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Fast Dissolving Ocular Insert

a technology of ocular insert and fast dissolution, which is applied in the direction of prosthesis, biocide, peptide/protein ingredients, etc., can solve the problems of low bioavailability of ophthalmic drugs when administered, limited application range, and patients' difficulty in administering conventional eye drops

Inactive Publication Date: 2015-07-30
UNIVERSITY OF THE WITWATERSRAND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent is about a pharmaceutical dosage form that delivers an active pharmaceutical ingredient (API) to a specific target site in a human or animal. The dosage form is made up of a solid matrix formed by a combination of a polyethylene oxide block copolymer and hydroxpropyl cellulose (HPC). The matrix is designed to release the API slowly over time. The dosage form can also contain other ingredients such as an anti-collapsing agent, a lyoprotectant, a superabsorbent polymer, and an active pharmaceutical ingredient (API). The method of manufacturing the dosage form involves dissolving the polymers in a liquid and adding the other ingredients. The resulting solid ocular pharmaceutical dosage form is a tablet with circular or discoid dimensions. The technical effect of this patent is to provide a more effective and targeted delivery of active pharmaceutical ingredients to the eye.

Problems solved by technology

Despite the convenience and compliance using eye drops, limitations are evident.
This results in low bioavailability of ophthalmic drugs when administered using topical dosage forms such as eye drops (du Toit et al., 2011).
Patients often have difficulty administering conventional eye drops due to the following reasons: Firstly, compliance is a problem since eye drops typically have to be administered several times during the course of the day.
Secondly, certain patients with conditions such as arthritis have difficulty administering the eye drops since handling of the eye drop bottle poses a problem.
These patients are then disadvantaged due to lack of control and synchronization of the bottle together with the eye-lid closure reflex.
However, their use is associated with several disadvantages.
For example, gels and ointments can blur vision and cause reflex blinking.
Contact lenses may prove difficult to insert and requires removal (Saettone and Salimen, 1995).
This results in the liquid preparations being forced out or even prevents entry into the anterior eye altogether.
As mentioned, eye drops may be difficult to administer and are easily flushed out thus resulting in poor bioavailability especially in elderly patients (Davies, 2000).
Disadvantages of these systems are that they dissolve in the range of hours and may be displaced from their original position within the eye after administration causing some degree of irritation.
In terms of ocular delivery, the concept of fast disintegrating systems has not been thoroughly explored.
This results in the formation of the porous product.

Method used

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  • Fast Dissolving Ocular Insert
  • Fast Dissolving Ocular Insert
  • Fast Dissolving Ocular Insert

Examples

Experimental program
Comparison scheme
Effect test

example 1

References for Example 1

[0118]1. Abduljalil, K., Diestelhorst, M., Doroshyenko, O., Lux, A., Steinfeld, A., Dinslage, S., Süverkrüp, R., Fuhr, U., (2008). Modelling ocular pharmacokinetics of fluorescein administered as lyophilisate or conventional eye drops. European Journal of Clinical Pharmacology, 64, 521-529.

[0119]2. Ali, M., Horikawa, S., Venkatesh, S., Saha, J., Hong, J. W., and Byrne, M. E., (2007). Zero-order therapeutic release from imprinted hydrogel contact lenses within in vitro physiological ocular tear flow. Journal of Controlled Release, 124, 154-162.

[0120]3. El Magraby, G. H., and Alomrani, A. H. (2009). Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose. Scientia Pharmaceutica, 77, 401-417.

[0121]4. Anderson, M. J., and P. J., Whitcomb. (2007). DOE simplified practical tools for effective experimentation. Productivity Press, New York.

[0122]5. Anumolu, S. S., Singh, Y., Gao, D., Stein, S....

example 2

References for Example 2

[0239]1. Barrett, E. P., Joyner, L. G., Halenda, P. P., 1951. The determination of pore volume and area distributions in porous substances. Computations from nitrogen isotherms: J Amer Chem Soc. 73:373-380.

[0240]2. Choonara, Y. E., 2011. An in vitro study of the design and development of a novel donut-shaped minitablet for intraocular implantation. A thesis submitted to the Faculty of Health Sciences, University of the Witwatersrand in fulfillment of the requirements for the degree of Doctor of Philosophy.

[0241]3. Condon, J. B., 2000. Equivalency of Dubinin-Polanyi equations and QM based sorption isotherm equation. B. Simulations of heterogeneous surfaces. Microporous Mesoporous Mat, 38, 359-383.

[0242]4. Corveleyn, S., Remon, J. P., 1996. Maltodextrins as lyoprotectants in the lyophilization of a model protein, LDH. Pharm Res, 13, 146-50.

[0243]5. Costa, P., Lobo, J. M. S., 2001 Modeling and comparison of dissolution profiles. Eur J Pharm Sci, 213, 123-133.

[02...

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Abstract

This invention relates to a pharmaceutical dosage form, particularly to a topical ocular pharmaceutical dosage form comprising a polymeric matrix of polyethylene oxide block copolymer, preferably polyoxyethylene-polyoxypropylene block copolymer and hydroxpropyl cellulose, and a pharmaceutically active ingredient incorporated within the matrix. The invention extends to a method of manufacturing the pharmaceutical dosage form.

Description

FIELD OF INVENTION[0001]This invention relates to a pharmaceutical dosage form, particularly to a topical ocular pharmaceutical dosage form comprising a polymeric matrix of polyethylene oxide block copolymer, preferably polyoxyethylene-polyoxypropylene block copolymer and hydroxpropyl cellulose, and a pharmaceutically active ingredient incorporated within the matrix. The invention extends to a method of manufacturing the pharmaceutical dosage form.BACKGROUND TO THE INVENTION[0002]Ocular disorders, conditions or diseases of the anterior segment of eye require an effective topical, locally acting, drug delivery system that ensures penetration of the drug through the cornea, effective therapeutic drug levels and patient compliance. Topical methods for drug delivery to the anterior eye remain one of the most convenient and common means of drug delivery. In particular, the use of eye drops still dominates as the drug delivery system of choice by patients. Thus, focus has been directed to...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/00A61K31/5377A61K31/196A61K9/20
CPCA61K9/0051A61K9/2054A61K9/2031A61K9/2013A61K9/2095A61K9/2027A61K31/5377A61K31/196A61K9/2077A61K9/2059A61K9/2072A61K31/138A61K31/4196A61K45/06C07H15/02
Inventor CHOONARA, YAHYA ESSOPDU TOIT, LISA CLAIREKUMAR, PRADEEPPILLAY, VINESSMOOSA, RAEESA M.JHETAM, RAFEEQ
Owner UNIVERSITY OF THE WITWATERSRAND