

Metabolism of the pesticide aldrin to dieldrin in the rat was studied following topical and ip administration of 0.1-10 mg aldrin/kg body weight. When aldrin was applied topically to the dorsal skin at a dose of 10 mg/kg body weight, absorption was less efficient than after ip administration; lower blood levels of aldrin and dieldrin were seen and peak dieldrin levels were delayed. After ip administration of 1 or 10 mg aldrin/kg body weight, dieldrin was found at similar concentrations in the dorsal and ventral skin 7 hr later, whereas 7 hr after topical administration of 10 mg aldrin/kg, the dieldrin concentration in the skin at the dorsal site of application was four times higher than that at a ventral skin site. Similar differences in dieldrin concentrations between dorsal and ventral skin persisted throughout the 7-hr period following topical application. The results indicate that topically applied aldrin is metabolized to dieldrin in the skin during absorption, but the overall proportion of metabolism that takes place in the skin is small compared with the contribution of the liver. Dieldrin was not detected in the ventral skin remote from the application site 1 hr after topical application of aldrin, whereas a dieldrin concentration of 2.2 nmol/g was detected in the skin of the application site at this time; more than 99% of this dieldrin was probably formed locally by dermal metabolism of percutaneously absorbed aldrin. The efficiency of conversion of applied aldrin to dieldrin decreased with increasing aldrin dose in the range 0.1 to 10 mg/kg.     

Safety studies of topical imiquimod 5% cream on normal skin exposed to ultraviolet radiation

BACKGROUND: Imiquimod 5% topical cream is an immune response modifier that induces interferon alpha and interleukin-12, and exhibits antiviral and tumor-inhibiting properties. It is currently available for treatment of genital and perianal warts. Three randomized, open-label or assessor-blinded, placebo-controlled studies were carried out to assess its safety on normal white skin exposed to ultraviolet radiation (UVR). METHODS: Healthy white volunteer adult subjects between the ages of 18 and 60 years with skin types I, II or III (Fitzpatrick Scale, US Federal Register 43:38260, 1978) were invited to participate. Imiquimod 5% cream (each dose approximately 0.1-0.2 ml) was compared with placebo cream. Two preliminary studies assessed the potential photosensitizing properties of the drug, and the third study added measurement of sunburn cell counts (SBC) and deoxyribonucleic acid (DNA) pyrimidine dimer (PD) formation. The three studies were: a 6-week standard photocontact allergenicity bioassay; a 4-day standard phototoxicity bioassay; and a 4-week photodamage study using biopsy sample analyses to determine SBC or PD frequency. RESULTS: Imiquimod had no detectable potential for inducing either photocontact allergy (n=115) or phototoxicity (n=20). The final study further assessing photodamage potential of imiquimod included 44 subjects. There were no significant differences between imiquimod vs. the control (no drug+UVB) for SBC counts (mean 0.88 vs. 0.93), or PD frequency (mean 60.86 vs. 70.03). CONCLUSIONS: Results from the two preliminary safety studies suggest that imiquimod 5% cream does not possess a detectable photosensitizing potential in humans. Furthermore, topical imiquimod did not enhance UVR-induced damage to epidermal cells or DNA.     

Effect of mometasone furoate by topical application on allergic rhinitis model in rats

The effects of mometasone furoate on experimental allergic rhinitis in rats were studied in comparison with that of fluticasone propionate. Topical application of both drugs inhibited dose-dependently the increase of nasal symptoms (sneezing and nasal rubbing) after antigen challenge to the nasal cavity of actively sensitized rats. Mometasone furoate and fluticasone propionate at concentrations of 0.01 or 0.1% significantly inhibited both nasal rubbing and sneezing 1 h after topical application of both drugs. The relative potencies of mometasone furoate in nasal rubbing and sneezing compared to fluticasone propionate were 5.01 and 6.87, respectively. Mometasone furoate (0.02%) and fluticasone propionate (0.1%) significantly inhibited the increase of antigen-induced nasal rubbing even 6 h after topical application, indicating that both drugs have a long-lasting effect.     

Local and systemic tolerance of flutrimazole skin creams following single and repeated topical application in healthy volunteers.

A double-blind, randomized phase I study was performed in 21 healthy volunteers to evaluate the dermal tolerance of skin creams containing 1% and 2% 1-[(2-fluorophenyl)(4-fluorophenyl)phenylmethyl]-1H-imidazole (flutrimazole, UR-4056, CAS 119006-77-8) or only the excipient, versus a commercial skin cream containing 1% clotrimazole. The study was carried out using the patch-test procedure performed in three stages: 1. single application in the back skin; 2. induction period (usage test) using three skin areas on the volar side of the forearm of each subject, where skin cream samples were applied once a day for a period of three weeks; and 3. after a wash-out period of two weeks, challenge applications in the back and forearm skin. The systemic tolerance of the formulations was also tested. There was no evidence of allergic sensitization after the application of flutrimazole creams, or their excipients, with signs of mild and doubtful skin reactions being observed in few subjects with all formulations. Furthermore, no systemic side effects after topical administration were detected throughout the study.     

Improvement of acne vulgaris by topical fullerene application: unique impact on skin care

Oxidative stress plays a major role in acne formation, suggesting that oxygen radical scavengers are potential therapeutic agents. Fullerene is a spherical carbon molecule with strong radical sponge activity; therefore, we studied the effectiveness of fullerene gel in treating acne vulgaris. We performed an open trial using a fullerene gel twice a day; at 4 and 8 weeks, the mean number of inflammatory lesions (erythematous papules and pustules) significantly (P < 0.05) decreased from 16.09 ± 9.08 to 12.36 ± 7.03 (reduction rate 23.2%) and 10.0 ± 5.62 (reduction rate 37.8%), respectively. The number of pustules, consisting of accumulation of neutrophils, was significantly (P < 0.05) decreased from 1.45 ± 1.13 to 0.18 ± 0.60 (reduction rate 87.6%), and further in vitro assays of sebum production in hamster sebocytes revealed that 75 μM polyvinylpyrrolidone-fullerene inhibits sebum production, suggesting that fullerene suppresses acne through decreasing neutrophil infiltration and sebum production. After treatment for 8 weeks, the water content of the skin significantly (P < 0.05) increased from 51.7 ± 7.9 to 60.4 ± 10.3 instrumental units. Therefore, the fullerene gel may help in controlling acne vulgaris with skin care benefit. FROM THE CLINICAL EDITOR: Fullerenes, spherical carbon cages with strong oxygen radical scavenging, with formulated into a gel and used to successfully treat acne vulgaris, an inflammatory disease associated oxidative stress.