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Preparation and evaluation of once-daily sustained-release coated tablets of tolterodine-L-tartrate.
Int J Pharm. 2014 Jan 02; 460(1-2):205-11.IJ

Abstract

In this study, once-daily, sustained-release matrix tablets of tolterodine l-tartrate (TOL) for treatment of overactive bladder (OAB) were prepared by direct compression using various amounts of hydrophilic polymers such as HPMC 2910 and HPMC 2208 along with other tablet excipients; the tablets were then coated. In vitro dissolution studies were carried out under different pH conditions. The dissolution data were fitted into zero-order, first-order, Higuchi and Korsemeyer-Peppas models to identify the pharmacokinetics and mechanism of drug release. Among the four formulations (F1-F4), the dissolution profiles of formulation F2 were most similar to the marketed product with similarity and difference factors of 70.25 and 1.59 respectively. Furthermore, pharmacokinetic studies were carried out in healthy human volunteers after oral administration of the prepared TOL sustained-release matrix-coated tablet and the marketed product. The results revealed that the pharmacokinetic parameters of AUC, Cmax, Tmax, t1/2, Kel, and MRT of TOL for the developed formulation (F2) were not significantly different from that for the marketed product, suggesting that they were bioequivalent. Therefore, the developed sustained-release tablet formulation of TOL could be an alternative dosage form to the SR capsule for treatment of OAB.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Pradhan R
College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, Republic of Korea.
Kim YI
College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, Republic of Korea.
Chang SW
Research Laboratory, Dong-A Pharmaceutical Co., Ltd., 47-5, Sanggal, Kiheung, Yongin, Kyunggi 449 905, Republic of Korea.
Kim JO
College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, Republic of Korea. Electronic address: jongohkim@yu.ac.kr.

MeSH

Benzhydryl CompoundsCelluloseCresolsCross-Over StudiesDelayed-Action PreparationsDrug Administration ScheduleDrug CompoundingExcipientsFatty AcidsHardnessHumansHypromellose DerivativesMethylcellulosePhenylpropanolamineSolubilityTabletsTherapeutic EquivalencyTolterodine TartrateUrological Agents

Pub Type(s)

Clinical Trial
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24184032

Citation

Pradhan, Roshan, et al. "Preparation and Evaluation of Once-daily Sustained-release Coated Tablets of Tolterodine-L-tartrate." International Journal of Pharmaceutics, vol. 460, no. 1-2, 2014, pp. 205-11.
Pradhan R, Kim YI, Chang SW, et al. Preparation and evaluation of once-daily sustained-release coated tablets of tolterodine-L-tartrate. Int J Pharm. 2014;460(1-2):205-11.
Pradhan, R., Kim, Y. I., Chang, S. W., & Kim, J. O. (2014). Preparation and evaluation of once-daily sustained-release coated tablets of tolterodine-L-tartrate. International Journal of Pharmaceutics, 460(1-2), 205-11. https://doi.org/10.1016/j.ijpharm.2013.10.040
Pradhan R, et al. Preparation and Evaluation of Once-daily Sustained-release Coated Tablets of Tolterodine-L-tartrate. Int J Pharm. 2014 Jan 2;460(1-2):205-11. PubMed PMID: 24184032.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation and evaluation of once-daily sustained-release coated tablets of tolterodine-L-tartrate. AU - Pradhan,Roshan, AU - Kim,Yong-Il, AU - Chang,Sun Woo, AU - Kim,Jong Oh, Y1 - 2013/10/29/ PY - 2013/08/12/received PY - 2013/10/07/revised PY - 2013/10/17/accepted PY - 2013/11/5/entrez PY - 2013/11/5/pubmed PY - 2014/9/10/medline KW - HPMC KW - Matrix tablet KW - Pharmacokinetics KW - Sustained release KW - Tolterodine l-tartrate SP - 205 EP - 11 JF - International journal of pharmaceutics JO - Int J Pharm VL - 460 IS - 1-2 N2 - In this study, once-daily, sustained-release matrix tablets of tolterodine l-tartrate (TOL) for treatment of overactive bladder (OAB) were prepared by direct compression using various amounts of hydrophilic polymers such as HPMC 2910 and HPMC 2208 along with other tablet excipients; the tablets were then coated. In vitro dissolution studies were carried out under different pH conditions. The dissolution data were fitted into zero-order, first-order, Higuchi and Korsemeyer-Peppas models to identify the pharmacokinetics and mechanism of drug release. Among the four formulations (F1-F4), the dissolution profiles of formulation F2 were most similar to the marketed product with similarity and difference factors of 70.25 and 1.59 respectively. Furthermore, pharmacokinetic studies were carried out in healthy human volunteers after oral administration of the prepared TOL sustained-release matrix-coated tablet and the marketed product. The results revealed that the pharmacokinetic parameters of AUC, Cmax, Tmax, t1/2, Kel, and MRT of TOL for the developed formulation (F2) were not significantly different from that for the marketed product, suggesting that they were bioequivalent. Therefore, the developed sustained-release tablet formulation of TOL could be an alternative dosage form to the SR capsule for treatment of OAB. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/24184032/Preparation_and_evaluation_of_once_daily_sustained_release_coated_tablets_of_tolterodine_L_tartrate_ DB - PRIME DP - Unbound Medicine ER -