Hoshi K, Mizushima Y
Department of Internal Medicine, St. Marianna University, School of Medicine, Kawasaki, Japan.
Prostaglandins. 1990 Aug;40(2):155-64. doi: 10.1016/0090-6980(90)90081-6.
Lipo-PGI2 is a drug preparation of a PGI2 analogue (isocarbacyclin methylester) which is incorporated into lipid microspheres with a diameter of 0.2 mu. Lipo-PGI2 has been shown to accumulate at the vascular wall, particularly those of arteriosclerotic lesions, and it has a much stronger inhibitory activity on platelet aggregation than free isocarbacyclin. In this study, a preliminary double-blind cross over trial of lipo-PGI2 in cerebral infarction was carried out. Seventeen patients with chronic cerebral infarction received 2 micrograms of lipo-PGI2 and placebo daily for one week each in a cross-over double blind test. A significant improvement was noted for lipo-PGI2 compared with placebo in the overall improvement in neurological and mental symptoms (p less than 0.01). The patient's preference also indicated the effectiveness of lipo-PGI2 (p less than 0.05). Adverse reactions were noted in 3 patients receiving placebo, but not in any receiving lipo-PGI2. These results show that lipo-PGI2 at a very low dose would be beneficial as a treatment for relieving the clinical symptoms of chronic cerebral infarction and that lipid microspheres are a useful drug carrier for PGI2 analogue therapy.
前列地尔脂微球制剂是一种前列环素类似物（异前列环素甲酯）的药物制剂，它被包裹在直径为0.2微米的脂质微球中。前列地尔脂微球制剂已被证明能在血管壁尤其是动脉粥样硬化病变部位蓄积，并且它对血小板聚集的抑制活性比游离异前列环素强得多。在本研究中，进行了前列地尔脂微球制剂治疗脑梗死的初步双盲交叉试验。17例慢性脑梗死患者在交叉双盲试验中，分别接受每日2微克前列地尔脂微球制剂和安慰剂治疗，各治疗1周。与安慰剂相比，前列地尔脂微球制剂在神经和精神症状的总体改善方面有显著改善（p<0.01）。患者的偏好也表明了前列地尔脂微球制剂的有效性（p<0.05）。3例接受安慰剂治疗的患者出现了不良反应，但接受前列地尔脂微球制剂治疗的患者均未出现不良反应。这些结果表明，极低剂量的前列地尔脂微球制剂作为缓解慢性脑梗死临床症状的治疗方法将是有益的，并且脂质微球是前列环素类似物治疗的有用药物载体。
