Tetrahydrozoline Research Articles

A Comparative Kinetic and Mechanistic Study Between Tetrahydrozoline and Naphazoline Toward Photogenerated Reactive Oxygen Species

Kinetic and mechanistic aspects of the vitamin B2 (riboflavin [Rf])-sensitized photo-oxidation of the imidazoline derivates (IDs) naphazoline (NPZ) and tetrahydrozoline (THZ) were investigated in aqueous solution. The process appears as important on biomedical grounds, considering that the vitamin is endogenously present in humans, and IDs are active components of ocular medicaments of topical application. Under aerobic visible light irradiation, a complex picture of competitive interactions between sensitizer, substrates and dissolved oxygen takes place: the singlet and triplet ((3)Rf*) excited states of Rf are quenched by the IDs: with IDs concentrations ca. 5.0 mM and 0.02 mM Rf, (3)Rf* is quenched by IDs, in a competitive fashion with dissolved ground state oxygen. Additionally, the reactive oxygen species: O(2)((1)Delta(g)), O(2)(*-), HO(*) and H(2)O(2), generated from (3)Rf* and Rf(*-), were detected with the employment of time-resolved methods or specific scavengers. Oxygen uptake experiments indicate that, for NPZ, only H(2)O(2) was involved in the photo-oxidation. In the case of THZ, O(2)(*-), HO(*) and H(2)O(2) were detected, whereas only HO(*) was unambiguously identified as THZ oxidative agents. Upon direct UV light irradiation NPZ and THZ generate O(2)((1)Delta(g)), with quantum yields of 0.2 (literature value, employed as a reference) and 0.08, respectively, in acetonitrile.

Ophthalmic delivery systems based on drug–polymer–polymer ionic ternary interaction: In vitro and in vivo characterization

Aim of the work was to develop mucoadhesive eyedrops containing tetrahydrozoline hydrochloride (TZ), a decongestant drug, and based on a ternary interaction drug–polymer–polymer. The anionic polymers assessed were the anionic hyaluronic acid (HA) and polyacrylic acid (PAA), the cationic chitosan (HCS) and the polyelectrolyte gelatin (G). Formulations based on the ternary systems TZ/G/HA, TZ/HCS/HA, TZ/G/PAA and TZ/HCS/PAA at the stoichiometry ratios between cationic and anionic polymers and containing a 10 and 20 fold excess of the anionic polymers were prepared. The formulations were characterized for in vitro mucoadhesive and release properties. The ex vivo/in vivo residence properties were assessed for the formulations that combined the better in vitro mucoadhesive and release properties. The physical stability of the formulations selected was determined following steam sterilization and storage at 25 and 40 °C. The synergistic effect of G with HA and PAA improves the mucoadhesion of the formulations while the interaction of HCS with HA and PAA is likely to produce higher neutralization of the anionic polymer charge and minor chain flexibility resulting in a limited mucoadhesion improvement. Both G and HCS participate to control drug release. The selected formulations demonstrate to possess consistency (viscosity) sensitive to the ions of the medium, and probably for this reason the ex vivo/in vivo residence properties could not directly correlated to mucoadhesion and to drug release control properties. However, the formulations are able to maintain levels of TZ detectable until 20 min after the instillation in rabbits, while TZ was not detectable since 3 min after instillation of the drug solution. The physical stability, following steam sterilization and storage, the low viscosity combined with good residence time in conjunctival sac make the TZ/G/20HA the more promising formulation.

Simultaneous determination of ofloxacin, tetrahydrozoline hydrochloride, and prednisolone acetate by high-performance liquid chromatography.

