Document Detail

Disintegration/dissolution profiles of copies of Fosamax (alendronate).
MedLine Citation:
PMID:  14687450     Owner:  NLM     Status:  MEDLINE    
OBJECTIVE: Poor quality has been reported for some generics and other copies of original products. We performed a pilot study to compare the disintegration/dissolution profiles of FOSAMAX (alendronate) 70 mg tablets with those of copies of FOSAMAX that were manufactured outside the United States. RESEARCH DESIGN AND METHODS: We used the standard United States Pharmacopeia (USP) disintegration method to evaluate FOSAMAX 70 mg tablets and 13 copies. At least 12 (n = 12) dosage units were tested for each product (except Fosmin, n = 10). The dissolution profiles of FOSAMAX and one representative copy were also compared. RESULTS: Nine copies (Osteomax, Defixal, Fosmin, Endronax, Osteomix, Genalmen, Fixopan, Osteoplus, and Fosval) disintegrated two- to ten-fold faster than FOSAMAX. Three other copies (Neobon, Regenesis, and Ostenan) disintegrated at least five-fold slower than FOSAMAX. Neobon is a softgel capsule, so special consideration was given to this different dosage form. One copy (Arendal) did not fall into either category but exhibited potentially large inter- and intra-lot variability. Dissolution of alendronate from Regenesis lagged behind that from FOSAMAX. CONCLUSION: Slower disintegration may reduce efficacy because bisphosphonates must be taken in the fasting state and contact with food or even certain beverages severely reduces bioavailability. Faster disintegration (or the use of gel-caps or other alterations to the drug formulation) could increase the risk of esophagitis, an adverse event associated with prolonged contact of the esophagus with bisphosphonates. These disintegration and dissolution results suggest that important differences may exist between FOSAMAX and its copies with regard to bioavailability, pharmacokinetics, and clinical efficacy and safety profiles. Additional testing is warranted to evaluate the pharmacokinetics and clinical safety of these copies.
S Epstein; B Cryer; S Ragi; J R Zanchetta; J Walliser; J Chow; M A Johnson; A E Leyes
Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Current medical research and opinion     Volume:  19     ISSN:  0300-7995     ISO Abbreviation:  Curr Med Res Opin     Publication Date:  2003  
Date Detail:
Created Date:  2003-12-22     Completed Date:  2004-08-30     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0351014     Medline TA:  Curr Med Res Opin     Country:  England    
Other Details:
Languages:  eng     Pagination:  781-9     Citation Subset:  IM    
Mount Sinai School of Medicine, New York, NY, USA.
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MeSH Terms
Alendronate / chemistry,  pharmacokinetics*
Biological Availability
Drugs, Generic / chemistry,  pharmacokinetics*
Esophagitis / etiology
Latin America
Osteoporosis, Postmenopausal / drug therapy
Pilot Projects
Therapeutic Equivalency
Water / chemistry
Reg. No./Substance:
0/Drugs, Generic; 0/Tablets; 66376-36-1/Alendronate; 7732-18-5/Water
Comment In:
Curr Med Res Opin. 2004 Jul;20(7):1035-6; author reply 1036-7   [PMID:  15265248 ]
Erratum In:
Curr Med Res Opin. 2004 Apr;20(4):575

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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