Design of fast dissolving amlodipine besylate tablet formulations

Harekrishna Roy, Kirti R Parida, Sisir Nandi, Sanjay K Panda, Debendra K Mohapatra

Abstract


The demand for fast disintegrating tablets has been growing during the last decade especially for geriatric and pediatric patients because of swallowing difficulties. Amlodipine besylate is used commonly for the treatment angina pectoris, commonly known as angina, which is chest pain due to ischemia of the heart muscle, generally due to obstruction or spasm of the coronary arteries. Hence, in the present work an attempt has been made to formulate fast dissolving tablets of amlodipine besylate by direct compression technique using various concentration of super disintegrants like cross carmellose
sodium (Ac-Di-Sol), polyplasdone R-XL and sodium starch glycolate (SSG). The formulated tablets were evaluated for crushing strength, friability, thickness, diameter, weight variation, drug content, wetting time, water absorption ratio,
disintegration time, and percentage of drug release. All formulations showed satisfactory result. Among them formulation F3 containing 3% of Ac-Di-Sol exhibited complete release within 12 minutes and disintegration time was within 10 seconds. Dissolution data was compared with innovator for similarity factor (f2) exhibited an acceptable value >50 (82). Accelerated stability study indicated no significant difference in assay and crushing strength. Hence, three production validation scale batches were designed based on lab scale best batch (F3) and charged for stability. All parameters were within the limit of acceptance. There was no chemical interaction between the drug and excipients during FT-IR study;
considered in the present investigation.


Full Text:

PDF

References


Bhowmik D, Chiranjib B, Krishnakanth P, Chandira RM. Fast dissolving

tablet: An overview. J Chem Pharm Res 2009;1:163-77.

Setty CM, Prasad DV, Gupta VR, Sa B. Development of fast dispersible

aceclofenac tablets: Effect of functionality of superdisintegrants. Indian

J Pharm Sci 2008;70:180-5.

Mizumoto T, Masuda Y, Yamamoto T, Yonemochi E, Terada K.

Formulation design of a novel fast-disintegrating tablet. Int J Pharm

;306:83-90.

Schiermeier S, Schmidt PC. Fast dispersible ibuprofen tablets. Eur J

Pharm Sci 2002;15:295-305.

Aryal S, Skalko-basnet N. Stability of amlodipine besylate and atenolol in multi component tablets of mono-layer and bi-layer types. Acta Pharm

;58:299-308.

Ohmori M, Arakawa M, Harada K, Takasaki H, Hifumi S, Miyamori I, et al.Stereoselective pharmacokinetics of amlodipine in elderly hypertensive

patients. Am J Ther 2003;10:29-31.

Zhao N, Augsburger LL. Functionality comparison of 3 classes of

superdisintegrants in promoting aspirin tablets disintegration and

dissolution. AAPS PharmSciTech 2005;6:E634-40.

Bhagwati ST, Hiremath SN, Sreenivas SA. Comparative evaluation of

disintegrants by formulating cefixime dispersible tablets. Ind J Pharm

Edu Res 2005;39:194-7.

Sohi H, Sultana Y, Khar RK. Taste masking technologies in oral

pharmaceuticals: recent developments and approaches. Drug Dev Ind

Pharm 2004;30:429-48.

Chandrasekhar R, Hassan Z, Alhusban B, Smith AM, Mohammad AR.

The role of formulation excipients in the development of lyophilised

fast-disintegrating tablets. Eur J Pharm Biopharm 2009;72:119-29.

Gohel MC, Parikh RK, Brahmbhatt BK, Shah AR. Preparation and

assessment of novel coprocessed superdisintegrant consisting of

crospovidone and sodium starch glycolate: a technical note. AAPS

PharmSciTech 2007;8:9.

Fukami J, Yonemochi B, Yoshihashi Y, Terada K. Evaluation of rapidly

disintegrating tablets containing glycine and carboxymethylcellulose.

Int J Pharm 2006;310:101-9.

Madgulkar AR, Bhalekar MR, Padalkar RR. Formulation design and

optimization of novel taste masked mouth-dissolvingtablets of

tramadol having adequate mechanical strength. AAPS PharmSciTech

;10:574-81.

Bi Y, Sunada H, Yonezawa Y, Danjo K, Otsuka A, Iida K. Preparation and

evaluation of a compressed tablet rapidly disintegrating in the oral

cavity. Chem Pharm Bull (Tokyo) 1996;44:2121-7.

Chang R, Guo X, Burnside BA, Couch R. Fast-dissolving tablets. Pharm

Technol 2000;24:52-8.

Venkatesh DP, Geetha Rao CG. Formulation of taste masked oro-dispersible

tablets of ambroxol hydrochloride. Asian J Pharm 2008;2: 261-4

Jha SK, Vijayalakshmi P, Karki R, Goli D. Formulation and evaluation of

melt-in-mouth tablets of haloperidol. Asian J Pharma 2008;2:255-60.

Malke S, Shidhaye S, Kadam VJ. Formulation and evaluation of

oxcarbazepine fast dissolving tablets. Indian J Pharm Sci 2007;69:

-4.

Marais AF, Song M, Devilliers MM. Effect of compression force, humidity

and disintegrants and dissolution of directly compressed furosemide

tablets using croscarmellose sodium as disintegrants. Tropical J Pharm

Res 2003;2:125-35.

Sutariya VB, Mashru RC, Sankalia MJ. Preparation of rapidly

disintegrating tablets of ondansetron hydrochloride by direct

compression method. Ars Pharm 2006;47:293-311.

Kawtikwar PS, Zade PS, Sakarkar DM. Formulation, Evaluation

and optimization of fast dissolving tablet containing tizanidine

hydrochloride. Int J PharmTech Res 2009;1:34-42.

Gosai AR, Patil SB, Sawant KK. Formulation and evaluation of

orodispersible tablets of ondansetron hydrochloride by direct

compression using superdisintegrants. Int J Pharm Sci Nanotechnol

;1:106-11.

al-Gohary OM, al-Kassas RS. Stability studies of aspirin-magaldrate

double layer tablets. Pharm Acta Helv 2000;74:351-60.

Pokharkar V, Khanna A, Venkatpurwar V, Dhar S, Mandpe L. Ternary

complexation of carvedilol, beta-cyclodextrin and citric acid for mouth-

dissolving tablet formulation. Acta Pharm 2009;59:121-32.




DOI: http://dx.doi.org/10.22377/ajp.v6i1.73

Refbacks

  • There are currently no refbacks.