Fekete P
EGIS Gyógyszergyár Rt, Budapest.
Acta Pharm Hung. 1997 Jul;67(4):113-21.
The physical chemical properties, stability and incompatibility of captopril (the active ingredient of Tensiomin tablets) have been discussed. Captopril has two polimorphic crystal modifications, the form I. of higher melting point is applied in the therapy. Captopril has a better stability in solutions below pH 4, the degradation is accelerated by metallic ions (Cu, Fe). In solid phase the degradation is accelerated by the humidity of the air. No incompatibility was found with the tabletting excipients but stearic acid and sodium-carboxymethyl-starch. Under compaction at higher pressure captopril itself shows tendency for lamination. The dissolution rate of the Tensiomin tablets can meet the requirement of USP if direct tabletting method was used. In this case the breaking strength of the tablets has no influence on the dissolution rate. The main properties (weight uniformity, content uniformity, tensile strength, friability, disintegration time, dissolution time) of the Tensiomin tablets of 12.5 mg, 25 mg, 50 mg and 100 mg of captopril meet the requirement of USP not only after manufacturing but after the accelerated stability test of three month as well.
已对卡托普利（开博通片的活性成分）的物理化学性质、稳定性和不相容性进行了讨论。卡托普利有两种多晶型晶体变体，治疗中使用熔点较高的I型。卡托普利在pH值低于4的溶液中稳定性较好，金属离子（铜、铁）会加速其降解。在固相中，空气湿度会加速其降解。除硬脂酸和羧甲基淀粉钠外，未发现与压片辅料有不相容性。在较高压力下压片时，卡托普利本身有分层倾向。如果采用直接压片法，开博通片的溶出度可符合美国药典的要求。在这种情况下，片剂的抗碎强度对溶出度没有影响。含12.5毫克、25毫克、50毫克和100毫克卡托普利的开博通片的主要性质（重量均匀度、含量均匀度、抗张强度、脆碎度、崩解时间、溶出时间）不仅在生产后，而且在三个月的加速稳定性试验后均符合美国药典的要求。
