Dentistry Essay Example: The Properties of Chlorhexidine Diacetate Mucoadhesive Buccal Tablet

Chlorhexidine has been used for a long as an antimicrobial in preventing tooth decay. Research done on Streptococcus mutans shows the bactericidal activity of the chlorhexidine. Xylitol, on the other hand, is also known for its antimicrobial activity especially in the case of preventing dental caries. In addition, xylitol is used as a sweetener in chewing gums used in some places. Since both chlorhexidine and xylitol are of great importance for the maintenance of the oral health and hygiene, they can as well be used together. The combined antimicrobial activity of both the xylitol and chlorhexidine serves well in killing many microorganisms in the mouth.

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By combining the xylitol and chlorhexidine, some of the challenges do arises. The xylitol affects some of the properties of the chlorhexidine such as flowability of the drug, friability, diameter, weight, hardness, mucoadhesion, content uniformity, and swelling. If xylitol and chlorhexidine are combined, some the properties tend to change. The effect was assessed in the laboratory to come up with the data on each of the property affected. Discussion section utilizes the data provided to gauge the effect xylitol has on the properties of chlorhexidine and what attributing factors leads to such changes.

The paper has three sections with an introduction, results obtained from the laboratory experiment and finally the discussion that explains the data as well as conclusion section.

Effect Of Xylitol The Properties Of Chlorhexidine Diacetate Mucoadhesive Buccal Tablet Prepared With Non-Ionic Or Anionic Polymers.

Introduction

Xylitol is used as a sweetener in many of the medical drugs in healthcare centres (Walter, n.d). According to the researchers, an approved drug is less associated with the side effects (Riley, et al, 2015). Despite this, xylitol has anti-microbial properties, which helps break down of the bacteria present in the mouth (Auerkari, 1997). The mechanism of action of xylitol in killing the bacteria is quite complex. By it being sugar alcohol, the bacteria tend to take them in and unfortunately, it is not metabolized. The bacteria does not have necessary enzyme to use it as nutrient. It is therefore converted into xylitol 5-phosphate where it inhibit bacterial metabolism. This makes the bacteria to dies off since they cannot survive without metabolism process to liberate energy for their use (Riley, et al, 2015). Xylitol also hinders the bacteria from producing acid that cause erosion of the tooth enamel. Xylitol causes saliva production and an increase in plaque pH thus inhibiting the bacterial in the oral cavity. Xylitol helps in remineralisation of the demineralised tooth. It combines with free calcium from demineralised tooth to form a complex that is used for demineralization inside the tooth enamel (Walter, n.d). It also directly inhibits demineralization. Therefore, helps prevent tooth decay in most cases. This is proven through a research where the people who used it were prevented from having tooth decay (Nayak, et al, 2014). The sweetener is used in the medical aspects of drugs and even in chewing gums (Isokangas, 1987).

Chlorhexidine, on the other hand, is used as anti-microbial drugs against tooth decay (Richards, 2015). A number of pharmaceutical companies manufacture Chlorhexidine globally. This drug has chemical properties that are bactericidal to the microorganism especially streptococcus in the mouth. It hydrolyses the cell membrane of the microorganism by directly destroying it. This makes the microorganism lose their survival ability due to the loss of the cell membrane. They eventually die off and they are washed off and excreted in the faeces. Chlorhexidine also opsonises the microorganism thus preventing excessive multiplication. Opsonisation also makes it easy for the degradation of the microorganism. It causes clumping together of the microorganism. They prevent the bacteria and other microbial organisms in the mouth from causing tooth decay (Paula, Modesto, Santos & Gleiser, 2010). It works just like the fluoride present in the toothpaste. Chlorhexidine has a quicker rate at which it kills microbial than other antimicrobial with both bacteriostatic and bactericidal abilities. As mentioned above, it kills the bacterial by disrupting the cell membrane causing cell lyses. It has the ability to kill 100% gram positive and negative bacteria within 30 seconds (Paula, Modesto, Santos & Gleiser, 2010). Chlorhexidine being positively charged binds to the negatives charged sites of the cell membrane on the cell wall. This destabilizes the cell wall and thus interferes with the bacteria osmotic balance. The bacteria then take up chlorhexidine very rapidly in about 20 seconds only. It then damages the cell membrane also causing further effect on the survival of the bacteria (Richards, 2015). The damaged cell membrane causes leakage of cell components and thus death of the bacteria. Its effect in damaging the bacteria is very fast.

