Marketed Formulations: Quality Evaluation of Conventional Release Paracetamol Tablet

 

Mukesh P. Ratnaparkhi*, Shilpa P. Chaudhari, Suresh B. Dhiwar, Rahul R. Gurav,

Department of Pharmaceutics, Marathwada Mitra Mandal’s College of Pharmacy, Kalewadi (Thergaon),Pune

*Corresponding author Email id: mukeshparkhi@yahoo.co.in

 

The main purpose of this work was to compare the quality of several marketed formulation and to evaluate the specifications laid down by FDA. Conventional release dosage forms are designed to achieve therapeutic effect by releasing drug over a short period of time after administration of dose. It allows the administration of dosage repeatedly in a day for short period of time as compared to extended release dosage form. The conventional paracetamol tablets were collected from market and evaluated for hardness, friability, weight variation, drug content, disintegration and in-vitro dissolution studies.

 

 

INTRODUCTION:

Conventional-release tablets are expected to achieve fast tablet disintegration which would dissolve rapidly in the gastrointestinal tract for absorption into the blood stream. The quality of a tablet affects its disintegration and dissolution in the gastrointestinal tract. Tablet quality is dependent on the physicochemical properties of the active pharmaceutical ingredients (API) and excipients used, as well as the manufacturing conditions employed during tablet compression^1.

The quality of compressed tablets is judged by parameters such as uniformity of weight, uniformity of drug content, hardness or crushing strength, disintegration time, friability, and in-vitro dissolution time². All these parameters are measured by a series of tests some of which are usually specified in accredited official compendia. A tablet is said to be of good quality if it conforms to all the specifications applicable to that tablet in the official compendia^1-4_.

 

MATERIALS AND METHODS:

Five different brands of marketed conventional release paracetamol 500 mg tablets were collected and evaluated for In-vitro studies.

 

Marketed preparations:-

P- 500 (Apex lab. Private Ltd. Alatur-603110, Tamilnadu)

TEMPTAL - 500 (Twilight Litaka Pharma. Ltd.,Vasai, Dist- Thane)

FEPANIL (Veritaz Healthcare Ltd., Hydrabad)

CORINOL (SGS Pharmaceuticals Pvt. Ltd, Gaziabad. U.P)

CALPOL (Glaxo Smith Kline Pharmaceuticals ltd. Warali Mumbai)

 

EXPERIMENTAL DESIGN:

Methodology:

The conventional release paracetamol tablet were collected from market and evaluated for in-vitro (Hardness, Disintegration time, Content uniformity and Dissolution studies) ^{5, 6}_.

 

IN- VITRO Evaluation of Marketed Formulations:-

HARDNESS:-

Hardness which is the force required to diametrically cause a tablet to fracture was determined using a Monsanto hardness tester.  This test was repeated twice and the mean recorded.

 

FRIABILITTY:-

The friability (FR) of the tablets was determined with a Friability Test Apparatus (Veego, Mumbai, India). Twenty (20) tablets were collected, dedusted and weighed on a precision balance and the weight recorded. The tablets were delivered into the transparent drums of the apparatus and set to rotate at 100 revolutions. The weight of dedusted tablets after the test was taken and the difference in weight expressed as a percentage of the initial weight. The tablets that loose less than 1% weight were considered to be compliant

Table No. 1:- Hardness, Disintegration Time, Percentage Drug Content and Friability of Five Conventional Release Marketed Paracetamol Preparations:

Sr. No.	Product	Hardness kg/cm2	Friability (%)	Disintegration Time(minutes)	% Drug Content
1	P-500	5	0.524	12	99.5
2	TEMPTAL 500	4.	0.654	11	98.90
3	FEPANIL	4	0.628	10	98
4	CORINOL	1	1.6	6	97
5	CALPOL	3.9	0.788	9	99

 

DISINTEGRATION TEST:-

Disintegration test was carried out in distilled water using the Tablet Disintegration test Apparatus (Veego India). Six tablets were placed in the cylindrical glass and the time taken for the tablets to disintegrate was recorded as disintegration time (DT).

                                                                                                   

CONTENT UNIFORMITY:

Weigh and powder 20 tablets. Weigh accurately a quantity of the powder equivalent to about 0.15 g of Paracetamol, add 50 ml of 0.1M sodium hydroxide dilute with 100 ml of water, shake for 15 minutes and add sufficient water to produce 200.0 ml. Mix, filter and dilute 10.0 ml of the filtrate to 100.0 ml with water. To 10.0 ml of the resulting solution add 10 ml of 0.1M sodium hydroxide, dilute to 100.0 ml with water and mix. Measure the absorbance of the resulting solution at the maximum at about 257 nm, Calculate the content of C₈H₉NO₂ taking 715 as the value of A (1%, 1 cm) at the maximum at about 257 nm.

