This invention relates to a pharmaceutical composition capable of enhancing bioavailability of oral statins, which contains statins, acidity regulator, metabolic enzyme safety inhibitor, and capsule or coating for modifying release capability. The acidity regulator can adjust the pH value of the gastrointestinal tract absorbing the medicine to enhance the bioavailability of the pharmaceutical composition, so as to make the variation in blood concentration due to individual differences become smaller, reduce the variable range of increased drug absorption amount, and reduce the severe and even lethal side effects of drug, such as rhabdomyolysis, and thus enhance the drug safety. This special formulation design not only reduces the severe side effects that may be possibly lethal, but also extends the active duration, so as to reduce the number of administration, and greatly reduce treatment failure because the patient forgot to take the medicine.一種可提高口服他汀類藥物生體可用率之醫藥組合物，該醫藥組合物包含他汀類藥物、酸鹼值調節劑、代謝酵素安全抑制劑和修飾釋放性之包衣或塗層，該酸鹼值調節劑可將吸收藥物的腸胃道pH值調節而使該醫藥組合物由於生體可用率提高，所以因個體差異造成的體內血中濃度變異小，藥物吸收量的增加可變異範圍變小，藥物的嚴重副作用如橫紋肌溶解等的嚴重甚至致死副作用降低，藥物安全性增加；這一特殊劑型設計不但使可能致死的嚴重副作用降低，也可延長作用時間，減少給藥次數，可大幅降低因為病人忘記服藥所造成的治療失敗。
