Novel compositions of minoxidil

A technology of composition and polymer, applied in the field of inducing and/or stimulating hair growth and/or reducing hair loss, capable of solving problems such as incompatibility and pharmaceutical non-excellent products

Inactive Publication Date: 2003-10-22
麦克尼尔有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, high percentages of these solvents may often be incompatible with many pharmaceutical additives, such as thickeners, and may result in a pharmaceutically inelegant product

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment I

[0067] A gel composition containing 5% minoxidil within the scope of the present invention is prepared as follows:

[0068] Part I solution

[0069] Minoxidil USP 50.7mg

[0070] Propylene Glycol USP 526mg

[0071] Ethanol USP 130mg

[0072] AMP-95® (2-amino-2-methyl-1-propanol) 1.5mg

[0073] Part II Dispersion

[0074] Pemulen® TR-1 NF 2.5mg

[0075] Purified Water USP 153mg

[0076] Ethanol USP 136.3mg

[0077] Preparation Process

[0078] The ethanol and propylene glycol from Part I were mixed and minoxidil was dissolved into the resulting solvent mixture. Add AMP-95(R) to the solution and mix until dissolved. Mix the alcohol and water from Part II. Pemulen(R) was gradually added to the alcohol / water mixture until a uniform dispersion was formed. The Part I solution was then gradually added to the Part II dispersion with constant stirring until a uniform gel formed. The resulting gel had a good appearance with a smooth consistency, good clarity and moderat...

Embodiment II

[0080] Prepare minoxidil gel by the method described in embodiment 1, difference is not to use any ethanol in the solution of part I. The propylene glycol needs to be heated to dissolve the minoxidil, allowing it to remain in solution until cooled to room temperature. Ethanol was then added to the solution, and a gel was prepared as in Example 1. This example shows that mixing ethanol and propylene glycol prior to adding minoxidil can avoid the need to heat the solution to dissolve minoxidil.

Embodiment III

[0082] Prepare 5% minoxidil gel as follows:

[0083] Part I solution

[0084] Minoxidil USP 22.14mg

[0085] Propylene Glycol USP 526mg

[0086] Part II Dispersion

[0087] Pemulen® TR-1 NF 5mg

[0088] Purified Water USP 153mg

[0089] Ethanol USP 260.7mg

[0090] Part III Neutralizers

[0091] AMP-95® (2-amino-2-methyl-1-propanol) 5mg

[0092] process

[0093]Propylene glycol and minoxidil are mixed and heated to dissolve minoxidil as in Example II. Combine the alcohol and water from Part II and add the minoxidil solution from Part I and mix until homogeneous. Pemulen(R) was gradually added to the minoxidil solution formed by mixing Parts I and I1. As soon as Pemulen(R) was initially added to the minoxidil solution, the mixture began to form a gel. Continued addition of Pemulen(R) produced a non-uniform mixture of undispersed pieces of Pemulen(R) and "fish eyes" (ie, individual partially hydrated gel pieces of Pemulen(R)) in the dry state. Continued mixing...

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PUM

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Abstract

Novel compositions comprising minoxidil, a thickening agent, and a pharmaceutically acceptable solvent are presented. Also presented is a process for making a novel gel composition comprising minoxidil, and methods for using the novel compositions for treating and preventing hair loss in a region of a patient.

Description

technical field [0001] The present invention relates to novel compositions of minoxidil, methods of preparing compositions of the invention, and methods of inducing and / or stimulating hair growth and / or reducing hair loss using compositions of the invention. Background technique [0002] Minoxidil (i.e., 2,4-diamino-6-piperidinylpyrimidine-3-oxide) is the active ingredient of Loniten® (longatidine) and Rogaine®, which are marketed by Pharmacia & Upjohn, respectively, for the treatment of High blood pressure and the treatment and prevention of androgen-induced alopecia (typical hair loss in both men and women). US Patent No. 3,461,461 describes formulations and antihypertensive uses of minoxidil. U.S. Patent Nos. 4,139,619 and 4,596,812 describe methods and topical formulations for using the compounds to grow hair and treat typical male and female pattern hair loss. [0003] Pharmaceutical compositions for topical use, such as Rogaine(R), can take a variety of dosage forms ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/00A61K8/02A61K8/25A61K8/26A61K8/34A61K8/41A61K8/49A61K8/73A61K8/81A61K8/86A61K8/894A61K8/898A61K8/90A61K8/91A61K9/00A61K9/06A61K31/506A61K31/513A61K47/02A61K47/10A61K47/18A61K47/32A61K47/34A61K47/36A61K47/38A61P17/14A61Q5/00A61Q7/00
CPCY10S514/88A61K8/8158A61K8/8176A61K8/26A61K8/73A61K8/25A61K8/735A61K9/06A61Q7/00A61K8/731A61K8/8152A61K47/32A61K31/513A61K8/8117A61K8/8129A61K8/4953A61K8/894A61K9/0014A61K8/91A61K8/737A61K8/86A61K8/90A61P17/14C07D403/04
Inventor L·E·佩纳M-S·伍
Owner 麦克尼尔有限公司
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