藻酸鈉是由褐藻所抽出的天然多醣聚合物，廣泛的應用在製藥、食品工業及當作藥物包覆基質。本實驗以尼古丁作為模式藥物，可用於緩解尼古丁戒斷症狀，其副作用例如：不良味道、半衰期短等。本實驗研究目的是藉由發展不同處方之藻酸鈣微粒膠囊來改善尼古丁的不良性質、使其達控制釋放效果。利用微粒膠囊製造法中之化學法與機械法改良製成不同粒徑之微粒膠囊，藉由改變藻酸鈉、明膠、PEG 6000、甘油的比例來探討其型態、粒徑、包埋率。以逆相式高效率液相層析（RP-HPLC）分析尼古丁於擬胃液（pH 1.2）和擬腸液（pH 7.4）中之體外釋離。利用熱卡式分析儀（DSC）及霍式轉換紅外光譜儀（FTIR）進行物理化學性質及結構鑑定分析。所製備微粒膠囊之粒徑範圍介於2134.2μm～1854.0μm（處方B系列） 和764.4μm～553.3μm（處方S系列）間，包埋率分別為101.8％～92.0％（處方B系列）和77.7％～53.4％（處方S系列）。尼古丁微粒膠囊其表面產生凹槽和皺摺而內部呈現網狀結構。從DSC、FTIR判斷尼古丁與藻酸鈣微粒膠囊沒有產生化學性交互作用。模擬胃腸道中釋藥行為符合Higuchi釋放模式。使用一新穎和簡單方法來製備尼古丁微粒膠囊可以控制其粒徑大小和改變基質的特性來達到尼古丁之控制釋放。 Alginate is a natural polysaccharide found in brown algae. Alginate is widely used in the pharmaceutical and food, and has been employed as a matrix for the entrapment of drug. Nicotine has some unpleasant side effects, including bad taste and short half-life for some individuals. It can be used in smoking-cessation therapy and acted as a model drug in the study. The purpose of this study was to develop calcium alginate microcapsules with improved properties for controlled delivery and to enhance storage stability of the nicotine. The nicotine microcapsules were manufactured into different sizes of microcapsules by a novel method with combining the mechanical and the chemical method. The effect of sodium alginate, gelatin, PEG 6000 and glycerin added to varying amounts by different ratio, on the morphology, size and encapsulation efficiency of the microcapsules was investigated. The concentration of nicotine was determined by RP-HPLC. The release of nicotine microcapsules was in pH 1.2 HCl-KCl buffer and in pH 7.4 phosphate buffer solution.The physicochemical properties of nicotine microcapsules were determined by differential scanning calorimetry (DSC), Fourier-Transform Infrared Spectrometer (FTIR). The emulsification technique yielded particle sizes ranging from 2134.2μm～1854.0μm (formulation B) and 764.4μm～553.3μm (formulation S) of nicotine-sodium alginate microcapsules. The mean encapsulation efficiency of nicotine microcapsules ranged from 101.8％～92.0％（formulation B）and 77.7％～53.4％（formulation S） respectively. Nicotine microcapsules resulted in wrinkled and cavernous on the surface and formed a reticulated structure on the inside. The DSC and FTIR measurements indicated that the chemical interaction did not occur among the components during manufacturing processes and lyophilized microcapsules. The release profiles were fitted very well by the Higuchi release model. Using a novel and easy method for the nicotine microcapsules manufacture of controlled size and changed the matrix performance allowed the controlled release of nicotine.
