| Molecular Formula : C10H16ClNO
Molecular Weight : 201.69 CAS No. : 345-78-8 Chemical Name: 1. (1S,2S)-2-Methylamino-1-phenyl propan-1-ol, Hydrochloride 2. Benzenemethanol, a-[1-(methylamino)ethyl]-, [S-(R*,R*)], Hydrochloride Synonyms: (+)-PSI-EPHEDRINE HYDROCHLORIDE;PSI-EPHEDRINE HYDROCHLORIDE;PSEUDOEPHEDRINE HCL;PSEUDOEPHEDRINE HCL, (+)-1S,2S-;(+)-PSEUDOEPHEDRINE HYDROCHLORIDE;PSEUDOEPHEDRINE HYDROCHLORIDE;a)]-;alpha-(1-(methylamino)ethyl)-,hydrochloride,(s-(r*,r*))-benzenemethano;benzenemethanol,alpha-[1-(methylamino)ethyl]-,hydrochloride,[s-(theta,thet;hydrochloride,l-(+)-pseudoephedrin;l(+)- pseudoephedrinehydrochloride;novafed;sinufed;sudafed;symptom2;tussaphed;D-PSEUDOEPHEDRINE HYDROCHLORIDE;D-ISOEPHEDRINE HYDROCHLORIDE;ISOEPHEDRINE HYDROCHLORIDE;(1S,2S)-2-(METHYLAMINO)-1-PHENYL-1-PROPANOL HYDROCHLORIDE Specifications :
Therapeutic indications : Decongestant Packing : Packed in double lined polyethylene bags in 25 kg fiber drums. Storage : Store below 35°C.
|
Unlike antihistamines, which relieve multiple allergic symptoms by acting as antagonists at histamine receptors, pseudoephedrine primarily relieves nasal congestion commonly associated with colds or allergies.
The advantage of oral pseudoephedrine over topical nasal preparations, such as oxymetazoline, is that it does not cause rebound congestion (rhinitis medicamentosa); however, it is more likely to cause adverse effects including hypertension.
Pseudoephedrine is being phased out as an over-the-counter drug in some countries and replaced by less effective.
Chemistry
Pseudoephedrine is a phenethylamine, and a diastereomer of ephedrine. Pseudoephedrine is a chiral molecule, meaning it occurs in both "left-handed" and "right-handed" configurations which are not superimposable.
Pseudoephedrine is the International Nonproprietary Name (INN) of the (1S,2S)- diastereomer of ephedrine (which has 1R,2S- configuration). Other names are (+)-pseudoephedrine and D-pseudoephedrine.
L-Pseudoephedrine, also known as (-)-(1R,2R)-pseudoephedrine or (-)-pseudoephedrine, is the optical isomer of D-pseudoephedrine. It has fewer side-effects, fewer central nervous system (CNS) stimulatory effects, does not reduce to D-methamphetamine (which is the enantiomer used as a recreational drug), and yet it retains its efficacy as a decongestant.[citation needed] However, the patent holder for L-pseudoephedrine (Pfizer/Warner-Lambert)[has not yet sought or received government approval for its sale to the public.
Clinical uses
Indications
Pseudoephedrine is indicated for the treatment of:
* nasal congestion
* sinus congestion
* Eustachian tube congestion.
Pseudoephedrine is also indicated for vasomotor rhinitis, and as an adjunct to other agents in the optimum treatment of allergic rhinitis, croup, sinusitis, otitis media, and tracheobronchitis.
Adverse effects
Common adverse drug reactions (ADRs) associated with pseudoephedrine therapy include: CNS stimulation, sleeplessness, nervousness, excitability, dizziness and anxiety. Infrequent ADRs include: tachycardia and/or palpitations. Rarely, pseudoephedrine therapy may be associated with hallucinations, arrhythmias, hypertension, seizures and ischemic colitis;as well as severe skin reactions known as recurrent pseudo-scarlatina, systemic contact dermatitis, and nonpigmenting fixed drug eruption.Pseudoephedrine, particularly in high doses, may also cause episodes of paranoid psychosis.It has also been reported that pseudoephedrine, amongst other sympathomimetic agents, may be associated with the occurrence of stroke.
