THE PROCESS FOR MANUFACTURING TOPICAL FORMULATION OF PILOCARPINE WITH DISSOCIATION OF ITS EFFECT ON PUPIL AND I.O.P

摘要

The process for manufacturing topical formulation of Pilocarpine with dissociation of its effect on pupil and I.O.P. Pilocarpine is used to reduce I.O.P. in patients with glaucoma. It reduces I.O.P. by increasing outflow facility through trabecular meshwork. It is commonly used as 1%, 2% or 4% eye drops. It also has action on ciliary body and pupil. At 1%, 2% and 4% concentration, it causes miosis (contraction of pupil). Miosis caused by pilocarpine interferes with vision in poor illumination. It also reduces vision in presence of cataract in visual axis e.g. post-subcapsular cataract. It also hampers evaluation of visual field required to detect progress of glaucoma. Long term miosis causes rigidity of pupil and loss of its function to control light. Post-synechia are also seen in some individuals due to increased vascular permeability. Thus, there is a need of formulation, which does not have effect on pupil which is provided by beta-blockers. However, beta-blockers are not always adequate to control I.O.P. and additional drugs are used to control I.O.P. This includes Pilocarpine. It is desirable to have a formulation of Pilocarpine with more effect or identical effect on I.O.P and less pronounced effect on pupil. The process of manufacturing the formulation as per the present invention involves increasing viscosity to more than 3,00,000 caps. This can be achieved by using gelling substances to formulate gel. The concentration of gelling substances is to be adjusted in such a way that it is more than 3,00,000 cps. With Carbapol 940, it is achieved by 2% concentration.