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Norethindrone sustained release formulations and methods associated therewith

A technology of norethisterone and norethisterone acetate, which is applied in the directions of organic chemistry, pharmaceutical formulations, organic active ingredients, etc., can solve problems such as increasing the risk of pregnancy

Inactive Publication Date: 2005-08-17
WATSON PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Failure to achieve required norethindrone blood levels during the first day of transdermal patch administration may be equivalent to skipping a day of oral regimen administration due to the strict dosing requirements imposed by the contraceptive regime, for example, and may increase the risk of pregnancy

Method used

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  • Norethindrone sustained release formulations and methods associated therewith
  • Norethindrone sustained release formulations and methods associated therewith

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] The transdermal matrix system containing norethindrone and norethindrone acetate was prepared as follows. The solid content of the acrylic binder solution (Durotak 87-2074) is determined by placing a small amount in a pre-weighed aluminum dish and then placing it in a 75°C convection oven (A4718-Q, Blue M) overnight. After evaporating the solvent, the weight of the dry binder is obtained, and the solid content is calculated as the ratio of dry and wet weight.

[0062] Binder 87-2074 contains approximately 28-31% solids and has been used undiluted. Based on the pre-determined solid content, a known amount of binder is weighed into the glass bottle. For all preparations, first add an appropriate amount of norethindrone (NE) to the liquid binder in each bottle (1% w / w drug content is obtained after drying). Cap the bottle, seal with parafilm, and rotate until all NE is dissolved. Add an appropriate amount of norethindrone acetate (NEA) to the preparation bottle that does not r...

Embodiment 2

[0065] Using the adhesive matrix patch prepared according to the above process, the modified Franz diffusion cell was used to conduct in vitro skin flow studies. The epidermal membrane of a human cadaver is separated by heat. Cut the matrix patch of each formulation into 0.71 cm 2 Wafer. The release liner is removed, discarded, and the matrix sheet is laminated on the stratum corneum of the epidermal membrane. Then the skin-matrix assembly is sandwiched between the donor and recipient chambers of the diffusion cell and fixed so that the epidermis side faces the recipient chamber. Inject 0.02% w / v sodium azide (NaN 3 ) Solution. Then place the cuvette in a circulating water bath maintained at 32±1°C.

[0066] At 24, 48, 72, 96, 120, 144, and 168 hours, the entire contents of the recipient chamber were collected for drug quantitative analysis. Then reperfuse the receptor chamber with fresh receptor medium. After the HPLC analysis of the sample, the interval flow rate and cumulative ...

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Abstract

Sustained delivery formulations of norethindrone are disclosed and described. In one aspect, the formulation may be a transdermal formulation that includes both norethindrone and norethindrone acetate. In another aspect, the formulation may further include a penetration enhancer. Coadministration of norethindrone and norethindrone acetate has been found to provide a number of advantages, such as achievement of peak norethindrone serum levels substantially within 24 hours after initiation of administration.

Description

[0001] Priority date [0002] This application claims the priority of U.S. Provisional Patent Application Serial No. 60 / 383,790 filed on May 30, 2002, which is incorporated herein by reference. Invention field [0003] The invention relates to a sustained-release transdermal preparation of norethindrone and related methods. Therefore, the present invention covers the fields of pharmaceutical sciences, medicine and other health sciences. Background of the invention [0004] Female hormones such as estrogen and progesterone have been shown to have numerous medical uses, such as hormone replacement therapy (HRT) and contraception for women. Oral and transdermal dosage forms containing estrogen or progestin are well known, and both are often administered together in a single formulation. Due to the stringency and lifelong nature of HRT and contraception, transdermal formulations are an alternative to immediate-release oral dosage forms. However, because the skin is a strong barrier to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/10A61F13/00A61K9/70A61K31/56A61K31/565A61K31/567A61K47/22A61K47/32A61P5/30A61P15/18
CPCA61K31/567A61K31/565A61K31/56A61K9/7061A61P15/18A61P5/30
Inventor A·卢伊兹A·阿尼格博古D·全
Owner WATSON PHARMA INC
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