Skip to main content

Pharmacokinetics and Biopharmaceutical Aspects of Some Anti-Glaucoma Drugs

  • Conference paper
Book cover Ophthalmic Drug Delivery

Part of the book series: FIDIA Research Series ((FIDIA,volume 11))

Abstract

The therapy of glaucoma has used several classes of active ingredients which were mostly cholinergic and adrenergic drugs. The carbonic anhydrase inhibitors were essentially systemic drugs but recently new potent compounds have been described to be active after topical administration. Each class of drugs has a different pharmacokinetic behaviour due to the physico-chemical properties of the individual compounds. The dynamics of ocular fluids, especially the turnover of tears, are responsible for a poor availability of drugs administered topically in the conjunctival cul-de-sac. The recent galenic developments in ophthalmic formulations have essentially aimed at achieving better control of the residence of anti-glaucoma drugs close to the anterior segment of the eye and derivatization and prodrug approaches have improved transcorneal penetration.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 39.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 54.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  • Abshire R, Cash P (1986). Sterile ophthalmic ointment and suspension manufacturing. J. Parenteral Sci. and Technol. 40: 97–99

    CAS  Google Scholar 

  • Adler CA, Maurice DM, Paterson ME (1971) The effect of viscosity of the vehicle on the penetration of fluorescein into the human eye. Exp. Eye Res. 11: 34–42

    Article  CAS  PubMed  Google Scholar 

  • Ahmed I, Patton TF (1985) Importance of the noncorneal absorption route in topical ophthalmic drug delivery. Invest. Ophthalmol. Vis. Sci. 26: 584–587

    CAS  PubMed  Google Scholar 

  • Aldrete J, McDonald TO, De Sousa B (1983) Comparative evaluation of pilocarpine gel and timolol in patients with glaucoma. Glaucoma 5: 236–241

    Google Scholar 

  • Andermann C, Mialhe D, Arne JL, Vende D, Bec P (1983) Effet tensionnel après instillation d’une goutte de pilocarpine retard. Résultats cliniques de son action à moyen terme. J. Fr. Ophtalmol 6: 367–374

    CAS  PubMed  Google Scholar 

  • Anderson JA, Davis WL, Wei CP (1980) Site of ocular hydrolysis of a prodrug, dipivefrin, and a comparison of its ocular metabolism with that of the parent compound, epinephrine. Invest. Ophthalmol. Vis. Sci. 19: 817–823

    CAS  PubMed  Google Scholar 

  • Ariens EJ, (1974) Drug levels in the target tissue and effect. Clin. Pharmacol. Therap. 16: 155–175.

    CAS  Google Scholar 

  • Bar-Ilan A, Pessah NI, Maren TH (1986) Ocular penetration and hypotensive activity of the topically applied carbonic anhydrase inhibitor L-645,151. J. Ocular Pharmacol. 2: 109–120

    Article  CAS  Google Scholar 

  • Becker B (1954) Decrease in intraocular pressure in man by a carbonic anhydrase inhibitor, Diamox. Am. J. Ophthalmol. 37: 13–15

    CAS  Google Scholar 

  • Benedetto DA, Shah DO, Kaufman HE (1975) The instilled fluid dynamics and surface chemistry of polymers in the precorneal tear film. Invest. Ophthalmol. Vis. Sci. 14: 887–902

    CAS  Google Scholar 

  • Benson H (1974) Permeability of the cornea to topically applied drugs. Arch. Ophthalmol. 91: 313–327

    Article  CAS  PubMed  Google Scholar 

  • Blumenthal M, Ticho U, Zonis S, Gal A, Blank I, Mazor Z (1979) Further clinical trial with piloplex. A new long-acting pilocarpine salt. Glaucoma 1: 145

    Google Scholar 

  • Brown RH, Hotchkiss ML, Davis ED (1985) Creating smaller eye drops by reducing eye dropper tip dimensions. Am. J. Ophthalmol. 99: 460–464

    CAS  PubMed  Google Scholar 

  • Brown RH, Lynch MG (1986) Design of eyedropper tips for topical beta-blocking agents. Amer. J. Ophthalmol. 102: 123–124

    Article  CAS  Google Scholar 

  • Bundgaard H, Advances in drug delivery, Churchill College, Cambridge (UK) 7–9 July 1986.

