FORMULATION AND EVALUATION OF SUBLINGUAL TABLETS OF NIFEDIPINE
*DINESH BABU GOTTIPATI1, SREE DEVI ANANDHAM1, NANNAPANENI VENKATA BALAKRISHNA RAO2.
1 Department of pharmaceutics, M.E.S.college of pharmacy, Aradeshally gate, Bangalore -562110,India.
2 Research and Development Department, Natco Pharma Limited, Kothur.
The aim of this study was to evaluate the effect of increasing nifedipine on the characteristics of fast-disintegrating sublingual tablets for the potential emergency treatment of anginal pain and hypertension. Nifedipine undergoes first pass metabolism in liver and gut wall which has oral bioavailability of 43-77%. Sublingual dosage form bypasses the metabolism of the nifedipine in liver and offers a fast relieve from anginal pain and hypertension. An attempt has been made to prepare fast dissolving tablets of nifedipine were prepared by wet granulation technique using Crospovidone and croscarmellose sodium (CCS) as super disintegrants as super disintegrants, Flavor and sweetener impart the taste to the formulation. The porous granules were compressed in to tablets by 8mm punch rotary tablet machine. All the formulations were evaluated for weight variation, hardness, friability, content uniformity, wetting time, and disintegration time and dissolution rate. Among the formulations, F9 one containing to be the best acceptable in terms of palatability, fast dissolving tablet having adequate strength. The disintegration time was found to be 56 ± 0.4 seconds, hardness of 4.6 ± g /cm2, wetting time of 31sec and drug release of 99.85 % in 9 mins. All the formulations showed low weight variation. The present study demonstrated potentials for rapid absorption, improved bioavailability, effective therapy and patient compliance.
Reference Id: PHARMATUTOR-ART-1303
Tablet administration difficulties are common among all patient groups and can exacerbate compliance problems and undermine treatment efficacy. Physical problems with swallowing (dysphasia) can occur at any age but are particularly prevalent in the elderly and those with dementia, whereas refusal to swallow is often encountered in geriatric, pediatric, and psychiatric patients 1.Nonetheless, oral dosing remains the preferred mode of administration for many types of medication due to its simplicity, versatility, convenience, and patient acceptability. In recent years, sub-lingual oral drug formulations have been developed to overcome problems related to swallowing difficulties. It is dose dependently absorbed after oral administration and undergoes excessive first pass metabolism, thereby making it a suitable candidate for sublingual dosage form2.Sincethe drug can be absorbed partially or entirely into the systemic circulation from blood vessels in the sublingual mucosa, the sublingual route bypasses the hepatic first pass metabolic processes, thus producing rapid onset of action. The sublingual route is appropriate for drugs with Short delivery period requirements, for drugs which are inactivated by first pass – intestinal or hepatic metabolism
E.g. : Nifedipine , nitroglycerin.
These dosage forms dissolves or disintegrate in oral cavity within a minute without the need of water or chewing3. Nifedipine is a dihydropyridine calcium channel antagonist originally introduced for the treatment of angina pectoris4 hypertension and anti-atherosclerotic activity5. The sublingual6 dosage form offers fast release of drug from the formulation and it reaches the systemic circulation directly, which bypasses the metabolism of the nifedipine in the liver and offers a fast relive form the anginal pain, hypertension which will be worth in such conditions. The objective of study was to enhance safety and efficacy of drug molecule, achieve better compliance, solve swallowing problem, enhance onset of action and provide stable dosage form.
MATERIALS AND METHODS:
Materials: Nifedipinewas procured from MEDOPHARM, Karnataka. Aerosil ,talc, Aspartame, PVP ,mannitol, croscarmellose sodium ,Crospovidone, Raspberry flavor were procured from Karnataka fine chemicals, Bangalore. All other reagents and solvents used were of analytical grade.
Methods: The sublingual tablets of Nifedipine were prepared using different combinations of Crospovidone and croscarmellose sodium (CCS) as super disintegrants, mannitol as a diluents, Aspartame as sweetening agent, alcoholic solution of PVP(10 % w/v) as binder and aerosil with talc as a flow promoters (Table 1). The drug and other ingredients were mixed together, and a sufficient quantity of alcoholic solution of PVP (10 %w/v) was added and mixed to form a coherent mass. The wet mass was granulated using sieve no. 12 and dried at 600 C for 30 min. The dried granules were re-granulated by passing through sieve no. 16. The dried granules were then blended with talc, aerosil and compressed into tablets using a 8mm punch rotary tablet machine (Rimek, RSB-4minipress Cadmach, Ahmedabad, India).Experiments were carried out systematically to analyze the effect of different concentrations of disintegrants on the wetting time and In vitro dispersion time of the tablets, using a response surface methodology and to develop an optimized formulation.
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