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Formulation study and drug release mechanism of a new theophylline sustained-release preparation.
Int J Pharm. 2005 Nov 04; 304(1-2):91-101.IJ

Abstract

Two matrix theophylline tablets with different release mechanisms were compared. Tablet A was a swelling/disintegration-type wax matrix made of hydrophobic wax granules, consisting of stearic acid, hydrogenated oil and glycerol esters of fatty acids, and hydrophilic polymer granules composed primarily of hydroxypropyl methylcellulose (HPMC). We named Tablet A the cluster tablet. Tablet B was a gel matrix made of hydrophobic ethylcellulose granules, consisting of ethylcellulose and hydrogenated oil, and hydrophilic polymer granules consisting of HPMC and hydroxylpropylmethylcellulose acetate succinate (HPMCAS). The formulations were screened in vitro according to their dissolution characteristics. The drug release from each preparation was analyzed using release kinetics theories. In Tablet A, the value of the exponent(n) representing the apparent diffusion mechanism determined from the Korsmeyer-Peppas model equation was about 0.6 and was unlikely to be affected by the rotation speed. In Tablet B, the value of the exponent(n) by the Korsmeyer-Peppas model equation changed with the paddle rotation speed. These results suggested that the drug release mechanism of Tablet B is greatly affected by the extent of physical force in the gastrointestinal tract.

Authors+Show Affiliations

Hayashi T
Central Research Laboratories, SSP Co., Ltd., Nanpeidai 1143, Narita-shi, Chiba, and School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Shizuoka-shi, Shizuoka 422-8526, Japan. Tetsuo.Hayashi@ssp.co.jp
Kanbe H
No affiliation info available
Okada M
No affiliation info available
Suzuki M
No affiliation info available
Ikeda Y
No affiliation info available
Onuki Y
No affiliation info available
Kaneko T
No affiliation info available
Sonobe T
No affiliation info available

MeSH

Delayed-Action PreparationsDrug CompoundingExcipientsKineticsPolymersSolubilityTabletsTheophylline

Pub Type(s)

Journal Article

Language

eng

PubMed ID

16154302

Citation

Hayashi, Tetsuo, et al. "Formulation Study and Drug Release Mechanism of a New Theophylline Sustained-release Preparation." International Journal of Pharmaceutics, vol. 304, no. 1-2, 2005, pp. 91-101.
Hayashi T, Kanbe H, Okada M, et al. Formulation study and drug release mechanism of a new theophylline sustained-release preparation. Int J Pharm. 2005;304(1-2):91-101.
Hayashi, T., Kanbe, H., Okada, M., Suzuki, M., Ikeda, Y., Onuki, Y., Kaneko, T., & Sonobe, T. (2005). Formulation study and drug release mechanism of a new theophylline sustained-release preparation. International Journal of Pharmaceutics, 304(1-2), 91-101.
Hayashi T, et al. Formulation Study and Drug Release Mechanism of a New Theophylline Sustained-release Preparation. Int J Pharm. 2005 Nov 4;304(1-2):91-101. PubMed PMID: 16154302.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation study and drug release mechanism of a new theophylline sustained-release preparation. AU - Hayashi,Tetsuo, AU - Kanbe,Hideyoshi, AU - Okada,Minoru, AU - Suzuki,Makoto, AU - Ikeda,Yasuo, AU - Onuki,Yoichi, AU - Kaneko,Tetsuo, AU - Sonobe,Takashi, Y1 - 2005/09/08/ PY - 2005/02/03/received PY - 2005/07/26/revised PY - 2005/07/27/accepted PY - 2005/9/13/pubmed PY - 2006/1/25/medline PY - 2005/9/13/entrez SP - 91 EP - 101 JF - International journal of pharmaceutics JO - Int J Pharm VL - 304 IS - 1-2 N2 - Two matrix theophylline tablets with different release mechanisms were compared. Tablet A was a swelling/disintegration-type wax matrix made of hydrophobic wax granules, consisting of stearic acid, hydrogenated oil and glycerol esters of fatty acids, and hydrophilic polymer granules composed primarily of hydroxypropyl methylcellulose (HPMC). We named Tablet A the cluster tablet. Tablet B was a gel matrix made of hydrophobic ethylcellulose granules, consisting of ethylcellulose and hydrogenated oil, and hydrophilic polymer granules consisting of HPMC and hydroxylpropylmethylcellulose acetate succinate (HPMCAS). The formulations were screened in vitro according to their dissolution characteristics. The drug release from each preparation was analyzed using release kinetics theories. In Tablet A, the value of the exponent(n) representing the apparent diffusion mechanism determined from the Korsmeyer-Peppas model equation was about 0.6 and was unlikely to be affected by the rotation speed. In Tablet B, the value of the exponent(n) by the Korsmeyer-Peppas model equation changed with the paddle rotation speed. These results suggested that the drug release mechanism of Tablet B is greatly affected by the extent of physical force in the gastrointestinal tract. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/16154302/Formulation_study_and_drug_release_mechanism_of_a_new_theophylline_sustained_release_preparation_ DB - PRIME DP - Unbound Medicine ER -