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PubMed2004

New plastic membrane and carbon paste ion selective electrodes for the determination of triprolidine.

Triprolidine (Trip) ion selective electrodes of three types: the conventional polymer membrane (I), graphite coated electrode (II) and carbon paste electrode (III), have been prepared, based on the ion pair of triprolidine hydrochloride with sodium tetraphenylborate. The electrodes exhibit a linear response with a mean calibration graph slope of 56.12, 55.00 and 54.32 mV decade(-1) at 25 degrees C for I, II and III, respectively, within the concentration ranges 1.96 x 10(-5) - 1.00 x 10(-2) M for I and 3.84 x 10(-5) - 1.00 x 10(-2) M for II and III. The detection limits are 1.13+/-0.13 x 10(-5), 1.70+/-0.06 x 10(-5) and 1.78+/-0.05 x 10(-5) M for the three electrodes, respectively. The change of pH within the ranges 4.85 - 8.75 and 4.70 - 8.50 for I and III, respectively, did not affect the electrode performance. The standard electrode potentials were determined at different temperatures and were used to calculate the isothermal coefficient of the electrode. The electrodes showed a very good selectivity for Trip with respect to a large number of inorganic cations and compounds. The standard addition method was applied to the determination of TripCl in pure solution, pharmaceutical preparations, and urine samples.

Calibration↗
PubMed1983

[Rhinitis therapy. Experiences with triprolidine hydrochloride/pseudoephedrin hydrochloride, a decongestive and antiallergic therapeutic agent].

63 patients were treated with the combination of pseudoephedrine hydrochloride and triprolidine hydrochloride (Actifed). Indications were infectious, allergic and vasomotoric rhinitis. The 63 patients divided in 32 children in the age of 2 to 12 years and 31 adults in the age of 14 to 56 years. The daily dose range depending on age was 90.0 to 180.0 mg pseudoephedrine hydrochloride and 3.75 to 7.5 mg triprolidine hydrochloride, applicated either as syrup or as tablets. All patients accepted the drug well. In 58 cases the effect of the drug for treatment of common cold was very good and good. Side-effects were not observed, apart from tiredness in 18 cases, which--however--did only occur at the first day of treatment.

Adolescent↗
PubMed1981

An evaluation of triprolidine and pseudoephedrine in the treatment of allergic rhinitis.

A double-blind, parallel, placebo-controlled study was performed to assess the efficacy of a combination drug product containing the antihistamine, triprolidine, and the sympathomimetic, pseudoephedrine, in the treatment of allergic rhinitis. Allergic rhinitis was defined on the basis of coexistent nasal congestion and an aggregate symptom complex score which exceeded a pre-established value. Pseudoephedrine and triprolidine were shown to make distinct and separate contributions to the treatment of allergic rhinitis defined in this manner.

Airway Resistance↗
PubMed1988

The simultaneous assay of triprolidine, pseudoephedrine and dextromethorphan in combined preparations by derivative-difference spectrophotometry.

Difference spectrophotometric procedures are described for the assay of triprolidine hydrochloride, dextromethorphan hydrobromide and pseudoephedrine hydrochloride in Actifed preparations. Triprolidine is assayed by the measurement of the difference absorbance at 301 nm between equimolar solutions of the sample extract in 0.1 M sulphuric acid and 0.1 M sodium hydroxide in ethanol (20% v/v). Dextromethorphan and pseudoephedrine are assayed by measurement of the amplitudes in the second and fourth derivative spectra of the difference absorption spectrum of the sample solutions. The measured values are proportional to the concentrations of the drugs. The accuracy, precision and selectivity of the procedures are discussed. Applications of the assay are described for Actifed Compound Linctus, Actifed Syrup and Actifed Tablets.

Journal Article↗
PubMed1990

Pharmacokinetics of oral and transdermal triprolidine.

In this open, nonrandomized, three-way crossover study, six healthy male volunteers received single doses of triprolidine (TPL) hydrochloride syrup orally (2.5 mg) and wore transdermal TPL patches (5 mg and 10 mg doses) to compare the pharmacokinetic profiles and dose tolerance of the two formulations. A washout period of at least 1 week was scheduled between the three dosing periods. Blood samples were collected at defined times, and plasma concentrations were determined using a radioimmunoassay. Maximum plasma drug concentration (Cmax) decreased from 5.6 +/- 2.9 ng/mL (mean +/- SD) with oral dosing to 2.0 +/- 1.0 ng/mL and 4.2 +/- 2.0 ng/mL following 5 mg and 10 mg transdermal doses, respectively. Time to reach peak concentration (tmax) increased from 2.0 +/- 1.2 hours with oral dosing to 12.0 +/- 5.9 and 14.3 +/- 9.9 hours following 5 mg and 10 mg transdermal doses, respectively. The differences between AUC0-alpha values with the oral syrup and the 5 mg and 10 mg transdermal doses were not significant when normalized to 2.09 mg (TPL base). The bioavailabilities of the 5 mg and 10 mg transdermal doses relative to the oral 2.09 mg doses were 0.89 +/- 0.32 and 1.04 +/- 0.33, respectively. Mild erythema and pruritus were the most common adverse effects secondary to TPL transdermal application. Drowsiness observed following oral TPL, was not evident following either transdermal dose. The results of this study, therefore, indicate that TPL can be absorbed transdermally, providing consistent plasma concentrations.

