Application of Design of Experiment for Polyox and Xanthan Gum Coated Floating Pulsatile Delivery of Sumatriptan Succinate in Migraine Treatment

Abstract

Migraine follows circadian rhythm in which headache is more painful at the awakening time. This needs administration of dosage form at night time to release drug after lag period when pain gets worse. Sumatriptan succinate is a drug of choice for migraine. Sumatriptan succinate has bitter taste, low oral bioavailability, and shorter half-life. Present work deals with application of design of experiment for polyox and xanthan gum in development of press coated floating pulsatile tablet. Floating pulsatile concept was applied to increase gastric residence of the dosage form. Burst release was achieved through immediate release tablet using crospovidone as superdisintegrant (10%). Pulse lag time was achieved using swellable polymer polyox WSR 205 and xanthan gum. 32 experimental design was applied. Optimized formulation was evaluated for physical characteristics and in-vitro and in-vivo study. From results, it can be concluded that optimized batch F8 containing polyox WSR205 (72.72%) and xanthan gum (27.27%) of total weight of polymer has shown floating lag time of 55 ± 2 sec, drug content of 100.35 ± 0.4%, hardness of 6 ± 0.1 Kg/cm2, and 98.69 ± 2% drug release in pulse manner with lag time of 7 ± 0.1 h. Optimized batch showed prolong gastric residence which was confirmed by in-vivo X-ray study.

Timing in drug absorption and disposition: The past, present, and future of chronopharmacokinetics

“…For example, the existence of higher BP in the late morning or early afternoon, in both normotensive and hypertensive subjects, has been associated with the occurrence of angina pectoris, acute myocardial infarction, or hypertensive crisis (Zhang et al, 2016). Other conditions such as migraine and rheumatoid arthritis also display worse symptoms in morning hours (Hadi, Raghavendra Rao, & Srinivasa Rao, 2016; Jagdale & Pawar, 2014). Therefore, in all these pathologies, it becomes important to ensure an adequate drug delivery at a critical time interval.…”

“…For instance, press‐coated floating tablets were developed for the chronomodulated delivery of sumatriptan, a drug with poor oral bioavailability (14%). A lag time of 7 hr was achieved, allowing drug administration at night and release in the early morning (Jagdale & Pawar, 2014). Previous studies had also pointed towards a higher systemic exposure when sumatriptan was administered in the morning (07.00 hr; Table 3), indicating that drug delivery in this period benefits from time‐dependent PK.…”

Progress in the development of gelling agents for improved culturability of microorganisms

“…Xanthan gum, in combination with chitosan membranes, is used in the treatment of dermo-epidermal wounds (Michel et al, 2003 ; Bellini and Caliari, 2014 ). Various reports suggest its wide range of applications in pharmaceuticals (Gardin and Pauss, 2001 ; Jagdale and Pawar, 2014 ; Kuo et al, 2014 ; Razavi et al, 2014 ) and cosmetic industries (Jianlong and Yi, 1999 ; Jamshidian et al, 2014 ).…”

“…It was derived from a bacterium called Xanthomonas campestris (García-Ochoa et al, 2000 ; Bellini and Caliari, 2014 ). Two other gelling agents came in two successive years: carrageenan in 1977 (Lines, 1977 ; Jagdale and Pawar, 2014 ; Kuo et al, 2014 ; Razavi et al, 2014 ) and gellan gum in 1978 (Nampoothiri et al, 2003 ; Jamshidian et al, 2014 ). Isubgol was proposed as another alternative in the year 1997 (Jansson et al, 1983 ; Jain et al, 1997 ; Harding et al, 2004 ; Fialho et al, 2008 ), which was followed by the latest of its kind guar gum in 2005 (Jain et al, 2005 ; Kirchmajer et al, 2014 ).…”

Circadian Variation of Migraine Attack Onset: A Review of Clinical Studies

“…A better understanding of the circadian variation of migraine attack onset could provide relevant information for migraine prevention and intervention. For example, a pulsatile press coated drug delivery of sumatriptan succinate for bedtime administration was created to ensure early morning release to prevent migraine attacks after sleep [4].…”