Pilocarpine nitrate

Name of Plant Commercial Name Constituents Amount of Total Alkaloid per cent. Amount of Crystalline Pilocarpine Nitrate obtai ned per cent. 

The extraction of alkaloids from jaborandi has been dealt with by Wurtzen, and the estimation of pilocarpine in the drug and its preparations by Jowett and by Bourcet and more recently by Taran and by Shupe.ii Elvidge has devised a colorimetric method based on Ekkert s test, < and a polarographic study has been made by Kirkpatrick. Tlie two first-pamed authors depend on the isolation of pilocarpine nitrate, which is also the basis of the process of manufacture described by Cheninitius.12... 

Pilocarpidine, CiqHiiOjNj. This alkaloid was obtained by Harnack from P. Jaborandi, and later by Merck from the mother liquors from crystallisation of pilocarpine nitrate. It does not occur in the leaves of P. microphyllus (Jowett, ). The free base is a viscid oil, [a]n + 81-3° (less in presence of alkali). The salts crystallise well the nitrate, B. HNO3, in colourless prisms, m.p. 137°, - -73-2°. The aurichloride, unlike... 

TF Patton, JR Robinson. (1976). Quantitative precorneal disposition of topically applied pilocarpine nitrate in rabbit eyes. J Pharm Sci 65 1295-1301. 

SC Miller, MD Donovan. (1982). Effect of poloxamer 407 gel on the mitotic activity of pilocarpine nitrate in rabbits. Int J Pharm 12 147-152. 

Calculate the sodium chloride equivalent of a 1% solution of pilocarpine nitrate. 

MW of NaCl i value of pilocarpine nitrate i value of NaCl MW of pilocarpine nitrate... 

Freezing point depression of 1% pilocarpine nitrate is 0.14°. Calculate the volume of iso-osmotic solution produced by 1 gram of pilocarpine nitrate by U.S.P. method. 

Vandamme and Brobeck [97] studied the residence time as well as the miotic and mydriatic effect of different generations of fluorescein, pilocarpine nitrate, and tropicamide-loaded PAMAM, respectively. A single dose of 25 pL of drug-loaded dendrimer solution was applied each time on the conjunctival sac of albino rabbit eye. PAMAM dendrimeric solutions... 

Vandamme, T.F., and L. Brobeck. 2005. Poly(amidoamine) dendrimers as ophthalmic vehicles for ocular delivery of pilocarpine nitrate and tropicamide. J Control Release 20 102. 

Cetylpyridinium chloride Inclusion of 0.02% cetylpyridinium chloride with pilocarpine nitrate applied topically to the rabbit eye was found to cause a miotic effect 10 times that obtained in the absence of cetylpyridinium [64]. In another study, cetylpyridinium chloride was shown to enhance penicillin penetration across the isolated rabbit cornea [65] with an intact epithelial layer. The penetration was even more than that shown by the de-epithelialized corneas. 

Loftssona et al. [98] found that with increases in the concentration of HP-(3-CD, the flux of a hydrophobic drug arachidonylethanolamide increased. Later, Tirucherai and Mitra [99] found that HP-(3-CD could also enhance the corneal permeation of the lipophilic drug ganciclovir dibutyrate (acyl ester prodrug of ganciclovir). Aktas [100] also found that addition of HP-(3-CD to the simple aqueous solution of pilocarpine nitrate increased the permeation of pilocarpine nitrate by four times in an in vitro permeability study using isolated rabbit cornea. 

A contact lens has been equilibrated with an aqueous solution of pilocarpine nitrate. The total amount of the drug loaded in the lens was 1.54 mg. The following drug release data were obtained ... 

Aktas et al. [141] showed an increased permeation of pilocarpine nitrate com-plexed with hydroxy-propyl-P-cyclodextrin using isolated rabbit cornea. They found a significant reduction in the pupil diameter compared to a simple aqueous solution... 

An example of a degradable matrix system is the pilocarpine-containing inserts formulated by Saettone et al. [148]. Pilocarpine nitrate and polyacrylic acid were incorporated into a matrix containing polyvinyl alcohol and two types of hydroxy-propyl methylcellulose. It was shown that all inserts significantly increased the pharmacological effect (miotic response) compared to a solution of pilocarpine nitrate. 

In order to avoid the undesirable isomerization to isopilocarpine (Section III,D,3) and, probably, to avoid enzymatic degradation, the Jaborandi leaves are processed as rapidly as possible. Acidification converts the alkaloids to their water-soluble salts, which allows defatting of the leaves with, for example, petroleum ether. Alkalinization and extraction with a suitable lipid-extracting solvent or solvent mixture gives the crude alkaloid mixture. (+)-Pilocarpine (mp 34°C) crystallizes only with difficulty it can be obtained readily as the nitrate salt (mp 178°C) in the absence of isopilocarpine. The separation of isopilocarpine nitrate from pilocarpine nitrate by crystallization is often difficult because mixtures may give products of constant melting points the same holds for the hydrochlorides. 

Parasympathomimetics such as physostigmine sulfate increase the level of acetylcholine, which contracts the ciliary muscle and opens the fluid pathway which leads to reduction in IOP. They are usually used with pilocarpine hydrochloride or pilocarpine nitrate, which acts on cholinoceptors. Parasympathomimetics cause poor night vision because of miosis. 

Fig. 9. spectrum of pilocarpine nitrate (10% solution in deuterium oxide). A, fully noise-decoupled B, off-resonance... 

Fenfluramine Hydrochloride Clorprenaline Hydrochloride Lysergic Acid Stilboestrol Dichlorophen Bufylline Orphenadrine Meptazinol Hydrochloride Methylphenidate Hydrochloride Halazone Sulphamethizole Tolbutamide Doxylamine Hexoestrol Oestrone Mecloqualone Nordazepam Chloroprocaine Medazepam Carbutamide Normorphine Pilocarpine Nitrate Sulphapyridine Sodium Cyclazocine Dextromethorphan Methoprotryne Meprylcaine Hydrochloride Procainamide Hydrochloride Muzolimine Clorgyline... 

Pilocarpine hydrochloride. 560 Pilocarpine nitrate. 560 Pimuricin, 2.37-2.38 Piininodine. 7.361. 737 Pimozide. SO)... 

Acetylcholine Cl (Miochol) Carbachol intraocular (Miostat) Pilocarpine HCL (Isopto Carpine) Pilocarpine nitrate (Ocusert Pilo-20) Echothiophate iodide (Phospholine Iodide) Physostigmine salicylate (Isopto Eserine) Betaxolol HC1 (Betoptic) Levobunolol HC1 Timolol maleate (Timoptic) Acetazolamide (Diamox) Brinzolamide ophthalmic sus. 1% Dichlorphenamide (Daranide) Dorzolamide (Trusopt) Methazolamide (Neptazane)... 

Pilocarpine Minims Pilocarpine Nitrate, Pilogel (also available as generic pilocarpine hydrochloride eye drops) Treatment of glaucoma... 

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