為了尋求一種具有緩釋作用基質型材質，本研究旨在探討萃取自某天然物(植物A)之萃取物，做為藥物緩釋添加物的可能性。然後以植物A萃取濃縮液，作黏度測試、紅外線水分測定，再以噴霧乾燥法及冷凍乾燥法製成粉末，所收集的粉末與直接粉碎植物A，個別打成三顆300 mg錠劑(Riboflavin 5'-phosphate sodium 50mg＋噴霧乾燥植物A 250 mg)(Riboflavin 5'-phosphate sodium 50mg＋直接粉碎植物A 250 mg)以pH6.8 buffer作溶離試驗。再以噴霧乾燥與冷凍乾燥作溶離試驗比較，及掃描式電子顯微鏡下的結構變化，接續以噴霧乾燥植物A 250 mg＋Riboflavin 5'phosphate sodium 50 mg與Lactose 250 mg＋Riboflavin 5' -phosphate sodium 50 mg個別打成六錠，在pH6.8、pH4.5、及pH1.2下比較噴霧乾燥植物A是否會影響主成份的緩釋，是否有pH值的依賴性？然後再比較噴霧乾燥植物A與Methocel系列中的A15LV、E15LV、E50LV、F50LV、K100LV是否有相等延緩藥物釋放，最後再作Hardness及Mucoadhesion，利用質地分析儀測試噴霧乾燥植物A錠劑，測試黏在豬胃黏膜上的黏著力，以便了解植物A的黏性張力。
研究結果證明 :
(1) 噴霧乾燥植物A基質錠的控制釋放比直接粉碎植物A延緩效果還要好。
(2) 噴霧乾燥植物A的溶離試驗在pH6.8、pH4.5、pH1.2下皆有緩釋效果。
(3) 直接粉碎植物A、與噴霧乾燥植物A、及冷凍乾燥植物A的電子顯微下差異性。
(4) 噴霧乾燥植物A的黏度及延緩效果與Methocel中的E15LV、A15LV相當。
(5) 噴霧乾燥植物A作Mucoadhesion的測試結果，更證明它的黏著性在控制釋放劑型上的重要性。 A novel and natural material extracted from plants was investigated as a possible sustained release matrix tablet excipient for gastrointestinal and buccal administration. The material could be prepared by the (1) direct milling of the plant (2) spray drying or freeze-drying of aqueous concentrate after boiling for 3 hours. For the convenience of analysis, the Riboflavin 5'-phosphate sodium was chosen as model compound for gastrointestinal administration. The benzyldamine HCl was chosen as model compound for buccal administration.
The matrix tablet was made by compressing the mixture of the model compound with the spray drying powder of the material under controlled condition (time and force). The dissolution profiles at pH 6.8, 4.5, and 1.2 were obtained for gastrointestinal administration. The dissolution profile at pH 6.8 was obtained for buccal administration. The mucoadhesion strength of this material was compared with some commonly used excipient.
The results show that the material in the matrix tablet form has sustained effect both in gastrointestinal and buccal routes. The material also has wonderful mucoadhesion strength. The above in-vitro results show this material might be a suitable sustained release excipient for in-vivo testing.