A simple, specific, and precise high-performance liquid chromatographic method has been developed for the simultaneous determination of ofloxacin (OFX), tetrahydrozoline hydrochloride (THC), and prednisolone acetate (PAC) in ophthalmic suspension using propylparaben (POP) as the internal standard. The mobile phase consists of 0.05 M phosphate buffer-acetonitrile (65:35, v/v), and the pH is adjusted to 2.7 with orthophosphoric acid. A column containing octadecyl silane chemically bonded to porous silica particles (Waters Spherisorb, 5 microm ODS 1, 4.6 x 150 mm) is used as the stationary phase. The detection is carried out using a variable wavelength UV-vis detector set at 210 nm for OFX and THC and 254 nm for POP (internal standard) and PAC. The solutions are chromatographed at a constant flow rate of 1.2 mL/min. Retention times for OFX, THC, POP, and PAC are approximately 2.5, 4.5, 7.8, and 9.5 min, respectively. The relative retention times are approximately 0.14 min for OFX, 0.35 min for THC, 1.00 min for POP, and 1.22 min for PAC. The linearity range and percent recoveries for OFX, THC, and PAC are 24-120, 4-16, and 16-80 microg/mL and 100.48%, 100.34%, and 100.21%, respectively.

Kinetics of hydrolysis of tetrahydrozoline hydrochloride in aqueous solutions

The kinetics of hydrolysis of tetrahydrozoline hydrochloride in aqueous solution at 353, 363 and 368 K in the pH-range from 2.00 to 12.20 has been investigated. The decomposition products have been investigated by HPLC.

Application of liquid pre-column capillary electrophoresis technique to the study of interaction between drug enantiomers and human serum albumin

Based on the chiral separation of several basic drugs, dimetindene, tetryzoline, theodrenaline and verapamil, the liquid pre-column capillary electrophoresis (LPC-CE) technique was established. It was used to determine free concentrations of dmg enantiomers in mixed solutions with human serum albumin (HSA). To prevent HSA entering the CE chiral srparation zone, the mobility differences between HSA and drugs under a specific pH condition were employed in thr LPC. Thus, the detection confusion caused by protein was totally avoided. Further study of binding constants determination and protein binding competitions was carried out. The study proves that the LPC technique could be used for complex mrdia, particularly the matrix of protein coexisting with a variety of dmgs.

Effect of beta-glycyrrhizinate on eye mucosa absorption of drugs

Dipotassium beta-glycyrrhizinate (GK2) is a saponin originated from "kanzo" plant. We studied such two functions of GK2 as a drug carrier and a penetration enhancer on the eye mucosa. The interactions of GK2 with various drugs were investigated using the 1-octanol/water partition method. GK2 increased the partition of cationic drugs, i.e., antihistamines (chlorpheniramine maleate (CM), diphenhydramine hydrochloride (DH)), as well as decongestants (naphazoline hydrochloride (NA), tetrahydrozoline hydrochloride (TH)). The carrier effect of GK2 is remarkable at its concentration above critical miceller concentration (CMC) and, especially at its pH value of between 4 to 5, resulting that transfers of drugs increased 2 to 10 times as compared to drugs without GK2. In vivo experiments were carried out using rats and rabbits. The effect of GK2 on the inhibition efficiency by CM was evaluated using experimental conjunctivitis formed by injection of histamine on rat upper eyelid. The Inhibition efficiency of edema by CM with GK2 was 4 times stronger than that without GK2. Cornea permeability of TH increased 1.8 times by the addition of GK2. These results indicated that GK2 is applicable as a carrier of cationic drugs on the eye mucosa and cornea.

