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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

(a) Contour plot showing the relationship between various levels of 2 independent variables. (b) Response surface plot showing the influence of film forming polymer (PVA) and superdisintegrant (SSG) over disintegration time. (c) Corresponding plot showing the interaction between two factors.
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fig5: (a) Contour plot showing the relationship between various levels of 2 independent variables. (b) Response surface plot showing the influence of film forming polymer (PVA) and superdisintegrant (SSG) over disintegration time. (c) Corresponding plot showing the interaction between two factors.

Mentions: The results of multiple linear regression analysis are shown in Table 6, indicating that for all response variables which are disintegration time, tensile strength, and % drug release, the amount of PVA (X1) had a negative effect while the concentration of SSG (X2) had a positive effect; it means that as the amount of SSG increases the tensile strength, disintegration time decreases and there is increase in % drug release, while as the amount of PVA is increased, both the tensile strength and disintegration time increase [34–36]. Therefore, high level of SSG and medium level of PVA should be selected for the rapid disintegration and a faster in vitro drug release of the film. The observed values are in good agreement with the predicted values for the optimized formulation, which demonstrate the feasibility of surface response method in the formulation of oral fast dissolving films. The comparison of observed values and predicted values with % prediction error is shown in Table 7. The data of the response surface plot as shown in Figures 5, 6, and 7 demonstrated that both X1 and X2 affect the disintegration time, tensile strength, and % release of drug.


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

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

(a) Contour plot showing the relationship between various levels of 2 independent variables. (b) Response surface plot showing the influence of film forming polymer (PVA) and superdisintegrant (SSG) over disintegration time. (c) Corresponding plot showing the interaction between two factors.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig5: (a) Contour plot showing the relationship between various levels of 2 independent variables. (b) Response surface plot showing the influence of film forming polymer (PVA) and superdisintegrant (SSG) over disintegration time. (c) Corresponding plot showing the interaction between two factors.
Mentions: The results of multiple linear regression analysis are shown in Table 6, indicating that for all response variables which are disintegration time, tensile strength, and % drug release, the amount of PVA (X1) had a negative effect while the concentration of SSG (X2) had a positive effect; it means that as the amount of SSG increases the tensile strength, disintegration time decreases and there is increase in % drug release, while as the amount of PVA is increased, both the tensile strength and disintegration time increase [34–36]. Therefore, high level of SSG and medium level of PVA should be selected for the rapid disintegration and a faster in vitro drug release of the film. The observed values are in good agreement with the predicted values for the optimized formulation, which demonstrate the feasibility of surface response method in the formulation of oral fast dissolving films. The comparison of observed values and predicted values with % prediction error is shown in Table 7. The data of the response surface plot as shown in Figures 5, 6, and 7 demonstrated that both X1 and X2 affect the disintegration time, tensile strength, and % release of drug.

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