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.
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References
Abshire R, Cash P (1986). Sterile ophthalmic ointment and suspension manufacturing. J. Parenteral Sci. and Technol. 40: 97–99
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
Ahmed I, Patton TF (1985) Importance of the noncorneal absorption route in topical ophthalmic drug delivery. Invest. Ophthalmol. Vis. Sci. 26: 584–587
Aldrete J, McDonald TO, De Sousa B (1983) Comparative evaluation of pilocarpine gel and timolol in patients with glaucoma. Glaucoma 5: 236–241
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
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
Ariens EJ, (1974) Drug levels in the target tissue and effect. Clin. Pharmacol. Therap. 16: 155–175.
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
Becker B (1954) Decrease in intraocular pressure in man by a carbonic anhydrase inhibitor, Diamox. Am. J. Ophthalmol. 37: 13–15
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
Benson H (1974) Permeability of the cornea to topically applied drugs. Arch. Ophthalmol. 91: 313–327
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
Brown RH, Hotchkiss ML, Davis ED (1985) Creating smaller eye drops by reducing eye dropper tip dimensions. Am. J. Ophthalmol. 99: 460–464
Brown RH, Lynch MG (1986) Design of eyedropper tips for topical beta-blocking agents. Amer. J. Ophthalmol. 102: 123–124
Bundgaard H, Advances in drug delivery, Churchill College, Cambridge (UK) 7–9 July 1986.
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
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
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
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
Buri P, (1985) Voie oculaire. In: Buri P, Puisieux F, Doelker E, Benoît JP, (eds) Formes pharmaceutiques nouvelles, Lavoisier, Paris.
Burstein NL, Anderson JA (1985) Review: corneal penetration and ocular bioavailability of drugs. J. Ocular Pharm. 1: 309–326.
Camber O (1985) An in-vitro model for determination of drug permeability through the cornea. Acta. Pharma. Suec. 22: 335–342.
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
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.
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
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
Chrai SS, Patton TF, Metha A, Robinson JR (1973) Lacrimal and instilled fluid dynamics in rabbits eyes. J. Pharm. Sci. 62: 1112–1121
Chrai SS, Robinson JR (1974) Ocular evaluation of mehtylcellulose vehicle in albino rabbits. J. Pharm. Sci. 63–1112–1121
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
De Santis LM, Schoenwald RD (1978) Lack of influence of rabbit nictitating membrane on miosis effect of pilocarpine. J. Pharm. Sci. 67: 1189–1190
Doane MG, Jensen AD, Dolhman Ch (1978) Penetration routes of topically applied eye medications. Am. J. Ophthalmol. 85: 383–386
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
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
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
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.
File RR, Patton TF (1980) Topically Applied Pilocarpine: Human pupillary response as a function of drop size. Arch. Ophthalmol. 98: 112–115
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.
Friedman Z, Allen RC, Raph SM (1985) Topical acetazolamide and methazolamide delivered by contact lenses. Arch. Ophthalmol. 103: 963–966
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
Gurny R (1981b) Preliminary study of prolonged acting drug delivery system for the treatment of glaucoma. Pharm. Acta. Helv. 56: 130–132
Gurny R, Boye T, Ibrahim H (1985) Ocular therapy with nanoparticulate systems for controlled drug delivery. J. Contr. Rel. 2: 353–361
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
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.
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
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
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
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
Harmia-Pulkkinen T, Ihantola A, Tuomi A, Kristoffersson E (1986) Nanoencapsulation of timolol by suspension and micelle polymerization. Acta Pharma. Fennica 95: 89–96
Heilman K (1984) Therapeutic systems for local use. Ocular therapeutic systems. In: Therapeutic systems ( 2nd ed). Stuttgart, Georg Thieme Verlag.
Holly FJ, Lemp MA (1973) The precorneal tear film and dry eye syndromes. In: Int. Ophthalmol. Clin. 13 (1) Boston, Little Brown Co.
