Design & Characterization of Nanocrystals of Lovastatin for Solubility & Dissolution Enhancement Dr. Basavaraj K. Nanjwade Dr. Basavaraj K. Nanjwade M. Pharm, PhD. M. Pharm, PhD. Department of Pharmaceutics Department of Pharmaceutics KLE University’s College of Pharmacy KLE University’s College of Pharmacy Belgaum-590010 Belgaum-590010 E-mail: E-mail: [email protected]Cell No: 00919742431000 Cell No: 00919742431000
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Design & Characterization of Nanocrystals of Lovastatin for Solubility & Dissolution Enhancement
Design & Characterization of Nanocrystals of Lovastatin for Solubility & Dissolution Enhancement. Dr. Basavaraj K. Nanjwade M. Pharm, PhD. Department of Pharmaceutics KLE University’s College of Pharmacy Belgaum-590010 E-mail: [email protected] Cell No: 00919742431000. Introduction. - PowerPoint PPT Presentation
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Design & Characterization of Nanocrystals of Lovastatin for
Solubility & Dissolution Enhancement
Dr. Basavaraj K. NanjwadeDr. Basavaraj K. Nanjwade M. Pharm, PhD.M. Pharm, PhD.
Department of PharmaceuticsDepartment of Pharmaceutics
KLE University’s College of PharmacyKLE University’s College of Pharmacy
f)f) In- vivo In- vivo evaluationevaluation In vivo drug release of pure LVS
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Time (Min.)
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i.v. control group Oral control group
In vivo drug release of F1A and F2A nanocrystals
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Time (Min.)
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F1A F2A
08/02/2010
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Comparison of Bioavailability of LVS nanocrystals
CodeAbsolute
bioavailabilityRelative
bioavailability
Area under curve(0-8) (µg/ml.hrs)
Cmax (µg/ml)Tmax (hrs.)
Oral control group
- - - - - - - - 802.8 5.849± 0.245 2
IV control group
- - - - - - - - 986.7 9.546± 0.094 5*
F1A 0.826 1.015 815.3 6.325± 0.324 2
F2A 0.821 1.010 810.9 5.590± 0.432 2
* Time in minute Values of Cmax are mean ± standard deviation
08/02/2010
Drug content after 30 days storage of F1A
Code Percent drug content at
40C
Percent drug content at 300C±20C / 65%± 5%
RH
Percent drug content at 400C±20C/ 65%± 5%
RH
F1A 66.46% 66.32% 60.54%
08/02/2010 15NIPER, Chandigarh
Continued…..Continued…..
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Release study of F1A stored at 40C, at 300C±20C / 65%± 5% RH and at 400C±20C/ 65%± 5% RH
Time (Min.)
% Cumulative LVS release stored at
40C
% Cumulative LVS release stored at
300C±20C / 65%± 5% RH
% Cumulative LVS release stored at
400C±20C/ 65%± 5% RH
15 44.96 45.23 41.03
30 59.16 59.63 54.24
45 70.20 70.86 65.03
60 75.03 75.53 71.26
90 82.97 83.18 79.06
120 87.06 87.45 82.36
150 90.31 90.35 88.65
180 93.76 93.06 89.30
08/02/2010
From the particle morphology by SEM, it was observed that LVS nanocrystals remain crystalline.
Less particle size was observed in case of F1A & F2A as compared to all other.
From PXRD and DSC data, it was observed that F1A , F2A & F3A showed no significant change in crystalline as compared to pure LVS.
Solubility was enhanced due to less particle size & solvent used (acetone & methanol).
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In-vitro release rate studies showed that the maximum drug release was found in the F1A & F2A in the required period of time.
In-vivo relative bioavailability of F1A & F2A was slightly increased as compared to absolute bioavailability.
From stability study data it was revealed that nanocrystals of lovastatin remained more stable at 4ºC. The maximum instability of nanocrystals was observed at 402C.