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Design optimization and in vitro-in vivo evaluation of orally dissolving strips of clobazam.

Bala R, Khanna S, Pawar P - J Drug Deliv (2014)

Bottom Line: Formulation (F6) was selected by the Design-expert software which exhibited DT (24 sec), TS (2.85 N/cm(2)), and in vitro drug release (96.6%).Statistical evaluation revealed no significant difference between the bioavailability parameters of the test film (F6) and the reference product.The mean ratio values (test/reference) of C max (95.87%), t max (71.42%), AUC0-t (98.125%), and AUC0-∞ (99.213%) indicated that the two formulae exhibited comparable plasma level-time profiles.

View Article: PubMed Central - PubMed

Affiliation: Chitkara College of Pharmacy, Chandigarh-Patiala National Highway, Rajpura, Patiala, Punjab 140 401, India.

ABSTRACT
Clobazam orally dissolving strips were prepared by solvent casting method. A full 3(2) factorial design was applied for optimization using different concentration of film forming polymer and disintegrating agent as independent variable and disintegration time, % cumulative drug release, and tensile strength as dependent variable. In addition the prepared films were also evaluated for surface pH, folding endurance, and content uniformity. The optimized film formulation showing the maximum in vitro drug release, satisfactory in vitro disintegration time, and tensile strength was selected for bioavailability study and compared with a reference marketed product (frisium5 tablets) in rabbits. Formulation (F6) was selected by the Design-expert software which exhibited DT (24 sec), TS (2.85 N/cm(2)), and in vitro drug release (96.6%). Statistical evaluation revealed no significant difference between the bioavailability parameters of the test film (F6) and the reference product. The mean ratio values (test/reference) of C max (95.87%), t max (71.42%), AUC0-t (98.125%), and AUC0-∞ (99.213%) indicated that the two formulae exhibited comparable plasma level-time profiles.

No MeSH data available.


Related in: MedlinePlus

Bioavailability study on clobazam optimized ODF F6 and marketed formulation (frisium5).
© Copyright Policy - open-access
Related In: Results  -  Collection


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fig12: Bioavailability study on clobazam optimized ODF F6 and marketed formulation (frisium5).

Mentions: The study was conducted in accordance with the principles of laboratory animal care. Six rabbits of either sex (weighed 2.5 ± 0.2 kg) were selected for the study. All the rabbits were healthy during the period of study. All the rabbits were fasted overnight before the administration of the selected fast dissolving film and marketed formulation but had free access to water. The rabbits were randomly divided into two groups with each group containing three rabbits (n = 3). The rabbits were positioned on a table with lower jaw supported in a horizontal position and orally dissolving strip was carefully placed on the rabbit tongue in one group as shown in Figure 12. The marketed tablet was administered orally to another group. Blood samples for pharmacokinetic analysis were collected from marginal ear veins of rabbits immediately before drug administration and at 5, 10, 15, 30, 60, 120, 180 min, 6 hrs, 12, and 24 hrs interval. The plasma samples were prepared by mixing 0.1 mL of plasma with 0.05 mL ibuprofen as internal standard (from the stock 6000 ng/mL) in a clean Eppendorf polypropylene tube and then extracting with 1.5 mL of acetonitrile after vertical agitation (1 min) and centrifugation at 1000 rpm, for 5 min. The upper organic layer was injected onto the HPLC system for analysis. The HPLC analysis was performed using Agilent 1200 series system by using a mobile phase composed of water pH 3.5, adjusted with orthophosphoric acid and acetonitrile (55 : 45 v/v), and binary eluted at a flow rate of 1.5 mL min−1 [30]. Protocols for all the animal studies were approved by institutional ethical committee [IAEC/CCP/12/PR-007].


Design optimization and in vitro-in vivo evaluation of orally dissolving strips of clobazam.

Bala R, Khanna S, Pawar P - J Drug Deliv (2014)

Bioavailability study on clobazam optimized ODF F6 and marketed formulation (frisium5).
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4195261&req=5

fig12: Bioavailability study on clobazam optimized ODF F6 and marketed formulation (frisium5).
Mentions: The study was conducted in accordance with the principles of laboratory animal care. Six rabbits of either sex (weighed 2.5 ± 0.2 kg) were selected for the study. All the rabbits were healthy during the period of study. All the rabbits were fasted overnight before the administration of the selected fast dissolving film and marketed formulation but had free access to water. The rabbits were randomly divided into two groups with each group containing three rabbits (n = 3). The rabbits were positioned on a table with lower jaw supported in a horizontal position and orally dissolving strip was carefully placed on the rabbit tongue in one group as shown in Figure 12. The marketed tablet was administered orally to another group. Blood samples for pharmacokinetic analysis were collected from marginal ear veins of rabbits immediately before drug administration and at 5, 10, 15, 30, 60, 120, 180 min, 6 hrs, 12, and 24 hrs interval. The plasma samples were prepared by mixing 0.1 mL of plasma with 0.05 mL ibuprofen as internal standard (from the stock 6000 ng/mL) in a clean Eppendorf polypropylene tube and then extracting with 1.5 mL of acetonitrile after vertical agitation (1 min) and centrifugation at 1000 rpm, for 5 min. The upper organic layer was injected onto the HPLC system for analysis. The HPLC analysis was performed using Agilent 1200 series system by using a mobile phase composed of water pH 3.5, adjusted with orthophosphoric acid and acetonitrile (55 : 45 v/v), and binary eluted at a flow rate of 1.5 mL min−1 [30]. Protocols for all the animal studies were approved by institutional ethical committee [IAEC/CCP/12/PR-007].

Bottom Line: Formulation (F6) was selected by the Design-expert software which exhibited DT (24 sec), TS (2.85 N/cm(2)), and in vitro drug release (96.6%).Statistical evaluation revealed no significant difference between the bioavailability parameters of the test film (F6) and the reference product.The mean ratio values (test/reference) of C max (95.87%), t max (71.42%), AUC0-t (98.125%), and AUC0-∞ (99.213%) indicated that the two formulae exhibited comparable plasma level-time profiles.

View Article: PubMed Central - PubMed

Affiliation: Chitkara College of Pharmacy, Chandigarh-Patiala National Highway, Rajpura, Patiala, Punjab 140 401, India.

ABSTRACT
Clobazam orally dissolving strips were prepared by solvent casting method. A full 3(2) factorial design was applied for optimization using different concentration of film forming polymer and disintegrating agent as independent variable and disintegration time, % cumulative drug release, and tensile strength as dependent variable. In addition the prepared films were also evaluated for surface pH, folding endurance, and content uniformity. The optimized film formulation showing the maximum in vitro drug release, satisfactory in vitro disintegration time, and tensile strength was selected for bioavailability study and compared with a reference marketed product (frisium5 tablets) in rabbits. Formulation (F6) was selected by the Design-expert software which exhibited DT (24 sec), TS (2.85 N/cm(2)), and in vitro drug release (96.6%). Statistical evaluation revealed no significant difference between the bioavailability parameters of the test film (F6) and the reference product. The mean ratio values (test/reference) of C max (95.87%), t max (71.42%), AUC0-t (98.125%), and AUC0-∞ (99.213%) indicated that the two formulae exhibited comparable plasma level-time profiles.

No MeSH data available.


Related in: MedlinePlus