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Formulation and evaluation of delayed-onset extended-release tablets of metoprolol tartrate using hydrophilic-swellable polymers.
Acta Pharm. 2012 Mar; 62(1):105-14.AP

Abstract

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.

Authors+Show Affiliations

Delhi Institute of Pharmaceutical Sciences and Research, University of Delhi, New Delhi, India.No affiliation info availableNo affiliation info available

Pub Type(s)

Evaluation Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22472453

Citation

Dadarwal, Subhash Chand, et al. "Formulation and Evaluation of Delayed-onset Extended-release Tablets of Metoprolol Tartrate Using Hydrophilic-swellable Polymers." Acta Pharmaceutica (Zagreb, Croatia), vol. 62, no. 1, 2012, pp. 105-14.
Dadarwal SC, Madan S, Agrawal SS. Formulation and evaluation of delayed-onset extended-release tablets of metoprolol tartrate using hydrophilic-swellable polymers. Acta Pharm. 2012;62(1):105-14.
Dadarwal, S. C., Madan, S., & Agrawal, S. S. (2012). Formulation and evaluation of delayed-onset extended-release tablets of metoprolol tartrate using hydrophilic-swellable polymers. Acta Pharmaceutica (Zagreb, Croatia), 62(1), 105-14. https://doi.org/10.2478/v10007-012-0003-4
Dadarwal SC, Madan S, Agrawal SS. Formulation and Evaluation of Delayed-onset Extended-release Tablets of Metoprolol Tartrate Using Hydrophilic-swellable Polymers. Acta Pharm. 2012;62(1):105-14. PubMed PMID: 22472453.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation and evaluation of delayed-onset extended-release tablets of metoprolol tartrate using hydrophilic-swellable polymers. AU - Dadarwal,Subhash Chand, AU - Madan,Sarika, AU - Agrawal,Shyam Sunder, PY - 2012/4/5/entrez PY - 2012/4/5/pubmed PY - 2012/7/31/medline SP - 105 EP - 14 JF - Acta pharmaceutica (Zagreb, Croatia) JO - Acta Pharm VL - 62 IS - 1 N2 - 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. SN - 1846-9558 UR - https://www.unboundmedicine.com/medline/citation/22472453/Formulation_and_evaluation_of_delayed_onset_extended_release_tablets_of_metoprolol_tartrate_using_hydrophilic_swellable_polymers_ L2 - https://www.degruyter.com/document/doi/10.2478/v10007-012-0003-4 DB - PRIME DP - Unbound Medicine ER -