INTRODUCTION:

Colon targeted drug delivery, is possible to prevent the side effects of drugs on healthy tissues and enhancement of drug uptake by targeted cells.¹ However, within the colon, absorption from the descending colon is less in comparison to the ascending colon.^2-7 RA causes swelling, pain, inflammation and joint destruction.^8,9 Fenoprofen Calcium is NSAID drug used in the treatment of pain, inflammatory diseases.^10,11 Fenoprofen is used as model drug due to its short half life (2-3 h), gets rapidly absorbed and peak plasma level achieved within 2h, so repeated dosing of drug required, which increases side effects.^12,13

To overcome these side effects, there was need to prepare fenoprofen once a bed time sustained release colon specific tablet, where delay in drug absorption is desirable from therapeutic point of view for treatment of diseases. So it will increases effectiveness, reduce dose, dosing frequency, decrease side effect, release the drug after lag time and improve patients compliance.¹⁴

Enteric-coated dosage forms remain intact in the stomach and thus formulation targeted at colon.¹⁵ Insta coat super II was used as pH- dependent polymer.^16-18 A statistical 3² full factorial design was used to simultaneously study the effect of the two formulation variables of the colonic drug delivery system on two response variable. The two formulation variables studies were the amount of HPC and amount of EC.^19-21 The studies were amount of drug release in 5 h and 12 h. The expected in vitro release pattern selected for the colon targeting was not more than 10% of drug release up to the end of small intestine (5h) and more than 85% of drug release up to 12h.^22-25 In the present study, effect of formulation variables on the two critical release properties, drug release in physiological environment of stomach and, small intestine and drug release in target area, colon was investigated.

MATERIALS AND METHODS:

Fenoprofen calcium was obtained as gift sample from SUVEN Life Sciences, Hyderabad, Instacoat EN super was obtained as gift sample from Idea cures Pvt. Ltd., Mumbai, Hydroxy propyl cellulose was purchased from Ipca laboratories, Mumbai, Ethyl cellulose N 22 and Sodium starch glycolate were purchased from Molychem Mumbai. Poly vinyl pyrollidone and Cross Carmellose sodium were purchased from Loba Chemie, Mumbai. All other reagents and chemicals used were analytical grade.

Preparation of core tablets:

The resulting powder mixtures were compressed into tablets using a rotary tablet machine equipped with 8 mm concave faced punch. Sufficient pressure was applied to keep the hardness 5kg/cm². Cross carmellose sodium, as super disintegrant was used in another core tablet batches. The composition of inner core tablet reported in table 1.

Table 1: Composition of inner core tablet

Sr. No.	Contents	Amount in (mg)
Sr. No.	Contents	C₁	C₂	C₃	C₄	C₅	C₆
1	Fenoprofen Calcium	200	200	200	200	200	200
2	Croscarmellose Sodium	20	30	40	-	-	-
3	Sodium Starch Glycolate	-	-	-	20	30	40
4	PVP K 30	40	30	20	40	30	20
5	Aerosil	30	30	30	30	30	30
6	Talc	20	20	20	20	20	20
7	Magnesium stearate	20	20	20	20	20	20
	Total	330	330	330	330	330	330

Full Factorial design:

A 3² randomized full factorial design was used in this study, two factors were evaluated, each at three levels and experimental trials were performed at all 9 possible combinations of batches.²⁶ The concentration of Hydroxy propyl cellulose (X1), the concentration of Ethyl cellulose N 22 (X2) were selected as independent variables. The percentage drug release at 5 hours and 12 hours were selected as dependent variables.

Coating of press coated tablets:

The enteric coated solution was prepared by dissolving 100 gm of Instacoat EN Super II into 400 ml of distilled water. Coating of press coated tablets was performed using a coating machine. Tablets were charged in coating pan for 30 min. Spray air pressure is 3 kg/cm², temperature 35 -50ºC, rotating speed of pan 20 rpm. The amount of coating was up to 18 mg (8% w/w) per tablet.²⁷

In vitro disintegration time:

In vitro disintegration time of six tablets from each formulation was determine by using disintegration apparatus (VEEGO). In vitro disintegration test was carried out at 37 ± 0.5 ºC in 900 ml of distilled water.

