Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Progestin co-micronized with a surfactant, pharmaceutical composition comprising same, methods for making same and uses thereof

a technology of surfactant and progestin, which is applied in the field of comicronized progestin, pharmaceutical composition comprising same, methods for making same, etc., can solve the problems of reducing the intrinsic androgenic activity of the molecule, affecting the function, and increasing the endometrial power

Inactive Publication Date: 2007-02-22
BESINS INT BELGIQUE
View PDF10 Cites 54 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These chemical modifications increase the endometrial power and decrease the intrinsic androgenic activity of the molecule.
This progesterone insufficiency may lead to functional impairment and various clinical manifestations, in particular: premenstrual syndromes, menstrual irregularities through disovulation or anovulation, benign mastopathies, perimenopause and menopause.
However, oral administration of progesterone suffers from a serious handicap due to the considerable metabolizing thereof in the liver.
The method for preparing such capsules proves, however, to be complex and expensive to carry out, and also requires considerable know-how.
However, that patent application underlines, at the same time, the fact that it is not automatic and inescapable that the bioavailability of an active principle is systematically improved by co-micronization in the presence of a surfactant.
The same authors underlined moreover—which is entirely relevant—that even though micronization or grinding of a substance in the presence of a surfactant or of a sugar can increase its solubility, these parameters are not always sufficient.
It is therefore perfectly established that the properties of a substance treated by micronization or grinding, in particular its solubility and its bioavailability, are not predictable, contradictory results possibly being obtained, and that the same pharmaceutical formulation can provide good results with one substance and produce an opposite result with another substance.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Progestin co-micronized with a surfactant, pharmaceutical composition comprising same, methods for making same and uses thereof
  • Progestin co-micronized with a surfactant, pharmaceutical composition comprising same, methods for making same and uses thereof
  • Progestin co-micronized with a surfactant, pharmaceutical composition comprising same, methods for making same and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Progesterone Co-Micronized with Sodium Lauryl Sulfate

[0067] 1) 97 g of progesterone and 3 g of sodium lauryl sulfate are mixed for 5 minutes in a mixer of the LÖDIGE type.

[0068] 2) The mixture obtained in step (1) is introduced into an Alpine 200 AS airjet mill preset on the following parameters: [0069] injection: 5.5 B [0070] ring: 3.0B [0071] rate: 35 kg / h

[0072] 3) This mixture is ground in order to obtain a co-micronized material of progesterone / sodium lauryl sulfate.

example 2

Tablets Based on Progesterone Co-Micronized with A Surfactant

[0073] The formulations of progesterone tablets according to the invention, containing 100 and 200 mg of progesterone, are given in Table I below.

TABLE 1NAME OF THEUNIT AMOUNTBATCHCOMPONENTFUNCTIONmg / tabletSIZE (kg)MicronizedActive55.000progesterone*principle(sodium lauryl(progestin)200100sulfate (SLS))*(surfactant)6.183.09Povidone K30Binder9.604.802.561Solution at35% (m / m)MannitolDiluent29.8414.927.981CrosslinkedDisintegrating13.006.503.468sodiumagentcarboxymethylcelluloseMagnesiumLubricant1.300.650.347stearate

*Progesterone / SLS are co-micronized according to example 1.

[0074] To prepare the tablets in question, the following procedure was carried out:

Step 1: Preparation of the Wetting Solution

[0075] 4.756 kg of purified water are introduced into a container of suitable volume. 2.561 kg of Povidone K30 are then introduced into the purified water, gradually, and with stirring in a deflocculating-type stirrer (RAYNERI)...

example 3

Dissolving of the Progesterone Tablets Prepared According to the Invention, In Vitro

[0103] 100 mg and 200 mg progesterone tablets are prepared according to the method given in example 2, and the following operations are carried out in order to determine the in vitro dissolution curves (see FIG. 1).

[0104] The following material is used: [0105] SOTAX AT7 7-position revolving-paddle dissolution device [0106] PERKIN ELMER lambda 20 spectrophotometer [0107] ISMATEC IPC 12 cassette pump [0108] WINSOTAX data acquisition software.

[0109] The dissolving conditions are as follows: [0110] dissolving medium: 1000 ml of aqueous solution of β-hydroxypropylcyclodextrin having the trade mark KLEPTOSE® at 1% per cell [0111] rotation rate: 150 rpm [0112] temperature: 37° C.±0.5° C. [0113] number of cells: 7 [0114] circulation cell made of quartz with an optical path: 0.1 cm.

[0115] A control is prepared, consisting of a tablet of micronized progesterone:

Progesterone20mgHPLC ethanol20ml1% solution...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
diameteraaaaaaaaaa
disintegration timeaaaaaaaaaa
massaaaaaaaaaa
Login to View More

Abstract

The invention concerns a progestin co-micronized with a surfactant and a pharmaceutical composition comprising said gestagenic. The invention also concerns methods for preparing same.

Description

CROSS-REFERENCE TO RELATED PATENT APPLICATIONS [0001] This application claims priority under 35 U.S.C. § 119 to French Application 0102814, filed Mar. 1, 2001. This application is a continuation of U.S. application Ser. No. 10 / 469,441, filed Feb. 10, 2004, which is incorporated herein by reference in its entirety, and which is the U.S. National Stage of PCT / FR02 / 00714, filed Feb. 27, 2004. This application claims priority under 35 U.S.C. § 120 to these U.S. and PCT applications.FIELD OF THE INVENTION [0002] The present invention relates, as a new product, to a progestin co-micronized with a surfactant, to a pharmaceutical composition containing same, to methods for preparing same, and also to uses thereof. BACKGROUND OF THE INVENTION [0003] In the context of the present invention, the term “progestin” is intended to mean any steroid having affinities for progesterone receptors and capable of more or less fully reproducing the biological effects of progesterone. [0004] A progestin is...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/57B27N3/00A61K9/20A61K9/14A61P15/12
CPCA61K9/145A61K9/2018A61K9/2027A61K9/2054A61K31/57A61P15/12
Inventor BESSE, JEROME
Owner BESINS INT BELGIQUE
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com