多西环素凝胶的研制

目的：将多西环素制成局部应用的凝胶剂，提高其药效。方法：以多西环素为主药，羟丙甲基纤维素、甘油等为基质制成凝胶剂。以紫外分光光度法测定制剂含量。结果：经离心实验，凝胶不分层；2～8℃留样观察3～6个月，凝胶均匀度、透明度、稠度、药物含量及pH值均无变化。结论：本研究制备的多西环素凝胶处方工艺合理、质量稳定。     

多西环素分析方法研究进展

对多西环素的分析方法进行总结,为日后研究工作打下基础。     

高效液相色谱法测定盐酸多西环素脂质体凝胶中盐酸多西环素的含量

目的建立高效液相色谱法测定盐酸多西环素脂质体凝胶中盐酸多西环素的含量。方法采用RP-HPLC法,色谱柱为十八烷基硅烷键合硅胶柱,以0.05 mol.L-1草酸铵溶液-二甲基甲酰胺-0.2 mol.L-1磷酸氢二铵溶液(65∶50∶5),用氨试液调节pH 8.0±0.2为流动相;柱温40℃;在280 nm波长处检测。结果多西环素在0.329 8~16.492 0μg.mL-1浓度与峰面积呈良好的线性关系(r=0.999 8),方法平均回收率为99.9%(n=3),RSD为1.18%。结论该法简便、可靠、专属性强,适合于该制剂的含量测定及产品的质量控制。     

多西环素致脉管炎1例

患者,男,30岁。主因咳嗽、咯痰1周于2011年10月24日入院。体检:体温36.6℃,脉搏82次·min-1,呼吸18次·min-1,血压120/70 mmHg(1 mmHg=0.133kPa);一般状况好,神志清,咽无充血,扁桃体不大,心肺检查无异常,腹软,肝、脾肋下未触     

盐酸多西环素注射用缓释凝胶的体内释药研究

目的考察盐酸多西环素注射用缓释凝胶的体内释放特性及体内外相关性。方法将含药凝胶注射到家兔牙龈内 ,用HPLC法测定不同时间凝胶中的残余药量 ,从而计算药物的释放量。结果 7d盐酸多西环素的释放度达 99 7%。结论药物可缓释 7d ,体内外相关。     

多西环素引起颅内高压

本文报道多西环素引起急性严重颅内高压2例，其中发生永久视力缺损1例。     

多西环素治疗莱姆病第一期临床观察

目的探讨多西环素治疗莱姆病第一期的临床疗效。方法 62例莱姆病第一期患者随机分为两组,治疗组31例采用多西环素等综合性治疗,对照组31例采用注射用青霉素G等综合性治疗。结果治疗组31例患者总有效率为96.8%,对照组31例患者总有效率为74.2%,有明显的差异,且治疗组较对照组不良反应明显减少。结论多西环素治疗莱姆病第一期是有效方法。     

HPLC法测定盐酸多西环素缓释药线中盐酸多西环素的含量

目的 建立盐酸多西环素缓释药线中盐酸多西环素的含量测定方法.方法 采用HPLC法测定药线中盐酸多西环素的含量.Alltima C18(4.6 mm×250 mm, 5 μm)柱,流动相为0.05 mol·L-1草酸铵溶液∶N,N-二甲基甲酰胺∶0.2 mol·L-1磷酸氢二铵溶液(65∶30∶5),用氨试液调节pH值为8.0±0.2,检测波长280 nm,流速为1.0 ml·min-1.结果 盐酸多西环素在49～490 mg·L-1范围内线性关系良好,r=0.9997,A=43767C 562001;平均回收率为98.72%,RSD＝1.31%(n=6 ).结论 该法简单可行,结果准确,可用于该制剂的质量标准检测.     

Badam gum: a natural polymer in mucoadhesive drug delivery. Design,optimization, and biopharmaceutical evaluation of badam gum-based metoprolol succinate buccoadhesive tablets

Context: Applicability of natural polymers in pharmaceutical drug delivery.

