Pilocarpine Inserts: Experimental and Clinical Experiences

  • L. Salminen
Part of the FIDIA Research Series book series (FIDIA, volume 11)


During the last 15 years about ten pilocarpine ocular inserts — most of soluble hydrophilic polymers — have been presented. In vitro studies demonstrated prolongation of pilocarpine release from these systems as compared to pilocarpine solutions. In in vivo studies in rabbits the hydrophilic inserts gelled in minutes and dissolved in hours. The magnitude of maximum pupil size constriction was enhanced, with duration of miosis significantly increased over that of liquid dosage systems. Few pilocarpine inserts have been tested in human eyes and in clinical use is only one type (Maichuk, 1976).


Albino Rabbit Ocular Drug Delivery Pigment Rabbit Ocular Insert Pilocarpine Hydrochloride 
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  1. Ahmed I, Patton TF (1985) Importance of the noncorneal absorption route in topical ophthalmic drug delivery. Invest Ophthalmol Vis Sci 26: 584–587.PubMedGoogle Scholar
  2. Bensinger R, Shin DH, Kass MA, Podos SM, Becker B (1976) Pilocarpine ocular inserts. Invest Ophthalmol 15: 1008–1010.PubMedGoogle Scholar
  3. Birss SA, Longwell A, Heckbert S, Keller N (1978) Ocular hypotensive efficacy of topical epinephrine in normotensive and hypertensive rabbits: continous drug delivery vs eyedrops. Ann Ophthalmol 10: 1045–1054.PubMedGoogle Scholar
  4. Bloomfield SE, Dunn MW, Miyata T, Stenzel KH (1977) Soluble gentamycin ophthalmic inserts as a drug delivery system. Arch Ophthalmol 95: 247–250.PubMedCrossRefGoogle Scholar
  5. Chrai SS, Robinson JR (1974) Corneal penetration of topical pilocarpine nitrate in the rabbit. Am J Ophthalmol 77: 735–739.PubMedGoogle Scholar
  6. Dohlman CH, Pavan-Langston D, Rose J (1972) A new ocular insert for continuous constant-rate delivery of medication to the eye. Ann Ophthalmol 4: 823–832.PubMedGoogle Scholar
  7. Grass GM, Cobby J, Makoid MC (1984) Ocular delivery of pilocarpine from erodible matrices. J Pharm Sci 73: 618–621.PubMedCrossRefGoogle Scholar
  8. Kaila T, Salminen L, Huupponen R (1985) Systemic absorption of topically applied ocular timolol. J Ocular Pharmacol 1: 79–83.CrossRefGoogle Scholar
  9. Katz IM, Blackman WM (1977) A soluble sustained-release ophthalmic delivery unit. Amer J Ophthalmol 83: 728–734.Google Scholar
  10. Katz JI, Kaufman HE, Breslin C, Katz IM (1978) Slow-release artificial tears and the treatment of keratitis sicca. Ophthalmology 85: 787–793.PubMedGoogle Scholar
  11. Lee VHL, Robinson JR (1986) Review: Topical ocular drug delivery: recent developments and future challenges. J Ocular Pharmacol 2: 67–108.CrossRefGoogle Scholar
  12. Lerman S (1970) Simulated sustained release pilocarpine therapy. Ann Ophthalmol 2: 435–439.Google Scholar
  13. Loucas SP, Haddad HM (1972) Solid-state ophthalmic dosage systems in effecting prolonged release of pilocarpine in the cul-de-sac. J Pharm Sci 61: 985–986.PubMedCrossRefGoogle Scholar
  14. Maichuk YF (1976) Polymeric drug delivery systems in ophthalmology. In: Leopold IH, Burns RP (eds): Ocular therapy. John Wiley and Sons, New York; pp. 1–16.Google Scholar
  15. Maichuk YF, Erichev VP (1981) Soluble ophthalmic drug inserts with pilocarpine: experimental and clinical study. Glaucoma 3: 239–242.Google Scholar
  16. Maichuk YF (1985) Medicated eye films. Medexport, Moscow;pp.l-66.Google Scholar
  17. Maurice DM, Mishima S (1984) Ocular pharmacokinetics. In: Sears ML (ed): Handbook of experimental pharmacology, Vol. 69. Springer-Verlag, Berlin-Heidelberg; pp. 19–116.Google Scholar
  18. Mishima S (1981) Clinical pharmacokinetics of the eye. Invest Ophthalmol Vis Sci 21: 504–541.PubMedGoogle Scholar
  19. Pavan-Langston D, Langston RHS, Geary PA (1975) Idoxuridine ocular insert therapy. Arch Ophthalmol 93: 1349–1351.PubMedCrossRefGoogle Scholar
  20. Richardson KT (1975) Ocular microtherapy. Membrane-controlled drug delivery. Arch Ophthalmol 93: 74–86.PubMedCrossRefGoogle Scholar
  21. 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.PubMedCrossRefGoogle Scholar
  22. Saettone MF, Giannaccini B, Chetoni P, Galli G, Chiellini E (1984) Vehicle effects in ophthalmic bioavailability: an evaluation of polymeric inserts containing pilocarpine. J Pharm Pharmacol 36: 229–234.PubMedCrossRefGoogle Scholar
  23. Salminen L, Urtti A, Kujari H, Juslin M (1983) Prolonged pulse-entry of pilocarpine with a soluble drug inserts. Graefes Arch Clin Exp Ophthalmol 221: 96–99.PubMedCrossRefGoogle Scholar
  24. Salminen L, Urtti A, Periviita L (1984) Effect of ocular pigmentation on pilocarpine pharmacology.I. Drug distribution and metabolism. Int J Pharm 18: 17–24.CrossRefGoogle Scholar
  25. Shell JW (1984) Ophthalmic drug delivery systems. Sury Ophthalmol 29: 117–128.CrossRefGoogle Scholar
  26. Urtti A, Salminen L, Kujari H, Jantti V (1984) Effect of ocular pigmentation on pilocarpine pharmacology in the rabbit eye.II. Drug response. Int J Pharm 19: 53–61.CrossRefGoogle Scholar
  27. Urtti A, Periviita L, Salminen L, Juslin M (1985a) Effects of hydrophilicity of polymer matrix on in vitro release of pilocarpine and on its miotic activity in rabbit eyes. Drug Development and Industrial Pharmacy 11: 257–268.CrossRefGoogle Scholar
  28. Urtti A, Juslin M, Miinalainen 0 (1985b) Pilocarpine release from hydroxypropylcellulose-polyvinylpirrolidone matrices. Int J Pharm 25: 165–178.Google Scholar
  29. Urtti A (1985c) Pilocarpine release from matrices of alkyl half-esters of poly(vinyl methyl ether-maleic anhydride). Int J Pharm 26: 45–55.CrossRefGoogle Scholar
  30. Urtti A (1985d) Deliverial and pharmacokinetic aspects of ocular pilocarpine administration. University of Kuopio, Kuopio; pp. 1–94.Google Scholar
  31. Urtti A, Salminen L, Miinalainen 0 (1985e) Systemic absorption of ocular pilocarpine is modified by polymer matrices. Int J Pharm 23: 147–161.Google Scholar
  32. Yoshida S, Mishima S (1975) A pharmacokinetic analysis of the pupil response to topical pilocarpine and tropicamide. Jpn J Ophthalmol 19: 121–138.Google Scholar

Copyright information

© Springer Science+Business Media New York 1987

Authors and Affiliations

  • L. Salminen
    • 1
  1. 1.Department of OphthalmologyTurku University Central HospitalTurkuFinland

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