Formulation and evaluation of controlled release floating microspheres of tolperisone hydrochloride

Pooja Jani, Kantilal Vadalia, Hiral Bagdai, Ronak Dedania, Paresh Manseta


Main aim of this study was to develop controlled release (CR) floating multiparticulate drug delivery system of tolperisone hydrochloride. Microspheres were prepared by nonaqueous solvent evaporation technique consisting
of porous calcium silicate (Florite or FLR) as porous carrier, tolperisone hydrochloride (API), Ethyl cellulose (EC), and HPMC 15 cPs as rate controlling polymers. 23 full factorial design was applied for optimization of formulation. The
effect of various formulation and process variables on the particle morphology, micromeritic properties, in vitro floating behavior, entrapment efficiency, and in vitro drug release were studied. The size of microspheres was varied from 300 to
500 μm. The microspheres were found to be highly porous and regular in shape. All the formulations showed excellent flow properties. The percentage entrapment efficiency of all batches was greater than 80%. The percentage buoyancy
varied from 85% to 98% at the end of 12 h. The release rate was determined in simulated gastric fluids. The formulation demonstrated favorable in vitro floating and release characteristics. Different kinetic models were applied to study the
release mechanism. All formulations followed Higuchi model, which indicates the diffusion control release of water soluble drug from polymer matrix. Multiple regression analysis was applied for study of the effect of independent variables on
the dependent variables.

Full Text:



Arpan RP, Ashok NM, Dushyant AS. Preparation and in vitro

characterization of porous carrier-based floating microspheres of model

drug for gastric delivery. Der Pharmacia Lettre 2011;3:432-42.

Surana AS, Kotecha RK. An overview on various approaches to oral

controlled drug delivery system via gastroretention. Int J Pharm Sci

Rev Res 2010;2:68-72.

Samyuktha RB, Vedha HB, Brahma RA, Punitha S, Parimala D,

Victor R. The recent developments on gastric floating drug delivery

systems: An overview. Int J PharmTech Res 2010;2:524-34.

Chetan P, Sunil B, Bhushan R, Nayan G, Sunil P. Floating microspheres:

A promising approach for gastric retention. Int J Pharm Res Dev


Sarode SM, Mittal M, Magar RM, Shelke AD, Shrivastava B,

Vidyasagar G. Formulation and evaluation of floating microspheres of

Glipizide. J Chem Pharm Res 2011;3:775-83.

Sunil KJ, Awasthi AM, Jain NK, Agrawal GP. Calcium silicate based

microspheres of repaglinide for gastroretentive floating drug delivery:

Preparation and in vitro characterization. J Control Release 2005;107:300-9.

Pallab R, Aliasgar S. Multiparticulate formulation approach to pulsatile

drug delivery: Current perspectives. J Control Release 2009;134:74-80.

Dey NS, Majumdar S, Rao ME. Multiparticulate drug delivery systems

for controlled release. Trop J Pharm Res 2008;7:1067-75.

Dhole AR, Gaikwad PD, Bankar VH, Pawar SP. A review on floating

multiparticulate drug delivery system: A novel approach to gastric

retention. Int J Pharm Sci Rev Res 2011;2:205-11.

Japanese pharmacopoeia, official monographs, tolperisone

hydrochloride. 15th ed. 1190. Available from:

Pharmacopoeia/jp15/JP3644-61-9.pdf. [Last accessed on 2011 Nov 22].

Welzig S, Rothenburger J, Kalz B, Gungl J, Gerdes K. Tolperisone

controlled release tablet, US Patent 2010100249423A1, Patent

Application Publication, United States, 2010.

Welzig S, Rothenburger J, Kalz B, Gungl J, Gerdes K., Tolperisone

controlled release tablet, European Patent 2 228 056 A2, Patent

Application Publication, Europe, 2010.

Sunil KJ, Agrawal GP, Jain NK. Evaluation of porous carrier-based

floating orlistat microspheres for gastric delivery. AAPS PharmSciTech


Punitha K, Khadhir S, Ravichandiran V, Umadevi SK, Vaijayanthi V,

Padmapriya S, et al. Intragastric floating drug delivery system of

ranitidine hydrochloride: Formulation and evaluation. Int J Pharm

Pharm Sci 2010;2:105-8.

Goyal MK, Mehta SC. Preparation and evaluation of calcium silicate

based floating microspheres of amoxicillin. J Appl Pharm Sci

;1:137- 41.

Martin A. Micrometrics. Physical pharmacy. 4th ed. Philadelphia: PA Le Febiger; 1993. p. 431-2.

Bala V, Priya M, Murthy T. Studies on influence of process variables on performance of gliclazide mucoadhesive microcapsules. Asian J Pharm


Anand AM. Pharm thesis, preparation and in vitro evaluation of

gastroretentive floating hollow microspheres of carvedilol. Birla

Institute of Technology; Ranchi, 2010.



  • There are currently no refbacks.