FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF ATENOLOL
Abstract
Floating microspheres prepared with enteric coated polymer successfully by the solvent diffusion method. Upon incorporation of the hydrophilic polymer such as HPMC in the shell of microspheres, the amount of drug release form microspheres could enhance. In vitro data obtained from floating microspheres of show Atenolol excellent float ability, good buoyancy and prolonged drug release. Floating microspheres different size and drug content could be obtained by varying formulation variable. Diffusion found to be the main release mechanisms. Thus the prepared floating microspheres may prove to be potential candidate for multiple-unit delivery device adaptable to any intra gastric condition.
The formulations were evaluated for various Micromeritic and characteristic studies. It increases the bioavailability dosage form with prolonged effect, hence improve the patient compliance.
Ideal property of floating microspheres includes high buoyancy and sufficient release rate of drug. It is necessary to selected appropriate balance between buoyancy and release rate drug from all developing floating microspheres. F4formulation showed the best appropriate balance between buoyancy and release rate drug, which can be considered as a best fit floating microspheres.
The designed system F4 floats in the stomach and prolonged the gastric residence time (GIT) providing sustained release action, in addition floating microspheres enable to increase the absorption rate, as it gradually sank in the stomach and arrived at the absorption site. The developed formulation overcomes the drawback limitation of sustained release preparation. Therefore multiple units floating system i.e., floating microspheres will be possibly beneficial for sustained action.
Key words: Microsphere Polymer, Atenolol, floating microspheres
References
Bhosale UV. Kusum Devi, Jain N, Swamy P. Effect of polymer concentration and viscosity grade of Atenolol release from gastric floating drug delivery system. Indian J.Pharm .Educ.Res. 2010 July-sep; 44(3):267-72.
K. Deepa, M.Karthikeyan, Cefpodoxim Proxetil floating microspheres formulation and in–vitro evaluation , Indian journal 2009:5(2), 69-72.
Yuveraj Singh tanwar, pushpendra Singh Naruka, Garmia, Rani Ojha. Development and evaluation floating microspheres of varapamil hydrochloride, Indian journal of Pharmaceutical science 2007: 43,78-82.
Gohel, Parikh, Shital Bariya, Sustained release floating microspheres of acyclovir, internation journal drug development and research, 2011: 3,80-84.
Singh Bandana, Kanoujia Jovita, Manisha pandey, Saraf Shubhini, formulation and evaluation floating microspheres of Famotidine , international journal of pharmatech. Research 2010 :2, 414-420.
Najmuddin M, Sachin S, Asgar A, Patel V and Khan T. Formulation andInvitro Evaluation of Floating Microspheres of Ketoprofen Prepared by Emulsion Diffusion Method. International Journal of Pharmacy And Pharmaceutical Research. 2010; 2:13-19.[5]
Srivastava Anand Kumar, Ridhurkar Devendra Narayanrao, Wadhwa Saurabh, Floating microspheres of cimetidine: Formulation, characterization and in vitro evaluation, Acta Pharm, 2005, 55, 277–285.
Patel Asha, Ray Subhabrata and Thakur Ram Sharnagat, In Vitro Evaluation and Optimization of Controlled Release Floating Drug Delivery System of Metformin Hydrochloride, DARU, 2006, 14( 2), 57-63.
S.B. Gholap , Banarjee S.K. ,D.Gaulkurad , S. L. Jadhav Hollow microspheres review , Acta Pharma,2010:43,322-329.
Suddhasattya Dey, Dhiraj Kumar, D Sandeep Kumar, S. A. Sreenivas and V. Rahul, formulation and in vitro evaluation of floating microspheres Nateylinide ,international Journal and bioscience, 2008:50,147-156.
Sunit KS, Abdul AM and BB barik. Formulation and In-Vitro Evaluation of Eudragit Microspheres of Staudinger, Tropical Journal of Pharmaceutical Research. 2005; 4 (1) : 369-375.
Patel V, Patel N. Self correcting monolithic floating matrix tablet of dipyridamole: influence of formulation variables. International Jouranl of pharmaceutical sciences. 2009 Nov. 06:210-25.
