雷公藤甲素自微乳给药系统的制备及其质量评价

摘 要 目的：制备雷公藤甲素自微乳给药系统,并对其药剂学性质进行评价。方法: 通过溶解度试验及伪三元相图的绘制,筛选出雷公藤甲素自微乳的处方工艺;以自微乳平均粒径和自微乳化时间进一步优化雷公藤甲素自微乳处方;并对雷公藤甲素自微乳的药剂学性质进行考察。结果: 雷公藤甲素自微乳给药系统的最优处方为：油相中链甘油三酯（MCT）20%、表面活性剂聚氧乙烯蓖麻油（EL 35）40%、助表面活性剂聚乙二醇400（PEG 400）40%。自微乳化后平均粒径为43.48 nm,自微乳化时间小于30 s。结论:雷公藤甲素自微乳平均粒径和外观形态符合制剂学要求,具有较好的缓释效果,为进一步的药效学研究奠定基础。     

HPLC外标法测定复方樟脑乳膏中甘草次酸的含量

目的：建立HPLC外标法测定复方樟脑乳膏中的甘草次酸的含量。方法：采用Waters Atlantis T3(4.6*250mm, 5μm)色谱柱,以甲醇-水-冰醋酸(90∶10∶0.6)为流动相,检测波长为250nm,流速1.0mL/min,柱温30℃,进样量20μL。结果：甘草次酸在0.6048～3.6288μg浓度范围内与其峰面积的比值呈线性关系,低、中、高浓度平均回收率分别为99.8%(RSD=1.4%)。结论：采用HPLC法测定该品种中甘草次酸含量,方法科学合理,结果准确可靠,可用于复方樟脑乳膏中的甘草次酸测定。     

RP-HPLC法测定雷公藤微乳中雷公藤内酯甲的含量

目的采用RP-HPLC法测定雷公藤微乳中雷公藤内酯甲的含量。方法液相色谱条件为：Hypersil C18柱（150 mm×4.6 mm,5μm）,流动相为乙腈-水（90∶10）;流速1.0 ml/min;柱温为室温;检测波长210 nm;进样量20μl。结果雷公藤内酯甲在2.0～30.0μg/ml范围内线性关系良好（r=0.999 9）,平均回收率为（100.16±0.56）%（n=9）,3批样品中雷公藤内酯甲的平均含量分别为标示量的（98.92±0.92）%。结论该方法准确、灵敏,专属性强,重现性好,可作为雷公藤微乳中雷公藤内酯甲的含量测定方法。     

双藤巴布剂中青藤碱、雷公藤甲素的体外释放与体外透皮机制研究

目的:研究双藤巴布剂中青藤碱、雷公藤甲素的体外释放与体外透皮机制;比较以化学单体入药(青藤碱雷公藤甲素巴布剂,STP)与浸膏入药(双藤巴布剂,STEP)释放速率与透皮速率的差异。方法:通过释放度测定法测定体外释放度;通过Franze扩散池法测定药物的体外透皮性,皮肤为裸鼠背部皮肤。结果:STP与STEP中青藤碱、雷公藤甲素的体外释放以Higuchi方程拟合度较优(STP:r青=0.9955,r甲=0.9958;STEP:r青=0.9920,r甲=0.9963)。经皮渗透较好地拟合了零级动力学方程,青藤碱在STP、STEP中的r分别为0.9951与0.9926,透皮速率分别为21.729μg.cm-2.h-1与20.063μg.cm-2.h-1;雷公藤甲素在STP、STEP中的r分别为0.9942与0.9902,透皮速率分别为0.4783μg.cm-2.h-1与0.4168μg.cm-2.h-1。结论:青藤碱、雷公藤甲素在STP、STEP中的释放速率大于其经皮渗透速率,属于皮肤限速型经皮给药制剂。     

