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Development and characterization of solid oral dosage form incorporating candesartan nanoparticles.
Pharm Dev Technol. 2009; 14(3):290-8.PD

Abstract

Sparingly water-soluble drugs such as candesartan cilexetil offer challenges in developing a drug product with adequate bioavailability. The objective of the present study was to develop a tablet dosage form of candesartan cilexetil incorporating drug nanoparticles to increase its saturation solubility and dissolution rate for enhancing bioavailability while reducing variability in systemic exposure. The bioavailability of candesartan cilexetil is dissolution limited following oral administration. To enhance bioavailability and overcome variability in systemic exposure, a nanoparticle formulation of candesartan cilexetil was developed. Candesartan cilexetil nanoparticles were prepared using a wet bead milling technique. The milled nanosuspension was converted into solid intermediate using a spray drying process. The nanosuspensions were characterized for particle size before and after spray drying. The spray dried nanoparticles were blended with excipients for tableting. The saturation solubility and dissolution characteristics of the nanoparticle formulation were investigated and compared with commercial candesartan cilexetil formulation. The drug nanoparticles were evaluated for solid-state transitions before and after milling. This study demonstrated that tablet formulation incorporating drug nanoparticles showed significantly faster rate of drug dissolution in a discriminating dissolution medium as compared to commercially available tablet formulation. Systemic exposure studies in rats indicated a significant increase in the rate and extent of drug absorption.

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Authors+Show Affiliations

Nekkanti V
NCE and CPS Product Development, Dr Reddy's Laboratories Limited, Hyderabad, India.
Pillai R
No affiliation info available
Venkateshwarlu V
No affiliation info available
Harisudhan T
No affiliation info available

MeSH

Administration, OralAngiotensin II Type 1 Receptor BlockersAnimalsBenzimidazolesBiphenyl CompoundsDosage FormsDrug CompoundingEquipment DesignMaleNanoparticlesParticle SizeRatsRats, WistarSolubilityTetrazoles

Pub Type(s)

Journal Article

Language

eng

PubMed ID

19235553

Citation

Nekkanti, Vijaykumar, et al. "Development and Characterization of Solid Oral Dosage Form Incorporating Candesartan Nanoparticles." Pharmaceutical Development and Technology, vol. 14, no. 3, 2009, pp. 290-8.
Nekkanti V, Pillai R, Venkateshwarlu V, et al. Development and characterization of solid oral dosage form incorporating candesartan nanoparticles. Pharm Dev Technol. 2009;14(3):290-8.
Nekkanti, V., Pillai, R., Venkateshwarlu, V., & Harisudhan, T. (2009). Development and characterization of solid oral dosage form incorporating candesartan nanoparticles. Pharmaceutical Development and Technology, 14(3), 290-8. https://doi.org/10.1080/10837450802585278
Nekkanti V, et al. Development and Characterization of Solid Oral Dosage Form Incorporating Candesartan Nanoparticles. Pharm Dev Technol. 2009;14(3):290-8. PubMed PMID: 19235553.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development and characterization of solid oral dosage form incorporating candesartan nanoparticles. AU - Nekkanti,Vijaykumar, AU - Pillai,Raviraj, AU - Venkateshwarlu,Vobalaboina, AU - Harisudhan,T, PY - 2009/2/25/entrez PY - 2009/2/25/pubmed PY - 2010/10/29/medline SP - 290 EP - 8 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 14 IS - 3 N2 - Sparingly water-soluble drugs such as candesartan cilexetil offer challenges in developing a drug product with adequate bioavailability. The objective of the present study was to develop a tablet dosage form of candesartan cilexetil incorporating drug nanoparticles to increase its saturation solubility and dissolution rate for enhancing bioavailability while reducing variability in systemic exposure. The bioavailability of candesartan cilexetil is dissolution limited following oral administration. To enhance bioavailability and overcome variability in systemic exposure, a nanoparticle formulation of candesartan cilexetil was developed. Candesartan cilexetil nanoparticles were prepared using a wet bead milling technique. The milled nanosuspension was converted into solid intermediate using a spray drying process. The nanosuspensions were characterized for particle size before and after spray drying. The spray dried nanoparticles were blended with excipients for tableting. The saturation solubility and dissolution characteristics of the nanoparticle formulation were investigated and compared with commercial candesartan cilexetil formulation. The drug nanoparticles were evaluated for solid-state transitions before and after milling. This study demonstrated that tablet formulation incorporating drug nanoparticles showed significantly faster rate of drug dissolution in a discriminating dissolution medium as compared to commercially available tablet formulation. Systemic exposure studies in rats indicated a significant increase in the rate and extent of drug absorption. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/19235553/Development_and_characterization_of_solid_oral_dosage_form_incorporating_candesartan_nanoparticles_ L2 - https://www.tandfonline.com/doi/full/10.1080/10837450802585278 DB - PRIME DP - Unbound Medicine ER -