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Vehicle Effects in Ophthalmic Bioavailability: An Evaluation of Polymeric Inserts Containing Pilocarpine

Vehicle Effects in Ophthalmic Bioavailability: An Evaluation of Polymeric Inserts Containing Pilocarpine

M F Saettone, B Giannaccini, P Chetoni, G Galli, E Chiellini

J Pharm Pharmacol. 1984 Apr;36(4):229-34.

PMID: 6144768

Abstract:

A series of polymeric ophthalmic inserts containing pilocarpine were formulated with four different types of polyvinyl alcohol, PVA, and two types of hydroxypropylcellulose. Pilocarpine was present as the nitrate, or as the salt with polyacrylic acid, PAA. In-vivo miosis vs time experiments on albino rabbits, showed that all inserts increased significantly the bioavailability of pilocarpine, with respect to a standard solution of pilocarpine nitrate. Two PVA inserts, containing the PAA-salt of pilocarpine, were particularly effective. The preparations were also submitted to in-vitro release tests and to differential scanning calorimetry, to ascertain the release mechanism, and to verify, via the thermal behaviour, possible interactions between drug and polymers. The chemical and physiochemical factors, most likely to influence the ophthalmic bioavailability of pilocarpine from the present preparations, are briefly reviewed.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP148721-B	Pilocarpine nitrate salt		148-72-1	Price

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