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Paper Information

Journal:   IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)   SUMMER 2007 , Volume 6 , Number 3; Page(s) 159 To 165.
 
Paper: 

ENHANCING DISSOLUTION RATE OF CARBAMAZEPINE VIA COGRINDING WITH CROSPOVIDONE AND HYDROXYPROPYLMETHYLCELLULOSE

 
 
Author(s):  BARZEGAR JALALI M.*, VALIZADEH H., SIAHI SHADBAD M.R., ADIBKIA KH., MOHAMMADI GH., DASTMALCHI S., BARZEGAR JALALI A.
 
* DEPARTMENT OF PHARMACEUTICS, SCHOOL OF PHARMACY, TABRIZ UNIVERSITY OF MEDICAL SCIENCES, TABRIZ, IRAN
 
Abstract: 

Carbamazepine belongs to the class II biopharmaceutical classification system (BCS) which is characterized by a high per-oral dose, a low aqueous solubility and a high membrane permeability. The bioavailability of such a drug is limited by the dissolution rate. In order to increase the drug dissolution, its solid dispersions were prepared by the cogrinding technique using an insoluble but highly hydrophilic crospovidone and soluble hydroxypropylmethy1cellulose (HPMC) as the carriers. The ratios of drug to carrier were 1:1, 1:5 and 1:10. Comparison of the dissolution of the drug from its cogrounds with that of the ungrounded drug, its ground form and the corresponding physical mixtures revealed considerable differences. The percentage of drug dissolved during the first 30 min, (%D3o), for the ground and coground drug was 75-95, whereas the %D3o for unground drug and its physical mixtures ranged from 41-62. FT-IR spectra indicated no interaction between the drug and the carriers in the cogrounds. But reduced crystallinity of the drug in the ground and cogrounds was evident in the x-ray diffraction patterns. The decreased crystallinity together with a reduced particle size, enhanced deaggregation and increased wettability of the drug. This could be accounted for the increased dissolution from the cogrounds. From the dissolution point of view, the physical mixtures of HPMC were inferior to the cogrounds, but were slightly superior to the physical mixtures of crospovidone due to the solubilization effect of HPMC.

 
Keyword(s): CARBAMAZEPINE, HPMC, CROSPOVIDONE, COGRINDING, SOLID DISPERSION, DISSOLUTION RATE
 
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