Ethinylestradiol → Norgestimate and Ethinyl Estradiol

HRID 841849

反応式

HRID 841849 の反応式
[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

参加物

3

反応物 2

HCID 5991Ethinylestradiol4 回HCID 6540478Norgestimate3 回

生成物 1

HCID 9571023Norgestimate and Ethinyl Estradiol

実験手順

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.

後処理

  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

出典と根拠

ORDレコード
ord-150f6d9111cc41d1aaf6f36ab89c00fa
出典データセット
uspto-grants-2002_04
特許番号
US06372246B1

関連ノート

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