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ORIGINAL/BRIEF
Year : 2012  |  Volume : 4  |  Issue : 5  |  Page : 118-119  

Preparation and optimization of microemulsion of rosuvastatin calcium


Baroda College of Pharmacy, Limda, Vadodara, Gujarat, India

Date of Web Publication21-Mar-2012

Correspondence Address:
I Naazneen Surti
Baroda College of Pharmacy, Limda, Vadodara, Gujarat
India
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/0975-7406.94164

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   Abstract 

Due to very less bioavailability (20%) of Rosuvastatin calcium, an attempt was made to develop and optimize microemulsion formulation. Capmul MCM, Tween 20 and PEG 400 were selected as oil, surfactant and cosurfactant respectively as the drug is having higher solubility in them. 3:1% w/w S:CoS was selected as it gave higher microemulsion area. Optimized batch (ME-1) was selected having 5% Capmul MCM, 50% Tween 20:PEG 400 and 45% water based on evaluation parameters globule size, zeta potential, PDI, % transmittance.

Keywords: Microemulsion, bioavailability, solubility enhancement


How to cite this article:
Patel B Z, Patel S K, Shah S A, Surti I N. Preparation and optimization of microemulsion of rosuvastatin calcium. J Pharm Bioall Sci 2012;4, Suppl S1:118-9

How to cite this URL:
Patel B Z, Patel S K, Shah S A, Surti I N. Preparation and optimization of microemulsion of rosuvastatin calcium. J Pharm Bioall Sci [serial online] 2012 [cited 2020 Jan 28];4, Suppl S1:118-9. Available from: http://www.jpbsonline.org/text.asp?2012/4/5/118/94164

Rosuvastatin calcium (RST), a HMG-CoA Reductase inhibitor is a poorly water soluble hypolipidemic agent. It is also used in the treatment of osteoporosis, benign prostatic hyperplasia, and Alzheimer's disease. Due to its poor water solubility, it is having bioavailability of 20%. [1] Microemulsions are thermodynamically stable system composed of oil, surfactant (and/or cosurfactant) and water. Microemulsion provides advantages like high solubilization and hence improvement in bioavailability of poorly soluble drug, easy to prepare, high entrapment efficiency etc. The objective of the present research work was to prepare and optimize microemulsion containing Rosuvastatin calcium.


   Materials and Methods Top


Rosuvastatin calcium was gifted by S. Kant Healthcare Ltd., Vapi, India. Capmul MCM was gifted by Abitec Corporation, USA. Tween 20 and PEG 400 were purchased from Sulab Chemicals, Vadodara, India. All the other reagents were analytical grade.

Solubility study and phase diagram construction


For the selection of components of microemulsion, solubility study was carried out in number of components according to procedure given by Lianli et al. [2] The oil, surfactant and cosurfactant were selected on the basis of solubility of drug in the solvent, HLB value as well as their GRAS status. To find out the microemulsion region, phase diagram was constructed according to procedure given by Gannu et al. [3] Phase diagram was constructed using CHEMIX® software (ver 3.51).

Preparation of microemulsion and optimization

Microemulsions having different composition [Table 1] were prepared by dissolving the required amount of drug (27 mg/ ml) in a mixture of oil-Smix at 40±5°C and after cooling at 30±5°C adding required volume of water. They were evaluated for globule size, PDI, zeta potential and % transmittance for optimization.
Table 1: Different batches of microemulsion and results of evaluation parameters

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   Results and Discussion Top


Solubility study and phase diagram construction

From the solubility data, Capmul MCM, Tween 20 and Polyethylene Glycol 400 were selected as oil, surfactant and cosurfactant component respectively as rosuvastatin is having higher solubility in above solvents. Phase diagram was plotted using above components [Figure 1]. Tween 20:PEG 400 [3:1% w/w] resulted in higher microemulsion region compared to [1:1% w/w] and [2:1% w/w]. This indicates that increasing the surfactant concentration, maximum amount of oil can be solubilized.
Figure 1: Pseudo-ternary phase diagram

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Preparation and optimization of microemulsion

[Table 1] indicates the different batches of microemulsion and results of evaluation parameters. Optimized batch was selected which is having lower globule size, zeta potential, PDI and higher % transmittance. The logic behind selecting these criteria for optimization is that lower globule size can result in enhanced permeation as well as provide larger surface area for drug release, PDI is the measure of uniformity of the formulation and less than 1 is desirable. Lower the PDI more uniformity of the formulation is considered. More negative zeta potential is considered as more physical stability of the formulation and % transmittance was selected as higher as it shows the isotropic uniform system. From the results shown in [Table 1], batch ME-1 (5% Capmul MCM, 50% Smix) was selected as optimized batch having globule size of 19.56 nm, -2.62 mV zeta potential, 0.334 PDI and 99.2% transmittance.


   Conclusion Top


Microemulsion containing Rosuvastatin calcium was successfully prepared and optimized. Present study demonstrates the potential use of microemulsion system for enhancement in solubility and hence bioavailability for the poorly water soluble drug.

 
   References Top

1.Fritz Blatter. Crystalline forms of Rosuvastatin calcium salt. US Patent No. 20080194604A1, Aug-2008.  Back to cited text no. 1
    
2.Lianli, Indranil Nandi and Kim KH. Development of an ethyl laurate-based microemulsion for rapid-onset intranasal delivery of diazepam. International Journal of Pharmaceutics 2002; 237(1-2): 77-85.  Back to cited text no. 2
    
3.Ramesh Gannu, Chinna Reddy Palem, Vamshi Vishnu Yamsani, Enhanced bioavailability of lacidipine via microemulsion based transdermal gels: Formulation optimization, ex vivo and in vivo characterization. International Journal of Pharmaceutics 2010; 388: 231-241.  Back to cited text no. 3
    


    Figures

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    Tables

  [Table 1]


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