Document Detail


Relative bioavailability of new formulation of paracetamol effervescent powder containing sodium bicarbonate versus paracetamol tablets: a comparative pharmacokinetic study in fed subjects.
MedLine Citation:
PMID:  17931082     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
OBJECTIVE: the aim of this relative bioavailability study was to determine the rate and extent of absorption of Alikal Dolor (effervescent powder containing paracetamol 500 mg/sodium bicarbonate 2318 mg)--test formulation (T) in relation to Parageniol (paracetamol 500 mg coated tablets)--reference formulation (R). METHODS: 18 healthy volunteers (10 male and 8 female aged between 21 and 46 years) received, after 2 h of standardized breakfast, a single oral dose with 220 ml of water, in an open, randomized, crossover study, with a 7-day wash-out period. Paracetamol concentrations were established at 0, 10, 15, 20, 25, 30, 35, 40, 45, 50, 60, 75, 90 min and at 2, 4, 6, 8 and 10 h postdose by HPLC with an ultraviolet detector. RESULTS: the regression coefficient determined for paracetamol calibration curves was 0.9983 +/- 0.0034 and the working range was from 0.2 to 50 microg/ml. The quantification limit was 0.2 microg/ml. The rate of absorption was significantly greater (p < 0.03) for T (T(max) = 20.4 min) compared with R (T(max) = 38.4 min). Extent of absorption over the first 30 min postdose AUC((0-30 min)) was 4.21-fold greater (p < 0.03) for T compared with R, without differences between C(max.) The 90% CI on the geometric mean for C(max), AUC((0-10 h)) and AUC((0-)) ratios (T/R) were within the limits of 0.80-1.25, indicating both formulations were bioequivalent with respect to these parameters. CONCLUSION: paracetamol was absorbed at least twice as fast from T-containing sodium bicarbonate compared with R. This pharmacokinetic feature could prove crucial from the therapeutic point of view as it would allow a lower latency in the action time of paracetamol in producing its analgesic and antithermal effect.
Authors:
Guillermo Di Girolamo; Javier A W Opezzo; Marcela I Lopez; Daniel Schere; Guillermo Keller; Claudio D Gonzalez; Javier Martinelli Massa; María Cecilia de los Santos
Publication Detail:
Type:  Comparative Study; Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Expert opinion on pharmacotherapy     Volume:  8     ISSN:  1744-7666     ISO Abbreviation:  Expert Opin Pharmacother     Publication Date:  2007 Oct 
Date Detail:
Created Date:  2007-10-12     Completed Date:  2007-12-06     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  100897346     Medline TA:  Expert Opin Pharmacother     Country:  England    
Other Details:
Languages:  eng     Pagination:  2449-57     Citation Subset:  IM    
Affiliation:
Second Chair of Pharmacology, Universidad de Buenos Aires, Department of Pharmacology, School of Medicine, Ciudad Autónoma de Buenos Aires, Argentina. gdigirolamo@arnet.com.ar
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MeSH Terms
Descriptor/Qualifier:
Acetaminophen / chemistry*,  pharmacokinetics*
Adult
Biological Availability
Chemistry, Pharmaceutical / methods
Cross-Over Studies
Female
Food*
Humans
Intestinal Absorption / drug effects,  physiology
Male
Middle Aged
Powders
Sodium Bicarbonate / chemistry*,  pharmacokinetics*
Tablets
Chemical
Reg. No./Substance:
0/Powders; 0/Tablets; 103-90-2/Acetaminophen; 144-55-8/Sodium Bicarbonate

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


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