Release Study of Metronidazole from Some Gel Formulations

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Junior (College 3rd year) ・Chemistry ・MLA ・6 Sources

This document provides an extensive presentation of laboratory test results, Kinetic graphical representations and subsequent analysis of an experiment to learn about the relationship between absorption and concentration using ultraviolet–visible spectroscopy (UV-Vis). Since, most analytical strategies require calibration (a process that relates the measured analytical signal to the attention of analytic, the substance to be analyzed). The preparation and use of a calibration curve are employed in the calculation of the concentration via equation (X = (y-0.0003)/0.0305) that represents slop between absorption (y-axis) and concentration (x-axis). A statistical evaluation is utilized in the course of the results and discussion zone majors in the derivation of Zero Order kinetic graphs, the Second Order kinetic graphs. Ideally, the % reaction is plotted against time, the natural Logarithm (ln) of % reaction against time and inverse of % reaction against time for the Kinetic Orders graphs respectively.

Keywords:laboratory experiment results, ultraviolet–visible spectroscopy, calibration curve and Kinetic graph

Contents

Abstract 1
Introduction 2
Experimental 4
Methods and calculations 4
Results and discussion 4
Carbopol based 934 (1)4
Carbopol based 934 (2)6
MT212
Carbopol based 940 (complex 0.5)16
Conclusion 18
References 19

Tables

Table 1 5
Table 2 7
Table 3 9
Table 4 10
Table 5 12
Table 6 14
Table 7 16

Table of Figures

Figure 1 Zero Order Graph Kinetic 7
Figure 2 first order Graph Kinetic 7
Figure 3 Second Order Kinetic 8
Figure 4 Zero Order Graph Kinetic 8
Figure 5 first order Graph Kinetic 9
Figure 6 Second Order Kinetic 9
Figure 7 Zero Order Graph Kinetic 10
Figure 8 first order Graph Kinetic 10
Figure 9 Second Order Kinetic 11
Figure 10 Zero Order Graph Kinetic 12
Figure 11 first order Graph Kinetic 12
Figure 12 Second Order Kinetic 13
Figure 13 Zero Order Graph Kinetic 14
Figure 14 first order Graph Kinetic 14
Figure 15 Second Order Kinetic 15
Figure 16 Zero Order Graph Kinetic 16
Figure 17 first order Graph Kinetic 16
Figure 18 Second Order Kinetic 17
Figure 19 Zero Order Graph Kinetic 18
Figure 20 first order Graph Kinetic 18
Figure 21 18

Introduction

Metronidazole is a synthetic nitroimidazole, 1-(β-hydroxyethyl)-2-methyl-5-nitroimidazole. That acts as an antiprotozoal and an antibacterial agent when taking orally. Moreover, it is the drug of choice for anaerobic infections treatment, as well as mixed aerobic and anaerobic infection, yet metronidazole must be used in combination with other antibacterial drugs that are appropriate for the treatment and management of the aerobic infection. However, the topical antimicrobial efficacy of metronidazole alone is somewhat poor (Löfmark et.al 16). Löfmark et.al (17) appreciates the vulnerability of only utilizing metronidazole.
Topical metronidazole has been used as the treatment of choice of rosacea, a common chronic inflammatory disease of the skin that is associated with several etiology and triggering factors (Bleicher 610). Though, studies agree that this condition of the facial skin is an inflammatory and not a microbial in nature, which affects the blood vessels and pilosebaceous units (Cribier 188).According to Bleicher (613), topical metronidazole, 1 and 0.75%, is belief to be effective in managing rosacea as it demonstrates in vitro studies that metronidazole inhibits neutrophil release of reactive oxygen species which cause tissue injury at sites of inflammation (Miyachi et.al 233). Therefore, Miyachi et.al 234 acknowledges that antioxidant metronidazole activity is thought to be the cornerstone of its anti-inflammatory effect in rosacea.
Bacterial skin infections are very common and frequently treated infections in the office and the hospital as they are the 28th most common diagnosis in hospitalised patients (Riain 17) and (Cmunckhof 7). Riain 18 appreciates those common bacterial infections of the skin include impetigo, folliculitis, simple abscesses, erysipelas and another non-necrotizing cellulitis. Treatment guidelines have been wildly accepted. However, the full range of pharmacotherapeutic options is for oral or parenteral drug delivery. Which might achieve high desirable bioavailability, yet undesirable adverse effects. Cmunckhof 13 nonetheless, insists that bacterial skins infections can manifest as a systemic bacterial infection. Any topical antibacterial drug cannot be considered as a drug of choice to treat the underlying cause (JLopez 271). JLopez (277) advocates for the use of the topical antibacterial drug is appreciatively selective environments.
Lots of different types of polymers have been inspected as a potential transporter to deliver a drug in an efficient way (Khutoryanskiy 751). Khutoryanskiy (755) provides that originally polymers were used as solubilizers, stabilisers and mechanical supports for sustained release of drugs. But nowadays, polymers have been synthesised to fit specific needs or of drug delivery systems. A polymer gel such as polyacrylic acid (PAA) majorly contains an elastic crosslinked network and a fluid filling the interstitial spaces of the system. The nature of polyacrylic acid gels (e.g., carpool, polymethyl methacrylate) is appropriate to obtain for medical applications such as gels skin care products (Osada and Gong (833. The objective of this study was to develop a topical gel containing 0.75% metronidazole as the model drug. To achieve the objective, an independent formulation such as total percentage polymer content and method are utilised.

