Toddywalla V S, Mehta S, Virkar K D, Saxena B N
Contraception. 1980 Mar;21(3):217-23. doi: 10.1016/0010-7824(80)90002-5.
The release of contraceptive steroids through different drug delivery systems into serum and breast milk was investigated in a group of lactating women. Four women in each group were taking either a low dosage progestogen compound like norethisterone (NET) 350 micrograms or d-norgestrel (d-Ng) 50 micrograms alone or low dosage combination pills containing NET 1 mg or d-Ng 150 micrograms with 30 micrograms ethinyl estradiol (EE2) or a biodegradable implant containing 25 mg NET or d-Ng. Peak levels in plasma and milk were seen in oral contraceptive users around 2 hours. Of the two low dosage progestogen compounds, d-Ng was below the detection limit in milk within 4 hours whereas NET was still detectable at the 24-hour interval. In contrast to this, because of the larger quantity of steroids in the combination pills, the NET/d-Ng levels in serum as well as in milk were high throughout the 24-hour period. With the subdermal route because of the sustained low release of the drug from the biodegradable implants, the levels in milk were below the detection limit within a day with d-Ng and within a week with NET.
在一组哺乳期妇女中,研究了通过不同给药系统将避孕甾体激素释放到血清和母乳中的情况。每组中有四名妇女,分别单独服用低剂量孕激素化合物,如350微克炔诺酮(NET)或50微克左炔诺孕酮(d-Ng),或服用含1毫克NET或150微克d-Ng与30微克炔雌醇(EE2)的低剂量复方避孕药,或植入含25毫克NET或d-Ng的可生物降解植入剂。口服避孕药使用者血浆和乳汁中的峰值水平在2小时左右出现。在两种低剂量孕激素化合物中,d-Ng在4小时内乳汁中低于检测限,而NET在24小时间隔时仍可检测到。与此相反,由于复方避孕药中甾体激素含量较高,血清和乳汁中的NET/d-Ng水平在24小时内都很高。通过皮下途径,由于药物从可生物降解植入剂中持续低释放,d-Ng在一天内乳汁中的水平低于检测限,NET在一周内低于检测限。