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Inclusion complex of colchicine in hydroxypropyl-β-cyclodextrin tenders better solubility and improved pharmacokinetics.
Pharm Dev Technol. 2013 Mar-Apr; 18(2):313-22.PD

Abstract

CONTEXT

Colchicine (CLC) causes cell death by destabilizing the tubulin unit. However, it ionizes at physiological pH resultant low bioavailability and therapeutic efficacy.

OBJECTIVES

We have attempted to augment the bioavailability of CLC by fabricating the inclusion complex with hydroxypropyl-β-cyclodextrin (HP-β-CD).

MATERIALS AND METHODS

CLC-HP-β-CD inclusion complex was prepared and evaluated with Fourier-transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, scanning electron microscopy, (1)H nuclear magnetic resonance ((1)H NMR) spectroscopy and rotating frame overhauser enhancement spectroscopy (ROESY). Oral bioavailability of CLC-HP-β-CD inclusion complex was analyzed using high performance liquid chromatography method.

RESULTS AND DISCUSSION

Our phase-solubility data indicated the formation of a stable complex with K(c) ~0.31 mM(-1) at pH 7.4. (1)H NMR ascertains that NHCOCH(3) moiety of CLC enters in the HP-β-CD cavity and deshielded the H-3 and H-5 protons. ROESY also correlates the H(f) and H(g) of CLC with H-3 and H-5 protons of HP-β-CD and indicates that H(f) and H(g) protons of CLC are present either as cis and/or trans form in CLC-HP-β-CD inclusion complex. Pharmacokinetic studies showed a 1.82-fold increase in absolute bioavailability of CLC upon complexation.

CONCLUSION

CLC-HP-β-CD inclusion complex may potentially be used as a viable formulation of CLC.

Authors+Show Affiliations

Department of Pharmaceutics, Hindu College of Pharmacy, Sonepat, Haryana, India.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

21699389

Citation

Chauhan, Ritu, et al. "Inclusion Complex of Colchicine in Hydroxypropyl-β-cyclodextrin Tenders Better Solubility and Improved Pharmacokinetics." Pharmaceutical Development and Technology, vol. 18, no. 2, 2013, pp. 313-22.
Chauhan R, Madan J, Kaushik D, et al. Inclusion complex of colchicine in hydroxypropyl-β-cyclodextrin tenders better solubility and improved pharmacokinetics. Pharm Dev Technol. 2013;18(2):313-22.
Chauhan, R., Madan, J., Kaushik, D., Sardana, S., Pandey, R. S., & Sharma, R. (2013). Inclusion complex of colchicine in hydroxypropyl-β-cyclodextrin tenders better solubility and improved pharmacokinetics. Pharmaceutical Development and Technology, 18(2), 313-22. https://doi.org/10.3109/10837450.2011.591801
Chauhan R, et al. Inclusion Complex of Colchicine in Hydroxypropyl-β-cyclodextrin Tenders Better Solubility and Improved Pharmacokinetics. Pharm Dev Technol. 2013 Mar-Apr;18(2):313-22. PubMed PMID: 21699389.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Inclusion complex of colchicine in hydroxypropyl-β-cyclodextrin tenders better solubility and improved pharmacokinetics. AU - Chauhan,Ritu, AU - Madan,Jitender, AU - Kaushik,Dinesh, AU - Sardana,Satish, AU - Pandey,Ravi Shankar, AU - Sharma,Rakesh, Y1 - 2011/06/23/ PY - 2011/6/25/entrez PY - 2011/6/28/pubmed PY - 2013/7/9/medline SP - 313 EP - 22 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 18 IS - 2 N2 - CONTEXT: Colchicine (CLC) causes cell death by destabilizing the tubulin unit. However, it ionizes at physiological pH resultant low bioavailability and therapeutic efficacy. OBJECTIVES: We have attempted to augment the bioavailability of CLC by fabricating the inclusion complex with hydroxypropyl-β-cyclodextrin (HP-β-CD). MATERIALS AND METHODS: CLC-HP-β-CD inclusion complex was prepared and evaluated with Fourier-transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, scanning electron microscopy, (1)H nuclear magnetic resonance ((1)H NMR) spectroscopy and rotating frame overhauser enhancement spectroscopy (ROESY). Oral bioavailability of CLC-HP-β-CD inclusion complex was analyzed using high performance liquid chromatography method. RESULTS AND DISCUSSION: Our phase-solubility data indicated the formation of a stable complex with K(c) ~0.31 mM(-1) at pH 7.4. (1)H NMR ascertains that NHCOCH(3) moiety of CLC enters in the HP-β-CD cavity and deshielded the H-3 and H-5 protons. ROESY also correlates the H(f) and H(g) of CLC with H-3 and H-5 protons of HP-β-CD and indicates that H(f) and H(g) protons of CLC are present either as cis and/or trans form in CLC-HP-β-CD inclusion complex. Pharmacokinetic studies showed a 1.82-fold increase in absolute bioavailability of CLC upon complexation. CONCLUSION: CLC-HP-β-CD inclusion complex may potentially be used as a viable formulation of CLC. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/21699389/Inclusion_complex_of_colchicine_in_hydroxypropyl_β_cyclodextrin_tenders_better_solubility_and_improved_pharmacokinetics_ L2 - https://www.tandfonline.com/doi/full/10.3109/10837450.2011.591801 DB - PRIME DP - Unbound Medicine ER -