Objective: The objective of the present investigation was to evaluate the applicability of badam gum (BG) obtained from Terminalia catappa LINN, belongs to the family combretaceae as a buccoadhesive polymer using metoprolol succinate as a model drug.

Methods: Tablets were prepared by wet granulation technique. Compression coating technique was employed for the preparation of unidirectional release buccal tablets using cellulose acetate as an impermeable backing layer.

Results: Muco/buccoadhesive properties of the BG were increased with the increase in the concentration of polymer which was evident form the detachment force measurement, ex vivo residence time, and swelling studies. MBG 2 was found to be the optimized formulation based on drug dissolution studies and bioadhesion studies. FTIR and DSC studies performed on the optimized formulation indicated no drug–polymer interaction. MBG 2 was found to be stable after accelerated stability testing for 6 months as per ICH guidelines. Pharmacokinetic studies of the optimized formulation were performed in six healthy human volunteers in comparison with that of the commercial extended release oral tablet GUDPRESS XL-25 by estimating pharmacokinetic parameters and mean residence time (MRT). It was found that there is a significant increase in the bioavailability of metoprolol succinate from BG formulation which was evident from the high AUC and MRT values compared with the commercial formulation.

Conclusion: The above results clearly indicated that badam gum can be used as a mucoadhesive polymer for buccal drug delivery.     

盐酸多西环素注入用缓释凝胶的体外释放度研究

目的：考察盐酸多西环素注入用缓释凝胶的体外释放特性及机制;方法：考察聚乳酸(PLA)和聚乳酸-羟基乙酸共聚物(PLGA)型号、聚合物浓度、含药量、释放介质和释放装置对药物释放的影响,制定出盐酸多西环素注入用缓释凝胶的体外释放试验方案并进行体外释放度测定;结果：凝胶中药物在水中的释放分为2个阶段：第1个阶段为“突释”,第2个阶段符合Higuichi方程。结论：所定方法可用于盐酸多西环素注入用缓释凝胶的体外释放试验。     

卡维地洛胃漂浮片的制备和体外释放

目的：制备卡维地洛胃漂浮片,并通过紫外分光光度法考察其体外释放影响因素。方法：以卡维地洛为模型药物,分别以羟丙基甲基纤维素K4M（HPMC K4M）、碳酸钙和羟丙基甲基纤维素K15M（HPMC K15M）或以十八醇为基质制备胃漂浮片,用释放度测定法考察影响药物释放的因素。结果：随着HPMC K15M或十八醇用量的增加,药物的释放显著减慢,CaCO3用量的增加,药物释放加快。结论：制备的卡维地洛胃漂浮片漂浮性良好,且能够达到缓释的目的。     

格列吡嗪控释片体外药物释放特征和体内外相关性研究

目的考察格列吡嗪控释片体外药物释放特征和体内外相关性。方法分别采用3种不同pH值的缓冲溶液作为释放介质,并对pH6．8的释放介质分别采用3种不同的转速来测定格列吡嗪控释片的体外药物释放度,考察释放介质pH值和转速对释放度的影响。用Loo-Riegelman法计算格列吡嗪控释片在健康男性受试者体内吸收百分数,并与相应时间体外累积释放度线性回归,进行体内外相关性考察。结果格列吡嗪控释片在不同pH值释放介质中的释放度一致,均符合零级动力学,且不受转速影响。将体内累积吸收百分数y与相应时间在pH6．8释放介质中的体外释放百分数x进行线性回归（n=7）,回归方程为y=0．6904x＋22．941,r=0．9528。结论格列吡嗪控释片的释放度不受释放介质pH值和转速的影响,释药恒速。体外释放累积百分数与体内吸收百分数呈A级相关,具有良好的体内外相关性。     

Use of xanthan and its binary blends with synthetic polymers to design controlled release formulations of buccoadhesive nystatin tablets

