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Effect of auxiliary substances on complexation efficiency and intrinsic dissolution rate of gemfibrozil-beta-CD complexes.
AAPS PharmSciTech. 2010 Mar; 11(1):27-35.AP

Abstract

The studies reported in this work are aimed to elucidate the ternary inclusion complex formation of gemfibrozil (GFZ), a poorly water-soluble drug, with beta-cyclodextrin (beta-CD) with the aid of auxiliary substances like different grades of povidone(s) (viz. PVP K-29/32, PVP K-40, Plasdone S-630, and Polyplasdone XL), organic base (viz. triethanolamine), and metal ion (viz. MgCl(2).6H(2)O), by investigating their interactions in solution and solid state. Phase solubility studies were carried out to evaluate the solubilizing power of beta-cyclodextrin, in association with various auxiliary substances, to determine the apparent stability constant (K (C)) and complexation efficiency (CE) of complexes. Improvement in K (C) values for ternary complexes clearly proves the benefit of the addition of auxiliary substances to promote CE. Of all the approaches used, the use of polymer Plasdone S-630 was found to be the most promising approach in terms of optimum CE and K (C). GFZ-beta-CD (1:1) binary and ternary systems were prepared by kneading and lyophilization methods. The ternary systems clearly signified superiority over binary systems in terms of CE, solubility, K (C), and reduction in the formulation bulk. Optimized ternary system of GFZ-beta-CD-Plasdone S-630 prepared by using lyophilization method indicated a significant improvement in intrinsic dissolution rate when compared with ternary kneaded system. Differential scanning calorimetry, X-ray diffraction, Fourier transform infrared, scanning electron microscopy, and proton nuclear magnetic resonance were carried out to characterize the binary and optimized ternary complex. The results suggested the formation of new solid phases, eliciting strong evidences of ternary inclusion complex formation between GFZ, beta-CD, and Plasdone S-630, particularly for lyophilized products.

Authors+Show Affiliations

Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura 286001, Uttar Pradesh, India.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

20013079

Citation

Sami, Fareen, et al. "Effect of Auxiliary Substances On Complexation Efficiency and Intrinsic Dissolution Rate of gemfibrozil-beta-CD Complexes." AAPS PharmSciTech, vol. 11, no. 1, 2010, pp. 27-35.
Sami F, Philip B, Pathak K. Effect of auxiliary substances on complexation efficiency and intrinsic dissolution rate of gemfibrozil-beta-CD complexes. AAPS PharmSciTech. 2010;11(1):27-35.
Sami, F., Philip, B., & Pathak, K. (2010). Effect of auxiliary substances on complexation efficiency and intrinsic dissolution rate of gemfibrozil-beta-CD complexes. AAPS PharmSciTech, 11(1), 27-35. https://doi.org/10.1208/s12249-009-9350-y
Sami F, Philip B, Pathak K. Effect of Auxiliary Substances On Complexation Efficiency and Intrinsic Dissolution Rate of gemfibrozil-beta-CD Complexes. AAPS PharmSciTech. 2010;11(1):27-35. PubMed PMID: 20013079.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of auxiliary substances on complexation efficiency and intrinsic dissolution rate of gemfibrozil-beta-CD complexes. AU - Sami,Fareen, AU - Philip,Betty, AU - Pathak,Kamla, Y1 - 2009/12/15/ PY - 2008/12/12/received PY - 2009/11/07/accepted PY - 2009/12/17/entrez PY - 2009/12/17/pubmed PY - 2010/7/14/medline SP - 27 EP - 35 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 11 IS - 1 N2 - The studies reported in this work are aimed to elucidate the ternary inclusion complex formation of gemfibrozil (GFZ), a poorly water-soluble drug, with beta-cyclodextrin (beta-CD) with the aid of auxiliary substances like different grades of povidone(s) (viz. PVP K-29/32, PVP K-40, Plasdone S-630, and Polyplasdone XL), organic base (viz. triethanolamine), and metal ion (viz. MgCl(2).6H(2)O), by investigating their interactions in solution and solid state. Phase solubility studies were carried out to evaluate the solubilizing power of beta-cyclodextrin, in association with various auxiliary substances, to determine the apparent stability constant (K (C)) and complexation efficiency (CE) of complexes. Improvement in K (C) values for ternary complexes clearly proves the benefit of the addition of auxiliary substances to promote CE. Of all the approaches used, the use of polymer Plasdone S-630 was found to be the most promising approach in terms of optimum CE and K (C). GFZ-beta-CD (1:1) binary and ternary systems were prepared by kneading and lyophilization methods. The ternary systems clearly signified superiority over binary systems in terms of CE, solubility, K (C), and reduction in the formulation bulk. Optimized ternary system of GFZ-beta-CD-Plasdone S-630 prepared by using lyophilization method indicated a significant improvement in intrinsic dissolution rate when compared with ternary kneaded system. Differential scanning calorimetry, X-ray diffraction, Fourier transform infrared, scanning electron microscopy, and proton nuclear magnetic resonance were carried out to characterize the binary and optimized ternary complex. The results suggested the formation of new solid phases, eliciting strong evidences of ternary inclusion complex formation between GFZ, beta-CD, and Plasdone S-630, particularly for lyophilized products. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/20013079/Effect_of_auxiliary_substances_on_complexation_efficiency_and_intrinsic_dissolution_rate_of_gemfibrozil_beta_CD_complexes_ L2 - https://dx.doi.org/10.1208/s12249-009-9350-y DB - PRIME DP - Unbound Medicine ER -