This paper targets to explain how xylitol will be affecting the properties of the chlorhexidine diacetate mucoadhesive buccal tablet. Through the effects of xylitol on the properties of chlorhexidine, it promotes or inhibits the function of the chlorhexidine tablets as well as affects the efficiency (Nuuja, Meurman & Torkko, 1993). The paper has data collected on the experiment performed to help explain the effect of xylitol. The experiment is performed in four formulations and it is used to assess the effect of xylitol on the analysis of the result obtained.

Result and Discussion

Formulation per tablet:

formulation CHD HPC

Hydroxypropyl cellulose

CMC

Carboxymethyl cellulose

xylitol

F1 5mg 30mg 15mg

F2 5mg 15mg 30mg

F3 5mg 30mg 15mg

F4 5mg 15mg 30mg

Prepared 300 tablet

Magnesium stearate: before pressing the tablets (0.5%)

Formulation per tablet

Magnesium stearate: before pressing the tablet (0.5%) - 75mg

Formulation CHD(mg) HPC(mg) CMC(mg) Xylitol

F1 5mgx300=1500 30mgx300=9000 15mgx300=4500

F2 5mgx300=1500 15mgx300=4500 30mgx300=9000

F3 5mgx300=1500 30mgx300=9000 15mgx300=4500

F4 5mgx300=1500 15mgx300=4500 30mgx300=9000

Table 1: showing the four different formulations expressed in mg and the total weight of each formulation is 5mg

Absorbance @254 nm

Chx Concentration(mg/ml) Absorbance 1 Absorbance 2 Absorbance 3 average Std.dev

1 >2.5 >2.5 >2.5 >2.5 0

0.5 >2.5 >2.5 >2.5 >2.5 0

0.25 >2.5 >2.5 >2.5 >2.5 0

0.125 1.364 1.318 1.36 1.34733333 0.025482

0.0625 0.679 0.651 0.566 0.632 0.0588473

0.03125 0.325 0.313 0.28 0.306 0.0233024

0.01563 0.165 0.154 0.14 0.153 0.01253

0.00781 0.068 0.077 0.074 0.073 0.0045826

0.00391 0.048 0.04 0.041 0.043 0.0043589

0.00195 0.032 0.038 0.028 0.03266667 0.0050332

0.00098 0.03 0.036 0.023 0.02966667 0.0065064

Table 2: showing the Chx concentration and reader absorbance at 254 nm

Tab density

Samples number 1st tab density 2nd tab density 3rd tab density The weight of powder (g)after tab density

1 8.4 8.2 8.00 5.18

2 7.8 7.7 7.7 4.99

3 7.8 7.7 7.6 4.89

Table 3: showing tab density for formulation one to three times on 200 g/cm3 and final weight

Samples number 1st tab density 2nd tab density 3rd tab density The weight of powder (g)after tab density

1 7.7 7.6 7.6 5.32

2 7.9 7.4 7.1 5.69

3 8.00 7.9 7.9 5.79

Table 4: showing tab density for formulation two to three times on 200 g/cm3 and final weight

Samples number 1st tab density 2nd tab density 3rd tab density The weight of powder (g)after tab density

1 7.1 7.00 7.00 5.31

2 7.2 7.1 7.1 5.40

3 7.1 7.00 7.00 5.30

Table 5: showing tab density for formulation three on three times on 200 g/cm3 and final weight

Samples number 1st tab density 2nd tab density 3rd tab density The weight of powder (g)after tab density