松萝酸自微乳的处方优化及质量评价

目的:制备松萝酸自微乳,优化其处方,评价其质量。方法:采用乳化法,以中链甘油三酯-单亚油酸甘油酯(1∶1,m/m)为油相,聚氧乙烯氢化蓖麻油为乳化剂,二乙二醇单乙基醚为助乳化剂,制备松萝酸自微乳。在溶解度试验和伪三元相图的基础上,以自乳化时间(t)、透光率(T)、药物平衡溶解度(S)、5 min和60 min时药物的累积溶出度(Q_(5 min)、Q_(60 min))作为评价指标,采用星点设计-响应面法优化微乳处方中油相占比和乳化剂-助乳化剂质量比(K_m)。同时对最优处方进行验证试验,并对其形态、粒径、载药量、溶出度等进行考察。结果:最优处方中油相占比为25%、K_m为2.0,即处方中混合油相、乳化剂、助乳化剂的质量比分别为25%、50%、25%;最优处方所制松萝酸自微乳的t、T、S、Q_(5 min)、Q_(60 min)分别为1.96 min、87.67%、5.67 mg/g、66.58%、76.73%(RSD均小于3%,n=3),与预测值的相对误差均小于4%(n=3)。松萝酸自微乳经水稀释后为球形乳滴,乳化后平均粒径为39.4 nm,平均载药量为4.55 mg/g,在p H 6.8磷酸盐缓冲液中Q_(90 min)为99.58%(n=3)。结论:所制松萝酸自微乳的质量符合相关要求。关键词松萝酸;自微乳;伪三元相图;星点设计-响应面法;质量评价     

糠酸莫米松微乳的制备工艺研究

目的研究糠酸莫米松微乳的处方及制备工艺。方法通过滴加法绘制假三元相图,考察各因素对微乳形成的影响,以微乳区面积、最大载油量为指标,考察了油相、水相、表面活性剂、助表面活性剂、温度等对表面活性剂体系相行为的影响。结果初步确定微乳的制备工艺:精密称取处方量的辛癸酸甘油酯、RH 40/1,2-丙二醇(Km=3)的混合表面活性剂、处方量的糠酸莫米松组成油相,在60℃下磁力搅拌至油相混合均匀且澄清加入处方量的水溶液(含苯扎氯铵为0.01%,枸橼酸0.09%,枸橼酸钠0.07%),磁力搅拌10 min,形成澄清透明、带蓝色乳光的微乳。结论优选的处方及制备工艺用于制备糠酸莫米松微乳,重复性好,性质稳定。     

正交试验优化复方粉背雷公藤凝胶剂处方

目的:优化复方粉背雷公藤凝胶剂处方。方法:以成型性、光泽度、均匀度、黏度、pH、涂展性、稳定性等组成的综合评分(总分15.0分)为指标,以卡波姆940、丙二醇、三乙醇胺及药材提取液等在处方中的用量为考察因素,设计正交试验优化复方粉背雷公藤凝胶剂处方,并进行验证试验。结果:优化处方为卡波姆940 1.0 g、氮酮2.0 g、亚硫酸氢钠0.4 g、提取液50 m L、丙二醇10g、三乙醇胺1.0 g,加水至100 g。验证试验结果显示所制凝胶综合评分均值为14.8(RSD=1.35%,n=3)。结论:优化处方所制复方粉背雷公藤凝胶成型性好,质量符合要求。     

雷公藤甲素透皮吸收特性的初步研究

为研究雷公藤甲素透皮吸收的过程及甘草次酸、甘草酸对于雷公藤甲素的透皮吸收是否有促进作用 ,采用静态扩散装置 ,用 HPLC测定扩散池中不同时间药物的含量 ,计算渗透系数和累积透皮吸收百分率。结果显示 ,雷公藤甲素的渗透系数为 0 .0 194cm/ h,7小时雷公藤甲素的累积透皮吸收百分率为 2 8%。提示雷公藤甲素的透皮吸收符合 Fick s扩散定律     

