盐酸地尔硫(艹卓)卡波普骨架片体外释放影响因素研究

目的 :考察影响盐酸地尔硫 艹卓(DTZ)卡波普 (Carbepol)骨架片体外释放药物的因素。方法 :用Carbopol为骨架材料 ,采取粉末直接压片制备缓释制剂 ,并考察Carbopol规格、用量、不同溶出介质pH值对DTZ骨架片体外释药的影响。结果 :DTZ骨架片的体外释药符合Higuchi方程 ,Carbopol的规格、用量、溶出介质pH值对药物的释放速率均有显著性影响 ,释药速率随Carbopol用量增加、溶出介质pH升高而降低。结论 :Carbopol规格、用量及溶出介质pH值均显著影响骨架片药物释放     

Effect of D-Mannitol on the Microstructure and Rheology of Non-Aqueous Carbopol Microgels

D-mannitol is a common polyol that is used as additive in pharmaceutical and personal care product formulations. We investigated its effect on the microstructure and rheology of novel non-aqueous Carbopol dispersions employing traditional and time-resolved rheological analysis. We considered two types of sample, (i) fresh (i.e., mannitol completely dissolved in solution) and aged (i.e., visible in crystalline form). The analysis of the intracycle rheological transitions that were observed for different samples revealed that, when completely dissolved in solution, mannitol does not alter the rheological behaviour of the Carbopol dispersions. This highlights that the chemical similarity of the additive with the molecules of the surrounding solvent allows preserving the swollen dimension and interparticle interactions of the Carbopol molecules. Conversely, when crystals are present, a hierarchical structure forms, consisting of a small dispersed phase (Carbopol) agglomerated around a big dispersed phase (crystals). In keeping with this microstructural picture, as the concentration of Carbopol reduces, the local dynamics of the crystals gradually start to control the integrity of the microstructure. Rheologically, this results in a higher elasticity of the suspensions at infinitesimal deformations, but a fragile yielding process at intermediate strains.     

Formulation of sustained release bioadhesive minitablets containing solid dispersion of levofloxacin for once daily ocular use

This study aimed to increase ocular residence time of levofloxacin by formulation into zero-order sustained release mucoadhesive minitablets for once daily administration using a hydrophobic–hydrophilic polymeric matrix. Levofloxacin was first formulated into solid dispersion with different ratios of Eudragit^® RS then the resulting solid dispersion was mixed with different concentrations of Carbopol^® and other excipients to be finally compressed into minitablets. A 2⁴ full factorial design was employed to estimate the effects and interactions of two formulation factors, and to establish their relationships with selected responses in the developed minitablets. The studied factors were: drug to Eudragit^® RS ratio, and percent of Carbopol^® in the minitablets. Sixteen ocular minitablets formulations were prepared and evaluated for the cumulative percentages drug release at 6, 12, and 24?h, as well as mucoadhesion time, mucoadhesive strength, and swelling index as response variables. After optimizing the responses, the optimized formulation was found to be stable on sterilization using gamma-irradiation and storage at 40?°C/75% RH for six months. In vivo testing of the optimized formulation showed that the minitablets extended levofloxacin release up to 24?h without causing any ocular irritation. The optimized formulation exhibited superior microbiological activity compared to the commercial product.     

重组幽门螺杆菌尿素酶B亚单位鼻腔免疫凝胶剂的研制

目的研制重组幽门螺杆菌尿素酶B亚单位疫苗凝胶剂,考察其特性及免疫效果。方法以卡泊波为基质,脱氧胆酸钠为黏膜吸收促进剂,制备凝胶剂,以落球法测定凝胶的黏度,SDS-PAGE电泳分析脱氧胆酸钠对蛋白纯度的影响,以免疫印记检测疫苗蛋白的完整性,以留样观察法及离心法考察凝胶的稳定性,以含抗原凝胶剂鼻腔免疫BALB/c小鼠,并与溶液剂相比较,考察凝胶剂的免疫效果。结果制备的凝胶剂稳定性好,凝胶的黏度为8050mPa.s,脱氧胆酸钠不影响蛋白的纯度,抗原蛋白的完整性良好。小鼠鼻腔免疫凝胶剂后产生了较强的特异性血清IgG及胃肠sIgA反应,优于液体免疫。结论重组幽门螺杆菌尿素酶B亚单位凝胶剂性质稳定,具有生物黏附性,可提高免疫效果,是较好的鼻腔免疫剂型。     

以卡波普为黏附材料的三七总皂苷生物黏附片的研制与体外评价

 目的研制三七总皂苷生物黏附片,考察其体外释药动力学、对离体肠黏膜的黏附力。方法释放度测定方法按2005年版《中国药典》附录,采用显色法测定黏附片中三七总皂苷的释放,用零级释放、一级释放模型、Higuchi方程、Peppas方程对释放度进行动力学模拟,考察药物释放机制。以自制的黏附力测试装置测定生物黏附片对兔肠黏膜的黏附力。结果三七总皂苷生物黏附片体外释放符合设计要求,生物黏附片对于肠黏膜具有较大的黏附力。结论生物黏附片处方设计与制备工艺合理,达到了设计要求。     

