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Design, development and in-vitro evaluation of diclofenac taste-masked orodispersible tablet formulations.
Drug Dev Ind Pharm. 2015 Apr; 41(4):540-51.DD

Abstract

CONTEXT

Fast onset of action is prerequisite for acute pain medication. A palatable orodispersible medicine of diclofenac providing rapid analgesic effect should improve patient compliance and treatment.

OBJECTIVE

In the present study, diclofenac taste-masked orodispersible tablets (ODTs) with fast release characteristics were developed. Different taste-masking approaches and formulation concepts were screened in vitro for candidate selection.

MATERIALS AND METHODS

Diclofenac was used as free acid. Five taste-masked microgranule formulations were prepared by wet granulation and/or coating processes, and compressed to ODTs. Citric acid (pH-modifying agent) and Eudragit® E PO (amino methacrylate copolymer) were used as taste-masking agents. Evaluation criteria were (i) disintegration time, (ii) processability and (iii) in-vitro dissolution profiles in simulated saliva (pH 7.4, 5 mL, 3 min) and compendial pH-change media (paddle, 50 rpm). The prototypes were compared to reference ODTs (without taste-masking). Most suitable ODT prototypes were selected and further evaluated for taste-masking efficiency using an electronic tongue.

RESULTS AND DISCUSSION

In simulated saliva, the drug was slower released from the prototypes (between 1.1% and 15.5%) than from reference ODTs (23.7%). Less dissolved particles are thus expected in vivo for taste perception. Two ODT prototypes showed fast and complete drug release in phosphate buffer. The formulation providing the most efficient taste-masking was selected guided by electronic tongue data.

CONCLUSION

A novel palatable and fast acting diclofenac ODT formulation was successfully developed. Formulation design, development and in-vitro evaluation used in this study may serve as rational approach for manufacturing taste-masked orodispersible dosage forms.

Authors+Show Affiliations

Department of Pharmacy, Institute of Biopharmaceutics and Pharmaceutical Technology, University of Greifswald , Greifswald , Germany .No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

24495274

Citation

Guhmann, Marie, et al. "Design, Development and In-vitro Evaluation of Diclofenac Taste-masked Orodispersible Tablet Formulations." Drug Development and Industrial Pharmacy, vol. 41, no. 4, 2015, pp. 540-51.
Guhmann M, Preis M, Gerber F, et al. Design, development and in-vitro evaluation of diclofenac taste-masked orodispersible tablet formulations. Drug Dev Ind Pharm. 2015;41(4):540-51.
Guhmann, M., Preis, M., Gerber, F., Pöllinger, N., Breitkreutz, J., & Weitschies, W. (2015). Design, development and in-vitro evaluation of diclofenac taste-masked orodispersible tablet formulations. Drug Development and Industrial Pharmacy, 41(4), 540-51. https://doi.org/10.3109/03639045.2014.884122
Guhmann M, et al. Design, Development and In-vitro Evaluation of Diclofenac Taste-masked Orodispersible Tablet Formulations. Drug Dev Ind Pharm. 2015;41(4):540-51. PubMed PMID: 24495274.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design, development and in-vitro evaluation of diclofenac taste-masked orodispersible tablet formulations. AU - Guhmann,Marie, AU - Preis,Maren, AU - Gerber,Frédéric, AU - Pöllinger,Norbert, AU - Breitkreutz,Jörg, AU - Weitschies,Werner, Y1 - 2014/02/05/ PY - 2014/2/6/entrez PY - 2014/2/6/pubmed PY - 2016/1/29/medline KW - Diclofenac KW - ODT KW - electronic tongue KW - taste KW - taste-masking SP - 540 EP - 51 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 41 IS - 4 N2 - CONTEXT: Fast onset of action is prerequisite for acute pain medication. A palatable orodispersible medicine of diclofenac providing rapid analgesic effect should improve patient compliance and treatment. OBJECTIVE: In the present study, diclofenac taste-masked orodispersible tablets (ODTs) with fast release characteristics were developed. Different taste-masking approaches and formulation concepts were screened in vitro for candidate selection. MATERIALS AND METHODS: Diclofenac was used as free acid. Five taste-masked microgranule formulations were prepared by wet granulation and/or coating processes, and compressed to ODTs. Citric acid (pH-modifying agent) and Eudragit® E PO (amino methacrylate copolymer) were used as taste-masking agents. Evaluation criteria were (i) disintegration time, (ii) processability and (iii) in-vitro dissolution profiles in simulated saliva (pH 7.4, 5 mL, 3 min) and compendial pH-change media (paddle, 50 rpm). The prototypes were compared to reference ODTs (without taste-masking). Most suitable ODT prototypes were selected and further evaluated for taste-masking efficiency using an electronic tongue. RESULTS AND DISCUSSION: In simulated saliva, the drug was slower released from the prototypes (between 1.1% and 15.5%) than from reference ODTs (23.7%). Less dissolved particles are thus expected in vivo for taste perception. Two ODT prototypes showed fast and complete drug release in phosphate buffer. The formulation providing the most efficient taste-masking was selected guided by electronic tongue data. CONCLUSION: A novel palatable and fast acting diclofenac ODT formulation was successfully developed. Formulation design, development and in-vitro evaluation used in this study may serve as rational approach for manufacturing taste-masked orodispersible dosage forms. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/24495274/Design_development_and_in_vitro_evaluation_of_diclofenac_taste_masked_orodispersible_tablet_formulations_ L2 - https://www.tandfonline.com/doi/full/10.3109/03639045.2014.884122 DB - PRIME DP - Unbound Medicine ER -