    Google Scholar 

  • Bundgaard H, Buur A, Chang SC, Lee VHL (1986c) Prodrugs of timolol for improved ocular delivery: synthesis, hydrolysis kinetics and lipophilicity of various timolol esters. Int. J. Pharmac. 33: 15–26

    Article  CAS  Google Scholar 

  • Bundgaard H, Falch E, Larsen C, Mikkelson TJ (1986a) Pilocarpine prodrugs I. Synthesis, physicochemical properties and kinetics of lactonization of pilocarpic acid esters. J. Pharm. Sci. 75: 36–43

    Article  CAS  PubMed  Google Scholar 

  • Bundgaard H, Falch E, Larsen C, Mosher GL, Mikkelson TJ (1985) Pilocarpic acid esters as novel sequentially labile pilocarpine prodrugs for improved ocular delivery. J. Med. Chem. 28: 979–981

    Article  CAS  PubMed  Google Scholar 

  • Bundgaard H, Falch E, Larsen C, Mosher GL, Mikkelson TJ (1986b) Pilocarpine prodrugs II. Synthesis, stability, bioconversion and physicochemical properties of sequentially labile pilocarpine acid diesters. J. Pharm. Sci. 75: 775–783

    Article  CAS  PubMed  Google Scholar 

  • Buri P, (1985) Voie oculaire. In: Buri P, Puisieux F, Doelker E, Benoît JP, (eds) Formes pharmaceutiques nouvelles, Lavoisier, Paris.

    Google Scholar 

  • Burstein NL, Anderson JA (1985) Review: corneal penetration and ocular bioavailability of drugs. J. Ocular Pharm. 1: 309–326.

    Article  CAS  Google Scholar 

  • Camber O (1985) An in-vitro model for determination of drug permeability through the cornea. Acta. Pharma. Suec. 22: 335–342.

    CAS  Google Scholar 

  • Chang SC, Bundgaard H, Lee VHL (1986b) Prodrug administration is more effective than drop size manipulation in reducing the systemic absorption of topically applied timolol in the pigmented rabbit. 1st national meeting of the Americal Assocation of pharmaceutical Scientists, Washington DC, Nov. 2–6. Pharm. Res. 3: 90S

    Google Scholar 

  • Chang SC, Lee VHL (1986a) Vehicle factors influencing the systemic absorption of topically applied timolol in the pigmented rabbit. 1st national meeting of the American Association of Pharmaceutical Scientists, Washington DC, Nov. 2–6. Pharm. Res. 3: 86S.

    Google Scholar 

  • Chieu TW (1978) Methods to achieve sustained drug delivery–the physical approach. In: Sustained and controlled release drug delivery systems Robinson JR, (ed), New York, Marcel Dekker 228–286

    Google Scholar 

  • Chrai SS, Makoid MC, Erikson SP, Robinson JR (1974) Drop size and initial dosing frequency problems of topically applied ophthalmic drugs. J. Pharm. Sci. 63: 333–338

    Article  CAS  PubMed  Google Scholar 

  • Chrai SS, Patton TF, Metha A, Robinson JR (1973) Lacrimal and instilled fluid dynamics in rabbits eyes. J. Pharm. Sci. 62: 1112–1121

    Article  CAS  PubMed  Google Scholar 

  • Chrai SS, Robinson JR (1974) Ocular evaluation of mehtylcellulose vehicle in albino rabbits. J. Pharm. Sci. 63–1112–1121

    Google Scholar 

  • De Feo G, Piccinelli D, Putzolu S, Silvestrini B (1975) Effects of topically instilled drugs on intraocular pressure in rabbits. Arzneim.-Forsch (Drug Res.) 25: 806–809

    Google Scholar 

  • De Santis LM, Schoenwald RD (1978) Lack of influence of rabbit nictitating membrane on miosis effect of pilocarpine. J. Pharm. Sci. 67: 1189–1190

    Article  Google Scholar 

  • Doane MG, Jensen AD, Dolhman Ch (1978) Penetration routes of topically applied eye medications. Am. J. Ophthalmol. 85: 383–386

    CAS  PubMed  Google Scholar 

  • Dunn DL, Scott BS, Dorsey ED (1981) Analysis of pilocarpine and isopilocarpine in ophthalmic solutions by normal phase high performance liquid chromatography. J. Pharm. Sci. 70: 446–449

    Article  CAS  PubMed  Google Scholar 

  • Eller MG, Schoenwald RD, Dixson JA, Segarra T, Barfknecht CF (1985) Topical carbonic anhydrase inhibitors III: Optimization model for corneal penetration of ethoxzolamide analogues. J. Pharm. Sci. 74: 155–160

    Article  CAS  PubMed  Google Scholar 

  • Ellis PP, Matsumura M, Rendi MA (1985) Pilocarpine concentrations in aqueous humor following single drop application I. Effect of soft contact lenses. Current Eye Res. 4: 1041–1047

    Article  CAS  Google Scholar 

  • Eriksen SP (1980) Physiological and formulation constraints on ocular drug bioavailability. In: Robinson JR (ed) Ophthalmic drug delivery systems ( 1980 ) 55–70. Washington DC, American Pharmaceutical Association.