A reversed phase high performance liquid chromatographic method has been developed using Shimadzu HPLC-VP series, LC-10 ATV pump, SPD10 AVP and C8 column, for simultaneous determination of pseudoephedrine hydrochloride and cetrizine hydrochloride in three marketed tablet formulations (extended release). The mobile phase consists of phosphate buffer of pH 7.0 and acetonitrile HPLC grade in the ratio of 1:1. The flow rate was maintained at 1 ml/min and the ultraviolet detection was done at 242 nm, which is the isosbestic point. Linearity coefficients, assay values, recovery studies and repeatability studies showed that the method is accurate and precise.
Pseudoephedrine hydrochloride (PEH) is official in IP. Cetrizine hydrochloride (CEH) is official in BP. Fixed dose combinations of PEH and CEH are widely used for the symptomatic treatment of allergic rhinitis. Many methods have been reported in the literature for the determination of similar formulation with various other drugs using HPLC, HPTLC and spectrophotometry. However, a method for the simultaneous determination of PEH and CEH in tablets by HPLC has not been reported. In this present work, efforts have been made to develop an isocratic method using a simple mobile phase and UV detection for the simultaneous determination of the above drugs.
A high performance liquid chromatographic system from Shimadzu VP series, consisting of LC10 ATV Pump and SPD 10 AVP UV detector, was used for the analysis. C 8 (150´4.6 mm, 5 µ) column was used in the analysis with a flow rate of 1 ml/min. A Rheodyne injector with a 20 µl loop was used for injecting the samples. Ammonium hydrogen phosphate (AR grade) and acetonitrile (HPLC grade) were used for mobile phase preparation. Working reference standards of PEH and CEH were obtained from Dr. Ceeal Analytical Lab, Chennai. Three marketed tablet formulations were selected for the study. The brand names of the tablets are Alerid (batch no. T10593, Cipla Ltd.), Cetrizet (batch no. SK 10893, Sun Pharmaceuticals) and Zyncet (batch no. 14086, Noble Medicure Pvt. Ltd.). Phosphate buffer (20 mM), pH 7.0 and acetonitrile in the ratio 1:1 was used as the mobile phase with a flow rate of 1 ml/min. The HPLC procedure was carried out at an ambient temperature.
A stock solution containing 6 mg/ml of PEH and 250 µg/ml of CEH was prepared. Standard solution containing PEH and CEH was prepared from stock solution by suitable dilution to get a concentration of 3.6 mg/ml and 150 µg/ml respectively.
Twenty tablets were weighed and crushed to a fine powder. A powder quantity equivalent to 7.5 mg of CEH was weighed and transferred to a 50 ml volumetric flask. The powder was dissolved in water by shaking for 15 min, filtered and then made up to the mark with mobile phase. Dilutions were made to get the concentration of 3.6 mg/ml of PEH and 150 µg/ml of CEH. A volume of 20 µl each of standard and sample solutions was injected into the stabilized HPLC system. Detection was kept at 242 nm, which is the isobestic point. The retention times of PEH and CEH were found to be 5.59 min and 3.57 min respectively. The chromatogram of PEH and CEH is given in . The respective peak areas of standard and sample for each ingredient were used for quantification.
The assays were carried out by the proposed method, and the results are tabulated in . Accuracy of the method was established by performing recovery studies. The study was carried out by spiking the known concentration of the samples with active ingredients at three levels (20, 40, 60 µg/ml for PEH and 2, 4, 6 µg/ml for CEH), and the results are tabulated in . Linearity and range of the method was carried out by injecting five mixed standard solutions containing 1.2 to 6 mg/ml of PEH and 50 to 250 µg/ml of CEH. The calibration curves were plotted using peak area vs concentration. Linearity coefficients obtained are given in . Precision of the method was demonstrated by repeatability studies. This was assessed by using nine determinations for each tablet (3 concentrations/3 replicates each) covering the specified range for the procedure. Percentage RSD was calculated and given in . The system suitability studies were carried out to determine resolution factor, symmetry factor and precision of the instrument. Results are tabulated in . This systematic study revealed that the proposed method for the simultaneous determination of PEH and CEH is simple, sensitive, and with good precision and accuracy. This method can be used for the routine determination of pseudoephedrine hydrochloride and cetrizine hydrochloride simultaneously.
No comments:
Post a Comment