Parenteral formulation and thermal degradation pathways of a potent rebeccamycin based indolocarbazole topoisomerase I inhibitor

International Journal of Pharmaceutics

Volumn 390, Issue 2, 2010, Pages 128-133

  Sato, Yuichi ^a   Breslin, David ^b   Kitada, Hideyuki ^a   Minagawa, Wataru ^a   Nomoto, Takashi ^a   Qin, Xue Zhi ^b   Karki, Shyam B ^b  

^a BANYU PHARMACEUTICAL CO LTD   (Japan)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Buffer; Cosolvent; Indolocarbazole; PG; Solubility; Stability; Topoisomerase I

Indexed keywords

12,13 DIHYDRO 2,10 DIHYDROXY 6 N (1 HYROXYMETHYL 2 HYDROXYETHYLAMINO) 13 (BETA DEXTRO GLUCOPYRANOSYL) 5H INDOLO[2,3 A]PYRROLO[3,4 C]CARBAZOLE 5,7(6H)DIONE; DNA TOPOISOMERASE INHIBITOR; INDOLOCARBAZOLE DERIVATIVE; PROPYLENE GLYCOL; REBECCAMYCIN; UNCLASSIFIED DRUG;

ARTICLE; CHEMICAL REACTION; CLINICAL TRIAL; DEGRADATION KINETICS; DRUG DEGRADATION; DRUG FORMULATION; DRUG HYDROLYSIS; DRUG POTENCY; DRUG STABILITY; DRUG STRUCTURE; HUMAN; IMAGE ANALYSIS; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; NUCLEAR MAGNETIC RESONANCE; PARENTERAL DRUG ADMINISTRATION; PRIORITY JOURNAL; THERMOSTABILITY;

CARBAZOLES; CHEMISTRY, PHARMACEUTICAL; DNA TOPOISOMERASES, TYPE I; DRUG STABILITY; ENZYME INHIBITORS; HYDROLYSIS; INJECTIONS; MOLECULAR STRUCTURE; PROPYLENE GLYCOL; SOLUBILITY; TEMPERATURE;

EID: 77951498304     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2010.01.004     Document Type: Article

References (13)

1. Breslin, D., Sato, Y., Karki, S.B., in press. Mechanism of hydrolysis of a novel indolocarbazole topoisomerase I inhibitor. Eur. J. Pharm. Sci.
2. Cavazos C.M., Keir S.T., Yoshinari T., Bigner D.D., Friedman H.S. Therapeutic activity of the topoisomerase I inhibitor J-107088 [6-N-(1-hydroxymethyla-2-hydroxy)ethylamino-12,13-dihydro-13-(β-d-gluco pyranosyl)-5H-indolo[2,3-a]pyrrolo[3,4-c]-carbazole-5,7(6H)-dione] against pediatric and adult central nervous system tumor xenografts. Cancer Chemother. Pharmacol. 2001, 48:250-254.
3. Jain N., Yang G., Tabibi S.E., Yalkowsky S.H. Solubilization of NSC-639829. Int. J. Pharm. 2001, 225:41-47.
4. Nema S., Washkuhn R.J., Brendel R.J. Excipients and their use in injectable products. PDA J. Pharm. Sci. Technol. 1997, 51:166-171.
5. Ni N., Sanghvi T., Yalkowsky S.H. Solubilization and preformulation of carbendazim. Int. J. Pharm. 2002, 244:99-104.
6. Powell M.F., Nguyen T., Baloian L. Compendium of excipients for parenteral formulations. PDA J. Pharm. Sci. Technol. 1998, 52:238-311.
7. Strickley R.G. Parenteral formulations of small molecules therapeutics marketed in the United States (1999). Part I. PDA J. Pharm. Sci. Technol. 1999, 53:324-349.
8. Strickley R.G. Parenteral formulations of small molecules therapeutics marketed in the United States (1999). Part II. PDA J. Pharm. Sci. Technol. 2000, 54:69-96.
9. Strickley R.G. Parenteral formulations of small molecules therapeutics marketed in the United States (1999). Part III. PDA J. Pharm. Sci. Technol. 2000, 54:152-169.
10. Sweetana S., Akers M.J. Solubility principles and practices for parenteral drug dosage form development. PDA J. Pharm. Sci. Technol. 1996, 50:330-342.
11. Yalkowsky S.H., Rubino J.T. Solubilization by cosolvents I: organic solutes in propylene glycol-water mixtures. J. Pharm. Sci. 1985, 74:416-421.
12. Yoshinari T., Ohkubo M., Fukusawa K., Egashira S., Hara Y., Matsumoto M., Nakai K., Arakawa H., Morishima H., Nishimura S. Mode of action of a new indolocarbazole anticancer agent, J-107088, targeting topoisomerase I. Cancer Res. 1999, 59:4271-4275.
13. Zhao L., Li P., Yalkowsky S.H. Solubilization of fluasterone. J. Pharm. Sci. 1999, 88:967-969.