FORM-2
THE PATENT ACT, 1970
(39 of 1970)
&
THE PATENT RULES, 2003
PROVISIONAL SPECIFICATION
(See section 10 and Rule 13)
STERILE OPTHALMIC PREPARATIONS AND A PROCESS FOR PREPARATION THEREOF
M. J. BIOPHARM PVT. LTD.
an Indian Company
of 113, Jolly Maker Chambers No. 2, Nariman Point, Mumbai-400 021, Maharashtra, India,
THE FOLLOWING SPECIFICATION DESCRIBES THE INVENTION

The present invention relates to sterile opthalmic preparations and a process for preparation thereof..
3-Hydroxy-2,4,6-trimethylpyridine succinate and other such salts belong to a group of new biologically active compounds. These compounds exhibit antioxidant and geroprotective action. They are found to be useful as anti oxidant for the vascular and inflammatory eye pathology.
To deliver or dispense a therapeutic dose of a pharmaceutically active ingredient for treatment in eye pathological conditions, a stable and pharmaceutically acceptable dosage form is required.
It is an object of this invention to prepare simple and cost effective ophthalmic preparations containing biologically active antioxidants and gero-protective compounds and pharmaceutically acceptable salts thereof.
It is another object of this invention to prepare sterile and stable ophthalmic preparations containing biologically active antioxidants and gero-protective compounds and pharmaceutically acceptable salts thereof.
The term 'sterile ophthalmic preparations' as used in the context of this invention includes liquid preparations [eye drops, solutions and suspensions] as well as semi-solid preparations [eye ointment, eye gel].
In accordance with the present invention, there is provided a sterile, stable ophthalmic preparation containing at least one pharmaceutically acceptable


parent base substance 3-Hydroxy-2, 4, 6-trimethylpyridine and/or derivative and/or salt thereof either alone or in combination with other pharmaceutically acceptable active ingredient along with carriers and excipients.
Pharmaceutically acceptable salt of 3-Hydroxy-2, 4, 6-trimethylpyridine is selected from a group of pharmaceutically acceptable salts with organic acids or mineral acids consisting of salicylate, maleate, succinate, fumarate, malate, tartrate, oxalate, citrate, pamoate, hydrochloride, hydrogen sulfate, sulfate methanesulphonate, and benzenesulfonate.
The concentration of the active ingredients in the ophthalmic preparation as envisaged in this invention is in the range of about 0.01% w/v to about 10 % w/v, preferably below 5% w/v and more preferably l%w/v.
Typically, the preservative is at least one preservative selected from a group of preservatives consisting of benzalkonium chloride, chlorocresol and phenyl mercuric nitrite.
Typically, the excipients include at least one excipient selected from a group of excipients consisting of thickening agents, chelating agents, isotonicity adjusters, buffering agents, alkaline agents for pH adjustments and a vehicle.
Typically, the thickening agent is selected from a group of thickening agents consisting of cellulose derivatives: hydroxypropyl methylcellulose, hydroxypropyl cellulose, sodium carboxy methyl cellulose, and hydroxyethyl cellulose. Typically, the isotonicity adjuster used is selected from a group consisting of sodium chloride, mannitol or boric acid. Typically, the chelating


agent used is edetate disodium. Typically, the buffering agent used may be phosphate or acetate buffer.
In accordance with one of the preferred embodiments of this invention, the sterile ophthalmic preparations are in the form of at least one liquid preparation selected from a group of liquid preparations consisting of eye drops, solutions and suspensions.
Typically, eye drop preparations in accordance with this invention comprise a pharmaceutically acceptable parent base substance 3-Hydroxy-2, 4, 6-trimethylpyridine and/or derivative and/or salt thereof, with or without addition of a preservative substance and excipients.
The vehicle used may be aqueous or non-aqueous. Typically, water for injection is used as a vehicle.
The preparation solution is maintained at a suitable pH within a specified range.
In accordance with another preferred embodiments of this invention, the sterile ophthalmic preparations are in the form of at least one semi-solid preparation selected from a group of semi-solid preparations consisting of ointment and gel.
The formulated product is adjusted to required pH range with buffer, alkali or acid solutions. The dosage form in ointment or gel may be filled in aluminum tube or lami tube, or for unit dose application in soft gelatin capsules (applicap)


for a semisolid preparation; and in vials with eye drop applicator or in plastic bottles with applicator or in any other such suitable containers as unit dose or multi dose preparation for therapeutic application of the biologically active compound 3-hydroxy-2,4,6-trimethylpyridine or pharmaceutically acceptable derivative or salt thereof.
The invention also provides a process of preparation of sterile and non-toxic ophthalmic formulated dosage forms containing biologically active compounds with a concentration in the range of about 0.01% w/v to about 10 % w/v preferably below 5% w/v and more preferably l%w/v.
The entire process is carried out in a sterile environment. The resultant ophthalmic preparation is sterilized, either by sterile filtration or by autoclaving and or by a suitable and pharmaceutically acceptable sterilization process and then filled in containers. Such containers can be of various designs which can be used for sterile ophthalmic preparations.
The sterile ophthalmic preparations formulated as per description of this invention are pharmaceutically stable and meet standards of specifications prescribed. These preparations are stable under specified storage condition and meet various physico-chemical and microbiological standards of specification as per pharmacopoeal requirements.
The sterile ophthalmic preparations in accordance with this invention are meant for administering therapeutic dose of the biologically active ingredients in eye pathological conditions such as vascular and inflammatory eye pathology,


traumatic hemophthalmia, intra-ocular haemorrhages and inflammatory pathology of eye ball.
The ophthalmic preparations made with pharmaceutically acceptable parent base substance 3-Hydroxy-2, 4, 6-trimethylpyridine and/or derivative and/or salt thereof either alone or in combination with other pharmaceutically acceptable active ingredient along with carriers and excipients in accordance with this invention are pharmaceutically stable and are useful in clinical applications like traumatic hemophthalmia, intra-ocular haemorrhages and inflammatory pathology of eye ball.
While considerable emphasis has been placed herein on the specific ingredients of the preferred composition, it will be appreciated that many additional ingredients can be added and that many changes can be made in the preferred composition without departing from the principles of the invention. These and other changes in the preferred composition of the invention will be apparent to those skilled in the art from the disclosure herein, whereby it is to be distinctly understood that the foregoing descriptive matter is to be interpreted merely as illustrative of the invention and not as a limitation.