Solid-State Characterization and Dissolution Properties of Lovastatin Hydroxypropyl-β-Cyclodextrin Inclusion Complex - Pharmaceutical Technology

Latest Issue
PharmTech

Latest Issue
PharmTech Europe

Solid-State Characterization and Dissolution Properties of Lovastatin Hydroxypropyl-β-Cyclodextrin Inclusion Complex
The objectives of this study were to prepare and characterize inclusion complexes of lovastatin with hydroxypropyl-β-cyclodextrin (HPβ-CD) and to study the effect of the complexes on the dissolution rate of lovastatin (LVS). The findings suggest that LVS's poor dissolution profile can be overcome by preparing its inclusion complex with HPβ-CD.


Pharmaceutical Technology


Acknowlegment

The authors thank Roquette Frères, France for a generous gift of HPβ-CD. The authors thank Lincoln Pharmaceuticals Ltd. and Maan Pharmaceuticals Ltd., India for providing lovastatin and various formulation excipients, respectively as gift samples. The authors are grateful to the Department of Pharmacy, M.S. University, India for conducting differential scanning calorimetry studies and to Sun Pharmaceutical Advance Research Center, India for conducting X-ray diffraction studies of the samples.

Rakesh P. Patel* is an assistant professor and Madhabhai M. Patel is a professor and the head of the department of pharmaceutics, S K Patel College of Pharmaceutical Education and Research, Ganpat University, Ganpat vidyanagar, Kherva 382711, Mehsana, Gujarat, India,

*To whom all correspondence should be addressed.

Submitted: July 10, 2006. Accepted: Oct. 11, 2006.

Keywords: lovastatin, hydroxypropyl-β-cyclodextrin, inclusion complexation, in vitro dissolution studies.

References

1. J.S. MacDonald et al., "Preclinical Evaluation of Lovastatin," Am. J. Cardiol . 62 (15), 16J–27J (1998).

2. E.E. Slater and J.S. MacDonald, "Mechanism of Action and Biological Profile of HMG CoA Reductase Inhibitors: A New Therapeutic Alternative," Drugs 36 (Suppl. 3), 72–82 (1998).

3. S.B. Gerald, K.E Dean, and J.K. Micheal, "Lovastatin," in Analytical Profiles of Drug Substances and Excipients, Vol. 21, G.B. Harry, Ed., (Academic Press, Inc., New York, NY, 1992), pp. 277–315.

4. D.O. Thompson, "Cyclodextrins-Enabling Excipients: Their Present and Future Use in Pharmaceuticals," Crit. Rev. Ther. Drug Carrier Syst. 14 (1), 1–104 (1997).

5. C.M. Fernandes, V.M. Teresa, and F.J. Veiga, "Physicochemical Characterization and In Vitro Dissolution Behavior of Nicardipine-Cyclodextrins Inclusion Compounds," Eur. J. Pharm. Sci. 15 (11), 79–88 (2002).

6. M. Kamada et al., "Cyclodextrin Conjugate-Based Controlled Release System: Repeated- and Prolonged-Releases of Ketoprofen after Oral Administration in Rats," J. Control. Release 82 (2-32-3), 407–416 (2002).

7. K. Uekama and M. Otagiri, "Cyclodextrins in Drug Carrier Systems," Crit. Rev. Ther. Drug Carrier Syst. 3 (1), 1–40 (1987).

8. S. Baboota, M. Dhaliwal, and K. Kohli, "Physicochemical Characterization, In Vitro Dissolution Behavior, and Pharmacodynamic Studies of Rofecoxib-cyclodextrin Inclusion Compounds," AAPS PharmSciTech . 6 (1), E83–E90 (2005).

9. G. S. Tirucherai and A. K. Mitra, "Effect of Hydroxypropyl Beta Cyclodextrin Complexation on Aqueous Solubility, Stability, and Corneal Permeation of Acyl Ester Prodrugs of Ganciclovir," AAPS PharmSciTech. 4 (3), E45 (2003).

10. B. N. Nalluri et al.,"Physicochemical Characterization and Dissolution Properties of Nimesulide-Cyclodextrin Binary Systems," AAPS PharmSciTechnol . 4 (1), E2 (2003).


ADVERTISEMENT

blog comments powered by Disqus
LCGC E-mail Newsletters

Subscribe: Click to learn more about the newsletter
| Weekly
| Monthly
|Monthly
| Weekly

Survey
FDASIA was signed into law two years ago. Where has the most progress been made in implementation?
Reducing drug shortages
Breakthrough designations
Protecting the supply chain
Expedited reviews of drug submissions
More stakeholder involvement
Reducing drug shortages
38%
Breakthrough designations
13%
Protecting the supply chain
38%
Expedited reviews of drug submissions
13%
More stakeholder involvement
0%
View Results
Jim Miller Outsourcing Outlook Jim Miller Health Systems Raise the Bar on Reimbursing New Drugs
Cynthia Challener, PhD Ingredients Insider Cynthia ChallenerThe Mainstreaming of Continuous Flow API Synthesis
Jill Wechsler Regulatory Watch Jill Wechsler Industry Seeks Clearer Standards for Track and Trace
Siegfried Schmitt Ask the Expert Siegfried SchmittData Integrity
NIH Translational Research Partnership Yields Promising Therapy
Clusters set to benefit from improved funding climate but IP rights are even more critical
Supplier Audit Program Marks Progress
FDA, Drug Companies Struggle with Compassionate Use Requests
USP Faces New Challenges
Source: Pharmaceutical Technology,
Click here