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Effect of hydrophilic diluents on the release profile of griseofulvin from tablet formulations.

Umeh ON, Azegba JC, Ofoefule SI - Indian J Pharm Sci (2013)

Bottom Line: Based on these reports, the present study was undertaken to investigate the effect of some commonly used hydrophilic tablet diluents (lactose, sucrose, mannitol and dextrose) on the in vitro release properties of griseofulvin from compressed tablets.The relative enhanced dissolution effects of the four hydrophilic diluents is in the order of dextrose>sucrose>lactose>mannitol.The results of the dissolution efficiency (DE60min) are 91.7, 83.5, 48.7, 35.3 and 15.6% for dextrose, sucrose, lactose, mannitol and fulcin(®), respectively.

View Article: PubMed Central - PubMed

Affiliation: Departments of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka-410 001, Enugu state, Nigeria.

ABSTRACT
Studies have shown that when compressing drugs with low aqueous solubility, the solubility of diluents selected is very crucial as it influences the disintegration, dissolution and bioavailability of such drugs. Based on these reports, the present study was undertaken to investigate the effect of some commonly used hydrophilic tablet diluents (lactose, sucrose, mannitol and dextrose) on the in vitro release properties of griseofulvin from compressed tablets. Griseofulvin granules and tablets were prepared using the wet granulation method. Tablet properties evaluated as a function of the diluents used include, hardness, friability, dissolution profile and dissolution efficiency at 60 min. Results obtained indicated variability in griseofulvin release in the presence of the diluents. The relative enhanced dissolution effects of the four hydrophilic diluents is in the order of dextrose>sucrose>lactose>mannitol. All the griseofulvin tablet batches produced exhibited a better drug release (in terms of rate and extent of release) than a commercially available tablet sample of griseofulvin (Fulcin(®)). The results of the dissolution efficiency (DE60min) are 91.7, 83.5, 48.7, 35.3 and 15.6% for dextrose, sucrose, lactose, mannitol and fulcin(®), respectively. The overall results indicated that dextrose or sucrose can be utilised to improve the in vitro release profile and hence in vivo bioavailability of griseofulvin from compressed tablets.

No MeSH data available.


Related in: MedlinePlus

Release profiles of griseofulvin from the formulated and commercial SamplesThe percentage concentration of griseofulvin released from the lactose (─♦─), sucrose (─■─), mannitol (─▲─) and dextrose (─×─) formulations were compared with that of fulcin® (─ж─), a commercially available sample. There was a significant increase (P<0.05) in the amount of griseofulvin released from the batches containing the four hydrophilic diluents than from the Fulcin® tablets.
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Figure 1: Release profiles of griseofulvin from the formulated and commercial SamplesThe percentage concentration of griseofulvin released from the lactose (─♦─), sucrose (─■─), mannitol (─▲─) and dextrose (─×─) formulations were compared with that of fulcin® (─ж─), a commercially available sample. There was a significant increase (P<0.05) in the amount of griseofulvin released from the batches containing the four hydrophilic diluents than from the Fulcin® tablets.

Mentions: The presence of the diluents had variable effects on the hardness and friability of the tablets (Table 2). According to some published works, uncoated tablets with hardness of ≥4 kgf are considered adequate for handling and transportation[89]. From the results (Table 2), all the tablet batches are considered adequate in terms of hardness. The results for friability, also indicate that all the batches were within the acceptable limit of ˂1%[89]. The assay results of the batches ranged from 90.0 to 100.9% (Table 2). All the batches except the commercial sample (Fulcin®) had released up to 70% of griseofulvin within 45 min. There was a decrease in T50 (time taken for 50% of the drug to be released) as the DE increased. Batch D containing dextrose as diluent, had the highest DE while the commercial griseofulvin (Fulcin®) tablets had the least DE of 15.6%. A graphical representation of the dissolution profiles of the griseofulvin tablet batches are shown in fig. 1. Dextrose and sucrose enhanced the release of griseofulvin from the tablets than lactose and mannitol.