    Google Scholar 

  • File RR, Patton TF (1980) Topically Applied Pilocarpine: Human pupillary response as a function of drop size. Arch. Ophthalmol. 98: 112–115

    Article  CAS  PubMed  Google Scholar 

  • Friedland BR, Maren TH (1984) Carbonic anhydrase Pharmacology of inhibitors and treatment of glaucoma. In: Sears ML (ed), Pharmacology of the eye, Springer Verlag, Heidelberg.

    Google Scholar 

  • Friedman Z, Allen RC, Raph SM (1985) Topical acetazolamide and methazolamide delivered by contact lenses. Arch. Ophthalmol. 103: 963–966

    Article  CAS  PubMed  Google Scholar 

  • Grass GM, Robinson JR (1984) Relationship of chemical structure to corneal penetration and influence of low viscosity solution on ocular bioavailability. J. Pharm. Sci. 73: 1021–1027

    Article  CAS  PubMed  Google Scholar 

  • Gurny R (1981b) Preliminary study of prolonged acting drug delivery system for the treatment of glaucoma. Pharm. Acta. Helv. 56: 130–132

    CAS  PubMed  Google Scholar 

  • Gurny R, Boye T, Ibrahim H (1985) Ocular therapy with nanoparticulate systems for controlled drug delivery. J. Contr. Rel. 2: 353–361

    Article  CAS  Google Scholar 

  • Gurny R, Peppas NA, Harrington DD, Banker GS (1981a) Development of biodegradable and injectable latices for controlled release of potent drugs. Drug Develop. Ind. Pharm. 7: 1–25

    Article  CAS  Google Scholar 

  • Gurny R, Taylor D (1980) Development and evaluation of a prolonged acting drug delivery system for the treatment of glaucoma In: Rubinstein MH, Proceedings of the international symposium of the British Pharmaceutical Technology Conference ( London ), Liverpool Solid Dosage Research Unit.

    Google Scholar 

  • Habib FS, Attia MA, El-Shanawany SM (1985) Ocular bioavailability of pilocarpine hydrochloride in combination with physostigmine salicylate from different gel formulations. Arch. Pharm. Chem.Sci. 13: 33–38

    CAS  Google Scholar 

  • Hamard H, Schmitt C, Plazonnet B, Le Douarec JC (1975) Etude de la pénétration oculaire de la dexaméthasone. In: Demailly P, Hamard H, Luton JP (eds) Oeil et cortisone. Masson et Cie, Paris; 33–83

    Google Scholar 

  • Harmia T, Kreuter J, Speiser P, Boye T, Gurny R, Kubis A (1986b) Enhancement of the myotic response of rabbits with pilocarpine-loaded polybutylcyanoacrylate nanoparticles. Int. J. Pharm. 33: 187–193

    Article  CAS  Google Scholar 

  • Harmia T, Speiser P, Kreuter J (1986 a) A solid colloidal drug delivery system for the eye: encapsulation of pilocarpin in nanoparticles. J. Microencaps. 3: 3–12

    Google Scholar 

  • Harmia-Pulkkinen T, Ihantola A, Tuomi A, Kristoffersson E (1986) Nanoencapsulation of timolol by suspension and micelle polymerization. Acta Pharma. Fennica 95: 89–96

    CAS  Google Scholar 

  • Heilman K (1984) Therapeutic systems for local use. Ocular therapeutic systems. In: Therapeutic systems ( 2nd ed). Stuttgart, Georg Thieme Verlag.

    Google Scholar 

  • Holly FJ, Lemp MA (1973) The precorneal tear film and dry eye syndromes. In: Int. Ophthalmol. Clin. 13 (1) Boston, Little Brown Co.

    Google Scholar 

  • Huang HS, Schoenwald RD, Lach JL (1983a) Corneal penetration behaviour of ß-blocking agents II: Assessment of barrier contributions. J. Pharm. Sci. 72: 1272–1279

    Article  CAS  PubMed  Google Scholar 

  • Huang HS, Schoenwald RD, Lach JL (1983b) Corneal penetration behavior of n-blocking agents III: In-Vitro–In-Vivo correlations. J. Pharm. Sci. 72: 1279–1281

    Article  CAS  PubMed  Google Scholar 

  • Hui HW, Robinson JR (1985) Ocular delivery of progesterone using a bioadhesive polymer. Int. J. Pharm. 26: 203–213

    Article  CAS  Google Scholar 

  • Hui HW, Robinson JR (1986). Effect of particle dissolution rate on ocular drug bioavailability. J. Pharm. Sci. 75: 280–287.

