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Novel taste-masked orally disintegrating tablets for a highly soluble drug with an extremely bitter taste: design rationale and evaluation.
Drug Dev Ind Pharm. 2013 Sep; 39(9):1364-71.DD

Abstract

The purpose of this study was to evaluate the taste masking potential of novel solid dispersions (SDs) using Eudragit® EPO as the excipient when incorporated into the orally disintegrating tablets (ODTs) for delivering a highly soluble drug with an extremely bitter taste. The pyridostigmine bromides (PB) SDs (PBSDs) were prepared by solvent evaporation-deposition method. The physicochemical properties of PBSDs were investigated by means of differential scanning calorimetry and Fourier transformed infrared spectroscopy. The dissolution test showed that only about 8% of PB was released from PBSDs in the simulated salivary fluid in 30 s. Therefore, PBSDs were considered taste-masked and selected for formulation of PBODTs. A central composite design was employed for process optimization. Multiple linear regression analysis for process optimization revealed that the optimal PBODTs were obtained, when the microcrystalline cellulose and crospovidone were 17.16 and 5.55 (%, w/w), respectively, and the average in vivo disintegration time was 25 s. The bitterness threshold of PB was examined by a sensory test, and the threshold value was set as 3 mg in each tablet. Taste evaluation of PBODTs in 18 volunteers revealed considerable taste masking with bitterness below the threshold value. PBODTs also revealed rapid drug release (around 99%, 2 min) in the simulated gastric fluid. The mean PB plasma concentration-time profiles of PBODTs and that of the commercial tablets were comparable, with closely similar pattern. Bioequivalence assessment results demonstrated that PBODTs and the commercial tablets were bioequivalent. In conclusion, PBODTs are prepared successfully, with taste masking and rapid disintegration in the oral cavity.

Authors+Show Affiliations

Department of Thoracic Surgery, Institute of Surgery Research, Daping Hospital, Third Military Medical University, Chongqing, China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

22994163

Citation

Tan, Qunyou, et al. "Novel Taste-masked Orally Disintegrating Tablets for a Highly Soluble Drug With an Extremely Bitter Taste: Design Rationale and Evaluation." Drug Development and Industrial Pharmacy, vol. 39, no. 9, 2013, pp. 1364-71.
Tan Q, Zhang L, Liu G, et al. Novel taste-masked orally disintegrating tablets for a highly soluble drug with an extremely bitter taste: design rationale and evaluation. Drug Dev Ind Pharm. 2013;39(9):1364-71.
Tan, Q., Zhang, L., Liu, G., He, D., Yin, H., Wang, H., Wu, J., Liao, H., & Zhang, J. (2013). Novel taste-masked orally disintegrating tablets for a highly soluble drug with an extremely bitter taste: design rationale and evaluation. Drug Development and Industrial Pharmacy, 39(9), 1364-71. https://doi.org/10.3109/03639045.2012.718784
Tan Q, et al. Novel Taste-masked Orally Disintegrating Tablets for a Highly Soluble Drug With an Extremely Bitter Taste: Design Rationale and Evaluation. Drug Dev Ind Pharm. 2013;39(9):1364-71. PubMed PMID: 22994163.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Novel taste-masked orally disintegrating tablets for a highly soluble drug with an extremely bitter taste: design rationale and evaluation. AU - Tan,Qunyou, AU - Zhang,Li, AU - Liu,Guodong, AU - He,Dan, AU - Yin,Huafeng, AU - Wang,Hong, AU - Wu,Jianyong, AU - Liao,Hong, AU - Zhang,Jingqing, Y1 - 2012/09/20/ PY - 2012/9/22/entrez PY - 2012/9/22/pubmed PY - 2013/12/16/medline SP - 1364 EP - 71 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 39 IS - 9 N2 - The purpose of this study was to evaluate the taste masking potential of novel solid dispersions (SDs) using Eudragit® EPO as the excipient when incorporated into the orally disintegrating tablets (ODTs) for delivering a highly soluble drug with an extremely bitter taste. The pyridostigmine bromides (PB) SDs (PBSDs) were prepared by solvent evaporation-deposition method. The physicochemical properties of PBSDs were investigated by means of differential scanning calorimetry and Fourier transformed infrared spectroscopy. The dissolution test showed that only about 8% of PB was released from PBSDs in the simulated salivary fluid in 30 s. Therefore, PBSDs were considered taste-masked and selected for formulation of PBODTs. A central composite design was employed for process optimization. Multiple linear regression analysis for process optimization revealed that the optimal PBODTs were obtained, when the microcrystalline cellulose and crospovidone were 17.16 and 5.55 (%, w/w), respectively, and the average in vivo disintegration time was 25 s. The bitterness threshold of PB was examined by a sensory test, and the threshold value was set as 3 mg in each tablet. Taste evaluation of PBODTs in 18 volunteers revealed considerable taste masking with bitterness below the threshold value. PBODTs also revealed rapid drug release (around 99%, 2 min) in the simulated gastric fluid. The mean PB plasma concentration-time profiles of PBODTs and that of the commercial tablets were comparable, with closely similar pattern. Bioequivalence assessment results demonstrated that PBODTs and the commercial tablets were bioequivalent. In conclusion, PBODTs are prepared successfully, with taste masking and rapid disintegration in the oral cavity. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/22994163/Novel_taste_masked_orally_disintegrating_tablets_for_a_highly_soluble_drug_with_an_extremely_bitter_taste:_design_rationale_and_evaluation_ L2 - http://www.tandfonline.com/doi/full/10.3109/03639045.2012.718784 DB - PRIME DP - Unbound Medicine ER -