Ethinylestradiol → Norgestimate and Ethinyl Estradiol

HRID 841849

Reaction equation

HRID 841849 reaction equation
[CH3:1][C@@:2]12[C@:18]([OH:21])([C:19]#[CH:20])[CH2:17][CH2:16][C@H:15]1[C@H:14]1[C@@H:5]([C:6]3[CH:7]=[CH:8][C:9]([OH:22])=[CH:10][C:11]=3[CH2:12][CH2:13]1)[CH2:4][CH2:3]2.[CH3:23][CH2:24][C@@:25]12[C@:33]([O:36][C:37]([CH3:39])=[O:38])([C:34]#[CH:35])[CH2:32][CH2:31][C@H:30]1[C@@H:29]1[CH2:40][CH2:41][C:42]3[C@@H:49]([C@H:28]1[CH2:27][CH2:26]2)[CH2:48][CH2:47]/[C:44](=[N:45]\[OH:46])/[CH:43]=3>>[CH3:23][CH2:24][C@@:25]12[C@:33]([O:36][C:37]([CH3:39])=[O:38])([C:34]#[CH:35])[CH2:32][CH2:31][C@H:30]1[C@@H:29]1[CH2:40][CH2:41][C:42]3[C@@H:49]([C@H:28]1[CH2:27][CH2:26]2)[CH2:48][CH2:47]/[C:44](=[N:45]\[OH:46])/[CH:43]=3.[CH3:1][C@@:2]12[C@:18]([OH:21])([C:19]#[CH:20])[CH2:17][CH2:16][C@H:15]1[C@H:14]1[C@@H:5]([C:6]3[CH:7]=[CH:8][C:9]([OH:22])=[CH:10][C:11]=3[CH2:12][CH2:13]1)[CH2:4][CH2:3]2

Participants

3

Reactant 2

HCID 5991Ethinylestradiol4×HCID 6540478Norgestimate3×

Product 1

HCID 9571023Norgestimate and Ethinyl Estradiol

Procedure

PEG with molecular weight in the range of 1,000 to 20,000, preferably PEG 6000-8000, is micronized by Jet mill together with ethinyl estradiol at the ratio of ethinyl estradiol to PEG 1:1 to 1:60, , preferably 1:30 to 1:42. Adjust Jet mill to produce particle size of 1-100 μm, preferably 5-10 μm. Micronized norgestimate powder is electrically charged, and deposited on the substrate surface. Micronized PEG 6000/ethinyl estradiol mixture is electrically charged, and deposited on top of norgestimate. Surface deposited PEG is place under Infrared lamp until melt. PEG will form a coating film while cooling. In the similar manner, deposit PEG ethinyl estradiol mixture and coat bottom side and rest of the tablet surface. Adjust the charge of the substrate so that total of 250 μg of norgestimate and 35 μg of ethinyl estradiol are deposited on the substrate (placebo tablet) surface.

Workup

  1. customAdjust Jet mill to produce particle size of 1-100 μm, preferably 5-10 μm
  2. customPEG will form a coating film
  3. temperaturewhile cooling

Sources & evidence

ORD record
ord-150f6d9111cc41d1aaf6f36ab89c00fa
Source dataset
uspto-grants-2002_04
Patent number
US06372246B1

Linked notes

Loading…