    Article  CAS  PubMed  Google Scholar 

  • Jankowska LM, Bar-Ilan A, Maren TH (1986) The relations between ionic and non-ionic diffusion of sulfonamides across the rabbit cornea. Invest. Ophthalmol. Vis. Sci. 27: 29–37.

    CAS  PubMed  Google Scholar 

  • Kaila T, Salminen L, Huupponen R (1985) Systemic absorption of topically applied ocular timolol. J. Ocular Pharmacol. 1: 79–83

    Article  CAS  Google Scholar 

  • Katz IM, Berger ET (1979) Effects of iris pigmentation on response of ocular pressure to timolol. Surv. Ophthalmol. 23: 395–398

    Article  CAS  PubMed  Google Scholar 

  • Katz IM, Blackman WM (1977) A soluble sustained-release ophthalmic delivery unit. Am. J. Ophthalmol. 83: 728–734

    CAS  PubMed  Google Scholar 

  • Kennedy JM, McNamara PE (1981) High peformance liquid chromatographic analysis of pilocarpine hydrochloride, isopilocarpine, pilocarpic acid, and isopilocarpic acid in eye drop preparations. J. Chromatogr. 212: 331–338

    Article  CAS  PubMed  Google Scholar 

  • Klein HZ, Miguel L, Shields MB, Leon J, Duzman E (1985) A dose-response study of piloplex for duration of action. Am. J. Ophthalmol. 99: 23–26

    CAS  PubMed  Google Scholar 

  • Krause PD (1980) Dipivefrin (DPE): Preclinical and clinical aspects of its development for use in the eye. In: Robinson JR, (ed) Ophthalmic drug delivery systems. Washington, American Pharmaceutical Association, 91–104

    Google Scholar 

  • Kreienbaum MA, Page DP (1986) Stability of pilocarpine hydrochloride and pilocarpine nitrate ophthalmic solutions submitted by U.S. hospitals. Am. J. Hosp. Pharm. 43: 109–117

    CAS  PubMed  Google Scholar 

  • Lederer CM, Harold RE (1986) Drop size of commercial glaucoma medications. Amer. J. Ophthalmol. 101: 691–694

    Google Scholar 

  • Lee VHL (1983) Esterase activities in adult rabbit eyes. J. Pharm. Sci. 72: 239–244

    Article  CAS  PubMed  Google Scholar 

  • Lee VHL, Robinson JR (1982) Disposition of pilocarpine in the pigmented rabbit eye. Int. J. of Pharm. 11: 155–165.

    Article  CAS  Google Scholar 

  • Lee VHL, Robinson JR (1986) Review: Topical ocular drug delivery: recent developments and future challenges. J. Ocular Pharmacol. 2: 67–108

    Article  CAS  Google Scholar 

  • Lewis RA, Schoenwald RD, Barfknecht CF, Phelps CD (1986) Aminozolamide gel. A trial of a topical carbonic anhydrase inhibitor in ocular hypertension. Arch. Ophthalmol. 104: 842–849

    Article  CAS  PubMed  Google Scholar 

  • Lewis RA, Schoenwald RD, Eller MG, Barfknecht CF, Phelps CD (1984) Ethoxzolamide Analogue Gel: A topical carbonic anhydrase inhibitor. Arch. Ophthalmol. 102: 1821–1824

    Article  CAS  PubMed  Google Scholar 

  • Lotti VJ, Gautheron PD, Schmitt CJ (1984b) Topical ocular hypotensive activity and ocular penetration of dichlorphenamide sodium in rabbit. Graefe’s Arch. Clin. Exp. Ophthalmol. 222: 13–19

    Article  CAS  PubMed  Google Scholar 

  • Lotti VJ, Le Douarec JC, Stone CA (1984a) Autonomic nervous system: Adrenergic antagonists. In: Sears ML (ed) Pharmacology of the eye. Berlin-Heidelberg. Springer Verlag 248–277

    Google Scholar 

  • Ludwig A, Van Ooteghem M (1986a) The study of the precorneal dynamics of ophthalmic solutions by fluorophotometry. Pharm. Acta. Helv. 61: 236–240

    CAS  PubMed  Google Scholar 

  • Ludwig A, Van Ooteghem M (1986b) The influence of the dropsize on the elimination of an ophthalmic solution from the precorneal area of human eyes. Drug Development Ind. Pharm. 12: 2231–2242.

