Abstract
Loratadine is a long acting non-sedating anti-histaminic agent that was developed for the treatment of seasonal allergic rhinitis, whose anti-histaminic action is more effective than the other anti-histaminic drugs available commercially. This project was carried out to prepare an acceptable suspension through studying the release of drug in presence of different types and concentrations of suspending agents such as polysorbate 40, xanthan gum, sodium carboxymethylcellulose (NaCMC), aluminum magnesium silicate (veegum) and sodium alginate. The effects of these suspending agents were studied at pH 1.2 (0.1N HCl) and 37 Ù’C. The results showed that the release rate of loratadine in the presence of these suspending agents was dependent on their types and concentrations. The results showed that loratadine release from the formula prepared from xanthan gum is more than that prepared from other polymers in the following order: Sodium alginate < NaCMC < veegum < xanthan gum. However, elegancy of suspension was better on using xanthan gum in a concentration of 0.5%. The obtained results were utilized to formulate 0.1% suspension of loratadine which is physically stable with an optimum drug release. The rheology, sedimentation volume, resuspendability and expiration date were evaluated for the selected formula. The formula that contains loratadine, xanthan gum, glycerol, sorbitol, methyl paraben, propyl paraben, sodium edetate, raspberry flavor at pH 5.0 appears to be a promised formula to be present with estimated shelf life of about 3.8 years.
 Key word: loratadine, suspension, suspending agent, xanthan gum
Highlights
A coarse suspension is a dispersion of finely divided, insoluble solid particles in a fluid [1].A conventional suspension may be readily prepared in an aqueous solution with small percentage of hydrophilic polymers, as well as small percentage of surfactant like polysorbate 80
The results showed that loratadine release from the formula prepared from xanthan gum is more than that prepared from other polymers in the following order: Sodium alginate < NaCMC < veegum < xanthan gum
The suspending agent was used to achieve homogeneity of redispersed suspension while surfactants are used for wetting and dispersing of insoluble particles [2].For many patients, the liquid dosage form is preferred over the solid dosage form of the same drug because of the ease of the swallowing liquids and flexibility in the administration
Summary
A coarse suspension is a dispersion of finely divided, insoluble solid particles (the dispersed phase) in a fluid (dispersion medium or continuous phase) [1].A conventional suspension may be readily prepared in an aqueous solution with small percentage of hydrophilic polymers (like methyl cellulose, hydroxypropylcellulose and xanthan gum), as well as small percentage of surfactant like polysorbate 80. In addition the stability of the drugs when prepared as insoluble particles is higher compared to that of dissolved drug in syrup, as shown by the aminophylline suspension whose chemical and physical stability showed minimum rate of degradation after 91 days period [10]. Loratadine is a tricyclic antihistamine, which has a selective and peripheral H1-antagonist action It has a long-lasting effect and does not normally cause drowsiness because it does not readily enter the cerebro spinal fluid (CSF) [11].It is white to off-white powder, practically insoluble in water, but very soluble in acetone, alcohol and chloroform [12]. Loratadine rapidly absorbed after administration, peak plasma concentration being attained in about 1 hour. It is extensively metabolized; the major metabolite is desloratadine, which has potent antihistamine activity. The elimination t1/2 of loratadine and desloratadine are 8.4 and 28 hours respectively [13]
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Schedule a callMore From: Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)
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