跌打佳涂膜剂的研究

目的：通过开发丙烯酸树脂Ⅲ号新用途,寻求涂膜剂最佳成膜材料,研制出工艺稳定、质量可近的涂膜剂。方法：经过单因素考查,以丙烯酸树脂Ⅲ号、中药提取物、丙二醇、邻苯二甲酸二乙酯为基本配方,以下交表L9（3^4)筛选最佳配方;以薄层色谱法对主药白芷进行鉴别。结果：正交试验表明,A2B1C1D3为最佳配方;以吸附剂哇胶G、展开剂石油醚（30℃-60℃）-乙醚（0.9:1.1)为白芷最佳薄层条件。结论：丙烯酸树脂Ⅲ号作为该涂膜剂成膜材料较适合。     

金黄涂膜剂的制备工艺研究

目的探讨金黄涂膜剂的制备方法。方法采用正交试验设计,以外观性状和成膜时间为指标,筛选金黄涂膜剂的最优处方。结果以邻苯二甲酸二乙酯、聚乙烯醇(1788)、聚乙烯醇缩甲乙醛按比例1∶2∶5制得的制剂成膜性和稳定性均较好。结论优选的金黄涂膜剂制剂设计合理,制备工艺简便可行。     

壳聚糖复合膜剂的制备及性能研究

目的 制备物理性能良好的壳聚糖（CTS）复合膜.方法 将壳聚糖与明胶、可溶性淀粉、聚乙烯醇等3种不同材料共混成膜,使用甘油或聚乙二醇600（PEG600）为增塑剂,探讨所得膜的保湿性能、吸湿性能和水蒸气透过性能的变化规律.结果 含量为20%的增塑剂均能达到较好的保湿性能和水蒸气透过率,且大多数情况下,甘油的增塑效果优于PEG.吸湿性能方面,CTS-淀粉复合膜与其它复合膜有些不同,随增塑剂含量增加,吸湿率有极大值出现.结论 壳聚糖与其它水溶性高分子材料复合成膜后,其综合性能均有所提高.     

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。     

正交试验法优化甲冰缓释膜的处方

目的：优化甲冰缓释膜的处方。方法：以白及多糖与聚乙烯醇124（PVA-124）的质量比、甘油和羧甲基纤维素钠（CMC-Na）的用量为考察因素,以膜剂的外观、0.5 h与4 h甲硝唑的释放度为综合评价指标,采用正交试验对成膜材料的处方进行优化。结果：白及多糖与PVA124的用量比例是影响膜剂质量的关键因素,当白及多糖与PVA124的质量比为20∶80、甘油用量为3.5 g、CMC-Na用量为0.14 g时,所制得的膜剂外观符合要求,0.5 h及4 h的释放度分别为25.17%、69.64%,8 h平均累积释放率〉90%。结论：经优化的处方所制成的药膜平整光洁,柔软度适中,即能保持原处方透膜释放药物的特性,又能发挥白及的药理作用。     

甲硝唑口腔膜的制备及质量控制

目的建立甲硝唑口腔膜的制备及质量控制方法。方法采用聚乙烯醇树脂（PVA1788，PVA1799）为成膜材料，制成由药膜层和覆盖层组成的甲硝唑口腔膜，用紫外分光光度法测定甲硝唑含量。结果检测波长为320nm，甲硝唑质量浓度线性范围是2-20μg／mL，C=0．1173224＋18．42383A，r=0．99998（n=6），平均回收率为99、77％，RSD=1．27％（n=6）。制剂在室温（20±5）℃条件下6个月内稳定。结论该制剂稳定，制备工艺简便，含量测定方法简便、准确。     

基于层次分析法和正交设计优选长效缓释口腔溃疡膜的制备工艺研究

目的 研制具有较长的黏附时间与溶蚀时间的缓释膜剂,同市售口腔溃疡膜进行比较。方法 对该膜剂以黏附力、黏附时间、溶胀系数、溶蚀时间等作为考察指标,采用单因素考察与层次分析法相结合,对成膜材料进行筛选;考察处方中克霉唑、奥硝唑和冰片的分散方法,防止药物沉淀析出;采用正交试验与层次分析法相结合的方法对羧甲基纤维素钠（CMC-Na）、聚乙烯醇-1788（PVA-1788）及甘油的用量进行优化;并与市售产品进行比较。结果 通过单因素考察和正交试验,优选出辅料最佳配比为CMC-Na∶PVA-1788∶甘油（3∶1∶0.08）;采用物理凝聚法对水不溶成分克霉唑、奥硝唑和冰片分散效果良好;采用最优方法制备膜剂,黏附力为102 g,黏附时间为55 min,最大溶胀系数为1 939.52%,平均溶蚀时间为110 min,外观呈现白色,表面无气泡且柔软,有一定弹性,在60 ℃成膜时间为300 min,脱模效果较好可完全撕取,厚度适中。结论 本方法制备的口腔溃疡膜外观良好,使用舒适,黏附力强,具有较长的黏附时间和溶蚀时间,可长时间滞留于溃疡面形成物理隔离,并在溶蚀的过程中缓慢释放药物,对口腔溃疡起到长效止痛、抗菌、消炎和促愈合的作用。     