Various buccoadhesive nystatin tablets formulations containing xanthan, carbopols (934P, 971P, 974P), PVP K30 or PEG 6000 or their binary blends were prepared. The powders were compressed into tablets at a constant compression pressure. Drug release behaviour, swelling and erosion indices and strength of bioadhesion in vitro to a biological membrane were investigated. The interaction between nystatin and polymers was investigated by DSC and FT-IR. Tablets containing the different types of carbopol alone consistently showed an initial burst release of drug, whereas this was not observed for matrices containing xanthan or xanthan-carbopol. The presence of PEG in xanthan-containing formulations induced an increase in dissolution rate; however, in the absence of xanthan the amount of drug release from a PEG matrix was reduced to < 15% over 8?h dissolution. The presence of PVP increased the dissolution rate of nystatin due to the relative hydrophilicity of PVP. The presence of calcium ions induced a more rigid gel in the xanthan matrix as a result of interaction between the polymer and calcium ions. Xanthan can be used in potential mucoadhesive formulations containing nystatin to produce a controlled release of the drug and the outcomes of this work may provide a suitable strategy for matrix selection to provide more efficacious treatment alternatives for candidiasis and other disease processes for significant patient populations.     

盐酸氨溴索缓释片体内外相关性研究

目的考察盐酸氨溴索缓释片体外释放度与体内吸收的相关性。方法应用释放度测定法研究盐酸氨溴索缓释片体外释药行为 ,采用HPLC法测定盐酸氨溴索缓释制剂在家犬体内的血药浓度 ,按照Wagner Nelson公式计算药物的吸收分数。 结果 3种自制盐酸氨溴索缓释片与参比制剂生物等效 ,以药物累积吸收百分数 f(t)与相应时刻的体外累积释放百分数F(t)建立的一元线性回归方程 ,参比制剂与 3种自制制剂的体内外相关系数分别为 0 969、0 979、0 970和 0 983。结论盐酸氨溴索缓释片的体外释放度与体内吸收具有显著的相关性。     

酒石酸托特罗定渗透泵片的制备及释放度测定

目的制备酒石酸托特罗定渗透泵片,考察其体外释药特性。方法以阿拉伯胶和氯化钠为渗透活性物质制成片芯,以醋酸纤维素、邻苯二甲酸二丁酯和聚乙二醇400为包衣材料,丙酮为包衣溶剂,制备酒石酸托特罗定渗透泵片;采用高效液相色谱法测定其体外释放度。结果以单用阿拉伯胶为促渗剂,当主药与阿拉伯胶用量比为1∶25时,制得的酒石酸托特罗定渗透泵片10h内恒速释药,释药量达85%以上。结论本试验研制的酒石酸托特罗定渗透泵片释药恒速,制备简单,重现性好。     

In vitro release and in vivo serum fluoride levels and urinary excretion after different sodium fluoride tablets

Summary Various sodium fluoride tablets used for the treatment of osteoporosis were evaluated. The tablets were characterized in vitro by determining the release curves. The serum levels and urinary recovery of fluoride were determined after a single oral dose either of rapidly soluble (conventional), sustained release or enterocoated tablets. The in vivo study showed that administration of sustained release tablets eliminated high serum peaks and prolonged the duration of an elevated serum level as compared to conventional tablets. The biovailability of the fluoride was lower after intake of sustained release and enterocoated tablets, and there was an increase in the interindividual variance of biovailability.     

格列喹酮缓释片的研制及其体外释放度考察

目的研制格列喹酮缓释片并考察其释药机制。方法以HPMC为骨架材料,以乳糖、淀粉、微晶纤维素作为填充剂调节释放度,并采用正交试验筛选处方,采用数学模型拟合释放曲线。结果格列喹酮缓释片在24h内呈现良好的释药特征,释药行为符合0级方程,Peppas方程拟合曲线说明药物释放是骨架溶蚀作用的结果。结论格列喹酮缓释片体外释放试验显示缓释行为,可进一步研究开发。