Paracetamol-based pharmaceutical composition

Details Paracetamol-based pharmaceutical composition Paracetamol-based pharmaceutical composition

1991-11-12

1993-12-14

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Implant or insert

514912, 514914, 424 45, A61K 3174, A61K 31135

Patent

active

052700500

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to a paracetamol(n-acetyl-p-aminophenol)-based pharmaceutical composition.
Paracetamol is a compound well known for its antipyretic and analgesic activity.
This activity has been considered to be due to the inhibition of the synthesis of the prostallandins in the central nervous system. However, even though it inhibits the cyclo-oxygenase in the central nervous system, it shows no activity on this enzyme in the periphery (see, in particular, M. Scott Linscott, Clinical Therapeutics 9, 1, 1986).
Moreover, paracetamol has hitherto been administered, in practice, by the oral route.
The Applicant has made the surprising discovery that paracetamol administered to the eye has a useful pharmacological activity and may be used as an analgesic as well as for the treatment and prevention of cataracts.
Thus, the invention relates to an ophthalmic composition containing from 0.1 to 10% by weight of paracetamol in an ophthalmic excipient.
By ophthalmic excipient is meant an excipient which allows the administration of the active ingredient to the eye and which is not harmful to the eye. The composition may be made available in the form of an ophthalmic solution containing an aqueous solution, paracetamol and a buffer and, optionally, an antioxidant and a preservative.
The composition may also be constituted by an aqueous ophthalmic gel, an aqueous ophthalmic emulsion or an ophthalmic ointment.
Examples of ophthalmic compositions according to the invention will be given hereafter.


EXAMPLE 1



Collyrium Containing 1% Paracetamol

The following composition is prepared:


______________________________________ Paracetamol 1 g Sodium metabisulfite 0.1 g EDTA 50 mg Benzalkonium chloride 5 mg NaH.sub.2 PO.sub.4, 2H.sub.2 O 0.38 g Na.sub.2 HPO.sub.4, 10H.sub.2 O 1.6 g NaCl 0.16 g Purified water qsp 100 ml ______________________________________
The composition has a pH between 6.8 and 7.2.


EXAMPLE 2



Ophthalmic Aerosol Containing Paracetamol

The composition of Example 1 may be packaged in an aerosol container.


EXAMPLE 3



Collyrium Containing 5% Paracetamol

The following composition is prepared:


______________________________________ Paracetamol 5 g Sodium metabisulfite 0.1 g Nipagine 26 mg Nipasol 14 mg NaH.sub.2 PO.sub.4, 2H.sub.2 O 0.38 g Na.sub.2 HPO.sub.4, 10H.sub.2 O 1.6 g Cremophore.sup.R 25 g Water qsp 100 ml ______________________________________


EXAMPLE 4



Paracetamol-Based Ophthalmic Gel

1% carbopol is added to the composition of Example 1. The pH is adjusted to 7 with NaOH.


EXAMPLE 5



Paracetamol-Based Ophthalmic Ointment

The following composition is prepared:


______________________________________ Paracetamol 5 g Vaseline 50 g Viscous vaseline oil 15 g Lanolin 35 g ______________________________________


EXAMPLE 6



Ophthalmic Emulsion

The following emulsion is prepared:


______________________________________ Paracetamol 1 g Sodium metabisulfite 0.1 g EDTA 50 mg Benzalkonium chloride 5 mg NaH.sub.2 PO.sub.4, 2H.sub.2 O 0.38 g Na.sub.2 HPO.sub.4, 10H.sub.2 O 1.6 g NaCl 0.16 g Cremophore.sup.R 10 g Fatty excipient 30 g Water qsp 100 ml ______________________________________
Pharmacological results demonstrating the properties of the compositions according to the invention are given below.


I. Effect on Photokeratitis Induced by UV-B in the Rabbit

10 Male, albino New Zealand rabbits of means weight 2 kg and free of any ocular infection (prior ophthalmic examination) are used for the assays.
The irradiations were performed as follows:
50 .mu.l of physiological serum were instilled into the left eye. The animals were placed in a restraining cage under UV light. The left eye was irradiated with UV-B (312 nm) (the right eye being protected) at an intensity of 0.4 J/day (which corresponds to 3'30" of exposure) for 7 days.
Macroscopic ocular examinations were made every day. conjunctivae,


Treatment

These animals were divided into 2 homogeneous groups of 5 animals (groups A and B

REFERENCES:
patent: 4476115 (1984-10-01), Reed
patent: 4605754 (1986-08-01), Khanna
W. F. Williams et al., "The utilization of carbon-13 and phosphorus-31 nuclear magnetic resonance spectroscopy in the study of the sorbitol pathway and aldose reductase inhibition in intact rabbit lenses", Exp. Eye Res. (1987) vol. 44, pp. 717-730.

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