以鹽酸多西環素腸溶微粒為例，研究以不同溶解特性之腸溶包衣材料HPMC-P與EUDRAGIT? L30D-55，搭配不同的包衣製程，進行微粒之包覆並檢驗，0.06M HCl溶液與pH 5.5緩衝液中溶離度、圓整度及脆碎度之差異，探討強光、高溫及高濕對產品之影響以及加速安定性。初步結果顯示HPMC-P和EUDRAGIT? L30D-55的處方下，0.06M HCl溶液與pH 5.5緩衝液中溶離度並無太大的差異。比較以底噴流動床包衣所包覆之微粒，酸中溶離度以及其圓整度與脆碎度數據均優於側噴，因此選擇底噴，結合不同處方試製樣品，進行安定性以及虐待試驗研究。
相關實驗結果顯示在高溫下，有關物質及含量兩個指標中，EUDRAGIT? L30D-55表現比HPMC-P微粒更佳，且在強光、高溫及高濕環境下，皆具有良好的穩定性，樣品在0.06M HCl溶液中溶離度小於2%，故選擇為優化處方。
以EUDRAGIT? L30D-55為腸溶材料，配合底噴流動床包覆，是最符合質量穩定，兼具降低成本和環境無害之最佳選擇。
Coat hydrochloric acid doxycycline enteric-coated pellets with different dissolution characteristics enteric coating, HPMC-P and EUDRAGIT? L30D-55, in different coating process; identify their dissolution, roundness, and friability in 0.06M HCl solution and pH 5.5 buffer solution as well as impact of intense light, high temperature and high humidity on the product and its accelerated stability. Initial results suggest HPMC-P and EUDRAGIT? L30D-55 based products make no significant difference in acid and pH5.5 buffer solution in terms of dissolution. Particles coated by fluid bed granulation end up with better acid dissolution, roundness, and friability than their side granulation counterparts. We then take samples made by bed granulation and different formula for stability and puncture tests.
Test results suggest EUDRAGIT? L30D-55 based pellets outperm the HPMC-P ones with respect to substance and concentration while maintaining the same good stability in environment of intense light, high temperature and high humidity as well as less than 2% dissolution in 0.06M HCl solution. EUDRAGIT? L30D-55 is then poised the optimum prescription.
Coating EUDRAGIT? L30D-55 enteric material with fluid bed granulation is the best option in terms of reliable quality, lower costs and environment friendliness.