A thermogravimetric analysis of non-polymeric pharmaceutical plasticizers: Kinetic analysis, method validation, and thermal stability evaluation

Four non-polymeric plasticizers, propylene glycol, diethyl phthalate, triacetin, and glycerin have been subjected to rising temperature thermogravimetry for kinetic analysis and vaporization-based thermal stability evaluation. Since volatile loss of a substance is a function of its vapor pressure, the thermal stability of these plasticizers has been analyzed by generating vapor pressure curves using the Antoine and Langmuir equations. Unknown Antoine constants for the sample compounds, triacetin and glycerin have been derived by subjecting the vapor pressure curves to nonlinear regression. For the first time, the entire process of obtaining the unknown Antoine constants through thermogravimetry has been validated by developing an approach called the double reference method. Based on this method, it has been possible to show that this technique is accurate even for structurally diverse compounds. Kinetic analysis on the volatilization of compounds revealed a predominant zero order process. The activation energy values for vaporization of propylene glycol, diethyl phthalate, triacetin, and glycerin, as deduced from the Arrhenius plots, have been determined to be 55.80, 66.45, 65.12, and 67.54 kJ/mol, respectively. The enthalpies of vaporization of the compounds have been determined from the Clausius-Clapeyron plots. Rising temperature thermogravimetry coupled with nonlinear regression analysis has been shown to be an effective and rapid technique for accurately predicting the vapor pressure behavior and thermal stability evaluation of valatile compounds.     

渗透型丙烯酸树脂包衣控释膜中增塑剂的优选

目的　筛选适合渗透型丙烯酸树脂 Eudragit RS100 膜控释包衣的增塑剂。方法　通过测定膜玻璃化转变温度(Tg)、膜水化前后两种状态的力学性能,研究不同增塑剂的增塑效率;用溶出度和水平扩散池法考察增塑剂从介质中溶出;用加速试验考察贮存时增塑剂的损失。结果　Tg显示EudragitRS10 0具较强增塑剂相容性,水溶性增塑剂三醋酸甘油酯(TR)和水不溶性增塑剂邻苯二甲酸二丁酯(DBP)等均有较高增塑效率;膜水化前后力学性能变化显著,水溶性增塑剂遇介质从膜中快速溶出使湿膜脆碎,而水不溶性增塑剂则相对稳定;于(40±1)℃、相对湿度(RH)75%下贮存40d ,膜TR损失达6.46% ,而DBP仅损失0.29%。结论　DBP等水不溶性增塑剂是较理想的 Eudragit RS100 膜控释包衣膜增塑剂品种     

橘红总黄酮凝胶剂的制备工艺研究

目的：研究橘红总黄酮凝胶剂最优制备工艺。方法：以凝胶剂的涂展性和光泽度等为指标,通过正交实验法考察卡波姆940、氮酮、丙二醇、甘油的用量,优选橘红总黄酮凝胶剂的制备工艺。结果：橘红总黄酮凝胶剂的最优工艺处方为：橘红总黄酮/卡波姆940/氮酮/丙二醇/甘油=1.3%/0.8%/2%/15%/10%。结论：经过试验研究得出的制备工艺简单、稳定、可行,为橘红总黄酮凝胶剂的实际生产提供参考。     

The Effect of Plasticizers on Compatibility,Mechanical Properties,and Adhesion Strength of Drug-Free Eudragit E Films

The use of plasticizers to affect the properties of drug-free, self-adhesive Eudragit E-100 films with higher transparency was tested for possible transdermal drug delivery. Triacetin was found to be an effective first plasticizer for Eudragit E-100 polymer. In order to improve the flexibility and adhesiveness of Eudragit E-100 film plasticized with triacetin, a more flexible and adhesive, secondary plasticizer was added. Plasticizer–polymer compatibility was evaluated by measuring transparency, surface topography, and solubility. Secondary plasticizers with a low molecular weight and a solubility parameter similar to that of Eudragit E-100 polymer and triacetin were compatible. Further, a lower molecular weight or higher concentration of the secondary plasticizers might lead to greater plasticizing action, reduce tensile strength, and increase film elongation, independent of the hydrophilicity of the plasticizer. The adhesive strength of Eudragit E-100 film under a 180° peel test was also affected by the molecular weight and solubility parameter of the secondary plasticizers used. The results indicate that PEG 200, propylene glycol, diethyl phthalate, and oleic acid can serve as a secondary plasticizer to improve the transparency, flexibility, and adhesion of Eudragit E-100 film.     

