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Characterization of 5-fluorouracil release from hydroxypropylmethylcellulose compression-coated tablets.
Pharm Dev Technol. 2007; 12(2):203-10.PD

Abstract

Hydrogel compression-coated tablets are able to release the core drug after a period of lag time and have potential for colon-specific drug delivery based on gastrointestinal transit time concept. This study investigated the factors influencing in vitro release characteristics of a model drug 5-fluorouracil from hydroxypropylmethycellulose (HPMC) compression-coated tablets. The core tablet, prepared by a wet granulation compression method, was designed to disintegrate and dissolute quickly. To prepare the compression-coated tablets, 50% of the HPMC/lactose coat powder was precompressed first, followed by centering the core tablet and compressing with the other 50% of the coat powder. Release characteristics were evaluated in distilled water by using a Chinese Pharmacopoeia rotatable basket method. Effect of HPMC viscosity, lactose content in outer shell, and overall coating weight of outer shell on release lag time (T(lag)), and zero-order release rate (k) were studied. Release of drug from compression-coated tablets began after a time delay as a result of hydrogel swelling/retarding effect, followed by zero-order release for most of the formulations studied. HPMC of higher viscosity (K4M and K15M) provided better protection of the drug-containing core, showing increased release lag time and slower release rate. Incorporating lactose in outer shell led to decrease of T(lag) and increase of k. T(lag) and k are exponentially and linearly correlated to lactose content, expressed as weight percentage of the outer shell. Larger coating weight (W) of outer shell produced larger coating thickness (D) around core tablet, which resulted in increase in T(lag) and decrease in k. There was good fitting of a linear model for each of the four variables W, D, T(lag), and k. Hardness of the compression-coated tablets and pHs of the release media had little effect on drug release profile. It is concluded that the release lag time and release rate are able to be tailored through adjusting the formulation variables to achieve colon-specific drug delivery of 5-fluorouracil.

Authors+Show Affiliations

Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, China.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

17510892

Citation

Wu, Baojian, et al. "Characterization of 5-fluorouracil Release From Hydroxypropylmethylcellulose Compression-coated Tablets." Pharmaceutical Development and Technology, vol. 12, no. 2, 2007, pp. 203-10.
Wu B, Shun N, Wei X, et al. Characterization of 5-fluorouracil release from hydroxypropylmethylcellulose compression-coated tablets. Pharm Dev Technol. 2007;12(2):203-10.
Wu, B., Shun, N., Wei, X., & Wu, W. (2007). Characterization of 5-fluorouracil release from hydroxypropylmethylcellulose compression-coated tablets. Pharmaceutical Development and Technology, 12(2), 203-10.
Wu B, et al. Characterization of 5-fluorouracil Release From Hydroxypropylmethylcellulose Compression-coated Tablets. Pharm Dev Technol. 2007;12(2):203-10. PubMed PMID: 17510892.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Characterization of 5-fluorouracil release from hydroxypropylmethylcellulose compression-coated tablets. AU - Wu,Baojian, AU - Shun,Ningyun, AU - Wei,Xiuli, AU - Wu,Wei, PY - 2007/5/19/pubmed PY - 2007/8/24/medline PY - 2007/5/19/entrez SP - 203 EP - 10 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 12 IS - 2 N2 - Hydrogel compression-coated tablets are able to release the core drug after a period of lag time and have potential for colon-specific drug delivery based on gastrointestinal transit time concept. This study investigated the factors influencing in vitro release characteristics of a model drug 5-fluorouracil from hydroxypropylmethycellulose (HPMC) compression-coated tablets. The core tablet, prepared by a wet granulation compression method, was designed to disintegrate and dissolute quickly. To prepare the compression-coated tablets, 50% of the HPMC/lactose coat powder was precompressed first, followed by centering the core tablet and compressing with the other 50% of the coat powder. Release characteristics were evaluated in distilled water by using a Chinese Pharmacopoeia rotatable basket method. Effect of HPMC viscosity, lactose content in outer shell, and overall coating weight of outer shell on release lag time (T(lag)), and zero-order release rate (k) were studied. Release of drug from compression-coated tablets began after a time delay as a result of hydrogel swelling/retarding effect, followed by zero-order release for most of the formulations studied. HPMC of higher viscosity (K4M and K15M) provided better protection of the drug-containing core, showing increased release lag time and slower release rate. Incorporating lactose in outer shell led to decrease of T(lag) and increase of k. T(lag) and k are exponentially and linearly correlated to lactose content, expressed as weight percentage of the outer shell. Larger coating weight (W) of outer shell produced larger coating thickness (D) around core tablet, which resulted in increase in T(lag) and decrease in k. There was good fitting of a linear model for each of the four variables W, D, T(lag), and k. Hardness of the compression-coated tablets and pHs of the release media had little effect on drug release profile. It is concluded that the release lag time and release rate are able to be tailored through adjusting the formulation variables to achieve colon-specific drug delivery of 5-fluorouracil. SN - 1083-7450 UR - https://www.unboundmedicine.com/medline/citation/17510892/Characterization_of_5_fluorouracil_release_from_hydroxypropylmethylcellulose_compression_coated_tablets_ L2 - https://www.tandfonline.com/doi/full/10.1080/10837450601168722 DB - PRIME DP - Unbound Medicine ER -