In vitro dissolution study:

In-vitro drug release study was conducted using USP type II apparatus. The dissolution media (900 ml) comprised of buffer pH 1.2 for first 2 hrs then phosphate buffer (pH 6.8) for 10 hrs kept at 37±0.5⁰C and 100 rpm. The contents of fenoprofen Calcium were determined by measuring absorbance on an UV- Visible Spectrophotometer. An aliquot of 5 ml sample was withdrawn and replaced with same 5 ml of fresh dissolution medium at various time intervals. Initially drug release was conducted in 900ml of 0.1N HCL for 2 hr, then absorbance were recorded at 271nm and after 2 hr dissolution was continued in phosphate buffer pH6.8 till end of the test then absorbance were recorded at 272 nm.

RESULTS AND DISCUSSION:

Fourier transform infrared spectroscopy:

The spectrum was obtained using Jasco 4100, Japan, Infra red spectrophotometer. The drug exhibits peaks due to the strong -OH stretching of hydrate at 3648, 3602 and 3278 cm^-1. The very strong bond at 1565 and 1423 cm^-1 retained due to CO₂ asymmetric and symmetric stretching. The IR spectra of drug fenoprofen calcium shown in the figure 1.

Figure 1: FTIR spectrum of fenoprofen calcium

The formulated product is showed identical spectrum with respect to the spectrum of the pure drug and polymers, indicating there was no chemical interaction between the drug molecule and polymers. The overlay of IR spectrum of drug, physical mixture, and polymers shown in figure 2.

Figure 2: Overlay of IR spectrum of Drug (A), physical mixture (B), polymer HPC (C) and EC N-22 (D)

Evaluation of powder blends:

The bulk density of blends was found to be in the range of 0.3192 to 0.3812 g/cm³ and tapped density 0.3820 to 0.4250 g/cm³. This indicates good packing capacity of blends. Hausner’s ratio of all formulations was found to be 1.10 to 1.17 indicates the good flow properties of blends. Values of Carr’s index below 15% show good flow characteristics. Carr’s index of all formulations was in the range 9.11 to 15.05. The angle of repose of all the formulations was within range 21.47 º to 28.67 º. Results of bulk density, tapped density, hausner’s ratio, carr’s index and angle of repose shown in table 2.

Table 2: Evaluation of powder blends

Batch Codes	Bulk density (g/cm³)*	Tapped density(g/cm³)*	Angle of repose (θ)*	Carr’s index (%)*	Hausner’s ratio*
C1	0.3413 ± 0.3	0.3820 ± 0.02	25.39 ± 0.6	10.65± 0.08	1.11 ± 0.4
C2	0.3812± 0.08	0.4250 ± 0.08	26.19 ± 0.17	10.30 ± 0.02	1.11 ± 0.12
C3	0.3493 ± 0.01	0.4112 ± 0.7	21.47 ± 0.13	15.05 ± 0.5	1.17 ± 0.5
C4	0.3192 ± 0.06	0.3693 ± 0.11	23.78 ± 0.78	13.56 ± 0.05	1.15 ± 0.04
C5	0.3673 ± 0.5	0.4130 ± 0.3	28.67 ± 0.44	11.06± 0.12	1.12 ± 0.06
C6	0.3491 ± 0.04	0.3841 ± 0.06	22.49 ± 0.57	9.11 ± 0.05	1.10 ± 0.1

* Indicates average readings ± SD (n=3)

Evaluation of inner core tablet:

Thickness and diameter of all the formulation (C1–C6) varying from 3.85 to 3.97 mm and 10.18 to 10.25 mm respectively. Hardness of tablets was found to be in the range of 4.3–5.8 kg/cm². The average weight of inner core tablets was found to be 330.09 mg. Disintegration time of inner core tablet found to be in the range of 7.15 to 13.34 min. Tablets formulation showed uniformity of drug content as per IP specification i.e. 97.60 to 98.75 % indicating uniform distribution of drug. Results of evaluation of inner core tablet shown in table 3.

