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Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent.
Int J Pharm. 2015 Jul 15; 489(1-2):210-7.IJ

Abstract

To prolong the residence time of dosage forms within gastrointestinal trace until all drug released at desired rate was one of the real challenges for oral controlled-release drug delivery system. Herein, we developed a fine floating tablet via compression coating of hydrophilic polymer (hydroxypropyl cellulose) combined with effervescent agent (sodium bicarbonate) to achieve simultaneous control of release rate and location of ofloxacin. Sodium alginate was also added in the coating layer to regulate the drug release rate. The effects of the weight ratio of drug and the viscosity of HPC on the release profile were investigated. The optimized formulations were found to immediately float within 30s and remain lastingly buoyant over a period of 12 h in simulated gastric fluid (SGF, pH 1.2) without pepsin, indicating a satisfactory floating and zero-order drug release profile. In addition, the oral bioavailability experiment in New Zealand rabbits showed that, the relative bioavailability of the ofloxacin after administrated of floating tablets was 172.19%, compared to marketed common release tablets TaiLiBiTuo(®). These results demonstrated that those controlled-released floating tables would be a promising gastro-retentive delivery system for drugs acting in stomach.

Authors+Show Affiliations

Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China.Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China.Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China.Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China.Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China.Key Laboratory of Modern Chinese Medicines, China Pharmaceutical University, Nanjing 210009, PR China; Yangtze River Pharmaceutical Group, State Key Laboratory for Advanced Formulation Technologies, Taizhou 225300, PR China. Electronic address: zhenghongwu66@cpu.edu.cn.

Pub Type(s)

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

Language

eng

PubMed ID

25956047

Citation

Qi, Xiaole, et al. "Floating Tablets for Controlled Release of Ofloxacin Via Compression Coating of Hydroxypropyl Cellulose Combined With Effervescent Agent." International Journal of Pharmaceutics, vol. 489, no. 1-2, 2015, pp. 210-7.
Qi X, Chen H, Rui Y, et al. Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent. Int J Pharm. 2015;489(1-2):210-7.
Qi, X., Chen, H., Rui, Y., Yang, F., Ma, N., & Wu, Z. (2015). Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent. International Journal of Pharmaceutics, 489(1-2), 210-7. https://doi.org/10.1016/j.ijpharm.2015.05.007
Qi X, et al. Floating Tablets for Controlled Release of Ofloxacin Via Compression Coating of Hydroxypropyl Cellulose Combined With Effervescent Agent. Int J Pharm. 2015 Jul 15;489(1-2):210-7. PubMed PMID: 25956047.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent. AU - Qi,Xiaole, AU - Chen,Haiyan, AU - Rui,Yao, AU - Yang,Fengjiao, AU - Ma,Ning, AU - Wu,Zhenghong, Y1 - 2015/05/05/ PY - 2015/01/27/received PY - 2015/04/13/revised PY - 2015/05/04/accepted PY - 2015/5/10/entrez PY - 2015/5/10/pubmed PY - 2016/3/2/medline KW - Compression coating KW - Floating tablets KW - Hydroxypropyl cellulose KW - Ofloxacin KW - Sodium alginate KW - Zero-release SP - 210 EP - 7 JF - International journal of pharmaceutics JO - Int J Pharm VL - 489 IS - 1-2 N2 - To prolong the residence time of dosage forms within gastrointestinal trace until all drug released at desired rate was one of the real challenges for oral controlled-release drug delivery system. Herein, we developed a fine floating tablet via compression coating of hydrophilic polymer (hydroxypropyl cellulose) combined with effervescent agent (sodium bicarbonate) to achieve simultaneous control of release rate and location of ofloxacin. Sodium alginate was also added in the coating layer to regulate the drug release rate. The effects of the weight ratio of drug and the viscosity of HPC on the release profile were investigated. The optimized formulations were found to immediately float within 30s and remain lastingly buoyant over a period of 12 h in simulated gastric fluid (SGF, pH 1.2) without pepsin, indicating a satisfactory floating and zero-order drug release profile. In addition, the oral bioavailability experiment in New Zealand rabbits showed that, the relative bioavailability of the ofloxacin after administrated of floating tablets was 172.19%, compared to marketed common release tablets TaiLiBiTuo(®). These results demonstrated that those controlled-released floating tables would be a promising gastro-retentive delivery system for drugs acting in stomach. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/25956047/Floating_tablets_for_controlled_release_of_ofloxacin_via_compression_coating_of_hydroxypropyl_cellulose_combined_with_effervescent_agent_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(15)00417-2 DB - PRIME DP - Unbound Medicine ER -