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Acta Pharmaceutica

The Journal of Croatian Pharmaceutical Society

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1846-9558
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Volume 62, Issue 1 (Mar 2012)

Issues

Formulation and evaluation of delayed-onset extended-release tablets of metoprolol tartrate using hydrophilic-swellable polymers

Subhash Dadarwal
  • Delhi Institute of Pharmaceutical Sciences and Research (Formerly College of Pharmacy), University of Delhi, Pushp Vihar, Sec-III New Delhi-110017, India
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
/ Sarika Madan
  • Delhi Institute of Pharmaceutical Sciences and Research (Formerly College of Pharmacy), University of Delhi, Pushp Vihar, Sec-III New Delhi-110017, India
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
/ Shyam Agrawal
  • Delhi Institute of Pharmaceutical Sciences and Research (Formerly College of Pharmacy), University of Delhi, Pushp Vihar, Sec-III New Delhi-110017, India
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
Published Online: 2012-04-03 | DOI: https://doi.org/10.2478/v10007-012-0003-4

Formulation and evaluation of delayed-onset extended-release tablets of metoprolol tartrate using hydrophilic-swellable polymers

In view of the circadian rhythm of cardiovascular diseases, a delayed-onset extended-release (DOER) formulation of metoprolol tartrate (MT) was prepared. This was achieved through dissolution-guided optimization of the proportion of Methocel K4M and Methocel K15M. Core erosion ratio was greater than 50 %, thereby showing steady release of the drug after the lag time until complete dissolution. Optimized formulation produced a lag phase of 6 h followed by complete release of 98.7 ± 2.1 % in 24 h. Water uptake study revealed that Methocel K15M has lower water uptake (30 ± 1 %) than Methocel K4M (40 ± 2 %) after 24 h. Axial swelling of polymers was higher than swelling in the radial direction. Drug-polymer interaction study precludes any interaction between drug and polymer. Such a drug delivery system may provide a viable alternative for effective management of hypertension and other related disorders. This work also proposes an approach to attain DOER for a hydrophilic drug by using a hydrophilic swellable polymer in press coat.

Priprava i vrednovanje tableta metoprolol tartarata s odgođenim i produljenim oslobađanjem koristeći hidrofilne polimere koji bubre

Vodeći računa o cirkadijanom ritmu kardiovaskularnih bolesti, pripravljene su formulacije metoprolol tartarata (MT) s odgođenim i produljenim oslobađanjem (DOER). Optimizacija je provedena praćenjem oslobađanja pri čemu je mijenjan omjer hidroksipropilmetil celuloza Methocela K4M i Methocela K15M. Erozija obložnog sloja bila je veća od 50 %, što pokazuje ujednačeno oslobađanje ljekovite tvari nakon početne odgođene faze do potpunog oslobađanja. U optimiziranoj formulaciji oslobađanje je započelo nakon 6 h, nakon čega slijedi potpuno oslobađanje (98.7 ± 2.1 %) tijekom 24 h. Nakon 24 h ulazak vode u Methocel K15M bio je manji (30 ± 1 %) nego u Methocel K4M (40 ± 2 %). Aksijalno bubrenje polimera bilo je značajnije nego radijalno bubrenje. Nije zapažena interakcija lijeka i polimera. Opisani sustav za isporuku lijekova može biti korisna alternativa za učinkovitu terapiju hipertenzije i srodnih poremećaja. DOER s ovojnicom od hidrofilnih polimera koji bubre upotrebljiv je i za druge hidrofilne lijekove.

Keywords: metoprolol tartrate; delayed-onset extended-release (DOER); core erosion ratio

Keywords: metoprolol tartarat; odgođeno i produljeno oslobađanje (DOER); erozija ovojnice

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About the article


Published Online: 2012-04-03

Published in Print: 2012-03-01


Citation Information: Acta Pharmaceutica, ISSN (Online) 1846-9558, ISSN (Print) 1330-0075, DOI: https://doi.org/10.2478/v10007-012-0003-4.

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