ASSESSMENT OF EFFECT OF TABLET COATING ON THE TABLET DISINTEGRATION

5 minutes to 10 minutes. Modified-release tablets are meant to release Active Pharmaceutical Ingredient (API) in a gradual manner to achieve prolonged and slow therapeutic effect, or avoid disintegration in stomach acidic medium but promote disintegration in slightly basic intestinal fluids, or promote delayed time onset. The objective of this experiment was to evaluate the effects of coating on disintegration time of paracetamol, diclofenac, ibuprofen and fexofenadine. Paracetamol and ibuprofen were uncoated, while diclofenac and fexofenadine were coated. Disintegration is the mechanical breakup of compressed tablets into small granules when in contact with physiological media, resulting from breakdown of bonds responsible for intact nature of tablets after tablet compaction. 99 minutes to disintegrate. Diclofenac took the longest time to disintegrate in both water and acidic media because it was enteric coated with polymers that restrict fast disintegration.

In acidic media, diclofenac took more than 2 hours to disintegrate. Paracetamol and ibuprofen were uncoated and took least time to disintegrate. Fexofenadine and diclofenac took more time to disintegrate in acidic medium compared to water. 3 Hypothesis 8 1. 3 Coating Information 9 2. 0 Experiment 9 2. 1 Requirements 10 2. 2 Procedure 10 2. They are the most preferred dosage forms because they are cheap to manufacture, easy to administer, and have long shelf-life. These dosage forms are preferred for patients who have no problem swallowing. Choosing suitable physical and chemical properties, tablets are formulated to be immediate release, or modified release with the goal of promoting immediate drug release, reducing toxicity, promote therapeutic efficacy, and promote patient compliance (Ankit, Ajay, Maheshkumar, & Neetu, 2012). Immediate-release tablets are usually uncoated and they are meant to take least time to offer therapeutic effects after quick disintegration, dissolution, and absorbance.

Tablets can either be coated or uncoated. 1 Tablet information Paracetamol and ibuprofen (Ibux) were uncoated, while diclofenac (voltaren) and fexofenadine (telfast) were coated. 1 Paracetamol It is an antipyretic and analgesic that reduces mild to moderate pain by blocking cyclooxygenase III enzyme in the brain. Prostaglandins responsible for fever and pain are therefore not synthesized. It is mostly used to relief minor aches such as headaches, and other types of pain. It can be formulated in combination with muscle relaxants, and opioid analgesics. It is found in 120mg tablet. It blocks histamine binding to H1 receptors, hence treats allergies such allergic rhinitis, and urticaria. Fexofenadine tablet dosage form contains excipients such as iron oxide, powdered cellulose, maize starch, mannitol, magnesium stearate, colloidal anhydrous silica, and croscarmellose Sodium, and titanium oxide (Kumar, Alam, Meena, Jain, & Bansal, 2008).

4 Diclofenac (voltaren) Diclofenac is an NSAID used to relieve inflammation, joint stiffness, and pain in arthritis. Voltaren enteric coated or delayed release tablets are coated to provide protection from acidic stomach contents or give a delayed release of API within the intestines. Coating masks tablet taste and odor, promotes chemical and physical protection, protects stomach disintegration, controls API release, and increases mechanical drug dosage forms’ strength. Film coating is not as time consuming as sugar coating and requires less skills and few processes. Film coating machine has replaced human labor, and involves spaying a suitable polymer, plasticizer, and pigments onto tablets on a rotating bed. A thin and uniform film is formed on each tablet surface. The polymer choice depends on drug release site and anticipated release rate.

1 Procedure for disintegration in water 1. 600mL of tap water was placed in each 1000mL beaker. There pH was tested and all measured between pH 6. The disintegration tester was assembled and connected to power. In the disintegration tester, a tap water was added to form a water tub. Fresh clean tap water, 600mL, was placed in each 1000mL beakers and placed in the tester’s water tub. They were allowed to gain temperature to 370C. Repeat steps 7 – 10 with Diclofenac (Voltaren) tablets. Steps 11 and 12 were repeated after diclofenac disintegration. Repeat steps 7 – 10 with Fexofenadine (Telfast). The tester was set to run for 30 minutes 5. In each of the six tubes, a paracetamol tablet was placed. Each tube was placed in each beaker and the tester was started.