 

IN-VITRO DISSOLUTION STUDIES:-

Dissolution test of tablet is carried out by using 900 ml of phosphate buffer pH 5.8.as the medium and rotating the paddle at 50 rpm for 60 minutes. Withdraw a suitable volume of the sample and filter promptly. Reject the first few ml of the filtrate and dilute a suitable volume of the filtrate with the same solvent. Measure the absorbance of the resulting solution at the maximum at 257 nm. Similarly measure the absorbance of a solution of known concentration of paracetamol RS. Calculate the content of C₈H₉NO₂ from the declared content of C₈H₉NO₂ in paracetamol RS.

 

RESULT AND DISCUSSION:

The tablet P-500, TEMPTAL-500, FEPANIL, and CALPOL shows the disintegration test, it ranges to 9-12

Minutes. The tablet CORINOL fails the disintegration test as it disintegrated within 6 min in acidic pH. It also fails to pass the hardness test and friability test as per Indian and US Pharmacopoeia Limit.

 

CONCLUSION:

The tablet P-500, TEMPTAL-500, FEPANIL and CALPOL a marketed preparation complies with all the pharmacopoeia specifications except tablet CORINOL. The tablet corinol fails to pass hardness test, friability test, disintegration test and dissolution test. The tablet corinol get rapidly dispersed in 5.8 phosphate buffer and does not show desired release pattern.

 

Table No. 2:- Dissolution test conditions in pH5.8 phosphate buffer

Sr. No.	Parameter	Specification
1	Dissolution medium	pH 5.8 phosphate buffer
2	Volume of medium	900 ml
3	Temp. of medium	37 ± 0.5
4	Paddle rotation speed	50 rpm.
5	Sampling time interval	10 min.
6	Detection wavelength	257 nm

 

Tablet (P-500, TEMPTAL-500, FEPANIL,  and  CALPOL ) Hardness was found  to in the range of  3.9 -5 kg /cm²  in all the  products  indicate  good mechanical strength .  in all the formulations  friability  values is less  than 1 % giving  an indication  tablets  formulated   are  mechanically  stable .% weight variation  was  within the limits . drug  contents  was know  by performing  assay and it was  found  to be between  98 to 99.5 % and  it was within  the limits

 

(As shown in Table No.  1). The  disintegration  time of various  marketed  preparation  were   found in the range  of  9-12  minutes  and also the dissolution profile  of all the conventional release  product  were within the pharmacopeia specification (As shown in Table No. 3) and  (As shown in Figure No.  1).

 

 

 

 

Table No. 3:- % Drug releases in pH 5.8 phosphate buffer:-

Sr. No.	PRODUCT	% DRUG RELEASES IN pH 5.8 PHOSPHATE BUFFER.
		0 min.	10 min.	20 min.	30 min.	40 min.	50 min.	60 min.
1	P- 500	36.33	81.45	88.81	93.49	97.83	98.73	100
2	TEMPTAL- 500	38.68	84.77	90.71	93.25	93.43	96.16	100
3	FEPANIL	56.52	85.77	88.32	94.46	96.67	98.10	100
4	CORINOL	84.19	90.20	95.43	97.30	99.06	100	-
5	CALPOL	37.26	89.30	90.19	93.04	94.73	96.23	100

 

Fig No. 1:- % Drug Release in pH 5.8 Phosphate Buffer

 

ACKNOWLEDGEMENT:

The authors are thankful to Principal Marathwada Mitra Mandal’s College of Pharmacy, Thergaon (Kalewadi) Pune  for providing all facilities required to complete this project work.

 

REFERENCES:

1.   Leon Lachman, Herbert A Liberman, Joseph L;The Theory and Practice of Industrial  Pharmacy. 3^rd ed. Varghese Publishing House Bombay, India, 1991: 331-332, 346,366-368.

2.   Tripathi K D; Essential of Medical Pharmacology .5^th ed., Jaypee Brothers Medical Publisher Ltd New Delhi. 210-216.

3.   Barar F S K;Essential of Pharmaceutics.3^rd ed., S Chand and Company  Publishers Ltd Ramnagar   New Delhi,2000:317-324.

4.   Chowdary K.P.P and Rajlakshmi Y.the Estern Pharmacist 1987,New  Delhi, Pamposh Publication.p,51

5.   Effect of Dissolution Media pH on the Release of Paracetamol tablets. colorcon, 1996.

6.  Indian Pharmacopoeia 1996 Published by Controller of    Publication, Delhi .A- 9

 

 

Received on 28.12.2011          Modified on 15.01.2012

Accepted on 12.02.2012         © RJPT All right reserved