【摘要】 <正> 无味氯霉素即无苦味的氯霉素棕榈酸酯,是临床上特别是儿科常用的广谱抗菌素之一。多年来我国生产的无味氯霉素以片剂、糖粉和混悬剂等各种剂型畅销国内外市场。1961年后经研究发现,无味氯霉素有A、B及无定形等数种晶型,其中A型最稳定,但生物活性和抗菌作用都极低;B型为亚稳定型,具有生物活性。在生产过程中,更多还原

【Abstract】 Chloramphenicol Palmitate is one of the widely used broad-speotrum antibacterial antibiotics. It has 2 crystalline forms A and B, and an amorphous form, form A is most stable, but its antibacterial effect is very poor, almost without any biological activity, form B is less stable but possesses much stronger antibacterial activity than A. During process of production, both can undergo mutual transformations.Eecently, we have observed the serum concentrations of 14 preparations of chloramphenicol palmitate in 10 healthy volunteers in a crossover study. Serum concentrations of each preparation of 1.75gm ohloramphenicol palmitate (equal to 1 gm of ohloramphenicol) taken orally in a fasting stomach were determind by cup-plate method with B. subtilis as test organism. The blood levels of chlorampheniool were also determined after 1 gm. ohloramphenicol by oral route as control.The absorption rate of ohloramphenicol was the fastest and its peak concentration was achieved one hour after administration, the peak concentrations of different preparations of chloramphenicol palmitate were usually reached four hours after administration. The blood-level of either macro-granule A form capsule (No. 1) or macro-granule B form capsule (No. 2) was significantly lower than that of chloramphemicol in same dosage (P<0.01). The blood level of micro-granule B form tablet (No. 3) was significantly higher than that of macro-granule B form capsule (No. 2) (P<0.01). The blood level of micro-granule B tablet containing Tween 80 (No. 4) was the highest among all preparations of chloramphenicol palmitate, approximating that of ohloramphenicol. The level of macro-granule B tablet containing Tween 80 (No. 5) was higher than that of macrogranule B capsule without Tween 80 (No. 2), and close to that of micro-granule B tablet containing Tween 80 (No. 4).Therefore we conclude that the absorption of chloramphenicol palmitate is related to the following factors: (1) the form of crystalline; (2) the size of granule; (3) surface detergent and so on.更多还原