Mucosal Bioadhesive SLow Release Carrier for Delivering Active Principles

Inactive Publication Date: 2009-07-02
ONXEO SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0038]Methods of alleviating, treating, preventing or curing various medical conditions also are a part of the present invention. Thus, medical conditions or diseases such as orofacial herpes-herpes simplex virus 1 (HSV-1), genital herpes-herpes simplex virus 2 (HSV-2), oral mucositis, fungal infections such as Candidiasis, viral infections such as Epstein-Barr virus, oral hairy leukoplakia, variacella-Zoster virus, human papilloma virus, cytomegalovirus, Kaposi's sarcoma due to human herpes V8 and genital warts due to human papilloma virus and other oral lesions including oral ulcers and salivary gland disturbance, altered oral flora (decreased bacterial flora), taste dysfunction, periodontitis, xerostomia (sal

Problems solved by technology

One of the problems associated with a bioadhesive drug delivery system for mucous membranes is that the lubricious nature of the mucous membranes allows for the active substance to be washed away or diluted lowering the drugs bioavailability such that the administered drug does not effectively treat the medical condition at hand.
Another problem is that in the oral cavity, eating drinking and speaking and the constant replacement of the saliva often effects the delivery of the active substance.
However, many people are lactose intolerant or are allergic to corn.
Therefore, mucosal delivery systems containing lactose or corn are impossible to use by this population of people.
Moreover, in many of the above-mentioned slow release bioadhesive systems, the formulation of low aqueous soluble or insoluble active principles is difficult.
Various categories of medicinal agents such as antivirals, analgesics, anti-inflammatories, antibiotics and antiseptics have members, which are hard to formulate and administer due to their low aqueous solubility or insolubility.
Numerous antiviral and immunosuppressive agents such as acyclovir are also difficult to formulate, have poor percutaneous penetration and have complications arising due to intramuscular administration at a strongly alkaline pH of 10-11.
Local treatment of acyclovir as a cream is also poor due to poor percutaneous absorption.
The bioadhesive delivery system thus has to be changed frequently, which can result in added burden to the mammal receiving such treatment.
Thus, there are problems associated in the prior art for mucosal delivery that can deliver the active principle to treat various medical complications over a long period of time and more specifically greater than 20 hours.
Furthermore there are problems also associated with the prior art with respect to the delivery of active principles, which have low aqueous solubility or are insoluble.

Method used

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  • Mucosal Bioadhesive SLow Release Carrier for Delivering Active Principles
  • Mucosal Bioadhesive SLow Release Carrier for Delivering Active Principles
  • Mucosal Bioadhesive SLow Release Carrier for Delivering Active Principles

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of the Bioadhesive Slow Release Carrier of the Present Invention

[0128]100 mg of acyclovir, 15% by weight microcrystalline cellulose and 45% by weight of sodium lauryl sulfate were weighed and sieved with a 0.7 to 2 mm sieve before premixing in a blender to provide the “initial mix.”

[0129]At the same time, 0.4% by weight polyvinylpyrrolidone was dissolved in purified water: The resulting solution was added to the initial mix and further stirred. The wetted mixture was then granulated using a pharmaceutical mixer or granulator such as a planetary mixer or high sear mixer and dried and then calibrated to 500 μm. The resulting pellets formed the “primary granules.”

[0130]20% milk concentrate protein, 15% hypromellose, 1% magnesium stearate and 0.4% of colloidal silica were weighed and sieved using a 500 μm sieve. These ingredients were then added to the primary granulation to form the “final blending” mixture. The final blending mixture was then compressed using a tablet pres...

example 2

Particle Size Distribution of the Primary Granules

[0133]The primary granules obtained from the procedure in Example 1, after granulating, drying and calibrating, were then evaluated by sieve analysis based on the procedure described in the European Pharmacopoeia. Also an analysis was undertaken to determine the content of acyclovir in the different fractions of the granulations or in the whole granule. The acyclovir content in the granule was assayed using phosphate buffer at pH 6. Two different formulations were compared. The first formulation corresponded to those obtained in Example 1 of the present invention, while the “control formulation” was that disclosed in U.S. Pat. No. 6,916,485, to obtain the “primary grain” set forth in FIG. 1 therein.

[0134]The results are presented in FIG. 2. When granulations were prepared according to the formulation described in U.S. Pat. No. 6,916,485 (white bars), the size distribution of the granules reveals a strong heterogeneity, with the prese...

example 3

In Vitro Evaluation of an Acyclovir Bioadhesive Slow Release Carrier

[0136]The bioadhesive slow release carriers obtained by the process described in Example 1 were tested for acyclovir release through a dissolution method. The test was conducted according to the current dissolution testing described in U.S. Pharmacopoeia, 23rd edition, Chapter 711 (Dissolution) pages 1791-1793. More specifically, sample vessels were submerged in a water bath at 37° C., in a suitable dissolution medium of phosphate buffer at a pH of 6 and the content of the vessels were agitated using a “rotating basket” attached to a shaft that is also attached to another shaft. The solid bioadhesive slow release carriers of the present invention were placed in the medium filled vessel at time zero. The water bath was maintained at 37° C. throughout the experiment, as well as the mixing speed of 60 rpm. 1 ml aliquots were taken from the vessels every hour for the first eight hours, then at 10, 11, 12, 15 and 24 hour...

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Abstract

A mucosal bioadhesive slow release carrier comprising an active principle and devoid of starch, lactose, which can release the active principal for a duration of longer than 20 hours. This bioadhesive carrier contains a diluent, an alkali metal alkylsulfate, a binding agent, at least one bioadhesive polymer and at least one sustained release polymer, as well as a method for its preparation.

Description

FIELD OF THE INVENTION[0001]The present invention relates to a bioadhesive slow release carrier for the extended and controlled release of an active principle that can be used on mucosal surfaces. A process for manufacturing the bioadhesive system, a method for delivering an active ingredient to a mammal, as well as methods of treating, curing or preventing various medical conditions are also disclosed.BACKGROUND OF THE INVENTION AND RELATED PRIOR ART[0002]Mucous membranes are linings of ectodermic origin, covered in epithelium, and are involved in absorption and secretion. They line various body cavities that are exposed to the external environment as well as internal organs, such as the nostrils, the lips, the ears, the genital area, the digestive tract and the anus. Parts of the body featuring mucous membranes include most of the respiratory tract and the entire gastrointestinal tract, as well as the vagina, cervix, the clitoris, the covering of the glans penis and the inside of ...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K47/36A61K47/32A61K31/52A61K31/7072A61K31/662A61K31/708A61K31/13A61K38/21A61P31/12A61K47/38
CPCA61K9/0056A61K9/006A61K9/2027A61K47/38A61K31/4178A61K31/4468A61K31/522A61K9/2063A61P23/00A61P25/04A61P29/00A61P31/04A61P31/12A61K9/20
Inventor COSTANTINI, DOMINIQUELEMARCHAND, CAROLINE
Owner ONXEO SA
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