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

Controlled release doxycycline

a technology of doxycycline and doxycycline, which is applied in the direction of biocide, plant growth regulator, animal husbandry, etc., can solve the problems of reducing the availability of free fatty acids involved in inflammation, gastrointestinal irritation and nausea undesirable, and the class of compounds suffers from a major drawback associated with administration, so as to increase the efficacy of the antibiotic and reduce the release level. , the effect of increasing the tolerability

Active Publication Date: 2016-04-14
MAYNE PHARMA INT
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The new doxycycline formulations have a better release profile than other formulations, which improves the effectiveness of the antibiotic, makes it tolerable, and helps patients to take the medicine more easily.

Problems solved by technology

Doxycycline can also inhibit lipase produced by the bacterium Propionibacterium acnes and thus reduces the availability of free fatty acids that are involved in inflammation.
While tetracyclines have proven to be very beneficial and successful antibiotics, this class of compounds suffers from a major drawback associated with administration.
Namely, tetracycline antibiotics cause an undesirable degree of gastrointestinal irritation and nausea in subjects taking the medications.
The high localized concentration of the antibiotic in the patient's stomach leads to irritation and nausea.
However, many of these formulations suffer from inadequate dissolution profiles that do not provide an effective dose of antibiotic at the desired concentration and for the desired period of release.

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
  • Controlled release doxycycline
  • Controlled release doxycycline
  • Controlled release doxycycline

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Controlled Release Doxycycline Hyclate Pellets Core Preparation

[0169]The core is formed in a wet granulation process using a saturated solution of sodium chloride and in a high shear mixer.

[0170]The mixture is then extruded using a screen size of between 0.4 and 1.5 mm. The extrudate is then marumerised to produce rounded core elements. The core elements are dried in a fluidized bed or an oven.

[0171]Stabilizing Coat Application

[0172]A stabilizing coat is applied to the core using a fluidized bed coating process.

[0173]The stabilizing coat contains hydroxypropylmethyl cellulose and talc in a 2:1 mixture.

[0174]The desired polymer coat weight (i.e. the weight of the polymer only, not including the talc) is between 3% and 5% of the total weight of the core element and the stabilizing coat.

[0175]The polymer coat weight will vary due to a number of factors, such as the efficiency of the coating process, the batch of raw materials, etc.

[0176]Modified Release Coat Application

[...

example 2

Dissolution Profiles of Control (DORYX), Pellet A Formulation, & Pellet B Formulation Acidic Dissolution Profile

[0183]The acid environment dissolution profile of pellet A and B's formulation can be seen in FIG. 1.

[0184]As can be seen in FIG. 1, the formulations of pellet A and B release less than 10% of the doxycycline hyclate in an acid environment (pH of approximately 1.2) after 60 minutes of exposure under standard USP conditions.

[0185]The slow rate of release of doxycycline, in a pH of approximately 1.2, exhibited by the pellet formulations according to the disclosure is in stark contrast to the dissolution profile of the commercially available DORYX.

[0186]As can be seen in FIG. 1, the DORYX tablet released approximately 98%-100% of the doxycycline hyclate at 60 minutes.

[0187]Thus, the controlled release doxycycline formulations of the disclosure exhibit a beneficial and superior dissolution profile in acidic conditions, as compared to a commercially available doxycycline formul...

example 3

Clinical Data

[0195]The aforementioned controlled release pellet formulations (A and B) were loaded into capsules and administered to 10 test subjects to obtain in vivo data.

[0196]It is also contemplated that pellet formulations A and B may be formulated into tablets.

[0197]After all 10 completed subjects were analyzed; the following Geometric Mean Ratio (GMR) and Intra-Subject Coefficient of Variation (CV) were obtained for the two Test Formulations.

TABLE 2In Vitro Pharmacokinetics DataFormulationParameterGMR (%)CV (%)Pellet AAUC0-∞89.6417.24AUC0-t89.5817.71Cmax88.0819.87Pellet BAUC0-∞106.9017.24AUC0-t106.3717.71Cmax103.7319.87

[0198]Further, FIG. 3 and FIG. 4 illustrate the concentration of active substance in ng / mL of the two tested pellet A and pellet B formulations as compared to a doxycycline (DORYX) control.

[0199]As shown in FIG. 3, 90 mg controlled release pellet formulations (A and B) of the present invention have average AUC0-t values (ng·hr / ml) which differ from that of conv...

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
pHaaaaaaaaaa
pHaaaaaaaaaa
pHaaaaaaaaaa
Login to View More

Abstract

The disclosure provides controlled release compositions comprising tetracyclines and in some embodiments, doxycycline. The controlled release doxycycline compositions of the invention exhibit a superior dissolution profile and provide reduce side effects such as nausea and irritation.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]The present application is a U.S. Utility application claiming priority to U.S. Provisional Application No. 62 / 061,481, filed on Oct. 8, 2014, the entire contents of which are hereby incorporated by reference in their entirety.FIELD[0002]The present disclosure relates to the field of pharmaceutical compositions comprising tetracyclines. In specific aspects, the disclosure provides pharmaceutical compositions comprising doxycycline that have improved controlled release characteristics.BACKGROUND[0003]Tetracyclines, such as doxycycline, are used as broad spectrum antibiotics to treat various bacterial infections. Tetracyclines interfere with the protein synthesis of Gram positive and Gram-negative bacteria by preventing the binding of aminoacyl-tRNA to the ribosome. Their action is bacteriostatic (preventing growth of bacteria) rather than killing (bactericidal). The doses commonly used for doxycycline to achieve the antibiotic effect are 1...

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): A61K9/16A61K31/65
CPCA61K9/167A61K9/1652A61K31/65A61K9/5042A61K9/5047A61K9/5073A61K9/0053A61K9/4808
Inventor LUKAS, STEFANLEPORE, ANGELOMUDGE, STUART
Owner MAYNE PHARMA INT
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