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Solubility Enhancement of Budesonide and Statistical Optimization of Coating Variables for Targeted Drug Delivery.

Bhatt H, Naik B, Dharamsi A - J Pharm (Cairo) (2014)

Bottom Line: Variables studied in design were ratio of enteric polymers and the effect of percentage coating on in vitro drug release.The optimized batch from statistical design was kept under accelerated condition for three months.After accelerated stability study, there was no significant change in the drug release.

View Article: PubMed Central - PubMed

Affiliation: National Institute of Pharmaceutical Education and Research (NIPER), B. V. Patel Pharmaceutical Education and Research Development (PERD), S G Highway, Thaltej, Ahmedabad 380054, India.

ABSTRACT
The purpose of the research was to present Budesonide (BUD) as a novel formulation showing improved aqueous solubility, which may decrease variability in C max⁡ and T max⁡ found in inflammatory bowel disease (IBD) patients, and drug targeting to colon. To improve aqueous solubility, solid dispersion (SD) of the BUD with poloxamer 188 was prepared by melting method. Physical characterization of solid dispersion was performed. The SD was used to prepare tablet equivalent to 9 mg of BUD. The tablet was coated with enteric polymers Eudragit S100 and Eudragit L100 to target colon. The ratio of polymers and percentage coating was optimized using statistical design. Variables studied in design were ratio of enteric polymers and the effect of percentage coating on in vitro drug release. Dissolution at different pH showed that drug release in colon could be modified by optimizing the ratio of polymers and percentage coating. The dissolution data showed that the percentage coating and ratio of polymers are very important to get lag time and optimum formulation. The optimized batch from statistical design was kept under accelerated condition for three months. After accelerated stability study, there was no significant change in the drug release.

No MeSH data available.


Related in: MedlinePlus

2D contour plot of Y2.
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Related In: Results  -  Collection


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fig7: 2D contour plot of Y2.

Mentions: Two-dimensional contour plots and 3D response surface plots are shown in Figures 5, 6, 7, 8, 9, 10, 11, and 12 which are very useful to study the interaction effects of the factors on the responses. These types of plots are useful in the study of the effects of two factors on the response at one time. All the relationships among the two variables are nonlinear, although they exhibit a nearly linear relationship as shown in Figures 5, 6, 7, 8, 9, 10, 11, and 12.


Solubility Enhancement of Budesonide and Statistical Optimization of Coating Variables for Targeted Drug Delivery.

Bhatt H, Naik B, Dharamsi A - J Pharm (Cairo) (2014)

2D contour plot of Y2.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590827&req=5

fig7: 2D contour plot of Y2.
Mentions: Two-dimensional contour plots and 3D response surface plots are shown in Figures 5, 6, 7, 8, 9, 10, 11, and 12 which are very useful to study the interaction effects of the factors on the responses. These types of plots are useful in the study of the effects of two factors on the response at one time. All the relationships among the two variables are nonlinear, although they exhibit a nearly linear relationship as shown in Figures 5, 6, 7, 8, 9, 10, 11, and 12.

Bottom Line: Variables studied in design were ratio of enteric polymers and the effect of percentage coating on in vitro drug release.The optimized batch from statistical design was kept under accelerated condition for three months.After accelerated stability study, there was no significant change in the drug release.

View Article: PubMed Central - PubMed

Affiliation: National Institute of Pharmaceutical Education and Research (NIPER), B. V. Patel Pharmaceutical Education and Research Development (PERD), S G Highway, Thaltej, Ahmedabad 380054, India.

ABSTRACT
The purpose of the research was to present Budesonide (BUD) as a novel formulation showing improved aqueous solubility, which may decrease variability in C max⁡ and T max⁡ found in inflammatory bowel disease (IBD) patients, and drug targeting to colon. To improve aqueous solubility, solid dispersion (SD) of the BUD with poloxamer 188 was prepared by melting method. Physical characterization of solid dispersion was performed. The SD was used to prepare tablet equivalent to 9 mg of BUD. The tablet was coated with enteric polymers Eudragit S100 and Eudragit L100 to target colon. The ratio of polymers and percentage coating was optimized using statistical design. Variables studied in design were ratio of enteric polymers and the effect of percentage coating on in vitro drug release. Dissolution at different pH showed that drug release in colon could be modified by optimizing the ratio of polymers and percentage coating. The dissolution data showed that the percentage coating and ratio of polymers are very important to get lag time and optimum formulation. The optimized batch from statistical design was kept under accelerated condition for three months. After accelerated stability study, there was no significant change in the drug release.

No MeSH data available.


Related in: MedlinePlus