Evaluation of the effects of nasal decongestants with acoustic rhinometry

Acoustic rhinometry is a new method of evaluating the geometrical distributions of the cross-section and volume of the nasal cavity. Its characteristics are that of a nontraumatic procedure requiring minimal time for measurements. Eight males (27-39 years old) without nasal lesions were investigated with acoustic rhinometry before and after unilateral administrations of decongestants. Conventional nasal decongestants such as naphazolin nitrate 0.1% (Privina) and tetrahydrozoline hydrochloride 0.1%, as well as prednisolone 0.02% (Cor-tyzine), were used in solutions diluted 10 or 100 times. As to the method of decongestant application, we adopted the head tilt method, in the successive order of backward, lateral (toward the non-application side) tilt and backward. Each position was maintained for 30 seconds. Minimal cross sectional area of the nasal cavity, and nasal volume were evaluated with acoustic rhinometry. After the application of nasal drops, the minimal cross sectional area increased within 10 minutes, followed by a plateau level for one hour. With the application of nasal decongestants, an I-notch, corresponding to the nasal valve, was unchanged, whereas the C-notch, corresponding to the anterior and of the inferior turbinate, often shifted upwards. Thus, the minimal cross sectional area changed from an I-notch to a C-notch location. The volume of the nasal cavity increased within 10 minutes, and maintained a plateau level for one hour which was similar to that of the minimal cross sectional area. Changes in the ratio of the minimal cross sectional area were greater for less diluted solutions. Changes in the ratio of the nasal cavity were similar to those of the minimal cross sectional area.

Structure of tetrahydrozoline hydrochloride

Structure of tetrahydrozoline hydrochloride

Simultaneous high-performance liquid chromatographic determination of antazoline phosphate and tetrahydrozoline hydrochloride in ophthalmic solution

A method for the determination of 2-[(N-phenyl)ben2ylammomethyl]-2-imidazoline · H 3PO 4 (antazoline phosphate) and 2-(1,2,3,4-tetrahydro-1-naphthyl)-2-imidazoline · HCl (tetrahydrozoline hydrochloride) in ophthalmic solution is described. The pharmaceutical preparation is analysed directly by reversed-phase ion-pair high-performance liquid chromatography and the method is very rapid, selective and simple.

Stability-indicating determination of tetrahydrozoline hydrochloride in ophthalmic solutions by high-performance liquid chromatography

Stability-indicating determination of tetrahydrozoline hydrochloride in ophthalmic solutions by high-performance liquid chromatography

Effects of topical nasal decongestants on the cilia of a chicken embryo tracheal organ culture system.

There is little physiologic data concerning the possible toxicity of nasal decongestants on respiratory cilia. Consequently, a chicken embryo tracheal organ culture system was employed to study the effect on ciliary activity of various preparations and concentrations of the following medications: tetrahydrozoline hydrochloride (Tyzine), xylometazoline hydrochloride (Otrivin), Dristan, Sinex, NTZ oxymetazoline hydrochloride (Afrin), naphazoline hydrochloride (Privine), and phenylephrine (Neosynephrine). Only two dilutions of injectable phenylephrine 0.25% and 0.10% produced essentially no ciliotoxicity when compared to the cilia in control cultures. All the other topical nasal medications in the concentrations tested possessed some toxicity for cilia. The use of these medications should be tempered with the warning of possible cilia damage.

Nose-Drop Intoxication In an Infant

To the Editor:— Naphazoline (Privine) hydrochloride, tetrahydrozoline hydrochloride (Tyzine), oxymetazoline hydrochloride (Afrin), and xylometazoline (Otrivin) hydrochloride are potent vasoconstrictors used to relieve nasal stuffiness. The other major effect of these drugs is depression of the central nervous system. Several years ago,LETTERS TO THE EDITORinThe Journalreminded physicians of possible harmful side effects of this class of drugs in infants and small children. 1,2 A recent experience with xylometazoline nose drops demonstrates the importance of keeping this warning in mind. Report of a Case:— A 1-month-old Negro male infant was seen in the pediatric clinic at Martin Army Hospital, Ft. Benning, Ga. The patient exhibited poor responsiveness and gasping respirations. He was rushed to the ward with the initial impression of meningitis, encephalitis, or severe pneumonia. Physical examination, laboratory studies including salicylate level and spinal fluid examination, and chest x-ray film failed to reveal any specific abnormality. The

Therapeutic Experiences with Cor-Tyzine (Tetrahydrozoline Hydrochloride+Predonisolone) Nasal Solution in Several Diseases of Naso-Antral Regions