Administration, Cutaneous↗
PubMed1991

Evaluation of the primary skin irritation and allergic contact sensitization potential of transdermal triprolidine.

A transdermal patch for the OTC antihistamine, triprolidine (TP), might provide benefits in terms of increased efficacy and reduced sedative side effects. However, concerns over potential irritant or allergic contact sensitization (ACS) skin reactions necessitated through skin toxicity testing before and during initial clinical development. Initial effort was expended on development of a binary vehicle delivery system comprised of TP in 0.5% oleic acid (OA) in propylene glycol (PG). Rabbit skin irritation and Buehler guinea pig skin sensitization testing indicated that this TP/OA/PG formula had both skin irritation and ACS potential. Both tests underestimated, to some degree, the skin toxicities observed in later clinical testing. In clinical tests, skin irritation was due mainly to the OA/PG vehicle, but was enhanced in the presence of high TP concentrations. Of 26 subjects enrolled in a rising dose clinical pharmacokinetics study, one subject exposed twice to TP/OA/PG presented with delayed skin reactions suggestive of ACS. Positive diagnostic patch test results for this subject and four out of five other twice-exposed study subjects suggested that the TP/OA/PG formula had a very high ACS potential. Subsequent predictive clinical patch testing was conducted with a buffered aqueous TP formula which provided in vitro skin penetration of the drug equivalent to the TP/OA/PG formula. These clinical studies demonstrated that TP itself had no significant irritation potential but still induced ACS reactions in a high proportion of test subjects. The incidence of adverse skin reactions to TP was considered to be too high relative to the degree of improved therapeutic benefit of this delivery form. On this basis, all technology development effort was discontinued.

Administration, Cutaneous↗
PubMedDate not supplied

Adsorptive stripping voltammetric determination of triprolidine hydrochloride in pharmaceutical tablets.

The electrochemical behavior of antihistaminic drug, viz. triprolidine hydrochloride (TripCl), at a hanging mercury drop electrode (HMDE) is investigated. Chemical and electrical parameters affecting the adsorptive voltammetric measurements are optimized. Different modes of sweep, viz. direct current DC, normal pulse NP, differential pulse DP and square wave SW modes, over the potential range from -800 to -1400 mV, are used in the presence of 0.04 M Britton-Robinson buffer pH 11, with accumulation time 30 s, scan rate 50 mV/s and pulse amplitude 50 mV. The reduction process is irreversible and involved the transfer of two electrons and two protons. Their responses are linear over the concentration range 15-157 ng/ml with average correlation coefficient 0.9998, while the detection limit is 2.64, 6.24, 8.80 and 2.12 ng/ml for DC, DP, SW and NP mode, respectively. The differential pulse method has been applied successfully for the determination of the drug in Egyptian pharmaceutical preparation with mean recovery 99.55+/-0.67%.

Adsorption↗
PubMed1978

Histamine challenge and anterior nasal rhinometry: their use in the assessment of pseudoephedrine and triprolidine as nasal decongestants in subjects with hayfever.

1 Nasal airway resistance (NAR) was measured by anterior rhinometry in ten volunteers with allergic rhinitis. Measurements before and after challenge with three concentrations of histamine diphosphate showed significant rises in NAR for each challenge. 2 In a double-blind, crossover study with the same patients triprolidine (2.5 mg) and pseudoephedrine (60 mg) were shown to be equally effective in reducing the rise in NAR produced by histamine challenge to one nostril; both were significantly better than placebo. 3 The rise in NAR of both nostrils after histamine challenge to one nostril was significantly reduced after pseudoephedrine compared with placebo. This suggests that pseudoephedrine is effective in preventing reflex mucosal congestion in the unchallenged nostril. 4 No increase in the pulse rate or blood pressure of the volunteers was detected after either drug.

Adult↗
PubMed1975

A Double-blind crossover trial of pseudoephedrine and triprolidine, alone and in combination, for the treatment of allergenic rhinitis.

In a double-blind crossover trial of pseudoephedrine 60 mg and triprolidine 2.5 mg, alone and in combination, on 40 volunteers suffering from allergic rhinitis, both drugs were found superior to placebo in reducing the effects of allergic rhinitis and were of equal efficacy. The combination tablet was consistently better than either drug in several of the assessments and was the treatment which the subjects, as a whole, preferred. Side effects were not a problem with any of the medications.

Adult↗
PubMed1979

Effects of pseudoephedrine and triprolidine on visual performance.

The effects of q.i.d. administration of 60 mg pseudoephedrine (Sudafed) tablets or pseudoephedrine-triprolidine (Actifed) tablets after 5 d of medication were measured on tests of night vision, color perception, stereopsis, and reaction time. Neither drug appeared to impair performance.

Color Perception↗
PubMedDate not supplied

[Double blind crossover study of pseudoephedrine and triprolidine alone and in combination in the treatment of allergic rhinitis (author's transl)].

In a double-blind crossover trial of pseudoephedrine 60 mg. and triprolidine 2.5 mg. alone and in combination, on 40 volunteers suffering from allergic rhinitis, both drugs were found superior to placebo in reducing the effects of allergic rhinitis and were of equal efficacy. The combination tablet was consistently better than either drug in several of the assessments and was the treatment which the subjects, as a whole, preferred. Side effects were not a problem with any of the medications.

Adult↗