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Design and study of lamivudine oral controlled release tablets.
AAPS PharmSciTech. 2007 Dec 07; 8(4):E101.AP

Abstract

The objective of this study was to design oral controlled release matrix tablets of lamivudine using hydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of various formulation factors such as polymer proportion, polymer viscosity, and compression force on the in vitro release of drug. In vitro release studies were performed using US Pharmacopeia type 1 apparatus (basket method) in 900 mL of pH 6.8 phosphate buffer at 100 rpm. The release kinetics were analyzed using the zero-order model equation, Higuchi's square-root equation, and the Ritger-Peppas empirical equation. Compatibility of the drug with various excipients was studied. In vitro release studies revealed that the release rate decreased with increase in polymer proportion and viscosity grade. Increase in compression force was found to decrease the rate of drug release. Matrix tablets containing 60% HPMC 4000 cps were found to show good initial release (26% in first hour) and extended the release up to 16 hours. Matrix tablets containing 80% HPMC 4000 cps and 60% HPMC 15,000 cps showed a first-hour release of 22% but extended the release up to 20 hours. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation and therefore followed non-Fickian or anomalous release. No incompatibility was observed between the drug and excipients used in the formulation of matrix tablets. The developed controlled release matrix tablets of lamivudine, with good initial release (20%-25% in first hour) and extension of release up to 16 to 20 hours, can overcome the disadvantages of conventional tablets of lamivudine.

Links

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Authors+Show Affiliations

Ravi PR
Pharmacy Group, Faculty Division III, Birla Institute of Technology and Science, Pilani, Rajasthan, India.
Ganga S
No affiliation info available
Saha RN
No affiliation info available

MeSH

Administration, OralChemistry, PharmaceuticalCompressive StrengthDelayed-Action PreparationsDiffusionDrug CompoundingDrug StabilityExcipientsHardnessHypromellose DerivativesKineticsLamivudineMethylcelluloseModels, ChemicalPorosityReproducibility of ResultsReverse Transcriptase InhibitorsSolubilityTabletsTechnology, PharmaceuticalViscosity

Pub Type(s)

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

Language

eng

PubMed ID

18181522

Citation

Ravi, Punna Rao, et al. "Design and Study of Lamivudine Oral Controlled Release Tablets." AAPS PharmSciTech, vol. 8, no. 4, 2007, pp. E101.
Ravi PR, Ganga S, Saha RN. Design and study of lamivudine oral controlled release tablets. AAPS PharmSciTech. 2007;8(4):E101.
Ravi, P. R., Ganga, S., & Saha, R. N. (2007). Design and study of lamivudine oral controlled release tablets. AAPS PharmSciTech, 8(4), E101. https://doi.org/10.1208/pt0804101
Ravi PR, Ganga S, Saha RN. Design and Study of Lamivudine Oral Controlled Release Tablets. AAPS PharmSciTech. 2007 Dec 7;8(4):E101. PubMed PMID: 18181522.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design and study of lamivudine oral controlled release tablets. AU - Ravi,Punna Rao, AU - Ganga,Sindhura, AU - Saha,Ranendra Narayan, Y1 - 2007/12/07/ PY - 2008/1/10/pubmed PY - 2008/1/25/medline PY - 2008/1/10/entrez SP - E101 EP - E101 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 8 IS - 4 N2 - The objective of this study was to design oral controlled release matrix tablets of lamivudine using hydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of various formulation factors such as polymer proportion, polymer viscosity, and compression force on the in vitro release of drug. In vitro release studies were performed using US Pharmacopeia type 1 apparatus (basket method) in 900 mL of pH 6.8 phosphate buffer at 100 rpm. The release kinetics were analyzed using the zero-order model equation, Higuchi's square-root equation, and the Ritger-Peppas empirical equation. Compatibility of the drug with various excipients was studied. In vitro release studies revealed that the release rate decreased with increase in polymer proportion and viscosity grade. Increase in compression force was found to decrease the rate of drug release. Matrix tablets containing 60% HPMC 4000 cps were found to show good initial release (26% in first hour) and extended the release up to 16 hours. Matrix tablets containing 80% HPMC 4000 cps and 60% HPMC 15,000 cps showed a first-hour release of 22% but extended the release up to 20 hours. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation and therefore followed non-Fickian or anomalous release. No incompatibility was observed between the drug and excipients used in the formulation of matrix tablets. The developed controlled release matrix tablets of lamivudine, with good initial release (20%-25% in first hour) and extension of release up to 16 to 20 hours, can overcome the disadvantages of conventional tablets of lamivudine. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/18181522/Design_and_study_of_lamivudine_oral_controlled_release_tablets_ DB - PRIME DP - Unbound Medicine ER -