Nasal solution of Cor-Tyzine which consists mostly of Tetrahydrozolin hydrochloride that has a powerful anti-hyperemic effect on the mucous membrane and Predonisolone which is prominently anti-inflammatory and anti-allergic was used in the treatment of several diseases of the naso-antral regions, getting the following results.1) In the patients with chronic catarrhal rhinitis, the ciliated epithelial cells of the mucous membrane of the nasal cavity were noted so improved at 30 days after the use of the nasal solution as to be nearly the same as the ciliated epithelial cells of the mucous membrane of the nasal cavity in normal subjects.2) In the patients with chronic catarrhal rhinitis, hypertrophic rhinitis, acute catarrhal rhinitis, and allergic rhinitis, the results of use. of Cor-Tyzine were very good. In the patients with chronic sinusitis, the drug produced little or no improvements in objective signs but improved subjective 'symtoms to some extent. In the patients with post-operative chronic sinusitis, too, the drug was found to be worthy of use.3) Scarcely any side effect was observed except that 2 or 3 cases complained of a bitter taste at the naso-pharyngeal region and another case had nasal discharge and sneezing gradually after the nasal instillation of the drug. Those side effects which are generally known to be peculiar to adrenal cortical hormone did not occur at all following the administration of Cor-Tyzine. The therapeutic experiences with the drug have made us presume that it is suitable for administration over long periods of time.

Tetrahydrozoline hydrochloride solutions

Dr. A. J. Spiegel and C. F. Gerber concisely reveal the results of extensive compatibility studies made with the active ingredient of Tyzine nasal sol'Ut£ ons and V isine eye drops

New ophthalmic decongestant, tetrahydrozoline hydrochloride; clinical use in 1,156 patients with conjunctival irritation.

Tetrahydrozoline hydrochloride is a sympathomimetic agent which causes local vasoconstriction when topically applied and a rise of blood pressure when given systemically. Instilled as a 0.05% solution into the eye, it was found to afford prompt relief, lasting from one to four hours, from the congestion accompanying allergic or chronic conjunctivitis. It was administered in doses of a single drop instilled into each eye two to four times daily in 1,156 patients with these conditions. This dose, while sufficient to give the desired relief in the majority of patients, had no side-effects beyond a mild, transient irritation. It did not raise the intraocular pressure and had no adverse effects when used for periods up to two years in patients with cataracts. There was no evidence that it affected the course of cataract or hindered recovery from chronic conjunctivitis or from the subacute stage of acute conjunctivitis.

Severe respiratory depression following nasalinstillation of tetrahydrozoline hydrochloride

Summary A case of severe respiratory depressionfollowing the nasal instillation of tetrahydrozoline hydrochloride nose drops in a 10-week-old boy is described. The pharmacology and toxicology of this drug and related compounds are briefly discussed. Caution is advised in the administration of this medication to infants.

Clinical trial of tetrahydrozoline hydrochloride; a valuable new nasal decongestant.

This report presents details of a clinical trial of tetrahydrozoline hydrochloride (Tyzine), a new sympathomimetic agent useful in 0.1% aqueous solution as a topical vasoconstrictor and nasal decongestant. The effectiveness of tetrahydrozoline, as measured by its promptness of action, degree of relief provided, and the percentage of patients benefited, is superior. The decongestive action of tetrahydrozoline is notably prolonged, so that instillations every four to eight hours, or at longer intervals in some cases, are sufficient to maintain continuous relief; instillation at bedtime provides relief that carries through the night. Tetrahydrozoline is also free of both local and systemic side-effects. BACKGROUND Pharmacologic tests with tetrahydrozoline, which is designated chemically as 2-(1,2,3, 4-tetrahydro-1-naphthyl) imidazoline hydrochloride, suggested that this recently synthesized compound should prove highly effective and free of the disadvantages of its predecessors. The structural formula of tetrahydrozoline is as follows: Tetrahydrozoline consists structurally of an aromatic nucleus and a side radical