Dodov Marija Glavas, Goracinova Katerina, Simonoska Maja, Trajkovic-Jolevska Suzana, Ribarska Jasmina Tonic, Mitevska Marija Dastevska
Department of Pharmaceutical Technology Faculty of Pharmacy, University Ss Cyril and Methodious, 1000 Skopje, Macedonia.
Acta Pharm. 2005 Sep;55(3):251-61.
Diazepam (DZP) has become a commonly used drug for treatment of acute repetitive epileptic seizures and febrile convulsions in children. Considering the advantages of rectal administration of DZP, the objective of our study was to formulate and evaluate rectal hydrogels containing DZP as a drug substance in combination with suitable co-solvents and preservatives. Prepared HPMC (hydroxypropyl methylcellulose) hydrogels containing different concentrations of DZP (2, 4 and 6 mg mL(-1)) manifested good quality in respect to physico-chemical parameters (pH value, drug content, ingredients content and viscosity), antimicrobial efficiency and microbiological quality. Under the proposed HPLC conditions, satisfactory separation of DZP and the preservatives used was achieved. In vitro release studies have shown that the total amount of DZP was released in a period of 3 h. Prepared formulations were stable for four months at 26 degrees C (ambient temperature characteristic of the 2nd climate zone).
地西泮（DZP）已成为治疗儿童急性重复性癫痫发作和热性惊厥的常用药物。考虑到直肠给药DZP的优点，我们研究的目的是制备并评估含有DZP作为原料药，并与合适的助溶剂和防腐剂组合的直肠水凝胶。制备的含有不同浓度DZP（2、4和6 mg mL⁻¹）的羟丙基甲基纤维素（HPMC）水凝胶在物理化学参数（pH值、药物含量、成分含量和粘度）、抗菌效率和微生物质量方面表现出良好的质量。在所提出的高效液相色谱条件下，实现了DZP与所用防腐剂的满意分离。体外释放研究表明，DZP的总量在3小时内释放。制备的制剂在26℃（第二气候区的环境温度特征）下稳定四个月。