In vitro dissolution test:

Formulation containing crosscarmellose sodium shows maximum release and minimum disintegration time than the formulation containing sodium starch glycolate. The % cumulative release of inner core tablet shown in figure 3.

Figure 3: The % cumulative release of inner core table

Factorial design:

From % cumulative drug release data of press coated tablet, it was observed that as the concentration of polymers (HPC and EC N-22) increases the drug release decreases. The initial batches F1 to F6 shows more than 95 % drug release in 10 hrs and higher release in first 5 hrs i.e. all these batches shows drug release in intestine. The value of correlation coefficient (R²) of polynomial regression equation was greater than 0.99 which is equal to 1. Thus indicating best fit for all dependent variables.

Evaluation of Press coated tablet:

Thickness of all the formulations (F1–F9) varying from 5.53 to 6.77 mm. Diameter of all formulation (F1–F9) varying from 12.85 to 12.97 mm. Uniform thickness and diameter indicated uniform die fill, good flow, and uniform pressure. Hardness of tablets was found to be in the range of 8.6–9.2 kg/cm². The average weight of press coated tablets was found to be 646.66 mg. Result of thickness, diameter and hardness shown in table 4.

Table 4: Evaluation of press coated tablet

Batch Codes	Thickness (mm)*	Diameter (mm)*	Hardness (Kg/cm²)*
F1	5.53 ± 0.1	12.85 ± 0.04	8.6 ± 0.1
F2	5.78 ± 0.07	12.83 ± 0.07	8.1 ± 0.1
F3	5.82 ± 0.03	12.72 ± 0.2	8.1 ± 0.05
F4	5.56 ± 0.05	12.88 ± 0.4	9.3 ± 0.01
F5	5.66 ± 0.3	12.85 ± 0.1	9.2 ± 0.01
F6	5.97 ± 0.2	12.78 ± 0.1	8.4 ± 0.3
F7	6.19 ± 0.05	12.91 ± 0.03	8.5 ± 0.4
F8	6.43 ± 0.01	12.82 ± 0.02	9.1 ± 0.01
F9	6.77 ± 0.01	12.97 ± 0.2	9.2 ± 0.01

* Indicates average readings ± SD (n=3)

In vitro dissolution study:

The in vitro dissolution study depends upon the concentration of polymer. The concentration of polymer increases there was decrease in drug release. The % cumulative drug release of press coated tablet shown in figure 4.

Figure 4: % Cumulative drug release of press coated tablet (F1–F9)

Evaluation of enteric coated tablet:

Thickness of all the formulation (F1–F9) varying from 6.12 to 7.53 mm. Diameter of all formulation (F1–F9) varying from 12.86 to 12.94 mm. Hardness of tablets was found to be in the range of 8.5-9.6 kg/cm². The average weight of enteric coated tablets was found to be 656.28 mg. Result of thickness, diameter, hardness and % weight gain shown in table 5.

Table 5: Evaluation of enteric coated tablet

Batch Codes	Thickness (mm)*	Diameter (mm)*	Hardness (Kg/cm²)*	% Weight gain*
F1	6.12±0.04	12.86±0.02	8.9±0.1	7.16±0.11
F2	6.34±0.09	12.85±0.04	8.5±0.7	7.12±0.18
F3	6.45±0.1	12.85±0.3	8.6±0.11	8.21±0.23
F4	6.48±0.01	12.88±0.08	9.4±0.17	8.17±0.1
F5	6.61±0.1	12.87±0.2	9.1±0.01	7.22±0.04
F6	6.78±0.5	12.88±0.1	8.1±0.4	7.11±0.07
F7	7.31±0.03	12.91±0.04	8.3±0.04	8.21±0.7
F8	7.21±0.04	12.93±0.04	9.5±0.7	7.19±0.13
F9	7.53±0.07	12.94±0.01	9.4±0.9	8.12±0.15

* Indicates average readings ± SD (n=3)

In vitro dissolution study:

The in vitro drug release study shows that press coated tablets F8 and F9 shows % drug release at 5 h 20.75 and 14.52 respectively. The expected in vitro release pattern selected for the colon targeting was not more than 10% of drug release up to the end of small intestine (5 h), (Patel J.M et al,.2010). The % cumulative drug release of enteric coated tablet formulation shown in figure 5 and the coded level as per 3²factorial design with observed responses reported in table 6.

