复方甲硝唑口腔复合膜的制备及质量控制

复方甲硝唑口腔复合膜以ＰＶＡ＿（１７～８８）－ＣＭＣＮａ（２：１）为药膜材料、ＰＶＡ＿（１７～８８）为覆盖膜材料，采用涂膜法制备，用紫外分光光度法测定含量平均回收率１０２．９％，Ｒ８０＝１．１６％。     

Efectsofmoxonidineinjectedintorostralventrolateralmedulaonbloodpressure,heartrate,andrenalsympatheticnerveactivityinrats

目的：观察延髓腹外侧头端（ＲＶＬＭ）注射莫索尼定（Ｍｏｘ）对麻醉大鼠血压（ＢＰ）、心率（ＨＲ）及肾交感神经放电（ＲＳＮＡ）的影响．方法：麻醉大鼠ＲＶＬＭ注射１μＬＭｏｘ１，１０，１００μｍｏｌ·Ｌ－１，同步记录ＢＰ，ＨＲ及ＲＳＮＡ．结果：Ｍｏｘ１，１０，１００μｍｏｌ·Ｌ－１分别使ＢＰ从１３９±１０ｋＰａ降至１３０±１７ｋＰａ（Ｐ＜００５），１３８±１８ｋＰａ至１１４±１５ｋＰａ（Ｐ＜００１），ａｎｄ１３９±１９ｋＰａ至９４±１７ｋＰａ（Ｐ＜００１）．Ｍｏｘ不影响ＨＲ．Ｍｏｘ１μｍｏｌ·Ｌ－１增加ＲＳＮＡ５０％（Ｐ＜００５），１０μｍｏｌ·Ｌ－１对ＲＳＮＡ无影响（Ｐ＞００５），１００μｍｏｌ·Ｌ－１则降低ＲＳＮＡ２３％（Ｐ＜００５）．在缓冲神经切断大鼠，Ｍｏｘ１０μｍｏｌ·Ｌ－１抑制ＲＳＮＡ５０％（Ｐ＜００５），明显不同于缓冲神经完整的动物（Ｐ＜００１）．结论：麻醉大鼠ＲＶＬＭ注射Ｍｏｘ可降低ＢＰ，但不影响ＨＲ，且ＲＳＮＡ变化与其降压作用并不平行     

IHC-66对离体豚鼠心肌细胞慢反应电活动的影响

目的：为进一步观察ＩＨＣ－６６的电生理特性，探讨其抗心律失常的作用机制。方法：采用离体豚鼠窦房结、乳头状肌及部分除极化乳头状肌标本，观察了３，６－ｄｉ（ｄｉｍｅｔｈｙｌａｍｉｎｏ）－ｄｉｂｅｎｚｏｐｙｒｉｏｄｏｎｉｕｍｏｆｆｅｒｉｃＥＤＴＡ（ＩＨＣ－６６）对不同类型心肌细胞电活动的影响。结果：ＩＨＣ－６６１０μｍｏｌ·Ｌ－１使窦房结细胞动作电位４相除极速率（ＳＰ４）降低１１．４２％、增加动作电位复极９０％时程（ＡＰＤ９０）１８％、降低零相最大上升速率（Ｖｍａｘ）４７％、使部分除极化乳头状肌细胞动作电位（ＡＰ）之ＡＰＤ９０、动作电位复极５０％时程（ＡＰＤ５０）分别缩短９％、１３％，Ｖｍａｘ降低５８％，同时，ＩＨＣ－６６（１０、３０、５０μｍｏｌ·Ｌ－１）呈剂量依赖性降低Ｂａ２＋（２ｍｍｏｌ·Ｌ－１）诱发的自发性动作电位振幅（ＡＰＡ）与Ｖｍａｘ，缩短ＡＰＤ５０、ＡＰＤ９０，明显减慢自发性电活动的频率。结论：ＩＨＣ－６６的电生理学作用与其对慢内相电流的阻滞有关。     