    Article  CAS  Google Scholar 

  • Lyons JS, Krohn DL (1974) Pilocarpine uptake by pigmented uveal tissue. Am.J. Ophthalmol. 75: 883–885

    Google Scholar 

  • Maichuk YF (1975a) Ophthalmic drug inserts. Invest. Ophthalmol. 14: 87–90

    CAS  PubMed  Google Scholar 

  • Maichuk YF (1975b) Soluble ophthalmic drug inserts. The Lancet 1: 173

    Article  CAS  Google Scholar 

  • Mandell AI, Stentz F, Kitabachi AE (1978) Dipivalyl epinephrine: a new prodrug in the treatment of glaucoma. Ophthalmology 85: 268–275

    CAS  PubMed  Google Scholar 

  • March WF, Stewart RM, Mandell AI, Bruce LA (1982) Duration of effect of pilocarpine gel. Am. J. Ophthalmol. 100: 1270–1271

    CAS  Google Scholar 

  • Maren TH (1967) Carbonic anhydrase chemistry, physiology and inhibition. Physiol. Rev. 47: 595–781

    CAS  PubMed  Google Scholar 

  • Maren TH, Jankowska L (1985) Ocular pharmacology of sulfonamides: the cornea as barrier and depot. Current Eye Res. 4: 399–408

    Article  CAS  Google Scholar 

  • Maren TH, Jankowska L, Sanyal G, Edelhauser HF (1983) The transcorneal permeability of sulfonamide carbonic anhydrase inhibitors and their effect on aqueous humor secretion. Exp. Eye Res. 36: 457–480.

    Article  CAS  PubMed  Google Scholar 

  • Maren TH, Sanyal G (1983a) The activity of sulfonamides and anions against the carbonic anhydrases of animal plants and bacteria. In: George et al (eds), Maren TH, Sanyal G 23, Palo Alto Annual Review Inc.

    Google Scholar 

  • Maurice DM, Mishima S (1984) Ocular pharmacokinetics. In: Sears ML (ed) Pharmacology of the eye. Vol. 69, Springer Verlag, Heidelberg, pp. 19–116

    Chapter  Google Scholar 

  • McClure DA (1975) The effect of a prodrug of epinephrine (dipivaloyl epinephrine) in glaucoma–general pharmacology, toxicology and clinical experiences. In: Higuchi T, Stella V (eds): Pro-drugs as novel drug delivery systems (ACS Symposium 14 ) American Chemical Society, Washington D.C. pp. 224–235.

    Chapter  Google Scholar 

  • McLaughlin MA, Chiou GCY (1985) Review: a synopsis of recent developments in antiglaucoma drugs. J. Ocular Pharm. 1: 101–121.

    Article  CAS  Google Scholar 

  • Melis-Decerf C, Van Ooteghem M (1979) An in vitro method simulating drug release from viscous eye drops in rabbit and man. J. Pharm. Pharmacol. 31: 12–15

    Article  CAS  PubMed  Google Scholar 

  • Mikkelson TJ (1986) Ophthalmic drug delivery. Pharm. Technol. 8: 90–98

    Google Scholar 

  • Mindel JS, Smith H, Jacobs M, Kharlamb AB, Friedman AH (1984) Drug reservoirs in topical therapy. Invest. Ophthalmol. Vis. Sci. 25: 346–350.

    CAS  PubMed  Google Scholar 

  • Mishima S (1981) Clinical pharmacokinetics of the eye. Invest. Ophthalmol. Vis. Sci. 21: 504–541

    CAS  Google Scholar 

  • Mishima S, Gasset A, Klyce SD Jr, Baum JL (1966) Determination of tear volume and tear flow. Invest. Ophthalmol. 5: 264–276

    CAS  PubMed  Google Scholar 

  • Mitra AK, Mikkelson TJ (1982) Ophthalmic solution buffer systems I. the effect of buffer concentration on the ocular absorption of pilocarpine. Int. J. Pharm. 10: 219–229

    Article  CAS  Google Scholar 

  • Noordham A, Maat L, Beyerman HC (1981) Quantitative determination of pilocarpine, isopilocarpine, pilocarpine acid and isopilocarpic acid in clinical ophthalmic pilocarpine formulations by reverse phase liquid chromatography. J. Pharm. Sci. 70: 96–97

    Article  Google Scholar 

  • Olijnik 0, Stevens J, Wilson CG, Hardy J (1985) Ocular retention of ophthalmic vehicles evaluated in the rabbit by gamma scintigraphy. J. Pharm. Pharmacol. 37: suppl. 118 P

