Chronomodulated drug delivery system of Montelukast sodium 

By N. Kanaka Durga Devi, B.Sai Mrudula, A.Prameela Rani 


Many drugs have disadvantages like first pass metabolism, peak and valley absorptions at different absorption sites and drug instability problems. Pulsatile drug delivery systems (PDDS) are gaining interest as they can curtail most of the above mentioned disadvantages. Besides that, we can deliver the drug based on time dependent or site dependent theories as per requirement of the therapy. We can also treat those diseases which show dependency on chronopharmacology. Nocturnal asthma (NA) is one of such diseases that follow circadian rhythms where increasing of air way resistance and worsening of lung function is observed during the early morning time. So, in this research work we have done formulation and evaluation of simple orally applicable one pulse drug delivery system based on press coated tablet preparation taking Montelukast sodium as our drug molecule which have certain disadvantages like first pass metabolism and differences in absorption at different sites.  This helps in obtaining worthy effects in treating NA as well as to curtail extensive first pass metabolism of the drug. Here first we have prepared (F1-F9) core tablet formulations. We have selected primojel, Ac-di-sol and polyplasdoneXL10 as swelling polymers in the core tablet composition and we have optimized F8 formulation with 7.5% polyplasdoneXL10 as the best immediate release core tablet. It accommodates a helping hand in obtaining burst release of the drug. The lag time was maintained by press coating the core tablets with barrier layer. Among the different barrier compositions from(X1-X12), X12 was found to show single pulse drug delivery with considerable drug release for 2 hrs after maintaining the pre expected 5 ½ hrs lag time. 

Keywords: Pulsatile drug delivery systems (PDDS), Nocturnal asthma (NA), Chronopharmacology, Circadian rhythms, Burst release, Lag time.

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