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
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
Hui HW, Robinson JR (1985) Ocular delivery of progesterone using a bioadhesive polymer. Int. J. Pharm. 26: 203–213
Hui HW, Robinson JR (1986). Effect of particle dissolution rate on ocular drug bioavailability. J. Pharm. Sci. 75: 280–287.
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.
Kaila T, Salminen L, Huupponen R (1985) Systemic absorption of topically applied ocular timolol. J. Ocular Pharmacol. 1: 79–83
Katz IM, Berger ET (1979) Effects of iris pigmentation on response of ocular pressure to timolol. Surv. Ophthalmol. 23: 395–398
Katz IM, Blackman WM (1977) A soluble sustained-release ophthalmic delivery unit. Am. J. Ophthalmol. 83: 728–734
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
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
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
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
Lederer CM, Harold RE (1986) Drop size of commercial glaucoma medications. Amer. J. Ophthalmol. 101: 691–694
Lee VHL (1983) Esterase activities in adult rabbit eyes. J. Pharm. Sci. 72: 239–244
Lee VHL, Robinson JR (1982) Disposition of pilocarpine in the pigmented rabbit eye. Int. J. of Pharm. 11: 155–165.
Lee VHL, Robinson JR (1986) Review: Topical ocular drug delivery: recent developments and future challenges. J. Ocular Pharmacol. 2: 67–108
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
Lewis RA, Schoenwald RD, Eller MG, Barfknecht CF, Phelps CD (1984) Ethoxzolamide Analogue Gel: A topical carbonic anhydrase inhibitor. Arch. Ophthalmol. 102: 1821–1824
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
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
Ludwig A, Van Ooteghem M (1986a) The study of the precorneal dynamics of ophthalmic solutions by fluorophotometry. Pharm. Acta. Helv. 61: 236–240
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.
Lyons JS, Krohn DL (1974) Pilocarpine uptake by pigmented uveal tissue. Am.J. Ophthalmol. 75: 883–885
Maichuk YF (1975a) Ophthalmic drug inserts. Invest. Ophthalmol. 14: 87–90
Maichuk YF (1975b) Soluble ophthalmic drug inserts. The Lancet 1: 173
Mandell AI, Stentz F, Kitabachi AE (1978) Dipivalyl epinephrine: a new prodrug in the treatment of glaucoma. Ophthalmology 85: 268–275
March WF, Stewart RM, Mandell AI, Bruce LA (1982) Duration of effect of pilocarpine gel. Am. J. Ophthalmol. 100: 1270–1271
Maren TH (1967) Carbonic anhydrase chemistry, physiology and inhibition. Physiol. Rev. 47: 595–781
Maren TH, Jankowska L (1985) Ocular pharmacology of sulfonamides: the cornea as barrier and depot. Current Eye Res. 4: 399–408
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.
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.
Maurice DM, Mishima S (1984) Ocular pharmacokinetics. In: Sears ML (ed) Pharmacology of the eye. Vol. 69, Springer Verlag, Heidelberg, pp. 19–116
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.
McLaughlin MA, Chiou GCY (1985) Review: a synopsis of recent developments in antiglaucoma drugs. J. Ocular Pharm. 1: 101–121.
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
Mikkelson TJ (1986) Ophthalmic drug delivery. Pharm. Technol. 8: 90–98
Mindel JS, Smith H, Jacobs M, Kharlamb AB, Friedman AH (1984) Drug reservoirs in topical therapy. Invest. Ophthalmol. Vis. Sci. 25: 346–350.