红霉素缓释栓的制备及溶出度考察

目的：制备以卡波姆(Cb)为阻滞剂的红霉素缓释栓并研究其处方组成、制备工艺。方法：以PEG6000、PEG400为基质，加入生物粘附材料卡波姆制成红霉素缓释栓，采用紫外分光光度法测定红露素缓释栓中红霉素的含量及溶出度。结果：在1h以前的溶出动力学过程接近0级速度过程，普通栓2h溶出91．21％，5h溶出95．92％。缓释栓B 2h溶出76．26％，5h溶出94．02％。缓释栓C 2h溶出69．70％，5h溶出89．60％。缓释栓C的体外释放优于单独以Cb作缓释剂的缓释栓B。结论:与普通红霉素栓剂相比，采用粘附材料卡波姆作缓释剂可以有效地控制栓剂中药物的释放速率。     

口服姜黄素脂质体制备及其大鼠体内药动学考察

目的制备卡波姆包衣姜黄素脂质体,并考察其在大鼠体内的药物动力学。方法采用薄膜分散法制备姜黄素脂质体,通过孵育法对姜黄素脂质体进行卡波姆包衣。采用微柱离心法测定姜黄素脂质体包衣前后包封率的变化。姜黄素脂质体大鼠口服给药后,以高效液相色谱（HPLC）法测定大鼠血浆中的药物浓度。结果脂质体包衣后包封率略有下降,姜黄素脂质体大鼠口服给药后药物动力学呈双室模型特征,相对生物利用度F（%）为281%,是普通脂质体的2.22倍。结论姜黄素脂质体经卡波姆包衣可明显提高姜黄素的口服生物利用度,药物峰浓度显著增加。     

卡泊姆与羟丙基甲基纤维素在体内外与大鼠胃肠粘膜粘附性的考察

目的　为口服缓释制剂的处方设计提供理论依据。方法　体外评价用最大粘附力作指标,体内评价以其在胃的排空速率和一定时间内到达小肠的距离为指标。考察不同粘度规格的卡波姆(Cb)和羟丙基甲基纤维素(HPMC)与大鼠胃肠粘膜之间的生物粘附性。结果　与生物粘膜之间的粘附力粘度低的材料大于粘度高的材料;而胃肠道转运速度则粘度高的材料比粘度低的材料慢。结论　粘附材料与生物粘膜之间的粘附力与其在大鼠胃肠道内的转运速度无相关性;体内研究结果表明,Cb934在所考察的粘附材料中有最佳的生物粘附性,可以作为口服生物粘附制剂的优先选择的辅料     

Formulation and comparative evaluation of poly herbal anti-acne face wash gels

Context: Rauvolfia serpentina (L). Benth. ex Kurz. (Apocynaceae) possessing antibacterial properties are widely used in modern herbal medicines. Curcuma longa L. (Zingiberaceae), a readily available antiseptic, possess antioxidant, antibacterial, blood purifying and antiinflammatory properties and used in various skin creams. Azadirachta indica A. Juss. (Meliaceae) possess astringent, antiviral, discutient, stimulant and antibacterial properties and works excellently well against acne and keeps the skin healthy.

Objective: Acne is the common skin problem that 85% of the teenagers face today. In this study, poly herbal anti-acne face wash gels were prepared using two polymers Carbopol and hydroxy propyl methyl cellulose (HPMC) along with the extracts of plants Rawvolfia serpentina, Curcuma longa, and Azadiracta indica.

Materials and methods: The gel formulations were prepared in four different concentrations of 50, 100, 200?mg/ml as Gel-CRB 100, Gel-HPMC 50, Gel-HPMC 100, Gel-HPMC 200, respectively. The formulations were tested for the anti-acne activity by turbidimetric method.

Results: Results showed that the gels were non-irritant, stable and posses anti-acne activity. The efficacy when tested with a standard was almost same to that of Clindamycin gel.

Discussion and conclusion: From this study, Gel-HPMC 100 was proved to be stable and considered as an effective herbal formulation for acne treatment.     

金黄凝胶制剂成型工艺研究

目的研究金黄凝胶的成型工艺。方法以凝胶剂的成型性、稳定性、失水率、p H值为指标,从凝胶基质、保湿剂、黏合剂用量等方面进行成型工艺考察。结果优选成型工艺为卡波姆1 g静置溶胀4 h,加入甘油10 g、药粉4 g,搅匀后加入三乙醇胺1 g,加水至100 g,搅匀即得。结论本方法为凝胶剂的研究提供评价标准,同时为进一步优化金黄凝胶成型工艺提供了基础。