SHRI GURU RAM RAI INSTITUTE OF TECHNOLOGY AND SCIENCE

EXPERIMENT NO:Aim: To Design Mouth Dissolving Tablets Of Acyclovir. Requirements:Equipments:Tablet punching machine, U.V Spectrophotometer, Dissolution Apparatus (USP II) Laboratory apparatus:Mortar &pestle, Sieve #60, Measuring cylinder (100 ml), Beaker Chemical requirements:-Acyclovirl, Mannitol, Cross carmellose sodium,Cross povidone, Lactose, Clove oil, Micro crystalline cellulose, Talc, Mg stearate. Theory:Tablet:Tablets are representing unit dosage forms in which one usual dose of drug has been accurately placed by compression. Mouth Dissolving Tablets Mouth dissolving tablet undergo disaggregating in the mouth when in contact with the saliva in less then 60sec forming a suspension which is easy to swallow. Patient particularly pediatric and geriatric patient, have difficulty in swallowing solid dosage forms. These patients are unwilling to take these solid preparations due to a fear of choking. In order to assist systems has been developed. Mouth dissolving tablets dissolve rapidly in the saliva without the need for water, releasing the drug. The purpose of the present was to design Acyclovir mouth dissolving tablets using superdisintegrants, natural sweetner, flavouring agent in different proportion to achieve patient compliance. Drug Profile Acyclovir Acyclovir is a guanine analogue antiviral drug used for the treatment of herpes simplex virus. Acyclovir is poorly water soluble and has poor oral bioavailability (15-30%), hence intravenous administration is necessary if high concentration are required. When orally administered, peak plasma concentration occurs after 1-2 hours. Description: A white or almost white, crystalline powder. Mechanism of action: It is selectively converted into acyclo-guanosine monophosphate (acyclo-GMP) by viral thymidine kinase, which is far more effective (3000 times) in phosphorylation than cellular thymidine kinase.

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Adverse effects: Common adverse drug reactions (1% of patients) associated with systemic acyclovir therapy (oral or IV) include: nausea, vomiting, diarrhoea and /or headache. In high doses, hallucinations have been reported. Methodology:Preparation of standard curve of Acyclovir Weigh accurately 100mg of acyclovir and dissolve in 0.1N HCL make it upto 100ml and mark it as a stock solution having the concentration of 1000mcg/ml. Take 10ml of sample and dilute it to 100ml with 0.1N HCL. Prepare the dilution in the Beers range of 2-20g/ml. The preparation was scanned at 200-350 nm.
Preparation of Floating Tablets The entire ingredient was passed through sieve#60. Cetirizine hydrochloride, mannitol, micro crystalline cellulose and Stevia leaf powder were triturated in a glass mortar. MCC , Cross carmellose sodium, Cross povidone were incorporated in the powder mixture and finally magnesium state and talc were added. The mixed blend was then compressed with 10mm flat face surface punches using hydraulic press single tablet punching machine. Evaluation parameters:-

All prepared tablets were evaluated for: Thickness Hardness Friability and Weight variation test

Hardness test: -Hardness was measured by using Pfizer hardness tester. Friability test: -Friability was determined using Roche friabilator. Weight variation test: -Weight variation test was conducted as per the official procedure.

SHRI GURU RAM RAI INSTITUTE OF TECHNOLOGY AND SCIENCE

Table: - Limits of various evaluation parameters. S.no Evaluation parameters Limits

WEIGHT VARIATION 80 mg or less 80mg 250 mg 250 mg or more +10% +7.5% +5% Less than 1% Less than5 kg/cm2

FRIABILITY

HARDNESS

Result & Discussion Table 1: Standard curve of Acyclovir S.no 1 2 3 4 5 6 Concentration(/ml) 0 2 4 6 8 10 Absorbance(nm) 0 0.1355 0.2608 0.3699 0.5141 0.8350

SHRI GURU RAM RAI INSTITUTE OF TECHNOLOGY AND SCIENCE

0.9 0.8 0.7 0.6 y = 0.0774x - 0.0346 R = 0.956

Absorbance

0.5 0.4 0.3 0.2 0.1 0 -0.1 0 2 4 6 Con(g/ml) 8 10 12

Beers Range: - 2 to 20 g/ml Line of equation:-y = mx + c (y = 0.077x-0.034) Maximum wavelength: - 253 nm Maximum absorbance: -0.431 nm Regression coefficient (r2):-0.956

SHRI GURU RAM RAI INSTITUTE OF TECHNOLOGY AND SCIENCE

Table2:-Composition of Tablet formulation.

Formulation code Ingredients (mg/tab)

F1

F2

Acyclovir

10

10

2 3

Mannitol Cross carmellose Sodium Cross povidone Stevia leaf powder MCC

50 10

50 20

4 5 6

10 5 204

20 5 184

Mg Stearate

Talc

Clove oil

10

Total weight

300

300

SHRI GURU RAM RAI INSTITUTE OF TECHNOLOGY AND SCIENCE

Table 3:- Physical properties of Acyclovir mouth dissolving tablet. S.no Formulation Hardness (kg/cm2) wt. Variation Friability (%) Thickness (mm)

F1

4.38

23.08

0.45

23.08

F2

3.10

17.05

0.66

17.05

Discussion:

Conclusion:

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References: J.Padmavathy et al, Formulation and Evaluation of Ofloxacin Floating Tablets using HPMC IJPER, vol 3, issue 1, 2011, p.p- 171-173
Nayak A.K et al, Gastroretentive drug delivery system: a review AJPCR, vol 3, issue 1, 2010, p.p- 1-9