Experiment 3


TITLE: Evaluation of different effects of ingredients towards the ointment formulation.

OBJECTIVE:
To study the effect of ointment composition towards the physical properties of the ointment and the rate of drugs release from the ointment formulation.

INTRODUCTION:
Ointments are preparations that are used as an external application. Ointment has a greasy base and this would differentiate it with cream preparations. The base is usually anhydrous and immiscible with skin secretions. A medicament would usually be incorporated in the ointment. Sometimes, it can also contain a mixture of medicaments that is dissolved or dispersed in the base. Traditionally the base in an ointment would consist of a mixture of waxes, fats, and oils. Waxes are usually solid and hard at room temperature. Fats on the other hand would  be semi solid and soft at room temperature whilst oils would be liquid at room temperature. Wax would render the ointment to be more smooth and light in its consistency. By altering the proportions of oil, fat and wax in the ointment may vary the consistency. For example, if we were to add extra wax, then the ointments would be stiffer whereas if we were to add more oil, the ointment would be less viscous. Depending on the storage condition or the climatic condition, this proportion may vary.

APPARATUS:
Weighing instrument                                                   
Weighing boat                                                             
100ml beaker                                                              
Heater                                                                         
 1 set of cream and spatula                                          
Mortar and pestle
Dialysis bag (10cm)
Thread
Glass rod
Water-bath
1 set of pipette (5 ml) and pipette-bulb
1 plastic kuvet
Spectrophotometer UV/Vis 

MATERIALS:
Emulsifying wax
White soft paraffin
Liquid paraffin
Acetylsalicylic acid
 Distilled water


PROCEDURE:





1. 50g of Emulsifying Ointment was prepared for the following formulation:

Emulsifying Ointment
Ingredients (g)
Total (g)
Emulsifying wax
White soft paraffin
Liquid paraffin
I
21
25
4
50
II
17
25
8
50
III
13
25
12
50
IV
9
25
16
50

2. 5 g of cream was taken and put into the weighing boat and was labeled. The texture, clarity and the color of the cream was described and compared.
3. 1.5 g of Acetylsalicylic acid powder was incorporated into 30 g of cream which was prepared by levigation technique.
4. Acetylsalicylic acid was filled into the dialysis bag and the two side of the bag was tied.

5. The bag was put into a beaker (200ml) filled with distilled water (100ml) which was heated to 37°C.



6. Every 5 minutes, one aliquot sample (3 – 4 ml) was pipette and the release of Acetylsalicylic acid from the cream base was determined by using spectrometer UV-visible. The distilled water was stirred with glass rod before the sample was taken.

RESULT AND CALCULATION:

Time (min)
UV Absorption
0
5
10
15
20
25
30
35
40
45
50
55
60
UV Absorption on 310 nm
0.030
0.068
0.070
0.095
0.112
0.128
0.157
-
-
-
-
-
-
*(-) means no reading were taken since experiment stopped after 30 minutes
Time(min)
Average of UV absorption at 300 nm ( x ± SD)

0
5
10
15
20
25
30

I
0.0225 ± 0.0075
0.062 ± 0.006
0.066 ± 0.01
0.0945 ± 0.0005
0.1105 ± 0.0015
0.159 ± 0.031
0.139 ±  0.018
II
0.049 ± 0.024
0.285 ± 0.165
0.316 ± 0.176
0.3535 ± 0.1735
0.398 ± 0.155
0.422 ± 0.159
0.451 ± 0.165
III
0.037 ± 0.002
0.041 ± 0.001
0.0795 ± 0.0335
0.078 ± 0.023
0.11 ± 0.052
0.127 ± 0.065
0.1545 ± 0.0845
IV
0.0815 ± 0.0185
0.152 ± 0.031
0.218 ± 0.006
0.2225 ± 0.0015
0.2285 ± 0.0065
0.267 ± 0.027
0.321 ± 0.01




DISCUSSION

1.      Compare the physical appearance of the ointment formed and give your explanation.
Ointment 1 (21 g EW, 25 g WSP, 4 g LP) :
It has low spreadibility. It also has high greasiness compared to other ointment. The hardness is the most suitable compared to other ointment. The colour produce is white.
Ointment 2 (17 g EW, 25 g WSP, 8 g LP) :
Spreadibility is low. More greasiness compared to ointment III and IV and less greasiness compared to ointment I. It has the most suitable hardness compared to ointment III and IV but less compared to ointment I. white colour also has been produced as same to others.
Ointment 3 (13 g EW, 25 g WSP, 12 g LP) :
It has high spreadibility. It also has high greasiness compared to ointment IV and less greasiness compared to ointment I and II. The hardness is the most suitable compared to ointment IV and less hardness compared to ointment I and II. The colour produce is also white.
Ointment 4 (9 g EW, 25 g WSP, 16 g LP) :
Spreadibility is very high. Less greasiness compared to others ointment. The hardness is the lower compared to others ointment. White colour also has been produced as same to others.
EW : Emulsifying Wax, WSP : White Soft Paraffin, LP : Liquid Paraffin