Figure 5: % cumulative drug release of enteric coated batch (FT1–FT9)

Table 6: Coded level as per 3²factorial design with observed responses

Batch codes	X1	X2	(%) Drug release at 5 hrs*	(%) Drug release at 12 hrs*
F1	-1	-1	29.59±0.04	95.46±0.011
F2	-1	0	28.42±0.05	93.87±0.34
F3	-1	+1	27.27±0.06	90.92±0.09
F4	0	-1	25.03±0.12	90.72±0.056
F5	0	0	24.79±0.05	87.32±0.12
F6	0	+1	21.31±0.06	83.73±0.67
F7	+1	-1	19.12±0.01	81.37±0.11
F8	+1	0	10.82±0.09	79.69±0.34
F9	+1	+1	3.98±0.067	76.08±0.045

*Indicates average readings ± SD (n=3)

Response surface analysis:

As tablet comes in contact of dissolution medium HPC starts hydrating but as EC N-22 is hydrophobic in nature it retards the hydration of HPC. As HPC forms a compact with EC N-22 dissolution medium would not penetrate faster. Thus due both concomitance effect % drug release at 5 h and 12 h was decreases. Response surface plot showing effect of factorial variables on drug release at 5 h and 12 h shown in figure 6 and 7.

Y=23.71-8.0848X1-3.5300X2-2.8514X1X2-3.3681X1X1 …(5)

From the response surface plot it was observed that as the concentration of Hydroxy propyl cellulose increases the % drug release shows negative effect also increase in concentration of ethyl cellulose drug release goes on decreasing. By combining both polymers shows inverse relation with drug release i.e. decreases in % drug release at 5 h. At optimum concentrations of hydroxy propyl cellulose (200 mg) and ethyl cellulose N-22 (200 mg ) the % drug release at 5 h was found to be 3.98.

Y= 9.4144-7.1917X1-3.4500X2 …(6)

From the response surface plot it was observed that as the concentration of Hydroxy propyl cellulose increases the % drug release shows negative effect also increase in concentration of ethyl cellulose drug release goes on decreasing. By combining both polymers shows inverse relation with drug release i.e. decreases in % drug release at 12 hrs. At optimum concentrations of hydroxy propyl cellulose (200 mg) and ethyl cellulose N-22 (200 mg) the % drug release at 12 hrs was found to be 76.08 %.

Figure 6: Response surface plot showing effect on drug release at 5 hrs

Figure 7: Response surface plot showing effect on drug release at 12 hrs

Selection of optimized batch:

Selection on basis of low drug release at 12 h and minimum drug release (less than 10%) at 5 h. From all (FT1–FT9) enteric coated batches FT9 show sustained drug release. The optimized batch FT9 shows drug release 3.98 % at 5 hr and 76.08 % at 12 hr. So that FT19 batch shows sustained drug release of drug and maximum lag time.

Fourier transform infra red spectroscopy study:

FTIR studies, reveals that the fundamental peaks of the fenoprofen and polymers were retained in the optimised batch. Presence of -OH stretching of hydrate peak stretching at 3648cm^-1 confirm the presence of drug in optimised batch. Polymer HPC and EC N-22 also showed a -OH stretching of hydrate at 3450, 3366 cm^-1. The overlay of IR spectrum of drug (A) and optimised batch FT9 shown in figure8.

Differential scanning spectroscopy study:

Figure 8: Overlay of IR spectrum of Drug (A) and optimised batch FT9 (B)

DSC studies of drug and optimized batch results reveals that a sharp endothermic peak corresponding to the melting point of crystalline drug was found at 114.5ºC. The thermograms of the optimized batch showed peak at 105.3ºC indicating their crystallinity somewhat reduced. The Overlay of DSC Thermograms of pure drug (A) and optimized batch FT9 (B) shown in figure 9.

