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FORMULATION AND IN-VITRO EVALUATION OF CLOPIDOGREL BISULFATE IN PARENTERAL DOSAGE FORM USING LYOPHILIZATION TECHNIQUE

Journal Name:

  • The International Journal of Pharmaceutical Research and Bio-Science

Publication Year:

  • 2012

Key Words:

Author NameUniversity of Author
Abstract (2. Language): 
The aim of this work was to develop & evaluate in-vitro; a stable clopidogrel bisulfate formulation, in parenteral dosage form using lyophilization technique. Faxon DP et al. have reported use of antiplatelet therapy generally with clopidogrel bisulfate before percutaneous coronary interventions (PCI).1 Solubility of the drug in different solvents were determined. Solubility study suggested pH dependent solubility. Clopidogrel bisulfate hydrolyzes in aqueous phase into free base. In-order to get a stable parenteral dosage form, lyophilization technique was used. Optimized lyophilized cycle process along with graphical representation is presented. Compatibility study for rubber closures, tubing, and filter membrane were done and absences of any loss of drug due to the adsorption of any of the component were checked. Osmolarity of the lyophilized product was checked. Dilution studies with normal saline, 5% dextrose injection up to 150 mg/ml for 12 Hrs without any degradation and precipitation was observed. Stress studies for thermal cycling, effect in presence of nitrogen and oxygen and photo stability were carried out. Accelerated stability study indicated that the lyophilized product is stable at 40 °C/75% RH up to 3 months. Polymorphic change during the process was evaluated. Parenteral formulation of clopidogrel bisulfate is of considerable interest in the area of Novel drug dosage form for treating critical cardiovascular diseases.
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  • 5
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  • English

REFERENCES

References: 

1. Faxon DP: Use of antiplatelet agents and anticoagulants for cardiovascular disease: current standards and best practices Rev. Cardiovasc. Med. 2005; 6 Suppl 4: S3-14.
2. Payal Patel and Lily Cheng: The role of clopidogrel in the emergency department: Can J Emerg Med 2005; 7(1):22-7.
3. Jonathan D. Marmur, Cristina A. Mitre, Elliot Barnathan and Cavusoglu: Benefit of bolus-only platelet glycoprotein 11 b/I 11 a inhibition during percutaneous coronary
intervention: Insights from the very early outcomes in the evaluation of 7E3 for the prevention of ischemic complications (EPIC) trial: American heart journal 2006; 152( 5):
876-881.
4. Fontana P, DuPont A, Gandrille S, Bachelot-Loza C, Reny JL, Aiach M and Gaussem P: Adenosine diphosphate induced platelet aggregation is associated with P2Y12 gene sequence variations in
Available Online At www.ijprbs.com
Research Article
Sunil Kumar Panda, IJPRBS,
2012;
Volume 1(5): 436-455
healthy subjects: Circulation 2003; 108:989
-995.
5. Gladding
P
, Webster M, Zeng I, Farrell H, Stewart J, Ruygrok P, Ormiston J, El-Jack S, Armstrong G, Kay P, Scott D and Gunes A, ML: The antiplatelet effect of higher loading and Maintenance dose regimens of clopidogrel: the PRINC (Plavix response in coronary intervention) trial; J .Am Coll.
Cardiol. Intv. 2008; 1:612-619.
6. Jack WC
Ta
n and Kenneth WQ Guo: Antiplatelet therapy during acute percutaneous coronary intervention: New strategies and therapeutics: Annals academy of medicine. 2010; 39 (3):221-229.
7. Stefan C. Schneid, Henning Gieseler, William J. Kessler,Suman A. Luthra, and Michael J. Pikal: Optimization of the secondary drying step in freeze drying using TDLAS technology: AAPS PharmSciTech. 2011; 12(1): 379-387.
8. Aulton ME: Dosage form design and manufacture. Pharmaceutics: The science of dosage form design, 2nd Edition, 2002:
(307-339).
9. Kostecka D, Duncan MR and Wagenknecht D.: Formulation of a stable
ISSN: 2277-8713 IJPRBS
parenteral product; Clonidine
Hydrochloride Injection. PDA J Pharm Sci
Technol. 1998; 52(6):320-5.
10. Selina Hines and Steve Pleasance.: Compatibility of injectable hydromorphone formulations with typical diluents, components of giving sets and drugs for potential co-administration. EJHP Praticel.
2011, 17(3):47-53.
11. Xiaolin (Charlie) Tang and Michael J. Pikal: Design of freeze-drying processes for pharmaceuticals: practical advice: Pharmaceutical Research.2004, 21(2):191-200.
12. Jain Jain, Clara Fernandes and Vandana Patravale: Formulation development of parenteral phospholipid-based micro emulsion of Etoposide: AAPS
PharmSciTech.2010, 11(2): 826-831.
13. Sandhya chaurasia, Sneha Golani, Nishi prakash Jain, Manoj Goyal and Sofiya verma: Comprehensive review on aseptic fill/finish manufacturing as per regulatory guidelines: Journal of current pharmaceutical research 2011; 5 (1): 19-27.
Available Online At www.ijprbs.com
Research Article
Sunil Kumar Panda, IJPRBS,
2012;
Volume 1(5): 436-455
ISSN: 2277-8713
IJPRBS
14. ICH Topic Q1B: Photo stability testing of new active substances and medicinal products January 1998: CPMP/ICH/279/95
15. Daoussia R, Vessota S, Andrieua J and Monnierb O: Sublimation kinetics and sublimation end -point times during freezing of pharmaceutical active principle with organic co-solvent formulations.Chem Eng Res Des 2009;87:889-907.
16. Teagarden DL and Baker DS. Practical aspects of freeze-drying of pharmaceutical and biological products using non-aqueous co-solvents systems. Informa Healthcare;
2010; 47: 254-87.
17. Schneid SC and Henning G: Rational approaches and transfer strategies for the
scale up of freeze drying cycles. Chimica
Oggi 2011: 29: 43-6.
18. Lewis LM, Teagarden DL, Johnson RE and Ahmed SS: Rational design of a freeze dried formulation for a biologic. Am Pharm
Rev 2008; 11:91-6.
19. Eyster HC: Effect of temperature on catalase activity. Ohio J Sci 1950; 50: 273-7.
20. Blue J and Yoder HS: Successful lyophilization development of protein therapeutics Am Pharm Rev 2009; 12: 90-6.
21. Tang X and Pikal MJ: Design of freeze-drying processes for pharmaceuticals: Practical advice. Pharm Res 2004; 21:191¬200.
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