Effect of hydrophilic diluents on the release profile of griseofulvin from tablet formulations.

Umeh ON, Azegba JC, Ofoefule SI - Indian J Pharm Sci (2013)

Release profiles of griseofulvin from the formulated and commercial SamplesThe percentage concentration of griseofulvin released from the lactose (─♦─), sucrose (─■─), mannitol (─▲─) and dextrose (─×─) formulations were compared with that of fulcin® (─ж─), a commercially available sample. There was a significant increase (P<0.05) in the amount of griseofulvin released from the batches containing the four hydrophilic diluents than from the Fulcin® tablets.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3928738&req=5

Figure 1: Release profiles of griseofulvin from the formulated and commercial SamplesThe percentage concentration of griseofulvin released from the lactose (─♦─), sucrose (─■─), mannitol (─▲─) and dextrose (─×─) formulations were compared with that of fulcin® (─ж─), a commercially available sample. There was a significant increase (P<0.05) in the amount of griseofulvin released from the batches containing the four hydrophilic diluents than from the Fulcin® tablets.
Mentions: The presence of the diluents had variable effects on the hardness and friability of the tablets (Table 2). According to some published works, uncoated tablets with hardness of ≥4 kgf are considered adequate for handling and transportation[89]. From the results (Table 2), all the tablet batches are considered adequate in terms of hardness. The results for friability, also indicate that all the batches were within the acceptable limit of ˂1%[89]. The assay results of the batches ranged from 90.0 to 100.9% (Table 2). All the batches except the commercial sample (Fulcin®) had released up to 70% of griseofulvin within 45 min. There was a decrease in T50 (time taken for 50% of the drug to be released) as the DE increased. Batch D containing dextrose as diluent, had the highest DE while the commercial griseofulvin (Fulcin®) tablets had the least DE of 15.6%. A graphical representation of the dissolution profiles of the griseofulvin tablet batches are shown in fig. 1. Dextrose and sucrose enhanced the release of griseofulvin from the tablets than lactose and mannitol.

Bottom Line: Based on these reports, the present study was undertaken to investigate the effect of some commonly used hydrophilic tablet diluents (lactose, sucrose, mannitol and dextrose) on the in vitro release properties of griseofulvin from compressed tablets.The relative enhanced dissolution effects of the four hydrophilic diluents is in the order of dextrose>sucrose>lactose>mannitol.The results of the dissolution efficiency (DE60min) are 91.7, 83.5, 48.7, 35.3 and 15.6% for dextrose, sucrose, lactose, mannitol and fulcin(®), respectively.

View Article: PubMed Central - PubMed

Affiliation: Departments of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka-410 001, Enugu state, Nigeria.

ABSTRACT
Studies have shown that when compressing drugs with low aqueous solubility, the solubility of diluents selected is very crucial as it influences the disintegration, dissolution and bioavailability of such drugs. Based on these reports, the present study was undertaken to investigate the effect of some commonly used hydrophilic tablet diluents (lactose, sucrose, mannitol and dextrose) on the in vitro release properties of griseofulvin from compressed tablets. Griseofulvin granules and tablets were prepared using the wet granulation method. Tablet properties evaluated as a function of the diluents used include, hardness, friability, dissolution profile and dissolution efficiency at 60 min. Results obtained indicated variability in griseofulvin release in the presence of the diluents. The relative enhanced dissolution effects of the four hydrophilic diluents is in the order of dextrose>sucrose>lactose>mannitol. All the griseofulvin tablet batches produced exhibited a better drug release (in terms of rate and extent of release) than a commercially available tablet sample of griseofulvin (Fulcin(®)). The results of the dissolution efficiency (DE60min) are 91.7, 83.5, 48.7, 35.3 and 15.6% for dextrose, sucrose, lactose, mannitol and fulcin(®), respectively. The overall results indicated that dextrose or sucrose can be utilised to improve the in vitro release profile and hence in vivo bioavailability of griseofulvin from compressed tablets.

No MeSH data available.


Related in: MedlinePlus