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Fabrication and evaluation of pH-modulated solid dispersion for telmisartan by spray-drying technique.
Int J Pharm. 2013 Jan 30; 441(1-2):424-32.IJ

Abstract

The present study was undertaken to overcome the problems associated with solubility, dissolution and oral bioavailability of a poorly water-soluble ionizable drug, telmisartan (TMS). For these purposes, a solubility test was carried to select the appropriate formulation composition from various carriers and alkalizers. Solid dispersions (SDs) of TMS were prepared at different drug-to-carrier ratios by the spray-drying technique, and were characterized by dissolution and aqueous solubility studies. The optimum formulation was investigated by dissolution studies at different pH and water media and its solid state characterisations were performed by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies. In solubility and dissolution tests, all TMS-loaded pH-modulated SDs (pH(M)-SDs) exhibited marked improvement in the dissolution behavior when compared with crystalline TMS powder. The optimum formulation of pH(M)-SD consisted of TMS/PVP (polyvinylpyrrolidone) K30/Na(2)CO(3) at a weight ratio of 2/0.5/3 and showed significant improvement in the aqueous solubility and dissolution rate by approximately 40,000- and 3-fold, respectively, compared to TMS powder. Solid-state characterization revealed the changed in crystallinity of TMS into amorphous state. Furthermore, area under the drug concentration time-curve (AUC) of TMS from the pH(M)-SD increased by 13.4- and 2.1-fold, compared with TMS powder and commercial product, respectively. According to these observations, taken together with dissolution and pharmacokinetic behaviors, pH-modulated SD in the presence of an alkalizer for a poorly water-soluble ionizable drug, TMS, appeared to be efficacious for enhancing its bioavailability.

Authors+Show Affiliations

College of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Gyungsan, Gyungbuk 712-749, South Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23174408

Citation

Marasini, Nirmal, et al. "Fabrication and Evaluation of pH-modulated Solid Dispersion for Telmisartan By Spray-drying Technique." International Journal of Pharmaceutics, vol. 441, no. 1-2, 2013, pp. 424-32.
Marasini N, Tran TH, Poudel BK, et al. Fabrication and evaluation of pH-modulated solid dispersion for telmisartan by spray-drying technique. Int J Pharm. 2013;441(1-2):424-32.
Marasini, N., Tran, T. H., Poudel, B. K., Cho, H. J., Choi, Y. K., Chi, S. C., Choi, H. G., Yong, C. S., & Kim, J. O. (2013). Fabrication and evaluation of pH-modulated solid dispersion for telmisartan by spray-drying technique. International Journal of Pharmaceutics, 441(1-2), 424-32. https://doi.org/10.1016/j.ijpharm.2012.11.012
Marasini N, et al. Fabrication and Evaluation of pH-modulated Solid Dispersion for Telmisartan By Spray-drying Technique. Int J Pharm. 2013 Jan 30;441(1-2):424-32. PubMed PMID: 23174408.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Fabrication and evaluation of pH-modulated solid dispersion for telmisartan by spray-drying technique. AU - Marasini,Nirmal, AU - Tran,Tuan Hiep, AU - Poudel,Bijay Kumar, AU - Cho,Hyuk Jun, AU - Choi,Young Keun, AU - Chi,Sang-Cheol, AU - Choi,Han-Gon, AU - Yong,Chul Soon, AU - Kim,Jong Oh, Y1 - 2012/11/19/ PY - 2012/07/27/received PY - 2012/10/06/revised PY - 2012/11/09/accepted PY - 2012/11/24/entrez PY - 2012/11/24/pubmed PY - 2013/8/3/medline SP - 424 EP - 32 JF - International journal of pharmaceutics JO - Int J Pharm VL - 441 IS - 1-2 N2 - The present study was undertaken to overcome the problems associated with solubility, dissolution and oral bioavailability of a poorly water-soluble ionizable drug, telmisartan (TMS). For these purposes, a solubility test was carried to select the appropriate formulation composition from various carriers and alkalizers. Solid dispersions (SDs) of TMS were prepared at different drug-to-carrier ratios by the spray-drying technique, and were characterized by dissolution and aqueous solubility studies. The optimum formulation was investigated by dissolution studies at different pH and water media and its solid state characterisations were performed by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray diffraction (XRD) studies. In solubility and dissolution tests, all TMS-loaded pH-modulated SDs (pH(M)-SDs) exhibited marked improvement in the dissolution behavior when compared with crystalline TMS powder. The optimum formulation of pH(M)-SD consisted of TMS/PVP (polyvinylpyrrolidone) K30/Na(2)CO(3) at a weight ratio of 2/0.5/3 and showed significant improvement in the aqueous solubility and dissolution rate by approximately 40,000- and 3-fold, respectively, compared to TMS powder. Solid-state characterization revealed the changed in crystallinity of TMS into amorphous state. Furthermore, area under the drug concentration time-curve (AUC) of TMS from the pH(M)-SD increased by 13.4- and 2.1-fold, compared with TMS powder and commercial product, respectively. According to these observations, taken together with dissolution and pharmacokinetic behaviors, pH-modulated SD in the presence of an alkalizer for a poorly water-soluble ionizable drug, TMS, appeared to be efficacious for enhancing its bioavailability. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/23174408/Fabrication_and_evaluation_of_pH_modulated_solid_dispersion_for_telmisartan_by_spray_drying_technique_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(12)01019-8 DB - PRIME DP - Unbound Medicine ER -