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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

IR spectra of (a) BUD, (b) PXB, (c) optimized SD, and (d) Physical mixture.
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fig1: IR spectra of (a) BUD, (b) PXB, (c) optimized SD, and (d) Physical mixture.

Mentions: BUD may exist in the solid dispersion in 2 different forms, namely, crystalline and amorphous. The dissolution rate of solid dispersion depends on the proportion of the 2 forms, which in turn depends on the proportion of PXM in the solid dispersion. An enhancement of dissolution of BUD because of the proportion of the amorphous form of BUD may increase because of increase in weight fraction of PXM up to its saturated solubility [16, 17]. The solubility study was done in water in different ratios of BUD and PXM. The ratio 1 : 3 showed maximum solubility as compared to other ratios. The solubility decreased beyond 1 : 3 due to increase in proportion of the crystalline form of BUD in solid dispersion at higher ratio. The data of saturated solubility of solid dispersion are shown in Table 4 and FTIR of optimized solid dispersion as shown in Figure 1(c).


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

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

IR spectra of (a) BUD, (b) PXB, (c) optimized SD, and (d) Physical mixture.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig1: IR spectra of (a) BUD, (b) PXB, (c) optimized SD, and (d) Physical mixture.
Mentions: BUD may exist in the solid dispersion in 2 different forms, namely, crystalline and amorphous. The dissolution rate of solid dispersion depends on the proportion of the 2 forms, which in turn depends on the proportion of PXM in the solid dispersion. An enhancement of dissolution of BUD because of the proportion of the amorphous form of BUD may increase because of increase in weight fraction of PXM up to its saturated solubility [16, 17]. The solubility study was done in water in different ratios of BUD and PXM. The ratio 1 : 3 showed maximum solubility as compared to other ratios. The solubility decreased beyond 1 : 3 due to increase in proportion of the crystalline form of BUD in solid dispersion at higher ratio. The data of saturated solubility of solid dispersion are shown in Table 4 and FTIR of optimized solid dispersion as shown in Figure 1(c).

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