    Google Scholar 

  • Ono S, Hirano H, Obaka K (1971) Degradation in the side chain of cortisol by lens homogenate. Tohoku J. Exp. Med. 104: 171–175

    Article  CAS  PubMed  Google Scholar 

  • Park K, Robinson JR (1982) Polymer binding to epithelial cells. In: Bundgaard H, Bagger Hansen A, Kofod H (eds) Optimization of drug delivery. (Alfred Benzon Symposium 17) Copenhagen 1982,Munksgaard 35–49

    Google Scholar 

  • Patton TF (1977) Pharmacokinetic evidence for improved ophthalmic drug delivery by reduction of instilled volume. J. Pharm. Sci. 66: 1058–1059

    Article  CAS  PubMed  Google Scholar 

  • Patton TF, Ocular Drug Disposition In: Ophthalmic Drug Delivery Systems, Robinson JR, (ed), American Pharmaceutical Association, Washington D.C. 1980 pp. 28–54.

    Google Scholar 

  • Patton TF, Robinson JR (1975) Ocular evaluation of polyvinyl alcohol vehicle in rabbits. J. Pharm. Sci. 64: 1312–1316

    Article  CAS  PubMed  Google Scholar 

  • Patton TF, Robinson JR (1976) Quantitative precorneal disposition of topically applied pilocarpine. J. Pharm. Sci. 65: 1295–1301

    Article  CAS  PubMed  Google Scholar 

  • Plazonnet B, Cerdeno A (1976). In-vivo hydrolysis of pilocarpine in the rabbit presented at the 5th European Workshop on Drug Metabolism, Stockholm, June 14–18.

    Google Scholar 

  • Podos SM, Becker B, Assef C, Hartstein J (1972) Pilocarpine therapy with soft contact lenses. Am. J. Ophthalmol. 73: 336–341

    CAS  PubMed  Google Scholar 

  • Ponticello GS, Schwam H, Sugrue MF, Baldwin JJ (1986) Thienothiopyran2-sulfonamides: Topically effective water soluble carbonic anhydrase inhibitors. 192nd ACS National Meeting, Anaheim, CA. Sept 7–12.

    Google Scholar 

  • Prince JH (ed) (1964) The rabbit in eye research. Thomas, Springfield

    Google Scholar 

  • Robinson JR, Li VHK (1984) Ocular disposition and bioavailability of pilocarpine from Piloplex and other sustained drug delivery systems. In: Ticho U, and David R, (eds) Recent Advances in Glaucoma. Amsterdam, Elsevier; pp. 231–236

    Google Scholar 

  • Saettone MF, Giannaccini B, Barattini F, Tellini N (1982) The validity of rabbits for investigations on ophthalmic vehicles: a comparison of four different vehicles containing tropicamide in humans and rabbits. Pharm. Acta. Helv. 57: 47–55

    CAS  PubMed  Google Scholar 

  • Saettone MF, Giannaccini B, Chetoni P, Galle G, Chiellini E (1984b) Vehicle effect in ophthalmic bioavailability: an evaluation of polymeric inserts containing pilocarpine. J. Pharm. Pharmacol. 36: 229–234.

    Article  CAS  PubMed  Google Scholar 

  • Saettone MF, Giannaccini B, Guiducci A, Savigni P (1986) Semisolid ophthalmic vehicles. III. An evaluation of four organic hydrogels containing pilocarpine. Int. J. of Pharma. 31: 261–270.

    Article  CAS  Google Scholar 

  • Saettone MF, Giannaccini B, Ravecca S, La Marca F, Tota G (1984a) Polymer effects on ocular bioavailability–the influence of different liquid vehicles on the mydriatic response of tropicamide in humans and in rabbits. Int. J. of Pharm. 20: 187–202.

    Article  CAS  Google Scholar 

  • Saettone MF, Giannaccini B, Savigni P, Teneggi A (1981) Vehicle effects on ophthalmic bioavailability: the influence of various vehicles on the activity of pilocarpine of rabbit and man. In: Aiäche JM, 1st European Congress of Biopharmacy and Pharmacokinetics, Clermont Ferrand, Vol 1 pp 151–155.

