IN-VITRO IN-VIVO STUDIES OF LAMOTRIGINE TABLETS PREPARED BY HOT MELT EXTRUSION TECHNIQUE

Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2014, Vol 6, Issue 11

Abstract

Objective: Present study deals with improvement in dissolution and bioavailability of poorly water soluble Lamotrigine (Lamo), an antiepileptic drug (AED) of phenyltriazine class. Formulation of poorly water soluble drug for oral delivery is one of the biggest challenge. Amongst all the approaches, the novel solid dispersion (SD) technique known as hot melt extrusion (HME) has found to be the most widely used method in improving dissolution and bioavailability.Methods: Dissolution enhancement of Lamo were done by HME technology where crystalline form of API is converted to amorphous form using hydrophilic polymer Kollidon VA64. Plasticizers like Polyethylene glycol (PEG 4000), polyoxyl 35 castor oil (Cremophor EL) and Sorbiton monolaurate (Montane 20PHA) were used. Physical blends of drug, polymer and plasticizer were prepared in the ratio of 1:1:0.1. These physical mixtures were subjected to melt and the resultant formulations were subjected to physical characterization, dissolution, permeability and in vivo testing. Pharmacokinetics of Lamo was studied in rats. Drug efflux pump like P-glycoprotein (P-gp) was recognized to posses’ functional role in determining the pharmacokinetics of drugs.Results: Drug release showed the similar profile for all the HME formulations while the permeability studies showed improved permeability of formulations containing Montane 20PHA. In comparison to Non HME, HME formulations showed a significant enhancement in permeability. SD prepared by Cremophor EL resulted in 765.22% enhancement in extent of absorption.Conclusion: HME technology could be a promising formulation approach to enhance the dissolution and bioavailability of Lamo.

Authors and Affiliations

Smita Kolhe, Praveen D. Chaudhari, Dhananjay More

Keywords

Related Articles

STRUCTURE BASED DRUG DESIGNING, SCORING, AND SYNTHESIS OF SOME SUBSTITUTED SULPHONYLUREAS/GUANIDINE -BASED DERIVATIVES AS HYPOGLYCEMIC AGENTS

Objective: The present work deals with the designing, scoring, synthesis and, characterization of 1-(4-(2-(4-Substitutedphenylamino)-2-oxoethyl)phenylsulfonyl)-3-(4-substitutedbenzoyl)urea (5A-5B),1-(4-(2-(4-substitutedp...

CYTOTOXICITY AND ANTIMICROBIAL PROPERTIES OF NEEM (AZADIRACHTA INDICA) LEAF EXTRACTSCYTOTOXICITY AND ANTIMICROBIAL PROPERTIES OF NEEM (AZADIRACHTA INDICA) LEAF EXTRACTS

Objective: This study was conducted to evaluate the biological properties of Neem (Azadirachtaindica) leaves in terms of its cytotoxic and antimicrobial activities.Methods: The antimicrobial activity of A. indica leaf ex...

STUDY ON THE INTERACTION OF AMITRIPTYLINE HYDROCHLORIDE AND MALONIC ACID BY SPECTROPHOTOMETRIC AND SPECTROFLUORIMETRIC METHODS IN TABLETS: APPLICATION TO CONTENT UNIFORMITY TESTING

Objective: The objective of this research to study the interaction between amitriptyline hydrochloride in drug products via reaction with mixed acids anhydrides: Application to Content Uniformity Testing.Methods: Malonic...

A NEW STABILITY INDICATING UPLC METHOD DEVELOPMENT AND VALIDATION FOR THE SIMULTANEOUS ESTIMATION OF DULOXETINE AND MECOBALAMIN IN BULK AND IN ITS DOSAGE FORMS

Objective: The objective of the work is to develop and validate a stability indicating, new, simple, highly sensitive RP-UPLC method for simultaneous estimation of Duloxetine and Mecobalamin in bulk and in its dosage for...

GREEN SYNTHESIS AND EVALUATION OF BIOLOGICAL IMPACT OF Zn(II), Cd(II) AND Hg(II) COMPLEXES WITH PHENYLACETYLUREA AND BUTANOATE ION LIGANDS

Objective: To prepare Zn(II), Cd(II) and Hg(II) complexes containing Phenylacetyl urea (PAU), and butanoate (but) ligands and to characterize physic-chemical, spectral and biological properties.Methods: All the three met...

Download PDF file
  • EP ID EP579262
  • DOI -
  • Views 43
  • Downloads 0

How To Cite

Smita Kolhe, Praveen D. Chaudhari, Dhananjay More (2014). IN-VITRO IN-VIVO STUDIES OF LAMOTRIGINE TABLETS PREPARED BY HOT MELT EXTRUSION TECHNIQUE. International Journal of Pharmacy and Pharmaceutical Sciences, 6(11), 65-70. https://europub.co.uk/articles/-A-579262