1 7.3 7.2 7.2 5.65

2 7.4 7.2 7.2 5.69

3 7.2 7.1 7.1 5.57

Table 6: showing tab density for formulation four on three-times on 200 g/cm3 and final weight

Flowability test

formulation 1 2 3 4

Initial weight(g) 14.46 14.44 11.69 14.71

Powder flow(g/s) 7.4 28.9 11.7 24.5

Powder flow(g/s) 6.4 36.1 13.4 21

Powder flow(g/s) 7.4 28.1 11.7 24.5

Average 8.915 26.885 12.1225 21.1775

SD 3.72660256 9.043058 0.85168 4.616567

Table 7: showing Flowability test for four formulations on 25mm-orifice

formulation 1 2 3 4

Initial weight(g) 14.8 14.55 11.66 14.66

Powder flow(g/s) 10.1 11.2 3.9 9.2

Powder flow(g/s) 8.3 10.4 3.8 9.3

Powder flow(g/s) 9.4 11.2 2.8 10.5

Average 10.65 11.8375 5.54 10.915

SD 2.86414618 1.847239 4.110118 2.565586

Table 7: showing Flowability test for four formulations on 15mm-orifice

formulation 1 2 3 4

Initial weight(g) 14.05 14.26 11.23 14.56

Powder flow(g/s) 10.7 4.2 Impassable 3.7

Powder flow(g/s) Impassable 3.8 Impassable 4.4

Powder flow(g/s) Impassable 4.2 Impassable 4.2

Average 12.375 6.615 11.23 6.715

SD 2.36880772 5.100154 - 5.238279

Table 8: showing Flowability test for four formulations on 10mm-orifice

Flowability test aims at determining the effectiveness of the component. This measures how well the drug component can be able to pass in between orifice in the region of its action. The drug with good flowability is able to perform its function effectively (Measurement of powder flowability, 1993). In the mouth, the drug should be able to pass in between the teeth to provide maximum protection to the tooth structures.

In 25mm orifice, the ability of the drug to flow is present. The flow rate, however, is more in formulation 2 where the xylitol is more and in HPC. This is because the xylitol affects the package configuration of the particles thus making the flow rate on average to be quite higher in HPC (Raunhart, 1982). Same inHPC, as the flowability in 25mm orifice, is much greater in the formulation where the xylitol is more that is 30mg as compared to where it is 15mg.

In 15mm orifice, the flowability is quite lower than it in 25mm orifice. This is due to reduced size that hinders faster movement of the particle present in the formulation. However, the effect of xylitol is still evident as the more the formulation had xylitol the more the flowability of it. Therefore, the formulation 2 and 4 has a higher flowability.

In 10mm orifice, it clearly shows how xylitol amount helps in flowability. Where the xylitol was 15mg in formulation 1 and 3, the particles were impassable. This is because the particle kinetics cannot allow proper flow (Birch, 1979). However, with 30mg of xylitol, the drug particles were able to pass. This is due to the effective change in particle configuration with 30mg xylitol as compared to 15mg xylitol (Raunhart, 1982).

Since xylitol positively helps the flowability of the drug, the chlorhexidine with xylitol will be able to have a much higher flowability. This will make it possible for chlorhexidine to pass in between small orifices in the mouth and lyses as many microorganisms as possible as compared to a scenario where the chlorhexidine works alone. The data shows that when it is alone or even with little xylitol, the flowability is small.

Friability

Formulation Initial weight(g) Final weight(g) % friability Pass or fail

1 1.1573 1.1597 -0.20737924

2 1.18892 1.1866 0.195135081

3 1.2651 1.1814 6.61607778

4 1.2465 1.2436 0.232651424

Average 1.70912126

S.D 3.277362446

Table 9: showing friability test for four formulations in 4min

Friability refers to the process where the particle crumbles or do break upon compression or external force applied to it (Lindeberg & Hilmquist, 1987). It is now a standard measure of the tablets before they are issued out (Birch, 1979). A table should be designed in such a way that they are able to withstand compression and thus should not crumble. The a...