Figure 9: Overlay of DSC Thermograms of pure drug (A) and optimized batch FT9 (B)

Powder x-ray diffraction study:

P-XRD analysis shows that there was reduction in the peak intensity of the drug fenoprofen in formulation from 678 to 516 at 9.18 2θ and 691 to 526 at 18.83 2θ. This has indicated that to some extent drug might have got reduced crystallinity but full amorphosization has not been observed. The overlay of PX-RD patterns of fenoprofen and the optimized batch FT9 shown in the figure 10.

Diffraction angle 2θ

Figure 10: Overlay of P-XRD patterns of Drug(A), optimized batch FT9 (B), polymer HPC (C) and EC N-22 (D)

Stability studies:

Short-term stability studies of the batch FT9 batch indicated that there were no significant changes in physical parameters, % drug release after 12 h and (%) drug content at the end of three months period. The result of stability studies reported in table 7.

Table 7: Stability study of optimized formulation tablet

Parameters

Before

After 30 days

After 60 days

After 90 days

Thickness (mm)

7.53±

0.07

7.56±

0.44

7.48±

0.76

7.51±

0.16

Diameter (mm)

12.94±

0.01

12.96±

0.02

12.88±

0.03

12.81±

0.09

Hardness (kg/cm²)

9.30±

0.90

9.1±

0.12

9.1±

0.34

9.3±

0.14

% Drug release at 12 hrs

76.08±

0.045

76.13±

0.05

75.22±

0.15

75.12±

0.35

Drug content (%)

98.75±

0.95

97.05±

0.51

97.75±

0.29

97.15 ± 0.19

*Indicates average readings ± SD (n=3)

CONCLUSION:

The present study was to formulate colonic drug delivery of enteric coated tablet of fenoprofen calcium. The enteric coated tablet has been used to provide more uniform distribution of the drug in the colon and help the drug to spread on the colon surface in an appropriate way. Optimised formulation batch (FT9) showed desired drug release at 5 and 12 hr. Short term stability on the optimized F9 batch of tablet formulation indicated no significant changes in physical parameter like hardness, thickness, % drug content, and drug release. The study concluded that the formulation was prepared of enteric coating of tablet can be used successfully in the systems designed for colon specific drug delivery. Development of once a bedtime colon specific tablet of fenoprofen can be beneficial in chronotherapeutic treatment of RA.

ACNOWLEDGEMENTS:

Anilkumar J. Shinde and co-authors are thankful to Suven Life Sciences, Hyderabad, India Idea cures Pvt. Ltd., Mumbai for gift samples of Fenoprofen calcium and Instacoat EN super.

AUTHOR CONTRIBUTIONS:

The author designed and performed the experiment, analyzed data and prepared the manuscript. All authors played an equal role in completing this research work.

CONFLICT OF INTEREST:

The authors declared no conflict of interest.

REFERENCES:

1. Ashford M, Fell JT, Attwood D, Sharma H, Woodhead PJ. An in-vivo investigation into the suitability of pH-dependent polymers for colonic targeting. Int J Pharm. 1993; 95: 193.

2. Aswar PB, Khadabadi SS, Kuchekar BS,Wane TP, Matake, N. Development and in-vitro evaluation of colon-specific formulations for orally administered Diclofenac sodium. Arch Pharm Sci and Res. 2009; 1(1): 50-52.

3. Chang Yong Z, Xiang B, Du Q,Wang F. Studies of chitosan/Kollicoat SR 30D film- coated tablets for colonic drug delivery. International Journal of Pharmaceutics. 2009; 375: 8-15.

4. Cheng G, Feng A, Zou M, Sun J, Hao M. Time and pH-dependent colon-specific drug delivery for orally administered diclofenac sodium and 5-aminosalicylic acid. World J Gastroenterol. 2004; 10: 1769-74.

