Release rates of levonorgestrel from Silastic capsules, homogeneous rods and covered rods in humans

Contraception. 1983 May;27(5):483-95. doi: 10.1016/0010-7824(83)90045-8.

Abstract

Three forms of subdermal implants containing levonorgestrel are described. These are: capsules, in which the powdered drug is sealed inside of lengths of Medical Grade Silastic tubing; homogeneous rods, in which the drug is uniformly dispersed in Silastic 382 Medical Grade Elastomer; and covered rods, in which a core rod of drug and filler-free polydimethylsiloxane polymer (50:50, Wt:Wt) are sealed inside thin-walled Silastic tubing. Long-term in vivo release rates from human subjects are presented; 6.5 years for capsules, 3.6 years for homogeneous rods and 4 years for covered rods. Sets of six capsules release a decreasing amount of drug through the first few hundred days in situ and after 500 days a fairly constant rate of about 35 micrograms per day is released (2 micrograms/cm). Homogeneous rods deliver a continuously declining amount of drug during the entire time studied. In the first 100 days the release averages 136 micrograms per day from a set of three 3-cm rods (15 micrograms/cm), gradually declining to 30 micrograms per day (3.3 micrograms/cm) from day 800 to day 1300. The covered rods deliver at a constant rate of 17.5 micrograms per day for a 3-cm rod (5.83 micrograms/cm) through 4 years.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Capsules
  • Contraceptives, Oral, Combined / administration & dosage
  • Contraceptives, Oral, Combined / metabolism
  • Dimethylpolysiloxanes*
  • Drug Implants
  • Female
  • Humans
  • Levonorgestrel
  • Norgestrel / administration & dosage*
  • Norgestrel / metabolism
  • Silicones*

Substances

  • Capsules
  • Contraceptives, Oral, Combined
  • Dimethylpolysiloxanes
  • Drug Implants
  • Silicones
  • Norgestrel
  • Levonorgestrel