Wednesday, May 21, 2014

OINTMENT

Tittle: Effects of different component to the formulation of ointments

Objectives:
    1)      To determine whether the difference in ointment component will affect their physical characteristic.
    2)      To determine the rate of drug release from ointment.


Introduction:

        An ointment is a homogeneous, viscous, semi-solid preparation, most commonly a greasy, thick oil (oil 80% - water 20%) with a high viscosity, that is intended for external application to the skin or mucous membranes. They are used as emollients or for the application of active ingredients to the skin for protective, therapeutic, or prophylactic purposes and where a degree of occlusion is desired.
Ointments are used topically on a variety of body surfaces. These include the skin and the mucous membranes of the eye (an eye ointment), vulvaanus, and nose. An ointment may or may not be medicated.
Ointments are usually very moisturizing, and good for dry skin. They have a low risk of sensitization due to having few ingredients beyond the base oil or fat, and low irritation risk. There is typically little variability between brands of generics and name brand drugs. They are often disliked by patients due to greasiness. Therefore it need to be attractive and easy to apply on skin for patient compliance and also need to be in good rate of drug release.


Chemical and apparatus:   

     a)      Apparatus

Weighting scale, weighting boat, 500 ml beaker, heater, slap & spatula set, mortar & pestle set, dialysis bag, thread, glass rod, water-bath, 5ml pipette & pipette-bulb, Spectrometer UV-visible,

    b)      Chemicals

Emulsifying wax, White soft paraffin, liquid paraffin, Acetylsalicylis Acid, distilled water.

Procedure:

    1.      The Emulsifying Ointment (50 g) is prepared by using this formula



 2.      5g of ointments is put into the weighing boat and labeled. The ointment texture, clarity and colour had been compare and discuss.

       3.      1.5 g of Acetylic acid had been incorporated with the 30g of ointment with levigation technique.
       4.      The acetylic acid ointment is filled in the dialysis bag and tied at both edge.

      5.      The base was put in the 500ml beaker that contain distilled water that been heated to
       37 0C.
       6.      The aliquot sample is pipette out about 3-4 ml in every 5 minute intervals and the release of Acetylic              acid is determined from the ointment base by using Spectrometer UV-visible. The distiied water need to        be stir first with glass rod before take the sample.

RESULT


 DISCUSSION

    1.       Compare the physical texture of the ointment formed and give explanation.

The hardness of the ointment decreases from ointment I to ointment IV because the content of emulsifying wax is decreased from ointment I to IV. In ointment IV with emulsifying wax of only 9g, is not enough to produce “interlocking wax” structure, thus ointment IV is very soft and clear while ointment I with 21g of emulsifying wax is very hard and opaque. Emulsifying wax prevents the coalescence of globules of the dispersed phase and increases the viscosity of the ointments. Thus, high proportion of emulsifying wax in the ointment will decrease the spread ability of the ointments causes it difficult to be applied onto the skin.
The greasiness of the ointments increases as liquid paraffin amount is increases. Liquid paraffin’s function is to soften the ointment. This will aid in the ointment penetration through the skin but give greasy feeling on skin and difficult to remove by washing with water.

2. Plot graph of UV absorption against time



This graph is fluctuated but on the whole there shows an increase of UV absorption against time. The UV spectrometer measure the releasing of acetylsalicylic acid from the ointment in the dialysis bag immersed in the 100 ml 37˚C distilled water.                                  
            The great increase in the UV absorption value at the first 5 minutes is due to the great concentration difference between content in dialysis tube and the distilled water. The content of in the dialysis bag is hypertonic to the distilled water. So, large amount of ointment with acetylsalicylic acid diffuses to the distilled water with high concentration gradient different. The amount of ointment diffuse is proportional to the acetylsalicylic acid. The high value of UV absorption may due to the presence of residual at both end of the dialysis bag, left during the insertion of ointment into the dialysis bag. So when the dialysis bag is immersed in the distilled water, the residual will dissolve in the water.
This makes there are content of acetylsalicylic acid that are not from the diffusion through the dialysis bag. After the residual at both end of dialysis bag has dissolved, the acetylsalicylic acid diffused out only through the pore of dialysis bag, so the reading after 5 minutes shows regular increase. A sudden large increase in the UV absorption does not occur after 5 minutes as the concentration gradient across the dialysis bag decrease, the amount of acetylsalicylic acid in the distilled water increases with time. The gradual increase in the UV absorption indicates the gradual release of acetylsalicylic acid from the dialysis bag. The concentration of content in distilled water gradually increased until equal the concentration of the content in dialysis bag. This will result in the reduced increase in the UV absorption when times pass by.
            Due to time constriction, the results of this experiment are not complete. However, we can predict the pattern of the graph as it will increase gradually until a constant is achieved. If the experiment is continued beyond 60 minutes, it may result in a straight line graph as the concentration of acetylsalicylic acid in the distilled water equals to the concentration of acetylsalicylic acid at the dialysis bag. The content in dialysis bag is isotonic to the distilled water content concentration.
            Some of the precautions steps can be taken during conducting the experiment are to avoid over stirring the distilled water as this might break the dialysis bag and result a large amount release of the ointment from it. Besides, the residual that retained at both end of the dialysis bag should be removed before immersing the dialysis bag in the distilled water to ensure accuracy of the result. The rope should tie both end of the dialysis bag tightly to prevent leakage of the ointment. The cuette should be cleaned for the fingerprint around the surface of it so that the measurement is correct. The distilled water in the beaker should cover the whole dialysis bag to ensure consistent diffusion.
  


4. What are the functions of each material used in this preparation of ointment? How does the different emulsifying wax and liquid paraffin components affect the physical appearance of the ointment formed and the release rate of the drug from the ointment?
                Emulsifying wax is an emulsifying agent that is used to make the oil droplets in ointment becomes soluble and mixable with water in order to allow the formation of the ointment. It also allows the ointment to have self-emulsifying property. Liquid paraffin and soft paraffin are the hydrophobic bases of the ointment. Liquid paraffin softens the ointment formed and reduces the viscosity of the ointment in the presence of emulsifying wax. It increases the spreadibility and decreases the hardness of the ointment. White soft paraffin enhances the penetration of acetylsalicylic acid through skin surface as well as the absorption through the membrane into circulation.
                 From the experiment, different proportions of materials are used to produce 50g of emulsifying ointment. High concentration of emulsifying wax hardened the ointment while a high concentration of liquid paraffin produces a watery, greasy, and soft ointment due to the reduced viscosity of ointment. Therefore, higher concentration of emulsifying wax and lower concentration of liquid paraffin produce harder and less greasy ointment compared to lower concentration of emulsifying wax and higher concentration of liquid paraffin in an ointment formulation.In this formulation, the increased concentration of emulsifying wax reduces the rate of drug released from ointment. This is because higher amount of emulsifying wax will decrease the drug diffusion from ointment by holding the active ingredient (acetylsalicylic acid) tightly and thus retard the drug released. On the other hand, diffusion rate of acetylsalicylic acid from the dialysis tube is increased in a formulation of ointment with optimum concentration of liquid paraffin because acetylsalicylic acid which is hydrophilic is tend to diffuse into the surrounding distilled water. Hence, the release rate of drug is increased. However, the diffusion rate of acetylsalicylic acid will decrease when the concentration of liquid paraffin is beyond the optimum value. Thus, an optimum ratio of the phases is needed to produce an ointment with good physical property and also the drug releasing rate.

CONCLUSION
From the experiment, we can conclude that the rate of drug released from the ointment is reduced with increased concentration of emulsifying wax in the formulation of Ointment.

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