Buccal Delivery System

US20080317850A1Inactive Publication Date: 2008-12-25OZPHARMA
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Examples

Experimental program
Comparison scheme
Effect test

example 1

Comparative Example

[0075]This example shows the process for preparation of troches as per the prior art.

[0076]The ingredients used for 28 Troches is shown in Table 1.

TABLE 1IngredientsDrugAmountsStevia powder130mgMethocel E4M1.45gBase A PEG 1450q.s to 30gFlavour60 uL-800 uL

Preparation of Components

[0077]The required quantity of active ingredients is calculated (e.g. 200 mg progesterone for 30 lozenges requiring 6.0 g of progesterone).[0078]Required components are weighed out and placed into clean labelled weigh trays (eg 0.01 g).

Preparation of PEG Base

[0079]In a large 4 litre beaker, the base required for the day is calculated (see Table 2) and placed on the hotplate to melt inside a water bath. The bath is set at 60° C.[0080]Once Base A is melted, the other ingredients are added and stirred with a spatula.

TABLE 2Approx 1Approx 25Approx 50Approx 75Approx 100trochestrochestrochestrochestroches(29 mls)(725 mls)(1450 mls)(2175 mls)(2900 mls)Base A28.10 g702.5g1405g2107.5 g2810.0gStevia...

example 2

[0088]This example demonstrates the manufacture of LINGUET tablets according to the invention. Release powders containing the equivalent of 5, 10 and 40 mg of the active ingredient sodium alendronate were blended together with the following excipients:[0089]PEG 1000-8000 molecular weight, varied according to required hardness and time for dissolution of tablet

Magnesium Stearate:0.05-2%by weightKollidon:0.05-2%by weightStevia:0.05-2%by weightActive Ingredient:up to 60%by weight

[0090]Standard dry blending was performed in a horizontal low-energy laboratory blender for 60 mins. Powder mixtures were subsequently blended with PEG for 5 mins, and directly compressed via TabletPress Inc Benchtop single press tablet punch.

[0091]Dissolution times for these LINGUET tablets range from 10 to 20 mins, while a slightly longer period of 15-20 mins was required for complete dissolution following buccal administration.

example 3

[0092]This example investigated the bioavailability of hormone replacement therapy active ingredients using the buccal delivery system of the invention in a clinical trial in a hospital. The trial was conducted with approval of an ethics committee within the hospital.

[0093]LINGUET tablets were generated containing 17-p-oestradiol (0.5 mg), progesterone (200 mg), testosterone (2.0 mg) and DHEA (10.0 mg). The excipients in the LINGUET tablets consisted of silica gel, magnesium stearate, acacia, stevia and polyethylene glycol with a wildberry flavour. The LINGUET tablets employed in this trial were formulated in a single batch for the study using the process according to the invention as described in example 2 above. The LINGUET tablets were provided by Richard Stenlake Compounding Pharmacist (Bondi Junction, Australia).

Study Protocol

[0094]The study was an open-label investigation in six post-menopausal women. Before entry into the trial, subjects gave informed consent, and underwent m...

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Abstract

A buccal delivery system capable of being blended in a normal dry powder process and compressed using a standard tabletting machine, said buccal delivery system comprising a matrix of: (a) an effective amount of one or more active ingredients; (b) an amount of one or more polyethylene glycols or derivatives thereof having a molecular weight between 1000 to 8000 sufficient to provide the required hardness and time for dissolution of the matrix; (c) 0.05-2% by weight of the total matrix of one or more suspending agents; (d) 0.05-2% by weight of the total matrix of one or more flowing agents; and (e) 0.05-2% by weight of the total matrix of one or more sweeteners.

Description

FIELD OF THE INVENTION[0001]The invention relates to a buccal delivery system which provides improved delivery of therapeutic agents. In particular, the present invention relates to buccal dosage formulations. The present invention further provides easier and more economic methods of manufacturing a dosage formulation capable of delivering one or more active ingredients via buccal membranes.BACKGROUND OF THE INVENTION[0002]In this specification where a document, act or item of knowledge is referred to or discussed, this reference or discussion is not an admission that the document, act or item of knowledge or any combination thereof was at the priority date, publicly available, known to the public, part of common general knowledge; or known to be relevant to an attempt to solve any problem with which this specification is concerned.[0003]The ability to effectively deliver therapeutic agents to animals and, in particular, humans is frequently dependent on compliance of the recipient....

Claims

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Application Information

Patent Timeline
25 Dec 2008
Publication
US20080317850A1
IPC
A61K9/20; A61K47/34; A61K31/57; A61K31/565; A61K31/568; A61K31/66
CPC
A61K9/0056; A61K9/2031; A61K9/2095; A61P1/00; A61P3/02; A61P3/10; A61P5/26; A61P5/30
Inventors
HEWITT, ERNEST ALAN; STENLAKE, RICHARD JAMES