5. Chickpetty SM, Baswaraj R, Nanjwade BK. Studies on development of novel combined time and pH dependent solventless compression coated delivery systems for colonic delivery of diclofenac sodium. Asian J Pharma Clin Res. 2010; 3(2): 110 -113.

6. Dew, M. J., Hughes, P. J., Lee, M. G., Evans, B. K. and Rhodes, J. An oral preparation to release drugs in the human colon. Br. J. Clin. Pharmacol. 1982; 14: 405-408.

7. Friend D, Dang GW. A colon-specific drug delivery based on the drug glycosidases of colonic bacteria. J Med Chem. 1984; 27: 261-266.

8. Ibekwe VC, Fadda HM, Parsons GE, Basit AW. A comparative in vitro assessment of the drug release performance of pH-responsive polymers for ileo-colonic delivery. Int J Pharma. 2006; 308: 52–60.

9. Krishnaiah YS, Bhaskar PR, Reddy V, Satyanarayana RS. Studies on the development of oral colon targeted drug delivery systems for metronidazole in the treatment of Amoebiasis. Int J Pharm. 2002; 236: 43–55.

10. Najmuddin M, Patel V, Ahmed A, Shelar S, Khan T. Preparation and evaluation of Flurbiprofen microcapsule for colonic drug delivery system. Int J Pharm and Pharma Sci. 2010; 2: 25-31.

11. Patel JM, Brahmbhatt MR, Patel VB, Muley SV, Yeole PB. Colon Targeted Oral Delivery of Ornidazole Using Combination of pH and Time Dependent Drug Delivery System. Int J Pharm Res. 2010; 2(1): 28-35.

12. Rodríguez M, Vila JL, Torres D. Design of a new multiparticulate system for potential site-specific and controlled drug delivery to the colonic region. J Control Rel. 1998; 55: 67.

13. Salve P. Development and in vitro evaluation colon targeted drug delivery system using natural gum. Asian J Pharm Res. 2011; 10(4): 91-101.

14. Sharma A, Jain A. Colon targeted drug delivery using different approaches. Int J Pharm Studies and Res. 2010; 1(1): 60-66.

15. Tamara M. Drug targeting to the colon with lectins and neoglycoconjugates. Advanced Drug Del Rev. 2004; 56: 491– 509.

16. Zambito A, Baggiani V, Carelli MF, Serafini G. Matrices for site-specific controlled-delivery of 5-fluorouracil to descending colon, J Controlled Rel. 2005; 669–677.

17. Deshkar Sanjeevani,Talole Kranti, Shirsat Ajinath, Bhalerao Aparna, Shirolkar Satish Padm Development of Colon Targeted Delivery of Ketoprofen Using Natural Gums as Carrier, Research Journal of Pharmacy and Technology. 2009; 2 (4): 771-776.

18. Bhoyar P.K., Patil R.P., Barokar A.A., Baheti J.R., Khandare R.A., Gedam S.S. Formulation and In-Vitro Evaluation of Aceclofenac Matrix Tablet For Colon Specific Drug Delivery: By Using Dextrin. Research J. Pharm. and Tech. 2011; 4(4): 527-529.

19. P. B. Patil, A. A. Hajare, R. P. Awale. Development and Evaluation of Mesalamine Tablet Formulation for Colon Delivery. Research Journal of Pharmacy and Technology. 2011; 4(11): 1751-1756.

20. Anglina Jeniffer Samy, Elango K., Ramesh Kumar K., Rajesh Kumar N. Formulation and Evaluation of Dicyclomine Hydrochloride Matrix Tablets for Colon Specific Drug Delivery. Research Journal of Pharmacy and Technology. 2012; 5(4): 494-496.

21. Tiwari Vaibhav, Dangi J. S. Preparation and In-vitro and In-vivo evaluation of colon targeted delivery of antiamoebic drug: an approach to reduce dose. Research Journal of Pharmacy and Technology. 2012; 5(12): 1588-1595.