A stop watch was started immediately the tester was started. Time each paracetamol tablet took to disintegrate was recorded. 3 sec Time to complete Disintegration - 150 Sec - 140 Sec - 152 Sec 147 Sec Diclofenac (Voltaren) Time Before Start of disintegration 10 Minutes - 10 Minutes 10 Sec - 9 Minutes 52 Sec - 10 Minutes 40 Sec Time to complete Disintegration 60 Min - 60 Min 20 Sec - 59 Min 56 Sec - 60 Min 4 Sec Fexofenadine (Telfast) Time Before Start of disintegration 20 Sec - 23 Sec - 22 Sec - 22 Sec Time to complete Disintegration 60 Sec - 1 Min 11 Sec - 57 Sec - 63 Sec Ibuprofen (Ibux) Time Before Start of disintegration - 30 Sec - 33 Sec - 29 Sec 31 Sec Time to complete Disintegration - 8 Min - 8 Min 10 Sec - 7 Min 58 Sec 8 Min 4 Sec 2. 2 Disintegration time for the tablets in Acidic Media Tablet Disintegration Time Attempts 1st Attempt 2nd Attempt 3rd Attempt Average Time Coated Uncoated Coated Uncoated Coated Uncoated Paracetamol Time Before Start of disintegration - 23 Sec - 30 Sec - 28 Sec 27 Sec Time to complete Disintegration - 1 Minute 45 Sec - 1 Minute 38 Sec - 1 Minute 42 Sec 1 Minute 41 Sec Diclofenac (Voltaren) Enteric Coated Time Before Start of disintegration Never disintegrated within 2 hours - Never disintegrated within 2 hours - Never disintegrated within 2 hours - N/A Time to complete Disintegration Never disintegrated within 2 hours - Never disintegrated within 2 hours - Never disintegrated within 2 hours - N/A Fexofenadine (Telfast) Time Before Start of disintegration 42 Sec - 36 Sec - 30 Sec - 36 Sec Time to complete Disintegration 10 Min - 12 Min 10 Sec - 9 Min 57 Sec - 10 Min 40 Sec Ibuprofen (Ibux) Time Before Start of disintegration - 29 Sec - 33 Sec - 27 Sec 30 Sec Time to complete Disintegration - 70 Sec n/a 83 Sec n/a 68 Sec 74 Sec 2.

4 Calculations Disintegration time when each brand tablets disintegrated in both water and acidic media were calculated using the formula below, and shown in the average disintegration column in the results. Average disintegration time in water can be calculated as follows in minutes: For Paracetamol For Diclofenac For Fexofenadine For Ibuprofen Average disintegration time in acidic medium can be calculated as follows in minutes: For Paracetamol For Diclofenac For Fexofenadine For Ibuprofen 2. 5 Discussion Disintegration always refers to mechanical breakup of compressed tablets into small granules when in contact with physiological media. Swelling occurs when particles absorb the liquid, mostly water, and increases in diameter, building up pressure that pushes other particles apart leading to stress exertion on the tablet system. The tablet finally breaks (Desai, Liew, & Heng, 2016).

The media in which the tablets are immersed also exert force in pores of the tablets, promoting disintegration. Tablets are also formulated with disintegrants that promote disintegration, but the force developed due to fluid absorption is just enough to disintegrate the compact (Desai et al. Strain recovery is another mechanism that tablets use to undergo disintegration. Both results were recorded. Disintegration tests are used to evaluate whether the tablets meet the pharmacopoeial requirements of tablet disintegration. The wicking process is a key step in disintegration process. Entry rate of any liquid into a matrix that is porous is determined by capillary forces, which oppose movement of the liquid. Therefore, liquid flow and retention in unsaturated media that is porous are therefore determined by balance between adhesion between molecules of the liquid and particle surfaces, and cohesion forces between liquid molecules (Szymkiewicz, 2013).

Acidic media are more viscous than pure water, leading to slower penetration rate into the tablets, hence slower disintegration. Moreover, water has inferior surface tension to acids, resulting in rapid disintegration (Desai et al. In acidic media, the tablets were required to disintegrate within 2 hours. Paracetamol took 1. 55 minutes, diclofenac took more than 2 hours, fexofenadine took 11 minutes, and ibuprofen took 1. Disintegration Time (Minutes) Tablet Number Minimum Maximum Mean Paracetamol 6 2. 24 Diclofenac 6 58 62. 05 Fexofenadine 6 0. 23 Ibuprofen 6 7. 99 Table 2: Disintegration in water Figure 1: Disintegration in Water Disintegration Time (Minutes) Tablet Number Minimum Maximum Mean Paracetamol 6 1 2. Gastric pH was simulated by 0. 1M hydrochloric acid, which offered a pH of 1 – 2. Tablet disintegration is a required process for every tablet before dissolution and absorption. It is the first step that determines the bioavailability of a tablet’s API.

Therefore, failure of a drug to disintegrate within the required time shows that the drugs has failed to meet the pharmacopoeial requirements for tablet disintegration, and it is unfit for human consumption. European Journal of Pharmaceutics and Biopharmaceutics. https://doi. org/10. 1016/j. ejpb. jconrel. 014 Ankit, G. , Ajay, B. , Maheshkumar, K. , & Neetu, K. Bhasin, R. K. , Bhasin, N. , & Ghosh, P. K. Journal of Pharmaceutical Sciences. https://doi. org/10. 1016/j. xphs. S. , Meena, C. L. , Jain, R. , & Bansal, A. , Khan, a, … Gupta, N. Orally disintegrating tablets: formulation, preparation techniques and evaluation. Journal of Applied Pharmaceutical Science. Quodbach, J. , & Kleinebudde, P. , & Conway, B. R. The influence of excipients on the diffusion of ibuprofen and paracetamol in gastric mucus. International Journal of Pharmaceutics. https://doi.

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