Biomaterial Database

Pharmacological evaluation of a new timolol/pilocarpine formulation. 1998

C Bucolo, and A Spadaro, and S Mangiafico

Fidia Oftal Research Laboratories, Catania, Italy. bucocla@mbox.unict.it

A new formulation (HYA) based on timolol hyaluronate and pilocarpine hyaluronate salts has been shown to improve the bioavailability of the drugs and to extend the duration of their action. Extent of the intraocular pressure lowering effect, duration of action and aqueous bioavailability of timolol and pilocarpine of HYA were compared with a commercial preparation. Ocular hypertension in the rabbit was induced by alpha-chymotrypsin or by water loading. The hypotensive effect of HYA treatment was significantly greater and longer than that observed in rabbit eyes treated with the commercial preparation both in the normotensive and in the hypertensive animals. Furthermore, we evaluated the miotic response; due to pilocarpine, normotensive rabbits showed a greater miotic response and an extended duration when the eyes were treated with HYA. The new formulation increased the aqueous availability of timolol and pilocarpine compared to the commercial preparation as determined by HPLC. The pharmacodynamic and pharmacokinetic profiles of HYA indicate an increase in efficacy and duration of action along with an increase in bioavailability of timolol and pilocarpine in comparison with the commercial preparation.

UI	MeSH Term	Description	Entries
D007429	Intraocular Pressure	The pressure of the fluids in the eye.	Ocular Tension,Intraocular Pressures,Ocular Tensions,Pressure, Intraocular,Pressures, Intraocular,Tension, Ocular,Tensions, Ocular
D009798	Ocular Hypertension	A condition in which the intraocular pressure is elevated above normal and which may lead to glaucoma.	Glaucoma, Suspect,Hypertension, Ocular,Glaucomas, Suspect,Hypertensions, Ocular,Ocular Hypertensions,Suspect Glaucoma,Suspect Glaucomas
D010862	Pilocarpine	A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.	Isopilocarpine,Isoptocarpine,Ocusert,Pilocarpine Hydrochloride,Pilocarpine Mononitrate, (3S-cis)-Isomer,Pilocarpine Nitrate,Pilocarpine, Monohydrochloride, (3S-cis)-Isomer,Salagen,Hydrochloride, Pilocarpine,Nitrate, Pilocarpine
D011817	Rabbits	A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes.	Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus
D002626	Chemistry, Pharmaceutical	Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use.	Medicinal Chemistry,Chemistry, Pharmaceutic,Pharmaceutic Chemistry,Pharmaceutical Chemistry,Chemistry, Medicinal
D002851	Chromatography, High Pressure Liquid	Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.	Chromatography, High Performance Liquid,Chromatography, High Speed Liquid,Chromatography, Liquid, High Pressure,HPLC,High Performance Liquid Chromatography,High-Performance Liquid Chromatography,UPLC,Ultra Performance Liquid Chromatography,Chromatography, High-Performance Liquid,High-Performance Liquid Chromatographies,Liquid Chromatography, High-Performance
D002918	Chymotrypsin	A serine endopeptidase secreted by the pancreas as its zymogen, CHYMOTRYPSINOGEN and carried in the pancreatic juice to the duodenum where it is activated by TRYPSIN. It selectively cleaves aromatic amino acids on the carboxyl side.	Alpha-Chymotrypsin Choay,Alphacutanée,Avazyme
D000319	Adrenergic beta-Antagonists	Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.	Adrenergic beta-Antagonist,Adrenergic beta-Receptor Blockader,Adrenergic beta-Receptor Blockaders,beta-Adrenergic Antagonist,beta-Adrenergic Blocker,beta-Adrenergic Blocking Agent,beta-Adrenergic Blocking Agents,beta-Adrenergic Receptor Blockader,beta-Adrenergic Receptor Blockaders,beta-Adrenoceptor Antagonist,beta-Blockers, Adrenergic,beta-Adrenergic Antagonists,beta-Adrenergic Blockers,beta-Adrenoceptor Antagonists,Adrenergic beta Antagonist,Adrenergic beta Antagonists,Adrenergic beta Receptor Blockader,Adrenergic beta Receptor Blockaders,Adrenergic beta-Blockers,Agent, beta-Adrenergic Blocking,Agents, beta-Adrenergic Blocking,Antagonist, beta-Adrenergic,Antagonist, beta-Adrenoceptor,Antagonists, beta-Adrenergic,Antagonists, beta-Adrenoceptor,Blockader, Adrenergic beta-Receptor,Blockader, beta-Adrenergic Receptor,Blockaders, Adrenergic beta-Receptor,Blockaders, beta-Adrenergic Receptor,Blocker, beta-Adrenergic,Blockers, beta-Adrenergic,Blocking Agent, beta-Adrenergic,Blocking Agents, beta-Adrenergic,Receptor Blockader, beta-Adrenergic,Receptor Blockaders, beta-Adrenergic,beta Adrenergic Antagonist,beta Adrenergic Antagonists,beta Adrenergic Blocker,beta Adrenergic Blockers,beta Adrenergic Blocking Agent,beta Adrenergic Blocking Agents,beta Adrenergic Receptor Blockader,beta Adrenergic Receptor Blockaders,beta Adrenoceptor Antagonist,beta Adrenoceptor Antagonists,beta Blockers, Adrenergic,beta-Antagonist, Adrenergic,beta-Antagonists, Adrenergic,beta-Receptor Blockader, Adrenergic,beta-Receptor Blockaders, Adrenergic
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D001082	Aqueous Humor	The clear, watery fluid which fills the anterior and posterior chambers of the eye. It has a refractive index lower than the crystalline lens, which it surrounds, and is involved in the metabolism of the cornea and the crystalline lens. (Cline et al., Dictionary of Visual Science, 4th ed, p319)	Aqueous Flare,Intraocular Fluid,Aqueous Flares,Aqueous Humors,Flare, Aqueous,Fluid, Intraocular,Fluids, Intraocular,Humor, Aqueous,Humors, Aqueous,Intraocular Fluids