内源性腺苷和KATP通道介导缺氧窦房结起搏细胞的电生理效应

观察腺苷脱氨酶（ＡＤａｓｅ），８－苯茶碱（８－ＰＴ）和格列苯脲（Ｇｌｉ）在豚鼠缺氧窦房结起搏细胞的电生理效应。方法：以充１００％氮和无糖的Ｋ－Ｈ液灌流豚鼠窦房结２０ｍｉｎ引起其缺氧。用玻璃微电极记录起搏ＭＤＰ，ＡＰＡ，ＡＰＤ９０，Ｖｍａｘ，但减小ＶＤＤ等动作电位参数。结果：缺氧增加起搏细胞ＡＰＡ，ＭＤＰ和Ｖｍａｘ，但碱小ＶＤＤ和ＲＰＦ。Ａｄａｓｅ １０Ｕ．Ｌ＾－＾１，８－ＰＴ０．１μｍｏｌ．Ｌ＾－     

对HBVHBeAg/HBeAb血清的探讨

对１０１例ＨＢＶ血清中ＨＢＶＤＮＡ进行检测，发现４５例ＨＢｅＡｇ（＋）／ＨＢｅＡｂ（－）血清检出８８．８８％ＨＢＶＤＮＡ（＋），５６例ＨＢｅＡｂ（－）／ＨＢｅＡｂ（＋）血清检出４６．４２％ＨＢＶＤＮＡ（＋），ＨＢｅＡｇ／ＨＢｅＡｂ与ＨＢＶＤＮＡ关系显著性检验，差别无显著性（χ２＝１．１６，Ｐ＞０．０５），ＨＢｓＡｇ滴度与ＨＢｅＡｇ检出无相关性（ｒ＝０，Ｐ＞０．０５）。     

阿斯匹林与维拉帕米单用和合用对兔血液流变性的影响

观察阿斯匹林（Ａｓｐ）与维拉帕米（Ｖｅｒ）单用及合用对免血液流变性的影响。结果表明：ｉｖ生理盐水，Ａｓｐ１．２５ｍｇ·ｋｇ－１和Ｖｅｒ０．０５ｍｇ·ｋｇ－１对兔血液流变性各项指标均无明显影响；ｉｖＡｓｐ２．５、５ｍｇ·ｋｇ－１和Ｖｅｒ０．１、０．２ｍｇ·ｋｇ－１后，血液粘度（ＢＶ），血浆粘度（ＰＶ）和红细胞比积（ＨＣＴ）明显降低，红细胞电泳率（ＥＥＭ）显著提高，且呈明显量效关系；Ａｓｐ１．２５，２．５ｍｇ·ｋｇ－１和Ｖｅｒ０．０５，０．１ｍｇ·ｋｇ－１合用，呈明显协同效应。推测ＡｓＰ，Ｖｅｒ降低ＢＶ可能与ＰＶ，ＨＣＴ下降和ＥＥＭ提高有关。     

丙型肝炎在血液透析患者中感染状况分析

采用ＥＬＩＳＡ法对１４６例血液透析（ＨＤ）患者进行了抗－ＨＣＶ的检测，并与４５０例献血员做了对比分析，结果抗－ＨＣＶ阳性检出率分别为５５．５％与７．１％，两者相差非常显著（Ｐ＜０．０１）。同时对８１例抗－ＨＣＶ阳性ＨＤ患者进行ＨＢｓＡｇ、ＨＢｅＡｇ及抗－ＨＢＣ测定，结果表明：７４．１％（６０／８１）抗－ＨＣＶ阳性ＨＤ患者ＨＢＶ检测阳性。追访部分ＨＤ者发现：抗－ＨＣＶ阳性合并ＨＢＶ重叠感染者，ＡＬＴ升高者占８３．３％（５１６）。ＡＬＴ值多波动在０．０１４～０．０２８μｍｏｌ·ｓ￣（－１）。提示：乙型肝炎合并丙型肝炎感染者，可加速对肝脏的损伤作用。     

