Morkhade Dinesh M
Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University Campus, Nagpur, 440033 MS, India.
Asian J Pharm Sci. 2017 Sep;12(5):424-432. doi: 10.1016/j.ajps.2017.05.002. Epub 2017 May 10.
In this study, a natural gum mastic was evaluated as a microencapsulating and matrix-forming material for sustained drug release. Mastic was characterized for its physicochemical properties. Microparticles were prepared by oil-in-oil solvent evaporation method. Matrix tablets were prepared by wet and melt granulation techniques. Diclofenac sodium (DFS) and diltiazem hydrochloride (DLTZ) were used as model drugs. Mastic produced discrete and spherical microspheres with DLTZ and microcapsules with DFS. Particle size and drug loading of microparticles was in the range of 22-62 µm and 50-87%, respectively. Increase in mastic: drug ratio increased microparticle size, improved drug loading and decreased the drug release rate. Microparticles with gum: drug ratio of 2:1 could sustain DLTZ release up to 12 h and released 57% DFS in 12 h. Mastic produced tablets with acceptable pharmacotechnical properties. A 30% w/w of mastic in tablet could sustain DLTZ release for 5 h from wet granulation, and DFS release for 8 h and 11 h from wet and melt granulation, respectively. Results revealed that a natural gum mastic can be used successfully to formulate matrix tablets and microparticles for sustained drug release.
在本研究中，对天然树胶乳香作为用于药物缓释的微囊化和基质形成材料进行了评估。对乳香的理化性质进行了表征。采用油包油溶剂蒸发法制备微粒。通过湿法制粒和熔融制粒技术制备基质片剂。使用双氯芬酸钠（DFS）和盐酸地尔硫䓬（DLTZ）作为模型药物。乳香与DLTZ形成离散的球形微球，与DFS形成微囊。微粒的粒径和载药量分别在22 - 62 µm和50 - 87%范围内。乳香与药物比例的增加会使微粒尺寸增大、载药量提高且药物释放速率降低。乳香与药物比例为2:1的微粒可使DLTZ释放长达12小时，12小时内释放57%的DFS。乳香制成的片剂具有可接受的药学性质。片剂中30%（w/w）的乳香通过湿法制粒可使DLTZ释放5小时，通过湿法制粒和熔融制粒分别可使DFS释放8小时和11小时。结果表明，天然树胶乳香可成功用于制备用于药物缓释的基质片剂和微粒。
