The ORMULATION OF GLIMEPIRIDE AND ATORVASTATIN CALCIUM NANOPARTICLES BY 1 LIQUID ANTISOLVENT PRECIPITATION METHOD THROUGH DOUBLE STEP COMMINUTION 2 TECHNIQUE AND ITS EVALUATION

VISHAL S REDDY; GOWDA DV; VISHAL GUPTA N

doi:10.22159/ajpcr.2019.v12i5.32632

Authors

VISHAL S REDDY Department of Pharmaceutics, JSS College of Pharmacy, Sri Shivarathreeshwara Nagara, Mysuru, Karnataka, India.
GOWDA DV Department of Pharmaceutics, JSS College of Pharmacy, Sri Shivarathreeshwara Nagara, Mysuru, Karnataka, India.
VISHAL GUPTA N Department of Pharmaceutics, JSS College of Pharmacy, Sri Shivarathreeshwara Nagara, Mysuru, Karnataka, India.

DOI:

https://doi.org/10.22159/ajpcr.2019.v12i5.32632

Keywords:

Atorvastatin calcium, Antisolvent, Glimepiride, Hydroxypropyl methylcellulose, Nanoparticles

Abstract

Objective: The present research is to formulate Glimepiride and Atorvastatin Calcium Nanoparticles for the type-2 diabetes mellitus for improvement of glucose tolerance associated with dyslipidemia formulated by liquid antisolvent precipitation technique.

Method: Glimepiride nanoparticles and atorvastatin calcium nanoparticles were prepared by using a liquid antisolvent precipitation technique. Solvent to antisolvent ratio used was 3.5:6.5 and 2.5:7.5 and the drug concentration used was 40 mg/ml and 60mg/ml respectively.

Result: The XRD was determined, the data of the optimized Glimepiride formulation revealed that the prepared nanosized Glimepiride powder was existed in crystalline form. The percent yield for the formulations of Glimepiride and atorvastatin calcium nanoparticles was found to be 72.8±1.8%, 75.3±2.2% respectively. In-vivo studies in albino wistar rats demonstrated that the C_maxand AUC₀₋_24hof optimized Glimepiride and atorvastatin calcium nanosized formulation was found to be 24451.14±2170.5 ng/ml, 162945.12±241.5 ng/ml and 1385.43±153.3 ng/ml,3636.57±65.2 ng/ml respectively. Dissolution study of optimized formulations shows that marked enhancement of dissolution rate. The stability studies of mixture of Glimepiride and atorvastatin calcium powder when stored at 4±3^oC refrigerated temperature has shown no significant changes in physical appearance, drug content, particle size and PDI. Conversely the sample stored at room temperature has shown significant increase in particle size and PDI, with no significant changes in drug content and physical appearance.

Conclusion: The Formulation of glimepiride and atorvastatin calcium drug nanoparticles shows increase in the surface-to-volume ratio of API, resulting in better drug solubility and hence increasing the bio-availability when compared to its pure form.

Downloads

Download data is not yet available.

References

Koczkur KM, Mourdikoudis S, Polavarapu L, Skrabalak SE. Polyvinylpyrrolidone (PVP) in nanoparticle synthesis. Dalton Trans 2015;44:17883-905.

Ige PP, Baria RK, Gattani SG. Fabrication of fenofibrate nanocrystals by probe sonication method for enhancement of dissolution rate and oral bioavailability. Colloids Surf B Biointerfaces 2013;108:366-73.

About diabetes. World Health Organization. Archived From the Original on 31 March 2014. Available from(Please refer GP word file)

[Last accessed on 2014 Apr 4].

Pfizer Product Promotion Page (Lipitor). Available from: (please refer attached GP word file). [Last accessed on 2011 Dec 05].

Jogala S, Ankathi L, Jarupula RN. Glimepiride fast disintegrating tablets: Formulation, evaluation and in vivo disintegration and dynamic studies. Int J Pharm Pharm Sci 2016;8:271-8.

Behera A, Srikanth P, Rao YM, Sahoo SK. Formulation and characterisation of glimepiride loaded biodegradable nanoparticles for the management of Type 2 diabetes mellitus. Immunol Endocr Metab Agents in Med Chem (Formerly Current Medicinal Chemistry- Immunology,Endocrine and Metabolic Agents) 2016;16:49-60.

Ramadan AA, Mandil H, Sabouni J. Determination of atorvastatin calcium in pure and its pharmaceutical formulations using iodine in acetonitrile by Uv-visible spectrophotometric method. Int J Pharm Pharm Sci 2015;7:427-33.

Zhang HX, Wang JX, Zhang ZB, Le Y, Shen ZG, Chen JF, et al. Micronization of atorvastatin calcium by antisolvent precipitation process. Int J Pharm 2009;374:106-13.

Sola D, Rossi L, Schianca GP, Maffioli P, Bigliocca M, Mella R, et al. Sulfonylureas and their use in clinical practice. Arch Med Sci

;11:840-8.

Kim MS, Jin SJ, Kim JS, Park HJ, Song HS, Neubert RH, et al. Preparation, characterization and in vivo evaluation of amorphous atorvastatin calcium nanoparticles using supercritical antisolvent (SAS) process. Eur J Pharm Biopharm 2008;69:454-65.

Geinsen K. Special pharmacology of the new sulfonylurea glimepiride Drug Res 1988;38:1120-30.

Rabinow BE. Nanosuspensions in drug delivery. Nat Rev Drug Discov2004;3:785-96.

Lennernäs H. Clinical pharmacokinetics of atorvastatin. Clin Pharmacokinet 2003;42:1141-60.

Kawabata Y, Wada K, Nakatani M, Yamada S, Onoue S. Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: Basic approaches and practical applications. Int J Pharm 2011;420:1-0.

Rasenack N, Müller BW. Micron-size drug particles: Common and novel micronization techniques. Pharm Dev Technol 2004;9:1-3.

Won DH, Kim MS, Lee S, Park JS, Hwang SJ. Improved physicochemical characteristics of felodipine solid dispersion particles by supercritical anti-solvent precipitation process. Int J Pharm 2005;301:199-208.