The feasibility study of transdermal drug delivery systems for antidepressants possessing hydrophilicity or hydrophobicity

The feasibility studies on the transdermal drug delivery systems have been performed to avoid the systemic side-effects and gastric disorders that could be occurred due to the transient high blood concentration after oral administration of antidepressants such as venlafaxine HCl and citalopram. When surfactants of tween 80^? and plasticizer of diethyl phthalate were combined with citalopram?Cethylene vinyl acetate (EVA) matrix, the permeation of citalopram showed the best enhancement. As well as, venlafaxine HCl gels were prepared using carbomer, oleic acid and/or propylene glycol to enhance the skin permeation of venlafaxine HCl. The citalopram-EVA matrix containing tween 80^? and diethyl phthalate as permeation enhancers might be a good transdermal delivery system for providing sustained plasma concentrations of citalopram. Also, venlafaxine HCl showed the possibility to be enhanced skin permeation in the formulation of gels with carbomer including penetration enhancer, oleic acid and/or propylene glycol.     

Deproteinized natural rubber film forming polymeric solutions for nicotine transdermal delivery

Film forming polymeric solutions were prepared from DNRL blended with MC, PVA, or SAG, together with dibutylphthalate or glycerine used as plasticizers. These formulations were easily prepared by simple mixing. In a preliminary step, in situ films were prepared by solvent evaporation in a Petri-dish. Their mechanical and physicochemical properties were determined. The in vitro release and skin permeation of nicotine dissolved in these blended polymers were investigated by a modified Franz diffusion cell. The formulations had a white milky appearance, and were homogeneous and smooth in texture. Their pH was suitable for usage in skin contact. The mechanical property of in situ films depended on the ingredients but all compatible films were in an amorphous phase. The DNRL/PVA was shown to be the most suitable mixture to form completed films. The in vitro release and skin permeation studies demonstrated a biphasic release that provided an initial rapid release followed by a constant release rate that fitted the Higuchi’s model. Nicotine loaded DNRL/PVA series were selected for the stability test for 3 months. These formulations needed to be kept at 4°C in tight fitting containers. In conclusion, film forming polymeric solutions could be developed for transdermal nicotine delivery systems.     

甘油注射治疗原发性三叉神经痛临床分析

目的探索甘油封闭治疗原发性三叉神经痛的作用。方法对40例原发性三叉神经痛患者采用眶下孔、腭大孔、上牙槽后神经、下颌孔、颏孔注射纯甘油,观察罹患神经支配区注射前后面部感觉功能的改变,角膜反射、视力、下颌运动以及有无疱疹、麻痹、无茵性脑膜炎等并发症。结果随访6—24个月,疼痛完全缓解占80．00％,12月复诊复发率为22．58％,24月复诊复发率为16．66％,未发现严重并发症。结论甘油封闭治疗原发性三叉神经痛安全可靠,并发症少。     

Effect of various alcohols on intestinal net water flux and theophylline absorption in rats.

Previous studies in this laboratory demonstrated that the rate of intestinal absorption of theophylline in rats is increased significantly by ethanol in low concentrations and that this absorption enhancing effect is associated with an increased net water flux from the intestine. It is now shown that other alcohols, namely methanol, n-propanol, n-butanol, glycerin, propylene glycol, and, to a lesser extent, mannitol and sorbitol, can also increase net water flux from the small intestine of anesthetized rats. Polyethylene glycol 200 and 400 had no such effect, suggesting that these compounds do not penetrate to a site of action that elicits the increased net water flux. At initial concentrations of 0.1 and 1.0 M, glycerin and propylene glycol increase significantly the intestinal absorption rate of theophylline from the small intestine of anesthetized rats. The results show that the theophylline absorption enhancing effect of ethanol is not limited to that particular alcohol.     

In-vitro permeation of the insect repellent N,N-diethyl-m-toluamide (DEET) and the sunscreen oxybenzone

The permeation behaviours of the insect repellent N,N-diethyl-m-toluamide (DEET) and the sunscreen oxybenzone were assessed in a series of in-vitro diffusion studies, using piglet skin and poly (dimethylsiloxane) (PDMS) membrane. The transmembrane permeability of DEET and oxybenzone across piglet skin and PDMS membrane was dependent on dissolving vehicles and test concentrations. An enhanced permeation increase across piglet skin was found for DEET and oxybenzone when both compounds were present in the same medium (DEET: 289% in propylene glycol, 243% in ethanol and 112% in poly(ethylene glycol) (PEG-400); oxybenzone: 139% in PEG-400, 120% in propylene glycol and 112% in ethanol). Permeation enhancement was also observed in PDMS membrane (DEET: 207% in ethanol, 124% in PEG-400 and 107% in propylene glycol; oxybenzone: 254% in PEG-400, 154% in ethanol and 105% in propylene glycol). PDMS membrane was found to be a suitable candidate for in-vitro diffusion evaluations. This study shows that the permeations of the insect repellent DEET and the sunscreen oxybenzone were synergistically enhanced when they were applied simultaneously.