Cholorpheniramine tannate complexes: Physicochemical, chemometric, and taste masking evaluation

Ziyaur Rahman, Ahmed S. Zidan, Saeed R. Khan, Indra K. Reddy, Mansoor A. Khan

Research output: Contribution to journalArticle

Abstract

The focus of present investigation was to evaluate the tannic acid (TA) complexes of cholorpheniramine maleate (CPM) and characterize it by a variety of physicochemical, dissolution, and electronic tongue methods. The complexes were prepared in various molar ratios by solvent evaporation method. They were characterized by spectroscopic, thermal, powder X-ray, electronic tongue, solubility and dissolution methods. FTIR (infrared red) spectra showed complex formation between the TA and CPM. Complex formation has significantly lowered the drug solubility and sustained its release for more than 24 h in phosphate buffer pH 6.8. On the contrary, the release was much faster in the presence of Avicel PH 113 in the same molar ratio complex. The complex formulation has suppressed the bitter taste of CPM as indicated by Euclidean distance in electronic tongue evaluation. NIR-CI (near infrared chemical imaging) showed lower skew value that indicated the homogenous distribution of formulation components. The chemometric models were also developed using the NIR data. The model based on second derivative data was better in predicting the TA and CPM loading as indicated by higher values of R, R2 and lower values of root mean square error and standard errors. Furthermore, it has a better accuracy and less biased in comparison to other models. In conclusion, the CPM tannate has a sustained release behavior and excipients play a major role in modifying its release. Additionally, the complexes with varying molar ratio of tannate to CPM have differential taste masking abilities than that of the pure drug.

Original languageEnglish (US)
Pages (from-to)582-592
Number of pages11
JournalInternational Journal of Pharmaceutics
Volume436
Issue number1-2
DOIs
StatePublished - Oct 15 2012
Externally publishedYes

Fingerprint

Electronic Nose
Tannins
Solubility
Aptitude
Excipients
Fourier Transform Infrared Spectroscopy
Cellulose
Pharmaceutical Preparations
Powders
maleic acid
Buffers
Hot Temperature
Phosphates
X-Rays

Keywords

  • Bitter taste
  • Chemometric model
  • Cholorpheniramine maleate
  • Complex
  • Dissolution
  • Solubility
  • Tannic acid

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Cholorpheniramine tannate complexes : Physicochemical, chemometric, and taste masking evaluation. / Rahman, Ziyaur; Zidan, Ahmed S.; Khan, Saeed R.; Reddy, Indra K.; Khan, Mansoor A.

In: International Journal of Pharmaceutics, Vol. 436, No. 1-2, 15.10.2012, p. 582-592.

Research output: Contribution to journalArticle

Rahman, Ziyaur ; Zidan, Ahmed S. ; Khan, Saeed R. ; Reddy, Indra K. ; Khan, Mansoor A. / Cholorpheniramine tannate complexes : Physicochemical, chemometric, and taste masking evaluation. In: International Journal of Pharmaceutics. 2012 ; Vol. 436, No. 1-2. pp. 582-592.
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AB - The focus of present investigation was to evaluate the tannic acid (TA) complexes of cholorpheniramine maleate (CPM) and characterize it by a variety of physicochemical, dissolution, and electronic tongue methods. The complexes were prepared in various molar ratios by solvent evaporation method. They were characterized by spectroscopic, thermal, powder X-ray, electronic tongue, solubility and dissolution methods. FTIR (infrared red) spectra showed complex formation between the TA and CPM. Complex formation has significantly lowered the drug solubility and sustained its release for more than 24 h in phosphate buffer pH 6.8. On the contrary, the release was much faster in the presence of Avicel PH 113 in the same molar ratio complex. The complex formulation has suppressed the bitter taste of CPM as indicated by Euclidean distance in electronic tongue evaluation. NIR-CI (near infrared chemical imaging) showed lower skew value that indicated the homogenous distribution of formulation components. The chemometric models were also developed using the NIR data. The model based on second derivative data was better in predicting the TA and CPM loading as indicated by higher values of R, R2 and lower values of root mean square error and standard errors. Furthermore, it has a better accuracy and less biased in comparison to other models. In conclusion, the CPM tannate has a sustained release behavior and excipients play a major role in modifying its release. Additionally, the complexes with varying molar ratio of tannate to CPM have differential taste masking abilities than that of the pure drug.

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