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Comparison of enzymatic hydrolysis of pilocarpine prodrugs in human plasma, rabbit cornea, and butyrylcholinesterase solutions.
J Pharm Sci 1995; 84(5):656-60JP

Abstract

Various bispilocarpic acid diesters (double prodrugs of pilocarpine) were synthesized, and their in vitro esterase catalyzed hydrolysis was evaluated in diluted human plasma, rabbit cornea homogenate, and specific butyrylcholinesterase solution. The structural changes greatly affected the rate of enzymatic hydrolysis of the prodrugs. Bispilocarpic acid with 2 cyclopropane substituents was the most stable derivative, whereas bispilocarpic acid with 2 cyclobutane substituents was the most labile derivative. The charged bispilocarpic acid diester hydrolyzed more slowly than the unchanged form. Comparison of the results obtained from different plasma and cornea homogenate batches is difficult because of the variety of the enzyme systems involved. This variety also makes comparing the results between different laboratories difficult.

Authors+Show Affiliations

Department of Pharmaceutical Chemistry, University of Kuopio, Finland.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

7658361

Citation

Järvinen, T, et al. "Comparison of Enzymatic Hydrolysis of Pilocarpine Prodrugs in Human Plasma, Rabbit Cornea, and Butyrylcholinesterase Solutions." Journal of Pharmaceutical Sciences, vol. 84, no. 5, 1995, pp. 656-60.
Järvinen T, Poikolainen M, Suhonen P, et al. Comparison of enzymatic hydrolysis of pilocarpine prodrugs in human plasma, rabbit cornea, and butyrylcholinesterase solutions. J Pharm Sci. 1995;84(5):656-60.
Järvinen, T., Poikolainen, M., Suhonen, P., Vepsäläinen, J., Alaranta, S., & Urtti, A. (1995). Comparison of enzymatic hydrolysis of pilocarpine prodrugs in human plasma, rabbit cornea, and butyrylcholinesterase solutions. Journal of Pharmaceutical Sciences, 84(5), pp. 656-60.
Järvinen T, et al. Comparison of Enzymatic Hydrolysis of Pilocarpine Prodrugs in Human Plasma, Rabbit Cornea, and Butyrylcholinesterase Solutions. J Pharm Sci. 1995;84(5):656-60. PubMed PMID: 7658361.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Comparison of enzymatic hydrolysis of pilocarpine prodrugs in human plasma, rabbit cornea, and butyrylcholinesterase solutions. AU - Järvinen,T, AU - Poikolainen,M, AU - Suhonen,P, AU - Vepsäläinen,J, AU - Alaranta,S, AU - Urtti,A, PY - 1995/5/1/pubmed PY - 1995/5/1/medline PY - 1995/5/1/entrez SP - 656 EP - 60 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 84 IS - 5 N2 - Various bispilocarpic acid diesters (double prodrugs of pilocarpine) were synthesized, and their in vitro esterase catalyzed hydrolysis was evaluated in diluted human plasma, rabbit cornea homogenate, and specific butyrylcholinesterase solution. The structural changes greatly affected the rate of enzymatic hydrolysis of the prodrugs. Bispilocarpic acid with 2 cyclopropane substituents was the most stable derivative, whereas bispilocarpic acid with 2 cyclobutane substituents was the most labile derivative. The charged bispilocarpic acid diester hydrolyzed more slowly than the unchanged form. Comparison of the results obtained from different plasma and cornea homogenate batches is difficult because of the variety of the enzyme systems involved. This variety also makes comparing the results between different laboratories difficult. SN - 0022-3549 UR - https://www.unboundmedicine.com/medline/citation/7658361/Comparison_of_enzymatic_hydrolysis_of_pilocarpine_prodrugs_in_human_plasma_rabbit_cornea_and_butyrylcholinesterase_solutions_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)49794-1 DB - PRIME DP - Unbound Medicine ER -