Journal: JPR:BioMedRx:An International Journal

Article Id: JPRS-Ph-0000264
Title: Formulation and Physical Characterization of Microcrystals for Dissolution Rate Enhancement of Telmisartan
Category: Pharmaceutics
Section: Research Article
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    Telmisartan is a potent, long-lasting, nonpeptide antagonist of the angiotensin II type-1(AT1) receptor that is indicated for the treatment of essential hypertension. Telmisartan is practically insoluble in water and its dissolution is the rate-limiting step for its absorption, which leads to variable bioavailability. The aim of this investigation was to enhance the dissolution rate of Telmisartan by formation of microcrystals using solvent change method. The in-situ micronization process was carried out using solvent change method in the presence of Polyvinylpyrrolidone (PVP) as a stabilizing agent that limits the size of the particles generated. Telmisartan was dissolved in methanol and the stabilizing agent in water (as a non-solvent). The non-solvent was poured rapidly into the drug solution under stirring by a magnetic stirrer, and the resultant was oven-dried. Microcrystals were characterized by optical microscopy, SEM, FTIR, XRD and in vitro powder dissolution study. Telmisartan microcrystals showed narrow particle size and change in crystalline shape from avicular shape. FTIR results showed no interaction between the drug and the stabilizer. XRD diffractograms of microcrystals showed smaller peak height than untreated Telmisartan indicates that crystal habit modification occurred in the microcrystals without any polymorphic changes. Negative Gibb’s free energy change represented spontaneous solubility of microcrystals. Dissolution efficiency of Telmisartan microcrystals at 15 min (DE15%) was increased about 9 times. Microcrystals were found to have good flow property.

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    Author(s) Name:

    Sachin Namdeo Kothawade*, Amit Subhashchand Lunkad, Ujwala Ramesh Bagmar, Ashwini N. Panmand

    Affiliation(s) Name:

    SCSSS’s Sitabai Thite College of Pharmacy, Shirur (Ghodnadi),Pune-412 210, India

    *Corresponding author.
    Sachin Namdeo Kothawade
    SCSSS’s Sitabai Thite College of Pharmacy,
    Shirur (Ghodnadi),
    Pune-412 210, India


    Received on:18-10-2012; Revised on: 22-11-2012; Accepted on:26-01-2013

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    Author:

    Sachin Namdeo Kothawade*, Amit Subhashchand Lunkad, Ujwala Ramesh Bagmar, Ashwini N. Panmand

    Title:Formulation and Physical Characterization of Microcrystals for Dissolution Rate Enhancement of Telmisartan
    Journal:JPR:BioMedRx:An International Journal
    Vol(issue):1 (February)
    Year:2013
    Page No: (188-194)
  • Experimental Methods Keywords

    Methodology:Solvent change method, Dissolution efficiency.
    Research Materials:Telmisartan

Keywords

Telmisartan Microcrystal Solvent change method Dissolution efficiency.

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