胸腺α1和干扰素α1b联合治疗慢性病毒性乙型,丙型肝炎

选取慢性病毒性乙型肝炎５０例及丙型肝炎２０例，应用胸腺α１和干扰素α１ｂ联合治疗６个月，治疗后其ＰＣＲ－ＨＢＶ－ＤＮＡ的阴转率为６８．０％，ＰＣＲ－ＨＣＶ－ＲＮＡ的阴转率为７０．０％，较对照组（干扰素α１ｂ）的ＰＣＲ－ＨＢＶ－ＤＮＡ阴转率４４０％及ＰＣＲ－ＨＣＶ－ＲＮＡ的阴转率３０．０％为高（Ｐ〈０．０５）。通过治疗前，后检测Ｔ细胞亚群，ｓＩＬ－２Ｒα及ＴＮＦα发现，治疗前ＣＤ８，ｓＩＬ－２Ｒα和     

绞股蓝总皂甙对单个豚鼠心室肌细胞的钙、钠、钾电流及动作电位的影响

目的研究绞股蓝总皂甙（ＧＰ）对成年豚鼠单个心室肌细胞的动作电位（ＡＰ）、Ｌ－型钙通道电流（ＩＣａ）、快钠通道电流（ＩＮａ）以及内向整流钾通道电流（ＩＫ１）的影响。方法膜片钳全细胞记录。结果５０ｍｇＬ－１ＧＰ能使动作电位时程（ＡＰＤ９０）由给药前的（７０８±２４）ｍｓ缩短到给药后的（３９６±１６）ｍｓ（Ｐ＜０．０１），抑制率５８．１％，动作电位幅值（ＡＰＡ）由给药前的（１２１±７．２）ｍＶ降到给药后的（８６±８．６）ｍＶ（Ｐ＜０．０１），抑制率２４．１％，静息膜电位无明显影响；５～５０ｍｇＬ－１的ＧＰ能浓度依赖性阻滞ＩＣａ和ＩＮａ，但对ＩＫ１无明显影响。结论ＧＰ对缺血心肌的保护作用在于减少“钙超载”和抑制异常兴奋性的产生。     

美西律对海马脑片突触功能缺氧损伤的保护作用

记录大鼠海马脑片ＣＡ１区锥体细胞的群锋电位（ＰＳ）和突触前排放（ＰＶ），缺氧３ｍｉｎ时对照组ＰＳ幅度下降至０．４±０．４ｍＶ，而提前１ｈ灌流美西律（Ｍｅｘ）１０或１００μｍｏｌ·Ｌ＾－１组ＰＳ仅下降至１．２±１．２或１．５±０．４ｍＶ。复氧３０ｍｉｎ后对照组ＰＳ恢复率为１１％，Ｍｅｘ１０或１００μｍｏｌ·Ｌ＾－１组分别为４８％和６５％。可见Ｍｅｘ减慢缺氧时ＰＳ下降过程，加速度复氧时ＰＳ恢复过程，…     

正交试验优选复方儿茶止泻膜的成膜材料

目的:优选复方儿茶止泻膜的成膜材料。方法:以膜剂的外观质量和体外透皮实验中儿茶素的累积释放量为评价指标,以聚乙烯醇(PVA)1750、羧甲基纤维素钠(CMC-Na)、白及胶用量为考察因素,采用正交试验优选最佳成膜材料。结果:最佳成膜材料为PVA17509mL、CMC-Na2mL、白及胶4mL。结论:改进后的复方儿茶止泻膜较单用白及胶作为成膜材料的原制剂,外观质量更好,体外透皮吸收含量更高,能够显著改善原制剂的不足之处。     

