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Effect of semicrystalline polymers on self-emulsifying solid dispersions of nateglinide: in vitro and in vivo evaluation.
Drug Dev Ind Pharm. 2018 Jan; 44(1):56-65.DD

Abstract

This study was undertaken to improve solubility and bioavailability of nateglinide by preparation of stable self-emulsifying solid dispersions (SESDs). The influence of semicrystalline polymers (poloxamer 407, gelucire 50/13) and method of preparation on dissolution behavior, in vivo performance and stability of nateglinide SESDs were investigated. After optimization, SESDs were prepared at 1:5 weight ratio of nateglinide and polymer individually. All the SESDs were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction and scanning electron microscopy. Aqueous solubility of nateglinide was enhanced by 91.82-fold. The SESDs (poloxamer 407-based solid dispersions) achieved rapid and complete drug release (∼100% within 45 min) at pH 2. The improved dissolution appeared to be well correlated with the enhanced bioavailability of nateglinide in rabbits. After oral administration of SESDs (poloxamer 407-based solid dispersions), Cmax and AUC of nateglinide were increased by ∼2.92 and 1.77-folds, respectively, signifying the effectiveness of solid dispersions to improve the bioavailability of nateglinide. Stability during storage was established to show prevention of recrystallization. In conclusion, SESDs with poloxamer 407 in solvent method appeared to be an economic and promising technique to improve the dissolution, bioavailability, and stability of nateglinide.

Authors+Show Affiliations

a Drug Development and Analysis Laboratory, School of Pharmaceutical Sciences , Siksha O Anusandhan University , Bhubaneswar , India. b Department of Pharmaceutical Technology , Maharajah's College of Pharmacy , Vizianagaram , India.a Drug Development and Analysis Laboratory, School of Pharmaceutical Sciences , Siksha O Anusandhan University , Bhubaneswar , India.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28845687

Citation

Swain, Ranjit Prasad, and Bharat Bhusan Subudhi. "Effect of Semicrystalline Polymers On Self-emulsifying Solid Dispersions of Nateglinide: in Vitro and in Vivo Evaluation." Drug Development and Industrial Pharmacy, vol. 44, no. 1, 2018, pp. 56-65.
Swain RP, Subudhi BB. Effect of semicrystalline polymers on self-emulsifying solid dispersions of nateglinide: in vitro and in vivo evaluation. Drug Dev Ind Pharm. 2018;44(1):56-65.
Swain, R. P., & Subudhi, B. B. (2018). Effect of semicrystalline polymers on self-emulsifying solid dispersions of nateglinide: in vitro and in vivo evaluation. Drug Development and Industrial Pharmacy, 44(1), 56-65. https://doi.org/10.1080/03639045.2017.1371739
Swain RP, Subudhi BB. Effect of Semicrystalline Polymers On Self-emulsifying Solid Dispersions of Nateglinide: in Vitro and in Vivo Evaluation. Drug Dev Ind Pharm. 2018;44(1):56-65. PubMed PMID: 28845687.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of semicrystalline polymers on self-emulsifying solid dispersions of nateglinide: in vitro and in vivo evaluation. AU - Swain,Ranjit Prasad, AU - Subudhi,Bharat Bhusan, Y1 - 2017/09/11/ PY - 2017/8/29/pubmed PY - 2018/1/13/medline PY - 2017/8/29/entrez KW - Nateglinide KW - bioavailability KW - recrystallization KW - self-emulsifying solid dispersion KW - semicrystalline polymer SP - 56 EP - 65 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 44 IS - 1 N2 - This study was undertaken to improve solubility and bioavailability of nateglinide by preparation of stable self-emulsifying solid dispersions (SESDs). The influence of semicrystalline polymers (poloxamer 407, gelucire 50/13) and method of preparation on dissolution behavior, in vivo performance and stability of nateglinide SESDs were investigated. After optimization, SESDs were prepared at 1:5 weight ratio of nateglinide and polymer individually. All the SESDs were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction and scanning electron microscopy. Aqueous solubility of nateglinide was enhanced by 91.82-fold. The SESDs (poloxamer 407-based solid dispersions) achieved rapid and complete drug release (∼100% within 45 min) at pH 2. The improved dissolution appeared to be well correlated with the enhanced bioavailability of nateglinide in rabbits. After oral administration of SESDs (poloxamer 407-based solid dispersions), Cmax and AUC of nateglinide were increased by ∼2.92 and 1.77-folds, respectively, signifying the effectiveness of solid dispersions to improve the bioavailability of nateglinide. Stability during storage was established to show prevention of recrystallization. In conclusion, SESDs with poloxamer 407 in solvent method appeared to be an economic and promising technique to improve the dissolution, bioavailability, and stability of nateglinide. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/28845687/Effect_of_semicrystalline_polymers_on_self_emulsifying_solid_dispersions_of_nateglinide:_in_vitro_and_in_vivo_evaluation_ L2 - https://www.tandfonline.com/doi/full/10.1080/03639045.2017.1371739 DB - PRIME DP - Unbound Medicine ER -