    Google Scholar 

  • Saettone MF, Giannaccini B, Teneggi A, Savigni P, Tellini N (1982) Vehicle effects on ophthalmic bioavailability: the influence of different polymers on the activity of pilocarpine in rabbit and man. J. Pharm. Pharmacol. 34: 464–466

    Article  CAS  PubMed  Google Scholar 

  • Schoenwald RD, Huang HS (1983) Corneal penetration behaviour of p-blocking agents I: Physicochemical factors. J. Pharm. Sci. 72: 1266–1272

    Article  CAS  PubMed  Google Scholar 

  • Schoenwald RD, Ward RL, De Santis LM, Roehrs R.E. (1978) Influence of high-viscosity vehicles on miotic effect of pilocarpine. J. Pharm. Sci. 67: 1280–1283

    Article  CAS  PubMed  Google Scholar 

  • Schwam H, Michelson SR, Sondy JM, Smith RL (1984) L-645,151 a topically effective ocular hypotensive carbonic anhydrase inhibitor: Part I, Biochemistry and metabolism. Invest.Ophthalmol. 25 (suppl): 181

    Google Scholar 

  • Sears ML (ed) (1981) New directions in ophthalmic research. New Haven, Yale University Press

    Google Scholar 

  • Shell JW (1982) Ocular drug delivery systems–a review. J. Toxicol.-Cut. Ocular Toxicol. 1: 49–63

    Article  CAS  Google Scholar 

  • Shell JW (1984) Ophthalmic drug delivery systems. Surv. Ophthalmol. 29: 117–128

    Article  CAS  PubMed  Google Scholar 

  • Shell JW, Baker RW (1974) Diffusional systems for controlled release of drugs to the eye. Ann. Ophthalmol. 6: 1037

    CAS  PubMed  Google Scholar 

  • Sheppard KL, Anderson PS, Graham SL, Schwam H, Smith RL, Sugrue MF (1986) Benzo [b] thiophene-, benzo Lb] furan and indole-2 sulfonamides: new classes of topically effective carbonic anhydrase inhibitors. Presented at the 192nd American Chemical Society meeting, Anaheim, Ca. Sept. 7–12

    Google Scholar 

  • Sieg JW, Robinson JR (1975) Vehicle effects on ocular bioavailability.l. Evaluation of fluorometholone. J. Pharm. Sci. 64: 931–936

    Article  CAS  PubMed  Google Scholar 

  • Sieg JW, Triplett JW (1980) Precorneal retention of topically instilled micronized particles. J. Pharm. Sci. 69: 863–864

    Article  CAS  PubMed  Google Scholar 

  • Smith RL, Anderson PS, Bicking JB, de Solms J, Graham SL, Hoffman JM, Michelson SR, Robb CM, Schwam ti, Shepard KL, Smith AM, Scholz TH, Sondey JM, Strohmaler KM, Woltersdorf OW Jr (1986) Topical carbonic inhibitor design. Presented at the 22èmes Rencontres Internationales de Chimie Thérapeutique, Clermont Ferrand (France) Sept. 3–5

    Google Scholar 

  • Stein A, Pinke R, Krupin T, Glabb E, Podos SM, Serle J, Maren TH (1983) The effect of topically administered carbonic anhydrase inhibitors on aqueous humor dynamics in rabbits. Am. J. Ophthalmol. 95: 222–228.

    Article  CAS  PubMed  Google Scholar 

  • Sugaya M, Nagataki S (1978) Kinetics of topical pilocarpine in the human eye. Japan J. Ophthalmol. 22: 127–141

    CAS  Google Scholar 

  • Sugrue MF, Gautheron P, Schmitt C, Viader MP, Conquet P, Smith RL, Share NN, Stone CA (1985) On the pharmacology of L-645,151: A topically effective ocu’ar hypotensive carbonic anhydrase inhibitor. J. Pharmacol. Exp. Therapeutics 232: 534–540

    CAS  Google Scholar 

  • Ticho U, Blumenthal M, Zonis S, Gal A, Blank I, Mazor Z (1979a) A clinical trial with piloplex. A new long-acting pilocarpine compound. Preliminary report. Ann. Ophthalmol. 11: 555–561

    CAS  PubMed  Google Scholar 

  • Ticho U, Blumenthal M, Zonis S, Gal A, Blank I, Mazor Z (1979b) Piloplex, a new long-acting pilocarpine polymer salt. A. Long-term study. Br.J. Ophthalmol 63: 45–47

    Article  CAS  Google Scholar 

  • Urbanyi T, Piedmont A, Willis E (1976) Simultaneous determination of pilocarpine and isopilocarpine in pharmaceutical preparations by liquid chromatography. J. Pharm. Sci. 65: 257–260

    Article  CAS  PubMed  Google Scholar 

  • Urquhart J, (1980) Development of the OCUSERT® pilocarpine ocular therapeutic systems–a case history in ophthalmic product development In: Ophthalmic Drug Delivery Systems, Robinson JR, (ed), American Pharmaceutical Association, Washington D.C. pp. 105–118

