Document Detail

Evaluation of self-dissolving needles containing low molecular weight heparin (LMWH) in rats.
MedLine Citation:
PMID:  17826015     Owner:  NLM     Status:  MEDLINE    
Feasibility study of self-dissolving needles containing polysaccharide was performed. Low molecular weight heparin (LMWH) was used as a representative polysaccharide. Using chondroitin, dextran and dextrin as the base, self-dissolving needles (SDN) were prepared. The obtained SDNs were evaluated in rat absorption experiment, where pharmacological availability (PA) was calculated by comparing the plasma anti-Xa activity vs. time curves between SDNs and i.v. solution. After the insertion of SDNs to rats skin where the doses of LMWH were 25, 50 and 100 IU/kg, plasma samples were collected for 6h and anti-Xa activity was measured as the pharmacological index of LMWH. The anti-Xa level was maintained above 0.2 IU/ml, the therapeutic level, for about 2h at a dose of 100 IU/kg. Almost the same PAs of LMWH were obtained with dextran and dextrin SDNs, 97.7% and 102.3%, though lower PA was obtained with chondroitin SDN, 81.5%. In vitro dissolution experiment showed that LMWH was released from dextran, dextrin and chondroitin SDNs within 10 min. The T(50%)s were 0.84+/-0.06 min for dextran SDN, 1.07+/-0.12 min for chondroitin SDN and 2.11+/-0.31 min for dextrin SDN, respectively. Plasma anti-Xa activity vs. time profiles showed good dose-dependency in the 25-100 IU/kg range and high PAs were obtained, 90.0% for 25 IU/kg, 95.4% for 50 IU/kg and 97.7% for 100 IU/kg from dextran SDNs. Stability experiment was performed with dextran SDNs for 3 months. Above 97% of LMWH were remained in SDNs under three different conditions, -80, 4 and 40 degrees C. These results suggest the usefulness of SDN to polysaccharide drug.
Yukako Ito; Aiko Murakami; Tomohiro Maeda; Nobuyuki Sugioka; Kanji Takada
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2007-08-06
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  349     ISSN:  0378-5173     ISO Abbreviation:  Int J Pharm     Publication Date:  2008 Feb 
Date Detail:
Created Date:  2007-12-31     Completed Date:  2008-03-11     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  124-9     Citation Subset:  IM    
Department of Pharmacokinetics, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8414, Japan.
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MeSH Terms
Anticoagulants / administration & dosage*,  pharmacokinetics
Chondroitin / chemistry
Dextrans / chemistry
Dose-Response Relationship, Drug
Drug Stability
Drug Storage
Factor Xa / metabolism
Heparin, Low-Molecular-Weight / administration & dosage*,  pharmacokinetics
Rats, Wistar
Reg. No./Substance:
0/Anticoagulants; 0/Excipients; 0/Heparin, Low-Molecular-Weight; 9004-54-0/Dextrans; 9007-27-6/Chondroitin; EC Xa

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