SUPPOSITORY WITH DIFFERENT PEG AMOUNT

DEVELOPMENT OF PHARMACEUTICAL PRODUCT 

NFNF2283

SEMESTER 2

SESSION 2016/2017

LAB REPORT

LECTURER : DR. HALIZA KATAS 

GROUP MEMBERS :

NISHAAL KORAN (A153334)

TAN MIN ANNE (A152663)

MUHAMMAD ROSMAN BIN JUNAIDI (A153262)

MUHAMAD HAZWAN BIN HARUN (A152983)

LEOW PUI MUN (A152593)

THE EFFECT OF DIFFERENT AMOUNT OF PEG ON THE PHYSICAL CHARACTERISTICS OF SUPPOSITORY

Introduction

            Suppositories are normally in solid dosage forms of various sizes, appearance and weights intended for administration by rectal route where they melt, soften or dissolve to exert their effect. It is meant to be easily inserted into the orifice without causing undue distention.

            The suppositories are usually composed of medicaments incorporated in a suppository base, whereby it may be intended for retention within the cavity for localized drug effect or to be absorbed for systemic functions.

            The drug must be spread in a suitable base of suppository. Ideal suppository bases should be easily formed by compression or molding, readily release any medicament, melt at body temperature or either dissolve or disperse in body fluids, shape maintained while handling, compatible with the drugs, non-irritant and non-toxic.

            Polyethylene glycol (PEG) polymers are the commonly used suppository bases in the recent era as they possess many favourable properties. They are chemically stable, non-irritating, miscible with water and mucous secretion, and can be formulated, either by molding or compression into a wide range of hardness and melting point. In addition, they do melt at body temperature but dissolve to provide a prolonged release of drug.

           

Objective

1. To calibrate suppository mould with PEG before preparing medicated suppositories.

2. To determine the effect of different compositions of PEG base on the physical characteristics of suppositories.

Apparatus

Analytical balance                                                       1 × 5 ml measuring cylinder

Water bath at 37^oC                                                     1 × suppository mould set

Hot plate                                                                     1 × spatula

4 × 50 ml beaker                                                         4 × weighing boat

1 × 5 ml pipette and pipette bulb                                2 × glass rod

Materials

Polyethylene glycol (PEG) 1000

Polyethylene glycol (PEG) 6000

Paracetamol

Distilled water

Liquid paraffin

Methodology

A)  Calibration of Suppository Molds with PEG Base

For these calibration exercise, 10 gram of the proportions consist of PEG 1000 and PEG 6000 were used as in the table below:

Ingredients	Percentage	Weight (g)
PEG 1000	60%	6
PEG 6000	40%	4

PEG suppository base were calibrated with the mold as follows:

1. Clean and dry mold was taken and lubrication of the mold are not necessary.

2. PEG 1000 was melt on the hot plate, and mixed with other PEG after the heat was reduced.

3. The mixture were removed from the heat and poured into the mold after the mixture cool down a bit.

4. The cavities in the mold are overfilled and let it solidified under room temperature.

5. The excess were removed carefully with a hot spatula, after that suppositories were removed from the mold.

6. The suppositories were weighed and the total weight were recorded. The average suppositories weight were calculated.

B) Preparation of paracetamol suppositories

1. Saturated stock solution of paracetamol are prepared by adding 10 g of paracetamol in 5 mL distilled water.

2. Paracetamol suppository (10g) were prepared using the formulation below :

Suppository	PEG 1000 (g)	PEG 6000 (g)	Paracetamol stock solution (mL)	Total (g)
I	9	0	1	10
II	6	3	1	10
III	0	9	1	10

3. One type of PEG was melted on a hot plate then mixed with the other PEG after the heat was reduced.

4. The mixture was removed from the heat and poured into the mold after allowing it to cool down.

5. The cavities in the mold were overfilled and the mixture was left to solidify into suppositories.

6. The excess were removed carefully with a hot spatula, then the suppositories were removed from the mold.

7. The shape, texture and color of the suppositories were observed.

8. Each of the suppositories was put into a separate beaker containing distilled water (10 ml) and pre-
warmed at 37℃ and then the beaker was put into a water bath (37℃).

9. The time for the suppositories to start melting was recorded.

Results

A) Calibration of suppository molds with PEG base

Mold #	6
Total weight for 6 suppositories	5.8715 g
Average weight for one suppository	0.9786 g

Discussion

1. Describe the importance of calibrating suppository mould before preparing medicated suppository.

Calibrating suppository is vital due to the reason that each individual mould is capable of holding a specific volume of material. However, this does not directly indicate the mass of certain suppositories produced due to differences in the density of the materials, such as suppository bases and medicaments. Different bases will produce suppositories with different mass in the final product depending on the displacement or density ratio. This enables us to determine the amount of base and medicaments to be used to prepare the requested suppositories.

2. Describe function of each ingredients in the suppository function.

Paracetamol is the active ingredient in the suppository formulation that acts as the pain killer to relief headache. PEG acts as the carrier base, absorption improver and solubilizer for the drug. The mixtures of PEGs are used to give varying degree of hardness for the compound. In this experiment, we used 2 types of PEG which are PEG 1000 and PEG 6000. PEG 6000 can form more hydrogen bond compared to PEG 1000. Thus, it makes the suppository harder to dissolve, hence it produces a dry, hard, smooth, coarse, tackier and clear white suppository. PEG 1000 can form less hydrogen bond so it gives softness to the suppository. It takes a longer time to solidify and makes the suppository to dissolve easily. It produces greasy and soft suppository.

3. Plot a graph time required to melt the suppository vs. the amount of PEG6000 in the formulation. Compare and explain the results.

Amount of PEG6000 (g)	0	3	9
Time (mins)	7.30	5.25	3.08

Theoretically, the more the amount of polyethylene glycol 6000 (PEG 6000), the more hydrogen bonds are able to form due to presence of hydroxyl groups. This means that it will become harder and requires more time to melt, thus releasing the paracetamol at a slower rate. However, our result shows otherwise. This inaccuracy is due to the error of accidental addition of water when immersed in the water bath, causing it to be able to form more hydrogen bonds. A Noyes-Whitney equation of dissolution can explain the theory behind the addition of water which will reduce the timing for it to melt and release paracetamol faster. 

Conclusion

The higher the amount of PEG used, the longer the time needed for it to melt. Hence, the release of medication from it happens at a slower rate.