2. Plot graph of UV absorption against time. Discuss.



This graph measures the release of acetylsalicylic acid from the ointment in the dialysis bag immersed in the 100ml 37C distilled water.  Generally, UV absorption increase with time. Initially, at the first 5 minutes, the UV absorption value surge up follow by gradual increasing of the UV absorption value until 30 minutes. This due to the hypertonicity of dialysis content to distilled water is at maximum now. As time increase further, the increasing pattern of UV absorption becomes smaller and almost constant. This is due to more acetylsalicylic acid diffuse out of dialysis bag, making the concentration of this solute between inside and outside dialysis bag reach to equilibrium (isotonic). If experiment continued to 60 minutes, UV absorption may increase further with smaller increasing pattern.
The present UV absorption value at 0 minute explains the present of acetylsalicylic acid in the distilled water. It might due to residue of ointment which sticks on outside of dialysis bag during insertion of the ointment into the dialysis bag’s hole.
                   



3. Plot a graph of UV absorption against time for different composition of emulsifying ointment. Compare and discuss your result.

Emulsifying wax is used to keep water and oil together. Liquid paraffin is used to reduce the viscosity of base so that it can be easily expelled out from container. In this experiment, the ratio of emulsifying wax and liquid paraffin are different for every group. This is to investigate the permeation of acetylsalicylic acid from the ointment which small amount of acetylsalicylic acid permeate the dialysis bag with the high content of emulsifying wax. Thus, the value of UV absorption will become smaller.



According to the theory, UV absorption of the formulation must increase with time because more amount of acetylsalicylic acid diffuse out of the dialysis bag when exposed longer in the water bath. Hence, more UV is absorbed by acetysalicyclic acid. As we can see in tthe graph, most of the formulation have increasing pattern which means the UV absorption increase as longer time remain in the water bath. The graph that shows most UV absorption is formulation from group IV followed by group II, III and I. The graph match with the theory as group I formulation with the highest content of emulsifying wax have lowest UV absorption, followed by group II,III and IV. Group IV have the lowest content of emulsifying wax, thus have highest UV absorption.




4. Discuss the functions of the materials in the ointment. How does the different composition of the emulsifying wax and liquid paraffin components affect the physical appearance of the ointments formed and the releasing rate of the drug from the ointments?
            One of the materials used is the emulsifying ingredients. The emulsifying wax is an emulsifying agent that is used to prepare oil in water emulsion that makes the oily form becomes soluble in water and miscible with water. It allows the ointment to have self-emulsifying property. It also acts as a surfactant that reduces the surface tension and hence increases acetylsalicylic acid released from the formulation. A high concentration of emulsifying wax results in a hard ointment. Big and coarse crystals can be formed by a high percentage of emulsifying wax and a low content of liquid paraffin.
            The white soft paraffin oil is also known as white petroleum jelly. This is not an active ingredient but it acts as a moisturizer by providing a thin layer of oil on the skin surface to prevent water to evaporate from the skin surface. It is a very greasy moisturizer and thus used as a base that enhances the absorption of acetylsalicylic acid through the membrane into the circulation.
            Besides, the liquid paraffin acts to soften and reduce the viscosity of the ointment due to the addition of emulsifying wax. It also acts as an emollient. It increases the spreading ability of the acetylsalicylic acid and also decreases the hardness of the ointment. A high composition of liquid paraffin reduces the amount of the emulsifying wax needed in the formulation. A high proportion of liquid paraffin used in the formulation produces a watery, greasy and soft ointment which subsequently decreases the rate of drug released from the ointments.
            The acetylsalicylic acid used in the formulation acts as active ingredient. It is a salicylate drug which often used as an analgesic to relieve minor aches and pains. Besides, it also acts as an antipyretic to reduce fever, and as an anti-inflammatory drug. Distilled water is the solution in which its impurities are removed by the process of distillation. It allows the measurement of the UV absorption to be taken. It increases the accuracy of the reading of the UV absorption taken.

CONCLUSION:

The composition of ointment will affect its physical property and the drug’s release rate from the ointment.

REFERRENCES:

1.      Pharmaceutics: the science of dosage form design, Aulton, M.E.2002
2.      http://www.teachsoap.com/emulsifywax.html
3.      http://www.esoapsupplies.com/emulsifying_wax.htm
4.      www.buzzle.com/articles/liquid-paraffin-oil.html
5.      www.chemicalland21.com/lifescience/phar/ACETYLSALICYLIC%20ACID.htm
6.      www.pharmpedia.com/Emulsifying_agent