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STUDYING THE IMPACT OF FORMULATION AND PROCESSING PARAMETERS ON THE RELEASE CHARACTERISTICS FROM HYDROXYPROPYL METHYLCELLULOSE MATRIX TABLETS OF DICLOFENAC.
Acta Pol Pharm. 2016 Mar-Apr; 73(2):439-52.AP

Abstract

Hydrophilic matrices, especially HPMC based, are widely used to provide sustained delivery where drug release occurs mainly by diffusion. A 3(2) full factorial design was used to develop and evaluate HPMC matrix tablet for sustained delivery of diclofenac. The influences of polymer concentration/viscosity, diluent type/ratio, drug load/solubility, compression force and pH change on drug release were investigated. Ten tablet formulations were prepared using wet granulation. HPMC K15M (10-30% w/w) was used as the polymer forming matrix. The release kinetics, compatibility studies, lot reproducibility and effect on storage were discussed. Increasing polymer concentration and compression force showed antagonistic effect on release rate. Mannitol tends to increase release rate more than lactose. Reversing diluent ratio between lactose and MCC did not affect drug release. Changing pH resulted in burst release whereas drug solubility is pH independent. F1 showed similar release to Voltaren SR and followed Higuchi model. Drug and polymer were compatible to each other. The formulation is stable at long and intermediate conditions with a significant increase in release rate at accelerated conditions due to water uptake and polymer swelling. The developed formulation was successful for a sustained delivery of diclofenac.

Authors

Elzayat EM
No affiliation info available
Abdel-Rahman AA
No affiliation info available
Ahmed SM
No affiliation info available
Alanazi FK
No affiliation info available
Habib WA
No affiliation info available
Sakr A
No affiliation info available

MeSH

Anti-Inflammatory Agents, Non-SteroidalCalorimetry, Differential ScanningChemistry, PharmaceuticalCrystallography, X-RayDelayed-Action PreparationsDiclofenacDrug CarriersDrug StabilityHydrogen-Ion ConcentrationHypromellose DerivativesKineticsModels, ChemicalSolubilitySpectroscopy, Fourier Transform InfraredTabletsTechnology, PharmaceuticalViscosity

Pub Type(s)

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

Language

eng

PubMed ID

27180437

Citation

Elzayat, Ehab M., et al. "STUDYING the IMPACT of FORMULATION and PROCESSING PARAMETERS ON the RELEASE CHARACTERISTICS FROM HYDROXYPROPYL METHYLCELLULOSE MATRIX TABLETS of DICLOFENAC." Acta Poloniae Pharmaceutica, vol. 73, no. 2, 2016, pp. 439-52.
Elzayat EM, Abdel-Rahman AA, Ahmed SM, et al. STUDYING THE IMPACT OF FORMULATION AND PROCESSING PARAMETERS ON THE RELEASE CHARACTERISTICS FROM HYDROXYPROPYL METHYLCELLULOSE MATRIX TABLETS OF DICLOFENAC. Acta Pol Pharm. 2016;73(2):439-52.
Elzayat, E. M., Abdel-Rahman, A. A., Ahmed, S. M., Alanazi, F. K., Habib, W. A., & Sakr, A. (2016). STUDYING THE IMPACT OF FORMULATION AND PROCESSING PARAMETERS ON THE RELEASE CHARACTERISTICS FROM HYDROXYPROPYL METHYLCELLULOSE MATRIX TABLETS OF DICLOFENAC. Acta Poloniae Pharmaceutica, 73(2), 439-52.
Elzayat EM, et al. STUDYING the IMPACT of FORMULATION and PROCESSING PARAMETERS ON the RELEASE CHARACTERISTICS FROM HYDROXYPROPYL METHYLCELLULOSE MATRIX TABLETS of DICLOFENAC. Acta Pol Pharm. 2016 Mar-Apr;73(2):439-52. PubMed PMID: 27180437.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - STUDYING THE IMPACT OF FORMULATION AND PROCESSING PARAMETERS ON THE RELEASE CHARACTERISTICS FROM HYDROXYPROPYL METHYLCELLULOSE MATRIX TABLETS OF DICLOFENAC. AU - Elzayat,Ehab M, AU - Abdel-Rahman,Ali A, AU - Ahmed,Sayed M, AU - Alanazi,Fars K, AU - Habib,Walid A, AU - Sakr,Adel, PY - 2016/5/17/entrez PY - 2016/5/18/pubmed PY - 2016/6/21/medline SP - 439 EP - 52 JF - Acta poloniae pharmaceutica JO - Acta Pol Pharm VL - 73 IS - 2 N2 - Hydrophilic matrices, especially HPMC based, are widely used to provide sustained delivery where drug release occurs mainly by diffusion. A 3(2) full factorial design was used to develop and evaluate HPMC matrix tablet for sustained delivery of diclofenac. The influences of polymer concentration/viscosity, diluent type/ratio, drug load/solubility, compression force and pH change on drug release were investigated. Ten tablet formulations were prepared using wet granulation. HPMC K15M (10-30% w/w) was used as the polymer forming matrix. The release kinetics, compatibility studies, lot reproducibility and effect on storage were discussed. Increasing polymer concentration and compression force showed antagonistic effect on release rate. Mannitol tends to increase release rate more than lactose. Reversing diluent ratio between lactose and MCC did not affect drug release. Changing pH resulted in burst release whereas drug solubility is pH independent. F1 showed similar release to Voltaren SR and followed Higuchi model. Drug and polymer were compatible to each other. The formulation is stable at long and intermediate conditions with a significant increase in release rate at accelerated conditions due to water uptake and polymer swelling. The developed formulation was successful for a sustained delivery of diclofenac. SN - 0001-6837 UR - https://www.unboundmedicine.com/medline/citation/27180437/STUDYING_THE_IMPACT_OF_FORMULATION_AND_PROCESSING_PARAMETERS_ON_THE_RELEASE_CHARACTERISTICS_FROM_HYDROXYPROPYL_METHYLCELLULOSE_MATRIX_TABLETS_OF_DICLOFENAC_ DB - PRIME DP - Unbound Medicine ER -