紫草膜剂的制备及左旋紫草素的含量测定

目的:确定并优化紫草膜剂的处方工艺,建立稳定可靠的左旋紫草素含量测定方法,对紫草膜剂进行质量控制。方法:以紫草提取物为原料药,采用聚乙烯醇为成膜材料,加入甘油、羧甲基纤维素钠制备紫草膜剂。通过单因素实验与正交试验,以膜的机械性能为评价指标,筛选优化处方工艺。采用高效液相色谱法对膜剂中主要活性成分左旋紫草素的含量进行测定。结果:PVA的种类与用量,增塑剂甘油的用量及载药量均会明显影响膜剂的成型与机械性能。优化处方中成膜材料聚乙烯醇205S与540S的用量比为1∶3,甘油的用量为7.6%,聚乙烯醇:紫草提取物为9∶1。含量测定的HPLC方法日内、日间精密度分别为0.77%与0.74%,加样回收率为99.67%(n=9),重复性好。结论:所制备的紫草膜剂含量均匀,机械性能良好,符合膜剂质量要求。     

正交设计法优化创伤涂膜剂的成膜溶液

目的 探讨创伤涂膜剂成膜溶液的优化处方.方法 选择聚乙烯醇(PVA)为成膜材料,采用正交试验设计方法,以PVA聚合度(A)、PVA浓度(B)和甘油含量(C)为考察因素,通过对成膜时间、黏度、水蒸汽透过率、抗张强度和断裂伸长率等指标的综合评价,筛选出最优成膜溶液组成.结果 正交试验极差分析和方差分析结果表明,三个因素对成膜性能的影响次序由大到小为:A>B>C.结论 最优水平搭配为A1B2C2,即由8%高黏度PVA和2%甘油组成的涂膜剂基质成膜性能最优.     

褐藻胶浆在皮肤外用制剂中的应用——Ⅰ.涂膜材料的研究

本文以自行研制的褐藻胶浆作成膜材料,制备了药物涂膜剂,并以褐藻酸钠,聚乙烯醇的相同药物制剂作对照,进行了抑菌,稳定性,药物释放等实验研究。结果表明,褐藻胶浆是一较理想的皮肤外用制剂新辅料。以该原料制备的制剂治疗渗出性皮肤病,疗效满意。     

Evaluation of glucan/poly(vinyl alcohol) blend wound dressing using rat models

Aqueous mixture of beta-glucan and poly(vinyl alcohol) (PVA) was cast into films and dried at 110 degrees C without chemical crosslinking. The content of glucan in the film varied from 7% to 50%. The hydrophilicity of the resulting films was evaluated with swelling tests, wet area diffusion tests, and water vapor transmission tests. The swelling ratio, the wetting ratio, and the water vapor transmission rate increased with the glucan content. When contacting water, glucan was released, and the percent release of glucan increased with the glucan content. The addition of glucan made the film more ductile than pure PVA. The results of hemocompatibility test showed no significant effect on the activated partial thromboplastin time (APTT) and thrombin time (TT) and minor adsorption of human serum albumin (HSA). On observing the wound healing of rat skin, the healing time was shortened by 48% using PVA/glucan film comparing to cotton gauze. Therefore, a wound dressing made of PVA/glucan can greatly accelerate the healing without causing irritation.     

Design of freeze-dried Soluplus/polyvinyl alcohol-based film for the oral delivery of an insoluble drug for the pediatric use

Abstract

Spironolactone (SL) is a poorly water-soluble drug. Being poorly soluble affects its dissolution rate which in turn affects its oral bioavailability. This work aimed to prepare freeze-dried SL-Soluplus®/polyvinyl alcohol (PVA) oral thin film in an attempt to enhance the drug solubility on one hand and at the same time prepare a solid dosage form convenient for the pediatric use. SL-Soluplus®/PVA films were prepared using polyethylene glycol 400 (PEG 400) as a plasticizer applying the solvent-casting technique. The prepared films were evaluated for their thickness, tensile strength, and in vitro dissolution studies. Box–Behnken design (17 runs) was applied to optimize the effects of the formulation variables on the film properties. The optimized film formulation was freeze-dried after casting so as to enhance the drug dissolution. Moreover, the optimized freeze-dried film was re-characterized in vitro and evaluated in vivo in human volunteers to investigate its palatability and satisfaction. The results showed that the optimized formulation composed of 10% polymer concentration containing Soluplus®:PVA (0.33:0.66) and plasticized with 30% PEG 400 possessed the highest desirability value (0.836). Freeze-drying of the optimized formulation succeeded to improve SL in vitro dissolution due to the preparation of a more porous film compared to the non-freeze-dried one. In vivo evaluation of the optimized freeze-dried film showed high satisfaction among the participating volunteers concerning the ease of administration and sensation thereafter, where all the film specimens dissolved without the need for water and no film residues remained in the mouth following film dissolution. In conclusion, freeze-dried Soluplus®/PVA-based oral thin film proved to be a successful carrier for the oral delivery of insoluble drugs like SL for pediatrics.     

