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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

X-Ray diffractograms of (a) BUD, (b) PXM, and (c) optimized SD (1 : 3).
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fig3: X-Ray diffractograms of (a) BUD, (b) PXM, and (c) optimized SD (1 : 3).

Mentions: The X-ray diffractogram of pure Budesonide (Figure 3(a)) clearly showed the peak indicating that the drug is in crystalline form. The peak intensity of drug in solid dispersion (Figure 3(c)) was reduced, indicating that the drug was converted into amorphous nature. In the X-ray diffractograms of BUD, sharp peaks at a diffraction angle of 5°, 10°, 11°, 12°, 15°, 16°, and 22° indicate the crystallinity of the drug. The solid dispersion showed sharp peaks at 11.7°, 16°, and 16.5° revealed that some of the crystalline peaks of the drug were still detectable but with reduced intensity and less number in the diffractogram. This data confirms that the little amount of crystalline drug is still present in the solid dispersion although the complete disappearance of its melting peak in the corresponding DSC curves. The sharp drug peaks of drug are absent in the diffractogram of solid dispersion. This indicates that crystallinity of drug is reduced in the solid dispersion which leads enhancement of dissolution of the drug.


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

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

X-Ray diffractograms of (a) BUD, (b) PXM, and (c) optimized SD (1 : 3).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig3: X-Ray diffractograms of (a) BUD, (b) PXM, and (c) optimized SD (1 : 3).
Mentions: The X-ray diffractogram of pure Budesonide (Figure 3(a)) clearly showed the peak indicating that the drug is in crystalline form. The peak intensity of drug in solid dispersion (Figure 3(c)) was reduced, indicating that the drug was converted into amorphous nature. In the X-ray diffractograms of BUD, sharp peaks at a diffraction angle of 5°, 10°, 11°, 12°, 15°, 16°, and 22° indicate the crystallinity of the drug. The solid dispersion showed sharp peaks at 11.7°, 16°, and 16.5° revealed that some of the crystalline peaks of the drug were still detectable but with reduced intensity and less number in the diffractogram. This data confirms that the little amount of crystalline drug is still present in the solid dispersion although the complete disappearance of its melting peak in the corresponding DSC curves. The sharp drug peaks of drug are absent in the diffractogram of solid dispersion. This indicates that crystallinity of drug is reduced in the solid dispersion which leads enhancement of dissolution of the drug.

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