Synonyms
trans-Triprolidine hydrochloride;2-[(1E)-1-(4-Methylphenyl)-3-pyrrolizino-1-propenyl]pyridine·hydrochloride
Molecular Formula
C19H23ClN2
Smiles
CC1=CC=C(C=C1)/C(=C\CN2CCCC2)/C3=CC=CC=N3.Cl
General Description
Triprolidine Hydrochloride is a potent first-generation antihistamine of the propylamine (alkylamine) class, recognized for its relatively high H1 receptor binding affinity and favorable pharmacokinetic profile with a rapid onset and moderate duration of action. The hydrochloride salt is well absorbed orally and provides consistent plasma concentrations at therapeutic doses. It is frequently combined with sympathomimetic decongestants in multi-symptom cold and allergy preparations.
Mechanism of Action
Triprolidine Hydrochloride is a competitive antagonist at peripheral and central H1 histamine receptors. By blocking histamine-induced increases in vascular permeability, bronchoconstriction, and sensory nerve stimulation, it effectively reduces allergic symptoms including rhinorrhea, sneezing, itching, and watery eyes. Its relatively low molecular weight and lipophilicity allow efficient blood-brain barrier penetration, producing clinically significant sedation in many patients.
Application
Triprolidine Hydrochloride is indicated for the symptomatic relief of allergic rhinitis, common cold symptoms, and allergic skin conditions characterized by itching and urticaria.
Triprolidine hydrochloride (TPH)-loaded pH-sensitive microspheres were developed using blends of polycaprolactone (PCL) and cellulose acetate phthalate (CAP) via a double emulsion solvent evaporation method. The maximum drug loading was 66%. Microspheres were characterized by DSC, X-RD, particle size analysis, and SEM. DSC showed blend compatibility; X-RD confirmed molecular dispersion of TPH; SEM revealed spherical microspheres with rough surfaces. Release kinetics followed the Korsmeyer-Peppas model with n values ranging from 0.581 to 1.038 at pH 7.4, indicating anomalous (non-Fickian) diffusion. Release duration exceeded 10 hours. These microspheres are suitable for oral controlled-release formulations.
Fig. 1 SEM micrographs of TPH loaded microspheres (a) before dissolution and (b) after dissolution. (Sudhakar K.; et al. 2014)
References
- Sudhakar K, et al. Development of pH-sensitive polycaprolactone-based microspheres for in vitro release studies of Triprolidine Hydrochloride. Designed Monomers and Polymers, 2014, 17(7): 617-623.
What is the recommended storage condition for Triprolidine Hydrochloride?
It should be stored at 2-8°C in a well-sealed container, protected from moisture and direct light, to maintain its chemical integrity throughout the shelf life.
Can we obtain batch-specific analytical data for Triprolidine Hydrochloride?
Batch-specific COA documents are standard with every shipment. Additional analytical reports, including HPLC chromatograms or spectral data, may be provided upon request.
Does your company offer custom packaging for Triprolidine Hydrochloride?
Yes, custom pack sizes are available. Specific quantity requirements can be discussed directly with our team to align with your production or research scale.
Is Triprolidine Hydrochloride compatible with both oral and topical formulations?
Compatibility with oral solid dosage forms and topical formulations is well documented in the literature. Formulation-grade material is available for both application types.