HPLC法测定复方雷公藤糖浆中雷公藤甲素的含量

目的：建立高效液相色谱法测定复方雷公藤糖浆中雷公藤甲素的方法。方法：采用DiamonsilC18（150mm×4．6mm,5μm）色谱柱分离,甲醇-水（46：54）为流动相,流速为1．0ml·min-1,检测波长为224nm,柱温为30℃,进样量为10μl。结果：雷公藤甲素在5．66～33．96μg·ml-1（r=0．9998）范围内质量浓度与峰面积呈良好的线性关系,其平均回收率为99．35％（RSD=1．02％,n=9）。结论：苓方法简便、灵敏、重复性好,可用于复方雷公藤糖浆中雷公藤甲素的质量控制。     

汉防已甲素壳聚糖微球的制备和质量研究

目的 对汉防己甲素壳聚糖微球的制备工艺和制得的微球的质量进行研究.方法 以壳聚糖为载体,采用乳化交联法制备汉防己甲素壳聚糖微球.在单因素考察的基础上,利用正交试验设计优化汉防己甲素壳聚糖微球制备工艺,并对制得微球的粒径,形态,工艺重复性,稳定性,体外突释情况等进行研究.结果 制得的微球的形态圆整,微球的平均粒径为(9.73±1.34)μm,粒径在9～12 μm的占总数的85%以上,载药量为(32.21±3.21)%,包封率为(40.33±5.32)%,最佳工艺条件重复性良好.结论 筛选的最佳处方工艺可制备性质优良的微球.     

Degraded and undegraded carrageenans and experimental gastric and duodenal ulceration

The prevention of histamine-induced gastric and duodenal ulceration in the guinea-pig has been examined using a series of undegraded and degraded carrageenans. Undegraded carrageenans were active at lower doses than degraded carrageenans. The high viscosity of the undegraded carrageenans in solution prevented their use in larger doses. Degradation of carrageenan without serious loss of sulphate, gives a product which allows the dose to be increased to an extent that its effect more than offsets the slight loss in activity caused by the degradation. No single feature of carrageenan structure can be related to anti-ulcer activity although degradation, and hence reduction of molecular size, generally reduces activity. Sulphate contents over 30% have little apparent effect on activity; κ-carrageenans were not consistently different in anti-ulcer activity from Λ-carrageenans. This contrasts with the antipeptic activity of carrageenans where κ-carrageenans are less active than their Λ-counter-parts. As with antipeptic activity, the degree of anti-ulcer activity is probably determined by a combination of structural features which includes molecular size and polyanionic properties.     

Affective and Anxiety Disorders and Alcohol and Drug Dependence:

Depression and anxiety frequently coexist in patients with substance use disorders. This clinically-oriented article examiens the relationship between these conditions and emphasizes data showing that substances of abuse can cause signs and symptoms of both depression and anxiety. These substance-related syndromes appear to have a different course and prognosis than uncomplicated, independent anxiety and major depressive disorders, and clinicians should consider the role of alcohol and other drugs in all patients presenting with these complaints. The authors will also outline an approach for diagnosing and managing patients with the combination of a substance use and depressive or anxiety disorder.     

Alcohol and Substance Use and Abuse in Women and Children

No abstract available for this article.     

Glucosidase and fucosidase inhibitors and Advances in nucleosides and nucleotides.

The American Chemical Society Symposium "Glucosidase and fucosidase inhibitors" took place on 1 April 1998 and was organized by Professors Zbigniew J Witczak (UConn, School of Pharmacy, CT, USA), Kuniaki Tatsuta (Waseda University, Tokyo, Japan) and Waldemar Priebe, MD (Anderson Cancer Center, University of Texas, USA). Professor Witczak provided introductory remarks including the status of existing glucosidase inhibitors, and chaired the morning session, which consisted of six lectures. The symposium was well received, and was particularly attractive for those interested in networking, as attendance was about sixty. In addition, some participants and attendees presented posters on the subject during the regular poster session organized by the Division of Carbohydrate Chemistry.