Document Detail

In vivo brain microdialysis as a formulation-screening tool for a poorly soluble centrally acting drug.
MedLine Citation:
PMID:  23298323     Owner:  NLM     Status:  Publisher    
Abstract Objective: Efficacy of a formulation of a poorly soluble centrally acting drug was evaluated by measuring dopamine responses using in vivo brain microdialysis. Methods: Co-crystals (1:1) of carbamazepine and nicotinamide (CBZ-NCT) were complexed with cyclodextrins (γ-CDs) using supercritical fluid processing. Phase solubility and intrinsic dissolution were studied. Pharmacodynamic studies were performed on rats divided into three groups getting either CBZ-NCT in CD (20 mg/kg CBZ), pure CBZ solution or vehicle. A guide cannula was implanted to attach the microdialysis probe. Dialysate samples were analyzed for dopamine levels, which were compared between groups. Results: The optimized CBZ formulation (5% w/w in γ-CD) with solubility - 10 mg/mL showed stepwise increase in dopamine response (maximum 250% of baseline) compared to neat CBZ or vehicle (p < 0.05). The pharmacokinetics of the drug required 30 min to elicit CNS response, which peaked at about 1.5-2 h. Conclusion: Hence, brain microdialysis was successfully used to evaluate a dissolution rate enhancing formulation.
Murali Mohan Bommana; Bharat Kirthivasan; Abhijat Shikhar; Simerdeep Singh Gupta; Emilio Squillante
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-1-9
Journal Detail:
Title:  Drug development and industrial pharmacy     Volume:  -     ISSN:  1520-5762     ISO Abbreviation:  Drug Dev Ind Pharm     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-1-9     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7802620     Medline TA:  Drug Dev Ind Pharm     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, St. John's University , Jamaica, NY , USA.
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