    Google Scholar 

  • Urtti A (1985) Pilocarpine release from matrices of alkyl half-esters of poly(vinyl methyl ether/maleic anhydride). Int. J. Pharm. 26: 45–55

    Article  CAS  Google Scholar 

  • Urtti A, Juslin M, Miinalainen O (1985a) Pilocarpine release from hydroxypropyl-cellulose-polyvinylpyrrolidone matrices. Int. J. Pharm. 25: 165–178

    Article  CAS  Google Scholar 

  • Urtti A, Salminen L, Miinalainen O (1985b) Systemic absorption of ocular pilocarpine is modified by polymer matrices. Int. J. Pharm. 23: 147–161

    Article  CAS  Google Scholar 

  • Vadnere M, Amidon G, Lindenbaum S, Haslam JL (1984) Thermodynamic studies on the gel-sol transition of some pluronic polyols. Int. J. Pharm. 22: 207–218

    Article  CAS  Google Scholar 

  • Van Ooteghem M (1983) Viskosität. In: Dolder R, Skinner FS (eds) Ophthalmika, Stuttgart. Wissenschaftliche Verlagsgesellschaft 372–384

    Google Scholar 

  • Vareilles P, Schmitt C, Lotti VJ, Le Douarec JC (1978) Etude expérimentale du timolol: un nouvel hypotenseur oculaire. J. Fr. Ophtalmol. 12: 717–721

    Google Scholar 

  • Vareilles P, Silverstone D, Plazonnet B, Le Douarec JC, Sears ML, Stone CA (1977) Comparison of the effects of timolol and other adrenergic agents on intraocular pressure in the rabbit. Invest. Ophthalmol. Vis. Sci. 16: 987–996

    CAS  PubMed  Google Scholar 

  • Vedani A, Meyer EF (1984) Structure-activity relationships of sulfonamide drugs and human carbonic anhydrase C: Modeling of inhibitor molecules into the receptor site of the enzyme with an interactive computer graphics display. J. Pharm. Sci. 73: 352–358

    Article  CAS  PubMed  Google Scholar 

  • Waltman SR,Kaufman HE (1970) Use of hydrophilic contact lenses to increase ocular penetration of topical drugs. Invest. Ophthalmol. 9: 250–255

    Google Scholar 

  • Wei CP, Anderson JA, Leopold I (1978) Ocular absorption and metabolism of topically applied epinephrine and a dipivalyl ester of epinephrine. Invest. Ophthalmol. Vis. Sci. 17: 315–321.

    CAS  PubMed  Google Scholar 

  • Wilson CG, Olijnik O, Hardy JG (1983) Precorneal drainage of polyvinyl alcohol solutions in the rabbit assessed by gamma scintigraphy. J. Pharm. Pharmacol. 35: 451–454.

    Article  CAS  PubMed  Google Scholar 

  • Wood Rid, Li VHK, Kreuter J, Robinson JR (1985) Ocular disposition of poly-hexyl-2-cyano 3–14C acrylate nanoparticles in the albino rabbit. Int. J. Pharm. 23: 175–183

    Article  Google Scholar 

  • Yakovlev AA, Lenkevich MM (1966) Use of pilocarpine impregnated alcohol films in the treatment of glaucomatous patients. Vestn. Oftal. 79: 40–42

    Google Scholar 

  • Zaki I, Fitzgerald P, Hardy JG, Wilson CG (1986) A comparison on the effect of viscosity on the precorneal residence of solutions in rabbit and man. J. Pharm. Pharmacol. 38: 463–466

    Article  CAS  PubMed  Google Scholar 

  • Zimmermann TJ, Kaufman HE (1977) Timolol: a B-adrenergic blocking agent for the treatment of glaucoma. Arch. Ophthalmol. 95: 601–604

    Article  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1987 Springer Science+Business Media New York

About this paper

Cite this paper

Plazonnet, B., Grove, J., Durr, M., Mazuel, C., Quint, M., Rozier, A. (1987). Pharmacokinetics and Biopharmaceutical Aspects of Some Anti-Glaucoma Drugs. In: Saettone, M.F., Bucci, M., Speiser, P. (eds) Ophthalmic Drug Delivery. FIDIA Research Series, vol 11. Springer, New York, NY. https://doi.org/10.1007/978-1-4757-4175-9_13

Download citation

  • DOI: https://doi.org/10.1007/978-1-4757-4175-9_13

  • Publisher Name: Springer, New York, NY

  • Print ISBN: 978-1-4757-4177-3

  • Online ISBN: 978-1-4757-4175-9

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics