Microenvironmental pH modulation based release enhancement of a weakly basic drug from hydrophilic matrices

Journal of Pharmaceutical Sciences

Volumn 95, Issue 7, 2006, Pages 1459-1468

  Tatavarti, Aditya S ^a,b   Hoag, Stephen W ^a  

^a UNIVERSITY OF MARYLAND SCHOOL OF PHARMACY   (United States)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Eudragit l100 55; Hydroxypropyl methylcellulose; Microenvironmental pH; pH modulators; Sustained release; Weak bases

Indexed keywords

CITRIC ACID; EUDRAGIT; FUMARIC ACID; HYDROXYPROPYLMETHYLCELLULOSE; L 100 55; MAGNESIUM STEARATE; MALIC ACID; METHACRYLIC ACID; POLYMER; SUCCINIC ACID; TRIMETHOPRIM;

ALKALINITY; ARTICLE; CORRELATION COEFFICIENT; DRUG DIFFUSION; DRUG FORMULATION; DRUG PENETRATION; DRUG RELEASE; DRUG SOLUBILITY; DRUG STRUCTURE; HYDROPHILICITY; MICROENVIRONMENT; PH; PHYSICAL CHEMISTRY; SCANNING ELECTRON MICROSCOPY; SUSTAINED DRUG RELEASE; WATER TRANSPORT;

EID: 33745900244     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.20612     Document Type: Article

References (17)

1. Vashi VI, Meyer MC. 1988. Effect of pH on the in vitro dissolution and in vivo absorption of controlled-release theophylline in dogs. J Pharm Sci 77:760-774.
2. Kohri N, Miyata N, Takahashi M, Endo H, Iseki K, Miyazaki K, Takechi S, Nomura A. 1992. Evaluation of pH-independent sustained release granules of dipyridamole by using gastric-acidity-controlled rabbits and human subjects. Int J Pharm 81:49-58.
3. Yamada I, Goda T, Kawata M, Shiotuki T, Ogawa K. 1990. Gastric acidity-dependent bioavailability of commercial sustained release preparations of indomethacin evaluated by gastric-acidity-controlled beagle dogs. Chem Pharm Bull 38:3112-3115.
4. Rao VM, Engh K, Qiu Y. 2003. Design of pH-independent controlled release matrix tablets for acidic drugs. Int J Pharm 252:81-86.
5. Thoma K, Zimmer T. 1990. Retardation of weakly basic drugs with diffusion tablets. Int J Pharm 58:197-202.
6. Streubel A, Siepmann J, Dashevsky A, Bodmeier R. 2000. pH-independent release of a weakly basic drug from water-insoluble and -soluble matrix tablets. J Control Release 67:101-110.
7. Espinoza R, Hong E, Villafuerte L. 2000. Influence of admixed citric acid on the release profile of pelanserin hydrochloride from HPMC matrix tablets. Int J Pharm 201:165-173.
8. Gabr K. 1992. Effect of organic acids on release patterns of weakly basic drugs from inert sustained release matrix tablets. Eur J Pharm Biopharm 38:199-202.
9. Tatavarti AS, Lee PI, Kou JH. 2002. Investigation into the mechanism of release and formulation development of controlled release matrix tablets of an antiallergenic, SCH 466036. Poster presentation, AAPS annual meeting, Toronto, CA. AAPS PharmSci Vol. 4, No. 4, Abstract T3208.
10. Oren PL, Seidler WMK. Sustained release matrix. US patent 4,968,508, November 6 1990.
11. Tatavarti AS, Mehta KA, Augsburger LL, Hoag SW. 2004. Influence of methacrylic and acrylic acid polymers on the release performance of weakly basic drugs from sustained release hydrophilic matrices. J Pharm Sci 93:2319-2331.
12. Dahlan R, McDonald C, Sunderland B. 1987. Solubilities and intrinsic dissolution rates of sulphamethoxazole and trimethoprim. J Pharm Pharmacol 39:246-251.
13. Moore JW, Flanner HH. 1996. Mathematical comparison of dissolution profiles. Pharm Technol 20:64-74.
14. FDA, Center for Drug Evaluation and Research. Guidance for Industry. September 1997. Modified release solid oral solid dosage forms; scale-up and post-approval changes: Chemistry, manufacturing and controls, in vitro dissolution testing, and in vivo bioequivalence documentations; www.FDA-gov/cder/guidance/1214fnl.pdf.
15. Akiyama Y, Yoshioka M, Horibe H, Hirai S, Kitamori N, Toguchi H. 1994. pH-independent controlled-release microspheres using polyglycerol ester-fatty acids. J Pharm Sci 83:1600-1607.
16. Varma MVS, Kaushal AM, Garg S. 2005. Influence of micro-environmental pH on the gel layer behavior and release of a basic drug from various hydrophilic matrices. J Control Release 103:499-510.
17. Siepmann J, Peppas NA. 2001. Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv Drug Deliv Rev 48:139-157.