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JOURNAL CLUB SEMINAR ON

FORMULATION AND EVALUATION OF NIFEDIPINE SUBLINGUAL BY TABLETS


S.VIJAYKUMAR M.PHARM(PHARMACEUTICS) ,1St SEM BALAJI INSTITUTE OF PHARMACEUTICAL SCIENCES, NARSAMPET.

SOURCE:ASIAN JOURNAL OF PHARMACEUTICAL AND CLINICAL RESEARCH VOL-2 ISSUE 3,JULY-SEPTEMBER 2009

CONTENTS:
      

Introduction Materials Preparation of sublingual tablets Evaluation of sublingual tablets Results and discussion Conclusions References

INTRODUCTION:  The sublingual route usually produces a faster onset of action than orally ingested tablets and the portion absorbed through sublingual blood vessels by passes the hepatic first phase metabolic processes.  Nifedipine is a dihydro pyridine calcium channel antagonist originally introduced for the treatment for the angina pectoris ,hypertension and anti- atherosclerotic activity..  These sublingual dosage forms offers fast release of drug from the formulation and it reaches systemic circulation directly, which bypasses the metabolism of nifedipine in the liver and offers the fast relive from the angina pain , hypertension.  various techniques can be used to formulate rapidly disintegrating and dissolving tablets. Direct compression is one of these techniques which requires incarporation of a super disintegrate into the formulation or the use of highly water soluble excipients to achieve fast tablet disintegration.

 Direct compression does not require water or heating formulation process and is the ideal method for moisture and heat-labile medications .  Extremely fast tablet disintegration would be required to enhance the release of nifedipine from tablets for rapid absorption by the sublingual mucosa and blood vessels.  It was decide that nifedipine could be formulated into fast- disintegrating tablets for sublingual administration as potential emergency treatment of angina pectoris and hypertension. This could be achieved by selecting the appropriate pharmaceutical excipients in correct proportion , In combination with suitable manufacturing techniques.

MATERIALS: Nifedipine Avicel pH 101(binding agent) Mannitol (diluent) Lactose DCL(diluent) Magnesium stearate (Lubricant) Talc (Glidant) Sodium sacharine (sweetening agent) Cross povidone (enhance dissolution rate) Citric acid (antioxidant) Cross carmellose sodium (disintegrant) Sodium starch glycollate (disintegrant) Aerosil

PREPARATION OF SUBLINGUAL TABLETS:


 Nifedipine sublingual tablets were prepared by the direct compression method. using different excipients.  Different concentrations of excipients used to prepare different group of sublingual tablets. DIFFERENT FORMULATIONS OF NIFEDIPINE SUBLINGUAL TABLETS

 All the ingredients of sublingual tablets of nifedipine were weighed and mixed in a mortar with the help of a pestle, then finally 2mg magnesium stearate and 2mg of talc,1 mg of aerosil was added for lubrication and triturate well.  After trituration, the blended material was slightly compressed on 6mm flat faced punch using a Rimek MINI PRESS-2 MT tablet machine (karnawati Engg. Ltd., Mehsana,india).  The total weight of formulation was maintained 150mg

EVALUATION OF SUBLINGUAL TABLETS:


 Weight variation test  Hardness test  Friability test  Disintegration time  Dissolution studies 

Drug content

 Weight variation test:


weight variation test was conducted by selecting 20 tablets at random as per I.P  Friability test: Six tablets from each batch were examined for friability using ROCHE FRIABILATOR and the equipment run for 4 min at 25 revolutions per minute. The tablets were taken out ,dedusted and reweighed.

 Hardness test:
The hardness of the tablet was determined using Monsanto hardness tester.

 Disintegration time:
The test was carried out by using disintegration apparatus. Distilled water was used as a disintegration media at 24+_ 0.2o c.The time required to obtain complete disintegration of all the tablets were noted.

 Drug content:
Five tablets from each batch were finely powdered and the powder equivalent to 50mg of nifedipine was weighed and dissolved in suitable quantity of methanol. The solution filtered, suitably diluted and the drug content was analyzed spectrophotometrically (Shimadzu,UV-1601) at 350 nm.

 In-vitro drug release study: Dissolution study was conducted for all the formulations using USP apparatus type-2. 900 milliliters of phosphate buffer (pH7.5) was taken as the dissolution medium at 100 rpm and 37 0.50 c for 50 min. 5 milliliters of aliquots were periodically withdrawn ,and the sample volume was replaced with an equal volume of fresh dissolution medium. The samples analyzed spectrophotometrically at 350 nm.

Results and Discussion:


 Nifedipine sublingual tablets were prepared by direct compression method.  Three different groups(A,V,R) of formulation with various excipients were prepared.  All tablets were evaluated for physical parameters such as hardness, friability, disintegration, dissolution ,drug content.  All the tablets maintained hardness in the range of 4.9-6.8 kg /cm2.  The loss in total weight of the tablets due to friability in the range of 0.18-0.6 %.  The drug content in different formulations was highly uniform and in the range of 98-100%.  Formulation V was quickly disintegrated compared to other formulation A,R.  From the in-vitro dissolution studies ,it was observed that formulation V1 showed 99.49% dissolution efficiency in 50 min.

Evaluation data :

 In conclusion , this study clearly indicated that the fast disintegration and dissolution of the optimized nifedipine sublingual tablet ,which is prerquisite for the rapid management of anginal hypertension diseases.

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