Topical tetracycline compositions

A kind of composition, technology of tetracycline, applied in the field of topical tetracycline composition, can solve problems such as troublesome, not having

Inactive Publication Date: 2012-09-19
FOAMIX PHARMACEUTICALS LIMITED
View PDF6 Cites 13 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such products are cumbersome, requiring mixing of the two components prior to administration to the patient, and have little or no practical

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
  • Topical tetracycline compositions
  • Topical tetracycline compositions
  • Topical tetracycline compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0223] Example 1 - General manufacturing steps for the gel

[0224] The following steps were used to produce the gel samples described in the following examples, where only the steps relevant to each formulation were performed depending on the type and nature of the ingredients used.

[0225] Step 1: Heat the hydrophobic oil to 60 to 70°C.

[0226] Step 2: Add fatty alcohol (if present), fatty acid (if present), wax (if present) to hydrophobic oil and mix formulation until fully melted.

[0227] Step 3: Cool the formulation to 30 to 40°C, add the tetracycline antibiotic and mix the formulation until homogeneity is obtained.

[0228] Step 4: Cool the formulation to room temperature with stirring and pack into suitable containers.

[0229] As will be understood by those skilled in the art, the experiments are only briefly set forth below by way of non-limiting example.

[0230] Viscosity was measured with a Brookfield LVDV-II+PRO with spindle SC4-25 at ambient temperature and...

Embodiment 2

[0232] Example 2 - Low Viscosity Gel Formulation

[0233] The different hydrophobic oils suitable for use in topical pharmaceutical compositions are generally liquid oils with low viscosity. As described in Table 2, when these oils are used as such for topical delivery of active agents, they especially have two undesirable properties: (1) Due to their low viscosity, they tend to drip and flow easily, thus being easy on the patient. Applied on the skin, (2) they have poor suspension properties, resulting in rapid sedimentation of the insoluble active ingredient (API).

[0234] Table 2 - Low Viscosity Oily Formulations

[0235]

[0236] As shown in formulations 001P and 002P, the mixture of mineral oil and soybean oil has low viscosity. Formulations 001 and 002, show that after addition of minocycline hydrochloride, the viscosity of the formulation remains unchanged and the active ingredient is deposited.

Embodiment 3

[0237] Example 3 - Mineral Oil Formulations with Improved Viscosity

[0238] The effect of tetracycline in combination with fatty alcohols, fatty acids and waxes on formulation viscosity was evaluated as described in Table 3a. Formulations containing mixtures of mineral oil and fatty alcohols, fatty acids or waxes were prepared and their viscosities were measured before and after the addition of tetracycline, minocycline hydrochloride. Table 3a below shows the results for the viscosity of the formulations before and after the addition of tetracycline, and the percentage increase in viscosity due to the addition of the active ingredient.

[0239] Table 3a - Combinations of Tetracyclines with Fatty Alcohols, Fatty Acids and Waxes

[0240]

[0241] Quite surprisingly, it was found that the addition of minocycline hydrochloride to mineral oil based formulations 003 to 005B resulted in a very large increase in viscosity despite using a very low amount of minocycline hydrochlori...

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
Melting pointaaaaaaaaaa
Densityaaaaaaaaaa
Minimum inhibitory concentrationaaaaaaaaaa
Login to view more

Abstract

A topical therapeutic hydrophobic breakable composition includes a carrier comprising (a) about 60% to about 99% by weight of at least one hydrophobic oil; (b) at least one viscosity-modifying agents selected from the group consisting of a fatty alcohol, a fatty acid and a wax; and (c) a tetracycline antibiotic, characterized in that at least part of the tetracycline antibiotic is suspended in the composition; the viscosity of the composition is at least about 30% higher than the viscosity of the carrier without the tetracycline antibiotic; and is higher than the viscosity of the hydrophobic oil and the tetracycline antibiotic without the viscosity modifying agents; and the amount of viscosity modifying agents can optionally be reduced by at least an amount by weight that would have increased the viscosity of the carrier without the tetracycline antibiotic by at least 30%; wherein the tetracycline is chemically stable in the composition for at least six months; wherein more than about 90% of the tetracycline has not broken down; wherein when packaged in an aerosol container to which is added a liquefied or compressed gas propellant the composition affords upon release from the container a breakable foam of at least good quality that breaks easily upon application of shear force.

Description

[0001] Cross References to Related Applications [0002] Pursuant to Section 119(e) of the U.S. Patent Act, this application claims U.S. Provisional Application No. 61 / 248,144, filed October 2, 2009, and entitled "Surfactant-Free Anhydrous Foaming Compositions, Breakable Foams and Their Uses (Surfactant-Free Water-Free Foamable Compositions, Breakable Foams and Their Uses)”; U.S. provisional application 61 / 322, No. 148 filed on April 8, 2010, titled “Surfactant-Free Water-Free Foamable Compositions, Breakable Foams and Their Uses”; Fragile Foams and Uses Thereof"; U.S. Patent Provisional Application No. 61 / 349,911, filed May 31, 2010, and entitled "Surfactant-Free Anhydrous Foaming Compositions, Fragile Foams and Uses Thereof"; September 2010 U.S. Patent Provisional Application No. 61 / 385,385 filed on the 22nd, entitled "Surfactant-Free Water-Free Foamable Compositions, Breakable Foams and Gels and Their Uses)”; U.S. Patent Provisional Application No. 61 / 331,126, filed May 4, 2...

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
IPC IPC(8): A61K8/02
CPCA61K9/0014A61K8/361A61K9/0048A61K31/573A61K8/342A61K9/122A61K31/137A61K31/192A61K31/65A61K47/12A61K31/57A61K31/593A61K47/10A61K31/4164A61K8/31A61Q17/04A61Q19/00A61Q19/10A61K2800/33A61K2800/31A61P1/00A61P11/00A61P15/00A61P15/02A61P17/00A61P17/02A61P17/04A61P17/06A61P17/08A61P17/10A61P17/12A61P17/14A61P17/16A61P19/02A61P23/00A61P25/00A61P25/20A61P25/24A61P27/02A61P27/06A61P29/00A61P31/00A61P31/04A61P31/10A61P31/12A61P31/14A61P31/18A61P31/20A61P31/22A61P33/00A61P33/10A61P33/14A61P35/00A61P37/00A61P37/02A61P37/04A61P37/06A61P37/08A61P39/06A61P5/00A61P7/10A61P9/00A61P9/08A61K47/44A61K47/06A61K9/12A61K45/06A61K47/02A61K47/24A61K9/124
Inventor D·塔玛金E·盖扎尔I·帕皮阿希维利Y·哈佐特D·舒茨R·基南
Owner FOAMIX PHARMACEUTICALS LIMITED
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap