Steroid hormone products and methods for preparing them

• US 7,867,990 B2
• Filed: 12/13/2001
• Issued: 01/11/2011
• Est. Priority Date: 12/14/2000
• Status: Expired due to Term

• Current Assignee: Ortho-McNeil Pharmaceutical Incorporated (Johnson & Johnson)
• Original Assignee: Ortho-McNeil Pharmaceutical Incorporated (Johnson & Johnson)
• Inventors: Schultz, Thomas, Falzone, Angela, Clark, Bradley A.
• Primary Examiner(s): QAZI, SABIHA NAIM
• Application Number:
  US10/022,138
• Publication Number:
  US 20020173669A1
• Time in Patent Office: 3,316 Days
• Field of Search: 514/169, 514/177, 514/178, 514/182, 514/170, 514/179, 424/464, 552/648, 552/514, 552/610, 552/515, 552/516
• US Class Current: 514/182
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/567 substituted in position 17 alpha, e.g. mestranol, norethandrolone
• CPC Class Codes: A61K 31/569 substituted in position 17 alpha, e.g. ethisterone
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 31/575 substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• CPC Class Codes: A61K 9/145 with organic compounds
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/1694 resulting in granules or microspheres of the matrix type containing more than 5% of excipient
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 5/30 Oestrogens

Abstract

The present invention relates to steroid hormone products, such as oral contraceptive products, including at least one steroid active ingredient mixed with an excipient and having improved dissolution and release rate properties. The invention further relates to methods for making such steroid hormone products, wherein a mixture of the hormone and the excipient is subjected to sufficient mechanical energy to form a powder blend wherein the hormone is stabilized by the excipient in substantially non-crystalline form.

Claims

1. An oral steroid hormone product having improved dissolution and release rate properties, said product comprising norgestimate in admixture with lactose, wherein substantially all of said norgestimate is in non-crystalline form and wherein said lactose stabilizes said norgestimate in its non-crystalline form.

2. The steroid hormone product of claim 1, wherein the product is one of an oral contraceptive product and a hormone replacement therapy product.

3. The steroid hormone product of claim 2, wherein the product is an oral contraceptive product comprising from about 10 μ

g to about 50 ug of an estrogen and/or from about 50 μ

g to about 300 μ

g of norgestimate.