Garza-Flores J, Jimenez-Thomas S, Salomón-Andonie J, Díaz-Sanchez V
National Institute of Nutrition, School of Medicine, National University of Mexico, Mexico City.
Contraception. 1988 May;37(5):471-81. doi: 10.1016/0010-7824(88)90017-0.
Norethisterone (NET) in combination with mestranol (ME), in a macrocrystalline aqueous suspension that provides sustained release of steroids, was assessed as a once-a-month injectable contraceptive in ten healthy women of reproductive age. The ovarian function was studied before and after the intramuscular administration of 12mg NET plus 1.2mg ME, delivered as crystals of 150 micron average size. Serial blood samples were taken throughout the injection intervals in all women to measure serum progesterone (P), estradiol (E2), and NET. The NET/ME preparation effectively inhibited ovulation in 23 out of the 25 injection intervals studied. The administration of this formulation induced in some women a small degree of follicular maturation not followed by luteal activity. The endometrial bleeding patterns after each injection showed a bleeding-free period of two to three weeks. The overall data demonstrate that the parenteral administration of a macrocrystalline steroid preparation of NET/ME can bring about a sustained release contraceptive system at a substantially lower dose than those currently employed in once-a-month injectable contraception.
炔诺酮（NET）与炔雌醇甲醚（ME）组合，制成能使甾体激素持续释放的大晶体水混悬液，在10名育龄健康女性中作为每月注射一次的避孕药进行评估。在肌肉注射12毫克NET加1.2毫克ME（以平均大小为150微米的晶体形式给药）之前和之后研究卵巢功能。在所有女性的整个注射间隔期间采集系列血样，以测定血清孕酮（P）、雌二醇（E2）和NET。在所研究的25个注射间隔中，有23个间隔NET/ME制剂有效抑制排卵。该制剂的给药在一些女性中诱导了一定程度的卵泡成熟，但随后没有黄体活性。每次注射后的子宫内膜出血模式显示无出血期为两到三周。总体数据表明，胃肠外给予NET/ME的大晶体甾体制剂可以以比目前用于每月注射一次避孕的剂量低得多的剂量实现持续释放避孕系统。
