Hydrochloride Preparation Research Articles

Serum drug concentrations in patients with ischemic heart disease after administration of a sustained release procainamide preparation.

Despite widespread marketing of a sustained release preparation of procainamide hydrochloride (PROCAN-SR, Parke-Davis), published literature demonstrating its efficacy in maintaining uniform serum drug levels over a 6-hour dosing interval is derived from only normal healthy volunteers. Thirty-three patients with ischemic heart disease, ages 30-88 years, were administered 1-4g/24 hours (mean dose 34 mg/kg/day) of PROCAN-SR in 4 equally divided doses on a Q6H schedule. After achievement of steady-state equilibrium drug concentration, procainamide and N-acetylprocainamide levels were determined by high-performance liquid chromatography on sera obtained from blood samples drawn 2, 3.5 and 5 hours after an oral dose. Mean maximal procainamide and N-acetylprocainamide serum concentrations were 4.6 +/- 1.8 microgram/ml and 4.2 +/- 2.1 micrograms/ml respectively. Mean minimal concentrations were 3.5 +/- 1.7 microgram/ml and 3.6 +/- 2.0 micrograms/ml respectively. The mean change in drug concentration was small (1.1 microgram/ml procainamide and 0.6 microgram/ml N-acetylprocainamide) with procainamide and N-acetylprocainamide concentrations varying only by 27 and 15 percent respectively. These data demonstrate in a population of patients with ischemic heart disease, that Q6H dosing with a sustained release procainamide hydrochloride preparation (PROCAN-SR, Parke-Davis) is associated with only a small acceptable variation between maximal and minimal serum procainamide and N-acetylprocainamide concentrations. This preparation should, therefore, offer greater patient convenience and compliance without sacrificing antiarrhythmic efficacy.

Dissolution and Absorption of the Antineoplastic Agent Ellipticine

Ellipticine, a poorly water-soluble alkaloid, is active in several experimental tumor systems. Marked solubility increases were produced by polyvinylpyrrolidone of varying molecular weights (10,000–160,000) and were optimal (~13mg/ml at 25°) with polyvinylpyrrolidone mol. wt. 10,000. Dissolution of ellipticine-polyvinylpyrro-lidone (1:22 w/w) tablets in simulated gastric juice was superior to that of ellipticine hydrochloride. Release rates were controlled by combinations of polyvinylpyrrolidone polymers without affecting maximum dissolution at 37°. Physiological disposition of ellipticine-polyvinyl- pyrrolidone was compared with that of the hydrochloride salt and ellipticine in suspension following oral administration at 250mg/kg in fasted mice. In comparison to the suspension, ellipticine tissue levels were about threefold higher with polyvinylpyrrolidone or hydrochloride preparations. Antitumor activity of the three preparations was evaluated intraperito-neally and orally versus L-1210 leukemia. The optimal dose of ellipticine-polyvinylpyrrolidone and ellipticine hydrochloride was lower than that of the suspension and suggested improved absorption.

Complete Regressions of Mycosis Fungoides With Topical Mechlorethamine Hydrochloride

Survival of patients with mycosis fungoides, a lymphoma initially appearing in the skin and thereafter spreading to internal organs, has not been substantially improved by chemotherapeutic measures in use over the past two decades. In only a few instances has the disease been reported to undergo complete regression following therapy. In the past four years we have intensively treated more than 70 patients with topical mechlorethamine hydrochloride (nitrogen mustard) preparations, usually consisting of 10 mg of drug dissolved in 2 oz of water. These solutions have been applied to the entire body surface daily, or three times weekly, until disappearance of disease. Thereafter applications have been continued at less frequent intervals. In patients with disease limited to the skin, prior to lymph node involvement, complete regression of disease has been achieved and maintained in more than 50% of cases. Duration of therapy necessary to achieve complete disappearance of disease has

The effect of compound CIBA 34,276-Ba on the cortical electro-encephalogram of healthy persons.

The influence of 1-(3-methylaminopropyl)-di-benzo[b,e]-bicyclo-[2,2,2]octadiene hydrochloride (preparation Ciba 34,276-Ba) on the cortical EEG was studied in 50 healthy volunteers of both sexes aged b

Preparation and properties of alkyl 3-bromopropionimidate hydrochlorides

Preparation and properties of alkyl 3-bromopropionimidate hydrochlorides

Lidocaine vs Parabens as Convulsants

To the Editor:— In a recent letter to the editor (205:803, 1968) Richard S. Crampton, MD, intimated that the methylparaben present in the lidocaine hydrochloride preparation (Xylocaine, Astra 1%), used to control ventricular tachycardia, was a causative agent in convulsions and respiratory arrest. The source article for this intimation, by Schorr (204:859, 1968), refers toallergicreactions with thep-hydroxybenzoate family of bacteriostatic and fungistatic agents (administeredtopically) and would appear to have little bearing on the toxic reactions described. Matthews et al1in studying the acute and chronic toxic reactions ofp-hydroxybenzoic acid esters on dogs, rats, and mice revealed that the lethal dose (LD)50of methylparaben, as the sodium salt, given intravenously to mice was 170 ±8.4 mg/kg. In dogs, the fatal intravenous dose of methylparaben was 940 mg/kg, when injected at 20 mg/kg/min, and 80 mg/kg at a rate of 40

Notes - A New Method for the Preparation of Hydrochlorides (hydrobromides) of Amino Acids

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTNotes - A New Method for the Preparation of Hydrochlorides (hydrobromides) of Amino AcidsY. Liwschitz, A. Zikhs, and I. ShahakCite this: J. Org. Chem. 1956, 21, 12, 1530Publication Date (Print):December 1, 1956Publication History Published online21 February 2003Published inissue 1 December 1956https://doi.org/10.1021/jo01118a614RIGHTS & PERMISSIONSArticle Views135Altmetric-Citations3LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InReddit PDF (133 KB) Get e-Alerts Get e-Alerts