Mishima S (1981) Clinical pharmacokinetics of the eye. Invest. Ophthalmol. Vis. Sci. 21: 504–541
Mishima S, Gasset A, Klyce SD Jr, Baum JL (1966) Determination of tear volume and tear flow. Invest. Ophthalmol. 5: 264–276
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
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
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
Ono S, Hirano H, Obaka K (1971) Degradation in the side chain of cortisol by lens homogenate. Tohoku J. Exp. Med. 104: 171–175
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
Patton TF (1977) Pharmacokinetic evidence for improved ophthalmic drug delivery by reduction of instilled volume. J. Pharm. Sci. 66: 1058–1059
Patton TF, Ocular Drug Disposition In: Ophthalmic Drug Delivery Systems, Robinson JR, (ed), American Pharmaceutical Association, Washington D.C. 1980 pp. 28–54.
Patton TF, Robinson JR (1975) Ocular evaluation of polyvinyl alcohol vehicle in rabbits. J. Pharm. Sci. 64: 1312–1316
Patton TF, Robinson JR (1976) Quantitative precorneal disposition of topically applied pilocarpine. J. Pharm. Sci. 65: 1295–1301
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.
Podos SM, Becker B, Assef C, Hartstein J (1972) Pilocarpine therapy with soft contact lenses. Am. J. Ophthalmol. 73: 336–341
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.
Prince JH (ed) (1964) The rabbit in eye research. Thomas, Springfield
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
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
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.
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.
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.
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.
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
Schoenwald RD, Huang HS (1983) Corneal penetration behaviour of p-blocking agents I: Physicochemical factors. J. Pharm. Sci. 72: 1266–1272
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
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
Sears ML (ed) (1981) New directions in ophthalmic research. New Haven, Yale University Press
Shell JW (1982) Ocular drug delivery systems–a review. J. Toxicol.-Cut. Ocular Toxicol. 1: 49–63
Shell JW (1984) Ophthalmic drug delivery systems. Surv. Ophthalmol. 29: 117–128
Shell JW, Baker RW (1974) Diffusional systems for controlled release of drugs to the eye. Ann. Ophthalmol. 6: 1037
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
Sieg JW, Robinson JR (1975) Vehicle effects on ocular bioavailability.l. Evaluation of fluorometholone. J. Pharm. Sci. 64: 931–936
Sieg JW, Triplett JW (1980) Precorneal retention of topically instilled micronized particles. J. Pharm. Sci. 69: 863–864
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
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.
Sugaya M, Nagataki S (1978) Kinetics of topical pilocarpine in the human eye. Japan J. Ophthalmol. 22: 127–141
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
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
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
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
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
Urtti A (1985) Pilocarpine release from matrices of alkyl half-esters of poly(vinyl methyl ether/maleic anhydride). Int. J. Pharm. 26: 45–55
Urtti A, Juslin M, Miinalainen O (1985a) Pilocarpine release from hydroxypropyl-cellulose-polyvinylpyrrolidone matrices. Int. J. Pharm. 25: 165–178
Urtti A, Salminen L, Miinalainen O (1985b) Systemic absorption of ocular pilocarpine is modified by polymer matrices. Int. J. Pharm. 23: 147–161
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
Van Ooteghem M (1983) Viskosität. In: Dolder R, Skinner FS (eds) Ophthalmika, Stuttgart. Wissenschaftliche Verlagsgesellschaft 372–384
Vareilles P, Schmitt C, Lotti VJ, Le Douarec JC (1978) Etude expérimentale du timolol: un nouvel hypotenseur oculaire. J. Fr. Ophtalmol. 12: 717–721
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
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
Waltman SR,Kaufman HE (1970) Use of hydrophilic contact lenses to increase ocular penetration of topical drugs. Invest. Ophthalmol. 9: 250–255
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.
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.
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
Yakovlev AA, Lenkevich MM (1966) Use of pilocarpine impregnated alcohol films in the treatment of glaucomatous patients. Vestn. Oftal. 79: 40–42
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
Zimmermann TJ, Kaufman HE (1977) Timolol: a B-adrenergic blocking agent for the treatment of glaucoma. Arch. Ophthalmol. 95: 601–604
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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
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