Process for producing a sterile prednisolone gel

Details Process for producing a sterile prednisolone gel Process for producing a sterile prednisolone gel

1996-11-27

1998-09-22

Fay, Zohreh

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514178, A61K 3156

Patent

active

058114173

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

The invention concerns a method of producing a prednisolone gel.


BACKGROUND OF THE INVENTION

Prednisolone is a glucocorticoid, of which its anti-inflammatory effect is about two or three times stronger than other similar cortisones. Prednisolone is known as an anti-inflammatory and anti-rheumatic drug. For treating dermatological conditions and allergies, local application is preferred. As an anti-inflammatory and allergy medicine, prednisolone, to a large extent, is also used for ophthalmological purposes.
The previously used commercial preparations containing prednisolone, for topical application, particularly for the eyes, are either aqueous suspensions or ointments, since prednisolone is not sufficiently soluble in water and, therefore, must be put in suspension or in an ointment or suspension-ointment. The disadvantage of aqueous suspensions of active agents such as hormones is normally, as is known to the artisan skilled in pharmaceutical technology, the danger of so-called "caking," viz., the formation of sediment, which necessitates shaking before application of the suspension. This agitation of the medicine by the layperson is frequently not correctly carried out and, therefore, an inaccurate dosage can occur. The disadvantage of the ointment-suspension lies in the relatively poor compatibility on account of the particle size of the prednisolone. Although compliance by the patient can significantly reduce its occurrence, eye injury on account of sedimentation can occur. There exists, therefore, a need for prednisolone in the form of a gel that has good compatibility in a preparation for topical application, especially for application to the eye. The production of such a gel, however, is very difficult, because a suspension of prednisolone or its pharmaceutically acceptable ester is not sterilizable by means of autoclaving. Heat treatment accelerates the hydrolysis of the active ingredient and, moreover, presents the danger of causing undesirable crystal growth to occur. Gels, for example of a polyacrylate gel, are actually in principle heat sterilizable, but for application to the eye, the preparation must be isotonic and isotonic agents such as sorbitol, glycerin, and the like tend to change color on heating. In other words, the ingredients in a polyacrylate gel can turn a brownish color after autoclaving, which is not acceptable to the patient.
European patent publication EP 0562 445 A2 discloses a gel with a viscosity of 10,000 to 50,0000 mpas, comprising a polyacrylate and a further polymer or polymeric mixture, for application to the eye, with customary auxiliary ingredients and optionally with one or more known ophthalmologically active ingredients.


BRIEF DESCRIPTION OF THE INVENTION

The invention concerns a method for producing a sterile prednisolone gel. The method is characterized in that prednisolone or its pharmaceutically acceptable ester is sterilized and incorporated into a sterile polyacrylate gel, which has been per se conventionally produced, in appropriate amount under aseptic conditions, or else the sterile prednisolone or its pharmaceutically acceptable ester is suspended in a part of the amount of water required for producing the polyacrylate suspension and is then homogenously incorporated into the polyacryate, which is then made into a gel.


DETAILED DESCRIPTION OF THE INVENTION

According to one embodiment of the present invention, there is now a method of producing a sterile prednisolone gel that is characterized in that a sterile polyacrylate gel is produced, but that prednisolone or its pharmaceutically acceptable salt is separately sterilized and incorporated into the acrylate gel, in a suitable amount, under aseptic conditions. Alternatively, the sterile prednisolone or its pharmaceutically acceptable ester is suspended with a part of the solution, which may contain a sterile tonicity agent, used for the production of the polyacrylate gel, and this suspension is then homogenously mixed in with the separately sterilized polyacrylate gel.
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REFERENCES:
Chemical Abstracts 119:234-62 (1993). Lobering et al.

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