Nagesh, Venkatesh J. S. ,Santosh, Raj M., Jagadish, Sindhu Patil, Floating Drug Delivery system of Levofloxacin formulation and evaluation, Indian Pharma Sci & res 2011:3(6), 1265-1269.
Behera BC, sahoo SK, Dhal S, barik BB and Gupta BK.Characterization of Glipizide Loaded Polymethacrylate Microspheres Prepared by Emulsion Solvent Evaporation Method. Tropical Journal of Pharmaceutical Research. 2008;7(1):879-885.
Hemangi Patil. S, Moreshwar Patil. P, Bharat Tekade. W, Vinod Thakare. M and Vijay Patil, Formulation and in vitro Evaluation of Floating Microsphere of Acyclovir. Arch Pharm Science & Res. 2009; 1: 194-198.
Zhenqiu Yang , Baozhen Song, Qiaoxia Li, Honglei Fan and Fan Ouyang, Preparation of microspheres with microballoons inside for floating drug-delivery systems. Journal of Applied Polymer Science. 2004; 94(1):197-202.
Sunil Jain. K, Govind Agrawal. P and Narendra Jain .K , Evaluation of porous carrier-basedfloating orlistat microspheres for gastric delivery. AAPS Pharm Sci Tech.2008; E 54-E 62.
Umamaheshwari R.B.; Jain S.; Bhadra D.; Jain N.K.Floating microspheres bearing acetohydroxamic acid for the treatment of Helicobacter pylori.Journal of Pharmacy and Pha. rmacology.2003; 12(55):1607-1613. 33.
Kumar R. Development and in-vitro evaluation of sustained release floating matrix tablets of metformin Hydrochloride. International Journal of pharmaceutical sciences. 2010 July 13;1(8):96-100.
Yang L, Eshraghi J, Fassihi R. A new intragastric delivery system for the treatment of Helicobacter Pylori associated gastric ulcer: in-vitro evaluation. Journal of controlled release. 1998 April 12;57:215-22.
S.B. Gholap , Banarjee S.K. ,D.Gaulkurad , S. L. Jadhav Hollow microspheres review , Acta Pharma,2010:43,322-329.
Rajeev Garg, G.D. Gupta “gastroretentive floating microspheres of silymarin preparation in vitro evaluation, tropical journal of pharmaceuticals research 2010:9(1):56-66.
Ghodake.J.S., Shinde D.A., Kadam A.N “Formulation and evaluation of floating microspheres metformin hydrochloride, international research 2010:2(1):378-384.
Vandna Singh, Punita, Amrenara Chaudhury “Preparation on eudragit of floating microspheres of ranitidone hydrochloride 2011:68(6):975-980.
Sagar Balase Sanagale, B.V.Jain, Dr. S.D. Bortate “Formulation and evaluation of floating microspheres of felodipines 2011:3(2):11-16.
C. Sharon Kumar “Formulation and evaluation of floating microspheres of gabapentine by using solvent evaporation method 2010:1(1):76-79.
Biresh Kumar Sarkar, Sandeep Singh Tanwar, Prashant Soni, and Jain” Formulation and characterization and in-vitro evaluation of floating microspheres esomeprazole 2012:1(7):87-92.
Sarude, Mittal, Magar, and Shrivastava” Formulation and evaluation floating microspheres of glipizide 2011:3(3):775-783.
Bathani Sree Tejaswi, Durgaramanu Sivadasn, Shalini Devi, “Formulation and in-viro evaluation of floating microspheres clathromycin 2011:3(6):90-101.
Swapnila VShinde, Rohit Pawar , Hemant, “Domperidone floating microspheres and in- vitro evaluation, journal of pharmacy reaserch 2012 volume 5(4) 2012.
Y.S. Tanwar” Floating microspheres and development and characterization and application, Pharma research 2006: 32(2):29-32.
P.Puntane S.M.Sarude, M.Mittal, R.M.Magar, and A.D. Shrivastava” Formulation and evaluation floating microspheres of glipizide 2010:3(4):77-82.