Experimental Methods and Сalculations

The methods of this experiment were relatively straightforward. We first prepare carbopol-based gel using Carbopol 940 and Carbopol 934. They are polymers with a cross-linked polyacrylate. After that, we dissolved metronidazole tablets 500mg in sterile water after we examine three tablets weight variations. Then the process required a couple of days for all three preparations to settle.
Results and discussion
In a Zero-order kinetics reaction, in most cases, a straight line is obtained when you plot the concentration of the reactant [% Release] vs. Time (t). For a first order kinetics reaction, on the other hand, plotting ln [% Release] vs. Time to will give a straight line with a negative slope. The second order is derived from plotting the 1/ [% Release] vs. Time (t). The zero-order equation is dc/dt = –KoCo= –Ko and c/dt = –KC1= –KC so and so. The first order is a logarithmic derivative of the zero-order. The second order is inverse to the zero order.
The tabulated data below represents three sets of data;
The carbopol based 940 ( complex 0.5, 1 and 2), carbopol based 934 ( complex 0.5, 1 and 2) and metronidazole.
Carbopol based 934 (1)

Time

C

CX5

CX150

Total release

% Release

% rem

0.15

5.9

29.5

885

885

8.85

91.15

0.30

8.0

40

1200

1229.5

12.29

87.71

1.0

12.1

60.5

1815

1884.5

18.81

81.2

1.5

14.5

72.5

2175

2305

23.05

77

2.5

16.5

82.5

2475

2677.5

26

74

3.0

18.0

90

2700

2985

29

71

[% Release] vs. Time (t)

Carbopol based 934 (2)

Time

C

X

X

Total release

% Release

% rem

0.15

3.20

16

480

480

4.8

95.2

0.30

3.28

19.1

573

608

6.08

93.0

1.0

5.86

29.3

879

943.3

9.433

90.56

1.5

7.27

36.35

1080.5

1191.15

11.9115

88.68

2.0

8.35

41.75

1752.5

1394.9

13.949

86.05

2.5

9.33

46.65

1399.5

1588.55

15.8855

84.14

[% Release] vs. Time (t)

Time

C

5N

150

Total release

% Release

% rem

0.15

6.678

33.39

1001.7

1001.7

10.017

89.95

0.30

10.055

50.275

1508.22

1541.01

15.4101

84.58

1.0

14.809

74.045

2221.35

2305.015

23.05015

76.95

1.5

18.219

91.095

2732.85

2890.56

28.9056

71.1

2.0

20.973

104.865

3145.95

394.755

39.4755

60.3

2.5

21.981

109.905

3292.15

3650.82

36.5082

63.49

[% Release] vs. Time (t)

Conclusion

The type of carboxivinil polymers affected the rheological behaviour of the studied mucoadhesive gel systems containing 15% metronidazole in the form of fine suspensions of particles (Masoudi et.al 2821). This paper restates the justification for the study regarding the expected results. It is imperative at this point to specify the implications of the potential results and how the outcome of this research may inform future research or policy makers. Appreciably, the combination of metronidazole gel with SRP resulted in improved periodontal status, proving its efficiency in the treatment of periodontal disease.

Works cited

Bleicher P. Topical metronidazole therapy for rosacea. Archives of Dermatology. 1987;123(5):609-614.

Cmunckhof R. Antibiotics currently used in the treatment of infections caused by Staphylococcus aureus. Internal Medicine Journal. 2005;35(s2):S3-S16.

Cribier B. Pathophysiology of rosacea: redness, telangiectasia, and rosacea. Annales de Dermatologie et de Vénéréologie. 2011;138: S184-S191.

JLopez F. Skin Soft Tissue and Systemic Bacterial Infections Following Aquatic Injuries and Exposures. The American Journal of the Medical Sciences. 2015;349(3):269-275.

Khutoryanskiy V. Advances in Mucoadhesion and Mucoadhesive Polymers. Macromolecular Bioscience. 2010;11(6):748-764.

Löfmark S, Edlund C, and Nord C. Metronidazole Is Still the Drug of Choice for Treatment of Anaerobic Infections. Clinical Infectious Diseases. 2010;50(s1):S16-S23.

Masoudi M, Rafieian Kopaei M, Miraj S. Comparison between the efficacy of metronidazole vaginal gel and Berberis vulgaris (Berberis vulgaris) combined with metronidazole gel alone in the treatment of bacterial vaginosis. Electronic physician. 2016;8(8):2818-2827.

Miyachi Y, Imamura S, Niwa Y. The anti-oxidant action of metronidazole: a possible mechanism of action in rosacea. British Journal of Dermatology. 1986;114(2):231-234.

Osada YGong J. Soft and Wet Materials: Polymer Gels. Advanced Materials. 1998;10(11):827-837.

Riain U. Recommended Management of common bacterial skin infections. Prescriber. 2013;24(23-24):15-25.

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