白及胶—聚乙烯醇后马托品眼用膜的药效观察

用白及胶,聚乙烯醇（１７－８８,０５－８８）按不同质量比分别制得氢溴酸后马托品眼用膜,以２％氢溴酸后马托品滴眼液为对照,成年大耳白兔作实验对象,进行刺激性和药产学实验,结果表明,白及胶－聚乙烯醇（１７－８８）混合载药膜质地更加柔软,散瞳效果理想,刺激性及缓释作用优于单纯的聚乙烯醇载药膜。     

溶菌酶眼用膜剂的制备及相关性质考察

目的制备溶菌酶眼用膜剂,为感染性眼部疾病提供新的药物治疗。方法以脱膜性、粘附性、柔韧度、膜性能等相关指标为依据,筛选处方,采用涂膜法制备了溶菌酶眼用膜剂,并考察眼用膜剂的体外释放特性及眼部刺激性。结果以PVA124为膜材、甘油为增塑剂制备的眼用膜剂,8 h时累计释放量达到80%以上,对家兔眼部单次及多次给药后,根据评分标准,评分均为0,多次给药后的组织病理切片表明,给药组家兔虹膜有轻微充血。结论溶菌酶眼用膜剂制备工艺简单,符合眼部用药标准。     

正交试验优化复方奥硝唑阴道生物黏附膜处方

目的:优化复方奥硝唑阴道生物黏附膜的处方。方法:以辅料酸性壳聚糖浓度、明胶浓度、聚乙烯醇(PVA)浓度及主药浓度为考察因素,以生物黏附力为考察指标,采用正交试验设计优化处方,并测定优化处方的生物黏附力和体外释放度。结果:优化的处方组成是酸性壳聚糖浓度为2.0%,明胶浓度为1.0%,PVA浓度为1.0%,主药浓度为2.0%。优化处方所制3批膜剂的平均生物黏附力为2.1N·cm-2,12h时平均体外累积释放率大于89%。结论:按照优化处方制备的复方奥硝唑阴道生物黏附膜具有较好的生物黏附力和缓释性。     

Novel Starch‐Based PVA Thermoplastic Capsules for Hydrophilic Lipid‐Based Formulations

For decades, gelatin has been used in the rotary die process as a shell‐forming material of soft capsules because of its unique physicochemical properties. However, with respect to the encapsulation of comparatively hydrophilic lipid‐based formulations, gelatin has one considerable drawback: Immediately after production, the capsule shell contains a large amount of water (up to 35%). There is the potential for water to migrate from the capsule shell into the formulation, which will lead to a decrease in drug solubility and, in turn, the potential for drug crystallization. The present study introduces a novel capsule material that was obtained from extrusion. The starch‐based polyvinyl alcohol thermoplastic capsules (S‐PVA‐C) mainly comprised a blend of starch and PVA. Gelatin and the novel material were used to encapsulate a hydrophilic lipid‐based system of fenofibrate. Considerable water migration was observed from the soft gelatin shell to the hydrophilic formulation during drying and drug crystallization resulted in soft gelatin capsules. In contrast, S‐PVA‐C displayed no substantial water exchange or drug crystallization upon storage. The thermoplastic capsule material further exhibited more surface roughness and higher resistance to mechanical deformation compared with gelatin. In conclusion, S‐PVA‐C provided a robust drug product following encapsulation of a rather hydrophilic lipid‐based formulation.