Gaurang Patel, Ajay Tiwari, Nirav Rabadia,”Floating microspheres as a novel tool of H2 receptor blocker, international research journal of pharmacy 2012:3(2).
N. Pandya, M. Pandya, V.H. Bhaskar”Preparation and characterization in vitro of poruse carrier- based floating microspheres for gastric delivery. J young pharm 2011:3(2).
Nilamgiri Gawain , Garima Joshi, Krutika Sawant” Floating microspheres of Valacyclovir Hcl. For optimization and characterization in in-vitro and in-vivo studies, journal of pharmacy & bioailled science 2012 4(5) 8-9.
Harsoliya, Patel, Pathan “Formulation of floating microspheres of ritonavir by cross linking technique, international journal research of pharmaceutics and biological articles 2012; 3(1):108-111.
Ambati Brahma Reddy, M Karunanidhi, K Sudheer Karna, B Samyuktha Rani ‘Effect of SLS on ethyl cellulose containing cyclobenzaprine HCl floating, Research Journal of Pharmaceutical, Biological and Chemical Sciences 2010:1(8):898-1004.
Abdul Hasan Sathali.A, Kathiravan.S “Formulation and characterization of floating microspheres of perindopril erbumine, Journal of Pharmacy Research 2012,5(4),1862-1871. 35. . 38. Gohel, R. K. Parikh, Shital Bariya, Sustained release floating microspheres of amoxicillin, international journal drug development and research, 2011: 3,80-84.
Ambati Brahma Reddy, M Karunanidhi , K Sudheer Karna, B Samyuktha Rani ‘Effect of SLS on ethyl cellulose containing cyclobenzaprine HCl floating, Research Journal of Pharmaceutical, Biological and Chemical Sciences 2010:1(8):898-1004.
Abdul Hasan Sathali., Kathiravan.S “Formulation and characterization of floating microspheres of perindopril erbumine, Journal of Pharmacy Research 2012,5(4),1862-1871.
Nirav Rabadia, Mr. jay Tiwari, Gaurang Patel, Vishal Virani” Development and evaluation of floating microspheres of Pioglitazone hydrochloride using ethyl cellulose, Der Pharmacia , 2010, 2(5): 261-27 Vol. 3, No.1, pp 76-81,
Suresh Fartyal, Sajal Kumar Jha, Manvendra Singh Karchuli, “Formulation and Evaluation of Floating Microspheres of Boswellic acid, Int.J. PharmTech Res.2011, 3(1)
Shoufeng Li, et al., “Effect of formulation variables on the Floating properties of gastric floating drug delivery system” Drug Development Industrial Pharmacy by Taylor and Francis, volume 28 , 783 –792
Nakagawa T, Ichikondo S, Sasai Y, Kuzuya M. Preparation of floating drug delivery system by plasma technique. Chem Pharm. Bull 2006; 54(4): 514-518
Singh B, Kim HN: Floating drug delivery system: an approach to oral controlled drug via gastric retention.J Control Rel. 2000; 63: 235-259.
Khatri S, Girdhani D, Pahwa R: Recent advances in floating drug delivery system. The Indian Pharmacist.2007; 6: 17–20.
Arora S, Ali J, Ahuja A, Khar RK, Baboota S: Floating Drug Delivery Systems: A Review. AAPS PharmSciTech.2005;6(3) :372-390.
Deshpande, A. A., Shah, N.H., Rhodes, C.T., and Malick, W., Development of a novel controlled Release system for gastric retention, Pharm. Res. 1997; 14 (6): 815-9.
Shah S.H, Patel J.k, Patel N-Stomach Specific Floating Drug Delivery System: A Review Int. J. Pharm Tech Research (1), 623-633
El-Kamel AH, Sokar MS, Al Gamal SS, Naggar VF. Preparation and evaluation of ketoprofen floating oral drug delivery system. Int J Pharm.2001;220:13Y21
Kawashima Y, Niwa T, Takeuchi H, Hino T, Ito Y. Preparation of multiple unit hollow microspheres (microballoons) with acrylic resins containing tranilast and their drug release characteristics (in vivo).J Control Release. 1991;16:279Y290.