22. Mahesh S Nemade, Supriya S Thorat, Rajesh Y Chaudhari, Vijay R. Patil. Formulation development of controlled release drug delivery system for tegaserod maleate. Research Journal of Pharmacy and Technology. 2104; 7(9): 1046-1051.

23. Asma Sulthana, B. Ramu, G. Srikanth, Bigala Rajkamal. Formulation and evaluation of colon specific tinidazole matrix tablets. Res. J. Pharm. Dosage Form. and Tech. 2016; 8(3): 167-172.

24. Sagar Kadam, Pradip Yadav, Dhananjay Landge. Formulation and Evaluation of Colon Targeted Enteric Coated Tablets of Loperamide. Research Journal of Pharmacy and Technology. 2020; 13(3): 1447-1452.

25. Saikat Pande, Janu Vashi, Ajay Solanki. Formulation and Characterization of Ileo-colonic targeted Mucoadhesive Microspheres containing flurbiprofen for treatment of Ulcerative Colitis. Research J. Pharm. and Tech. 2020; 13(7): 3377-3382.

26. Anilkumar J. Shinde, Pritam R. Walave, Firoj A. Tamboli, Harinath N. More. Formulation and Optimization of 5-Amino Salicylic acid Tablet for Colon Targeting. Research Journal of Pharmacy and Technology. 2022; 15(10): 4490-8.

27. S. Nandhakumar, G. Sugreevudu, N. Harikrishnan. Formulation design and Evaluation of Extended-Release Tablets of Oxybutynin for Effective Management of Overactive Bladder Syndrome. Research Journal of Pharmacy and Technology. 2021; 14(12): 6558-4.

Received on 25.11.2023 Revised on 16.05.2024

Accepted on 09.09.2024 Published on 24.12.2024

Available online from December 27, 2024

Research J. Pharmacy and Technology. 2024;17(12):5901-5907.

DOI: 10.52711/0974-360X.2024.00895

Batch Codes	Thickness (mm)*	Diameter (mm)*	Hardness (Kg/cm²)*	*In vitro* disintegration time (min)*	Drug content (%)*
C1	3.97 ± 0.015	10.18 ± 0.017	5.3 ± 0.032	9.23± 0.012	98.65 ± 1.05
C2	3.86 ± 0.03	10.25 ± 0.04	5.8 ± 0.13	8.12± 0.02	97.60 ± 0.15
C3	3.85 ± 0.17	10.22 ± 0.08	4.3 ± 0.019	7.15± 0.062	98.75 ± 0.95
C4	3.93 ± 0.12	10.21 ± 0.19	5.5 ± 0.11	13.34± 0.012	97.15 ± 1.15
C5	3.87± 0.19	10.23± 0.013	5.4 ± 0.07	12.19± 0.042	98.45 ± 1.15
C6	3.93± 0.17	10.25± 0.012	4.7 ± 0.019	10.18± 0.09	98.05 ± 1.00

Table 1: Composition of inner core tablet

In vitro disintegration time:

In vitro disintegration time of six tablets from each formulation was determine by using disintegration apparatus (VEEGO). In vitro disintegration test was carried out at 37 ± 0.5 ºC in 900 ml of distilled water.

In vitro dissolution study:

Table 2: Evaluation of powder blends

In vitro dissolution test:

Figure 3: The % cumulative release of inner core table

Factorial design:

Evaluation of Press coated tablet:

Table 3: Evaluation of inner core tablet batch (C1 – C6)

In vitro dissolution study:

The in vitro dissolution study depends upon the concentration of polymer. The concentration of polymer increases there was decrease in drug release. The % cumulative drug release of press coated tablet shown in figure 4.

Table 5: Evaluation of enteric coated tablet

In vitro dissolution study:

Figure 5: % cumulative drug release of enteric coated batch (FT1–FT9)

Figure 6: Response surface plot showing effect on drug release at 5 hrs

Figure 7: Response surface plot showing effect on drug release at 12 hrs

Differential scanning spectroscopy study:

Figure 9: Overlay of DSC Thermograms of pure drug (A) and optimized batch FT9 (B)

ACNOWLEDGEMENTS: