Formulation and Evaluation of Mouth Dissolving Tablets of Deflazacort

Anju govind¹, Manjunath B Menden², Ravikumar²*, Simila¹, Mercy¹, Narayana Swamy VB³

¹M.Pharam (Pharmaceutics) Research Scholar, Karavli College of Pharmacy, Mangalore.

²Department of Pharmaceutics, Karavali College of Pharmacy, Vamanjoor, Mangalore.

³Department of Pharmacognosy, Karavali College of Pharmacy, Vamanjoor, Mangalore.

*Corresponding Author E-mail: ravikumar300@gmail.com

Received on 10.03.2016 Accepted on 08.04.2016

© Asian Pharma Press All Right Reserved

Asian J. Pharm. Tech. 2016; 6(2): 91-98.

DOI: 10.5958/2231-5713.2016.00013.1

ABSTRACT:

The present investigation of research is oriented through increasing safety and efficacy of existing drug molecule through novel concept of oral drug delivery Deflazacort is a synthetic steroid that has an anti inflammatory effect. It is used to decrease inflammation in various different diseases and conditions. Deflazacort works by acting within cells to prevent the release of certain chemicals that are important in the immune system. These chemicals are normally involved in producing immune and allergic responses; resulting in inflammation. By decreasing the release of these chemicals in a particular area, inflammation is reduced. This can help control a wide number of disease states characterized by excessive inflammation. These include severe allergic reactions, inflammation of the lungs in asthma and inflammation of the joints in arthritis.

Deflazacort also decreases the numbers of white blood cells circulating in the blood. And patients Nephritic Syndrome, required steroids for long times. Mouth dissolving tablets of Deflazacort were prepared by Superdisintegrant addition method using SSG, and Croscarmellose sodium as superdisintegrants at 5-10% w/w, showed minimum time to disintegrate the tablet (20.13 sec.) and almost complete release of drug within 15 minutes. The optimized formulation F14 was chosen and their optimum results were found to be in close agreement with experimental finding. The FTIR studies for the optimized formulation F14 shows that there was no interaction between drug and excipients. The stability studies for the optimized formulation F14 showed no significant changes.

KEY WORDS: Mouth dissolving tablets, Superdisintegrants, Diluents, Deflazacort, Direct compression.

INTRODUCTION:

Mouth dissolving system can be defined as a solid dosage form and designed to dissolve/disintegrate in the patient’s mouth within few seconds or minutes, without the need to drink or chew¹. The fear of taking solid tablets and the risk of choking for certain patient populations still exist despite their short disintegration/dissolution times. However some patients, particularly pediatrics and geriatric patients have difficulty swallowing or chewing solid dosage forms (conventional dosage forms) to fear of choking and unwillingness².

To overcome the problems associated with other dosage form which are commonly used to enhance patient compliance like effervescent tablets, dry syrup require intake of water and in the case of chewable tablets patients may experience bitter taste or unpleasant taste of drug. Injections generally are not favored by the patients due to invasiveness. So, the development of an appropriate dosage form is most desirable. One such approach is mouth dissolving tablets. The concept of mouth dissolving drug delivery system emerged from the desire to provide patient with more conventional means of taking their medication^3-7.

Table 1: Compositions of Mouth dissolving Deflazacort tablets using mannitol as diluent

Ingredients in mg	Formulation Codes
	F1	F2	F3	F4	F5	F6	F7	F8	F9
Deflazacort	30	30	30	30	30	30	30	30	30
Croscarmellose sodium	6	12	18	-	-	-	-	-	-
Crosspovidone	-	-	-	6	12	18	-	-	-
Sodium starch glycolate	-	-	-	-	-	-	6	12	18
Mannitol	41	35	29	41	35	29	41	35	29
Aspartame	15	15	15	15	15	15	15	15	15
Magnesium stearate	2	2	2	2	2	2	2	2	2
Talc	5	5	5	5	5	5	5	5	5
Aerosil	1	1	1	1	1	1	1	1	1
Total weight (mg)	100	100	100	100	100	100	100	100	100

Table 2: Compositions of Mouth dissolving Deflazacort tablets using spray dried lactose as diluent

Ingredients in mg	Formulation Codes
	F10	F11	F12	F13	F14	F15	F16	F17	F18
Deflazacort	30	30	30	30	30	30	30	30	30
Croscarmellose sodium	6	12	18	-	-	-	-	-	-
Crospovidone	-	-	-	6	12	18	-	-	-
Sodium starch glycolate	-	-	-	-	-	-	6	12	18
Spray dried lactose	41	35	29	41	35	29	41	35	29
Aspartame	15	15	15	15	15	15	15	15	15
Magnesium stearate	2	2	2	2	2	2	2	2	2
Talc	5	5	5	5	5	5	5	5	5
Aerosil	1	1	1	1	1	1	1	1	1
Total weight (mg)	100	100	100	100	100	100	100	100	100

Table 3: Compositions of Mouth dissolving Deflazacort tablets using dibasic calcium phosphate as diluent

Ingredients in mg	Formulation codes
	F19	F20	F21	F22	F23	F24	F25	F26	F27
Deflazacort	30	30	30	30	30	30	30	30	30
Croscarmellose sodium	6	12	18	-	-	-	-	-	-
Crospovidone	-	-	-	6	12	18	-	-	-
Sodium starch glycolate	-	-	-	-	-	-	6	12	18
Dibasic calcium phosphate	41	35	29	41	35	29	41	35	29
Aspartame	15	15	15	15	15	15	15	15	15
Magnesium stearate	2	2	2	2	2	2	2	2	2
Talc	5	5	5	5	5	5	5	5	5
Aerosil	1	1	1	1	1	1	1	1	1
Total weight (mg)	100	100	100	100	100	100	100	100	100

Deflazacort (11β, 16β)-21-(Acetyloxy)-11–hydroxy–2′-methyl–5′H-pregna1, 4- dieno [17, 16-d] oxazole–3, 20–dione. Is in a class of Glucocorticoids drugs and immune suppressant is about 30-40% at doses of 1-30 mg. Half-life is 1.9-2.3 hour and Protein binding 40% and excretion 70% renal and 30% faecal.^8,9.

The basic aim of the present investigation was to formulate and evaluate mouth dissolving tablets of Deflazacort which expected to provide the best remedy for patients suffering from hypersensitivity reaction and dysphagia especially Anaphylactic Reaction and adjuvant to Adrenaline to stabilize the patients and also to enhance the bioavailability of drug. The present investigation was to prepare fast dissolving tablets of Deflazacort using Superdisintegrants Croscarmellose sodium, sodium starch Glycolate, and study the performance of fast dissolving tablets.

MATERIALS AND METHOD:

Materials:

Deflazacort was obtained as a gift sample from Unicare Pvt. India Ltd. Roorkee. Microcrystalline cellulose, Sodium Starch Glycolate, Talc was obtained from CDH, New Delhi, India. Croscarmellose Sodium was obtained as a gift sample from Maple biotech Pune.

Methods:

Method of preparation mouth dissolving tablet of Deflazacort:^10-15

Deflazacort Mouth dissolving tablets were prepared by a direct compression method; all the ingredients were screened through sieve # 100, except lubricant all the other ingredients were thoroughly blended in a glass mortar with pestle for 15 min. After sufficient mixing lubricant was added and mixed for additional 2 to 3 min. The mixture is compressed using flat faced punch on Cemach 12 station rotary tablet compression machine and the compositions were given in Table 1, 2 and 3.

Precompression parameters:

Bulk density:

It is the ratio of total mass of powder to the bulk volume of powder. It was measured by pouring the weighed powder (passed through standard sieve # 20) into a measuring cylinder and the initial volume was noted, it is bulk volume. The bulk density is calculated according to the formula mentioned below. It is expressed in gm/cc and is given by

= M/

Where, = Bulk Density, M = mass of the powder, = bulk volume of powder.

Tapped density:

It is the ratio of total mass of powder to the tapped volume of powder. The volume was measured by tapping the powder for 500 times. It is expressed in gm/cc and is given by

= M/

Where, = Tapped density, M = mass of the powder, = tapped volume of powder.

Hausner’s ratio:

It is the ratio of tapped density to the bulk density. It is given by

Hausner’s ratio = /

Where, = Tapped density, = Bulk density.

Compressibility Index:

The flowability of powder can be evaluated by comparing the bulk density () and tapped density () of powder and the rate at which it packed down. Compressibility index is calculated by

Compressibility index (%) = / x 100

Where, = Bulk density, = Tapped density

Angle of repose

This is the maximum angle possible between the surface of a pile of powder or granules and the horizontal plane. The powders were allowed to flow through the funnel fixed to a stand at definite height (h). The angle of repose was then calculated by measuring the height and radius of the heap of granules formed.

tan q = h/r

q = tan^-1 (h/r)

Post compression parameters of Mouth dissolving Deflazacort tablets

Thickness:

Thickness of the tablets was measured using a calibrated Vernier Caliper. Three tablets of each formulation were picked randomly and thickness was measured individually.

Weight variation:

Twenty tablets were selected randomly from each batch and weighed individually to check for weight variation. A little variation was allowed in the weight of a tablet according to US Pharmacopoeia. The following percentage deviation in weight variation was allowed. In all formulations, the tablet weight is 100 mg, hence 7.5% maximum difference allowed.

Hardness:

Hardness indicates the ability of a tablet to withstand mechanical shocks while handling. The hardness of the tablets was determined using Monsanto hardness tester. It is expressed in kg/cm². Three tablets were randomly picked and hardness of the tablets was determined.

Friability:

The friability of tablets was determined by using Roche friabilator. It is expressed in percentage (%). Ten tablets were initially weighed (W_I) and transferred into friabilator. The friabilator was operated at 25 rpm for 4 minutes or run up to 100 revolutions. The tablets were weighed again (W_F). Percentage friability of tablets less than 1% was considered acceptable. The % friability was then calculated by

% F = 100 (1-W_I / W_F)

Drug content uniformity:

Ten tablets were weighed and grounded in a mortar with pestle to get fine powder; powder equivalent to the mass of one tablet was dissolved in methanol by sonication for 30 min and filtered through filter paper. The drug content was analyzed spectrophotometrically at 224 nm using an UV spectrophotometer.

In vitro drug release of Mouth dissolving tablets:

The in vitro drug release studies of Deflazacort Mouth dissolving tablets were determined using USP II rotating paddle type. The dissolution test was performed using 900 ml of phosphate buffer pH 7.4. The release was performed at 37°C ± 0.5°C, with a rotation speed of 50 rpm. The samples (5 ml) were withdrawn at predetermined time intervals and replaced with fresh medium. The samples were filtered through filter paper and analyzed after appropriate dilution by UV spectrophotometer at 224 nm.

Wetting time and Water absorption ratio:

The wetting time of the tablets was measured using a simple procedure. Five circular tissue papers of 10 cm in diameter were placed in a petridish containing 10 ml of water containing eosin, a water soluble dye. A tablet was carefully placed on the surface of tissue paper. The time required for water to reach the upper surface of the tablets was noted as the wetting time. The wetted tablet was taken and weighed. Water absorption ratio (R) was determined using following formula

R = 100 (Wa - Wa) / W

In vitro dispersion time:

The in vitro dispersion time of the prepared tablets were placed in 10 ml beaker containing 6 ml of 7.4 pH phosphate buffer and time taken for complete dispersion of tablet was observed.

Drug excipient compatibility studies

FTIR spectroscopic studies were conducted for Deflazacort pure drug and optimized formulation. Solid samples were milled with potassium bromide (KBr) to form a very fine powder. This powder is then compressed into a thin pellet under hydraulic press which can be analyzed. KBr is also transparent in the IR; the FTIR spectra were recorded between 400 and 4000 cm^-1.

Stability Studies:

Stability of a drug has been defined as the ability of a particular formulation, in a specific container, to remain within its physical, chemical, therapeutic and toxicological specifications.

The optimized batch of Mouth dissolving Deflazacort tablets were placed in desiccators and stored at ambient conditions; such as at room temperature, oven temperature (40±2°C) with 75% RH and refrigerator (2-8°C) for a period of 60 days, then evaluated for changes in physiochemical properties and in vitro drug release.

RESULTS AND DISCUSSION:

Drug excipient compatibility studies

FTIR studies revealed that, pure drug Deflazacort shown intense band at 1613.36 cm^-1, 1566.76 cm^-1, 1515.59 cm^-1 and 1052.22 cm^-1 corresponding to the functional groups C=O, COOH, NH and OH bending. The FTIR of drug and optimized formulation (F14) (superdisintegrants) shown intense bands at 1617.75 cm^-1, 1560.85 cm^-1, 1517.38 cm^-1 and 1052.19 cm-1 indicates no change in the functional groups C=O, COOH, NH and OH. From the above interpretation it is understood that there is no major shifting in the frequencies of above said functional groups. Hence the drug and superdisintegrants were compatible with each other. The FTIR spectras of pure drug Deflazacort and optimized formulation (F14) were shown in figure 1 and 2 respectively.

Figure 1: FTIR spectra of Deflazacort pure drug

Figure 2: FTIR spectra of optimized formulation of (F 14).

Precompression parameters:

The powder blend was evaluated for the physical properties such as angle of repose, bulk density, tapped density, compressibility index and Hausner’s ratio. The angle of repose of all the formulations F1-F27 ranged from 26.21^o to 33.15^o. The bulk density and tapped density for all the formulation varied in range of 0.20-0.49 gm/ml and 0.25-0.65 gm/ml. The values obtained lies within the acceptable range and with not much difference found between bulk density and tapped density. These results may further influence property such as compressibility and tablet dissolution (table 4).

Table 4: Precompression parameters of Mouth dissolving Deflazacort tablets (F1-9)

Formulations Code	Angle of repose (θ^0)	Bulk density (gm/ml)	Tapped Density (gm/ml)	Percentage Compressibility Index (%)	Hausner’s Ratio
F1	31.6	0.49	0.65	24.6	1.32
F2	32.2	0.30	0.36	16.6	1.20
F3	32.6	0.25	0.31	19.3	1.24
F4	30.2	0.21	0.25	16.0	1.19
F5	31.2	0.22	0.25	12.0	1.13
F6	30.9	0.37	0.43	13.9	1.16
F7	33.1	0.37	0.42	11.9	1.13
F8	32.5	0.33	0.37	10.8	1.12
F9	31.6	0.25	0.30	16.6	1.20
F10	30.9	0.25	0.30	16.6	1.20
F11	31.2	0.37	0.45	17.7	1.21
F12	31.3	0.21	0.25	16.0	1.19
F13	29.0	0.37	0.45	17.7	1.21
F14	27.6	0.21	0.25	20.0	1.25
F15	30.9	0.25	0.30	16.6	1.20
F16	29.8	0.25	0.30	16.6	1.20
F17	28.5	0.33	0.37	10.8	1.12
F18	26.2	0.37	0.45	17.7	1.21
F19	29.6	0.22	0.25	12.0	1.13
F20	30.2	0.37	0.45	17.7	1.21
F21	30.3	0.37	0.42	11.09	1.13
F22	29.0	0.36	0.42	14.28	1.03
F23	27.6	0.33	0.37	10.8	1.12
F24	28.4	0.20	0.26	23.0	1.30
F25	29.2	0.25	0.31	19.3	1.24
F26	27.5	0.36	0.43	16.27	1.19
F27	26.8	0.30	0.36	16.6	1.20

Table 5: Post compression parameters of Mouth dissolving Deflazacort tablets (F1- F27)

Formula- tion Code	Weight variation (mg)	Hardness (kg/cm^2)	Friability (%)	Thickness (mm)	Wetting time (sec)	In vitro dispersion time seconds)	Water absorption ratio (%)	Content uniformity (%)
F1	100.15±1.83	2.3±0.05	0.69	4.48±0.02	52±0.81	74^+1.24	66.3^+0.54	96
F2	99.7±1.99	2.2±0.17	0.79	4.44±0.03	53±0.21	69^+1.34	71.3^+0.56	97
F3	101.4±1.13	2.3±0.11	0.69	4.61±0.03	42±0.24	54^+1.32	77.4^+0.45	95
F4	101.6±1.16	2.2±0.05	0.64	4.49±0.03	55±0.25	73^+1.26	74.6^+0.64	97
F5	100.8±0.74	2.1±0.11	0.54	4.55±0.09	20±0.85	24^+1.26	84.1^+0.88	99
F6	94.6±0.33	2.2±0.17	0.64	4.38±0.06	24±0.92	46^+1.34	78.3^+0.78	98
F7	101.7±0.14	2.2±0.15	0.73	4.49±0.03	33±0.95	53^+1.45	77.3^+0.24	95
F8	105.9±0.28	2.3±0.05	0.59	4.58±0.03	35±0.13	63^+1.24	72.0^+0.45	94
F9	98.2±0.23	2.1±0.05	0.59	4.65±0.08	68±1.24	128^+0.98	62.6^+0.65	98
F10	97.5±1.15	2.3±0.04	0.54	4.61±0.07	71±0.25	142^+1.12	59.6^+0.48	104
F11	103.1±1.38	2.3±0.12	0.74	4.60±0.01	69±0.87	183^+1.54	53.8^+0.95	103
F12	105.7±0.74	2.3±0.05	0.59	4.67±0.02	73±0.99	197^+1.25	49.0^+0.35	94
F13	97.3±1.14	2.4±0.08	0.68	3.48±0.05	15±1.25	21^+1.08	83.6^+0.85	104
F14	107.6±0.85	2.3±0.06	0.59	4.60±0.03	19±1.35	19^+1.04	85.5^+0.92	99
F15	101.4±1.01	2.2±0.03	0.72	4.46±0.01	22±1.15	28^+0.89	79.6^+0.95	94
F16	95.1±0.52	2.3±0.07	0.75	4.62±0.06	31±0.98	29^+0.54	75.9^+0.58	103
F17	98.2±0.34	2.2±0.06	0.55	4.48±0.03	71±0.88	348^+1.14	42.5^+0.54	96
F18	102.1±0.48	2.4^+0.08	0.72	4.45±0.05	71±0.78	282^+0.68	45.6^+0.45	101
F19	100.15±1.83	2.4±0.05	0.68	4.46±0.02	50±0.61	72^+1.14	68.3^+0.24	98
F20	98.7±1.99	2.8±0.16	0.69	4.45±0.03	54±0.20	79^+0.36	61.3^+0.56	89
F21	100.4±1.13	2.5±0.11	0.89	4.60±0.03	44±0.34	64^+1.32	80.4^+0.40	94
F22	99.6±1.16	2.2±0.05	0.74	4.48±0.03	65±0.15	63^+1.16	78.6^+0.54	94
F23	102.2±0.74	2.6±0.14	0.54	4.53±0.09	48±0.85	44^+1.34	74.1^+0.82	96
F24	96.6±0.33	2.6±0.14	0.74	4.36±0.06	44±0.92	66^+1.34	68.3^+0.62	98
F25	98.7±0.14	2.4±0.14	0.83	4.46±0.03	43±0.85	63^+1.45	72.3^+0.26	94
F26	102.4±0.28	2.3±0.06	0.69	4.56±0.03	45±0.23	63^+1.24	72.0^+0.48	95
F27	96.2±0.23	2.4±0.05	0.68	4.62±0.08	62±0.24	78^+0.98	66.6^+0.62	98

Post compression parameters of Deflazacort Mouth dissolving tablets:

Mouth dissolving Deflazacort tablets were prepared by using different superdisintegrants (sodium starch glycolate, croscarmellose sodium and crospovidone) and diluents (mannitol, dicalcium phosphate and spray dried lactose) with various concentration by direct compression method.

The prepared Mouth dissolving Deflazacort tablets were evaluated for hardness, friability, thickness, weight variation, content uniformity. The values for all the formulations F1-F27 were found to be within the acceptable limits. The average percentage deviation of all the formulations F1-F27 was found to be within the limits.

The thickness of tablets for all the formulations F1-F27 ranged from 4.38-4.67 mm. The hardness of the tablets for all the formulations F1-F27 between 2.1-2.8 kg/cm² were shown in Table . Friability for all formulations F1-F27 was shown less than 0.89% indicating a good mechanical strength of tablets. The wetting time for all the formulations was 19-73 seconds. The wetting time for the optimized formulation (F14) 19 seconds indicates quicker disintegration among twenty seven formulations (table 5).

In vitro dissolution studies:

The maximum drug release in 30 seconds for the formulations F1, F2, F3, F4, F5, F6, F7, F8 and F9 using different concentration of super disintegrants croscarmellose sodium, crosspovidone and sodium starch glycolate and mannitol as diluent were 92%, 93%, 95%, 93%, 96%, 96%, 96%, 96% and 90% respectively. Similarly the maximum drug release for the formulation F10, F11, F12, F13, F14, F15, F16, F17 and F18 using different concentration of super disintegrants croscarmellose sodium, crosspovidone and sodium starch glycolate by using spray dried lactose as diluent were 91%, 89% , 85%, 88%, 99%, 89%, 95%, 72% and 77% respectively. The maximum drug release for the formulation F19, F20, F21, F22, F23, F24, F25, F26 and F27 using different concentration of super disintegrants croscarmellose sodium, crosspovidone and sodium starch glycolate and dibasic calcium phosphate as diluent were 95%, 94% , 90%, 92%, 92%, 92%, 92%, 93% and 94% respectively. Among the twenty seven formulations F14 contains crosspovidone as superdisintegrants and spray dried lactose as diluents shows good drug release of 98.5% within 30 seconds (table 6-8).

Table 6: In vitro dissolution studies for formulations F1-F9

Time (min)	F1	F2	F3	F4	F5	F6	F7	F8	F9
0	0	0	0	0	0	0	0	0	0
2	51.8	52.3	56.3	52.4	63.4	60.5	60.2	58.4	50.6
5	59.7	75.5	68.2	60.3	77.6	72.3	73.1	72.5	53.5
7	76.8	80.8	79.3	75.9	89.8	87.6	84.8	85.2	63.6
10	84.8	82.4	85.9	86.1	93.3	94.9	94.0	93.3	74.9
15	88.9	89.1	94.2	90.3	95.8	95.1	95.3	94.2	83.2
30	92.2	93.7	95.3	93.8	96.4	96.2	96.1	95.8	89.8

Table 7: In vitro dissolution studies for formulations F10-F18

Time (min)	F10	F11	F12	F13	F14	F15	F16	F17	F18
0	0	0	0	0	0	0	0	0	0
2	50.9	49.6	48.7	48.2	59.1	45.8	49.2	36.9	39.1
5	54.8	53	52.8	54.4	75.9	61.6	58.6	37.3	42.3
7	62.7	56.7	62.9	60.6	80.1	65.0	62.8	41.9	43.8
10	71.8	69.7	73.9	72.3	85.8	74.5	76.2	48.6	56.7
15	86.8	83.9	81.4	80.1	89.6	84.3	84.4	56.0	60.3
30	90.8	89.4	84.8	88.2	98.5	89.0	95.1	72.3	77.1

Table 8: In vitro dissolution studies for formulations F19-F27

Time (min)	F19	F20	F21	F22	F23	F24	F25	F26	F27
0	0	0	0	0	0	0	0	0	0
2	52.9	50.3	56.3	54.4	63.4	50.5	54.2	58.4	52.4
5	60.8	68.5	68.2	60.3	74.6	62.3	63.1	62.6	53.5
7	77.8	76.8	79.3	66.8	80.8	77.6	74.8	73.4	63.6
10	88.8	82.4	83.9	79.2	87.4	84.9	82.4	82.2	73.9
15	94.9	92.1	87.2	86.3	92.0	90.6	90.3	89.8	84.2
30	95.2	94.4	90.3	92.4	92.4	92.2	92.0	93.3	94.2

Stability Studies:

Stability studies of the prepared formulations were performed at room temperature, at 40°C with 75% RH and 2-8°C a period up to 60 days. The samples were withdrawn after periods of 30 days and were analyzed for its appearance, hardness, friability, drug content wetting time, water absorption ratio, in vitro dispersion time and in vitro release. The results obtained were shown in table 9-13.

The results revealed that no significant changes in physicochemical properties, wetting time, water absorption ratio, in vitro dispersion time and in vitro release for F14 formulation, when it is stored at the three storage condition. However there was slight variation in in vitro release when it is stored at room temperature and 40°C. There was no change when it is stored at 2-8°C.

Table 9: Physicochemical properties of formulation (F14) stored at 2-8°C

Formulation Code	Weight Variation (mg)	Hardness (kg/cm^2)	Friability (%)	Thickness (mm)	Wetting time (sec)	Water absorption ratio (%)
F14	206.6±0.54	2.3±0.04	0.69	4.60	20	85.4

Table 10: Physicochemical properties of formulation (F14) stored at room temperature

Formulation Code	Weight Variation (mg)	Hardness (kg/cm^2)	Friability (%)	Thickness (mm)	Wetting time (sec)	Water absorption ratio (%)
F14	107.2±0.80	2.4±0.16	0.58	4.60	19	85.5

Table 11: Physicochemical properties of formulation (F14) stored at 40°C

Formulation Code	Weight Variation (mg)	Hardness (kg/cm^2)	Friability (%)	Thickness (mm)	Wetting time (sec)	Water absorption ratio (%)
F14	107.4±0.65	2.3±0.26	0.76	4.60	18	85.6

Table 12: In vitro dispersion time and content uniformity of formulation (F14)

Formulation code	In vitro dispersion time (seconds)			Content uniformity (%)
F14	2-8°C	Room temperature	40°C	2-8°C	Room temperature	40°C
	85.5	85.8	86	99	99	98.5

Table 13: In vitro dissolution profile of stability formulation (F14)

Time (min)	Storage condition
	2-8° C	Room temperature	40° C
0	0	0	0
2	59.42	58.82	58.21
5	74.63	74.24	74.20
7	81.22	81.56	81.06
10	85.84	85.67	84.84
15	89.66	89.67	88.24
30	98.66	98.22	97.60

CONCLUSION:

Development of Mouth dissolving tablets was to increase the bioavailability of drug. It may conclude the Deflazacort tablet would be a promising Mouth dissolving drug for an administration. In the formulation the combination of cost effective and biocompatible excipients had been successfully used. Twenty seven formulations F1-F27 were prepared by direct compression method using crospovidone, croscarmellose sodium and sodium starch glycollate as superdisintegrants and comparative study with different diluents (mannitol, spray dried lactose and dibasic calcium phosphate). The optimum concentration was identified based on the in vitro dispersion time and in vitro drug release results. Based on the observation, it was concluded that formulation F14 containing 6% crospovidone with spray dried lactose was the optimized combination due to its fast in vitro dispersion time while compare with other formulations. FTIR studies revealed that there was no chemical interaction between pure drug and the excipients used in the study. Stability studies of promising formulation F14 indicated that there were no significant changes in drug content and in vitro dissolution studies. The results demonstrated the effective use of Mouth dissolving Deflazacort tablets and as an ideal drug release formulation for treatment.

ACKNOWLEDGEMENTS:

The authors are thankful to the Management and Principal of Karavali college of Pharmacy, Mangalore for providing all the facilities to conduct the research work and the authors are also thankful to Unicare Pvt. India Ltd. Roorkee, for generous gift sample of Deflazacort.

REFERENCE:

1. Lindgren S, Janzon L. Dysphagia: Prevalence of swallowing complaints and clinical finding. Med Clin North Am 1993; 77:3-5. 

2. Sastry SV, Nyshadham JR, Fix JA. Recent technological advances in oral drug delivery: A review. Pharm Sci Technol Today. 2000;3:138-45

3. Fu Y, Yang S, Jeong SH, Kimura S, Park K. Orally fast disintegrating tablets: Developments, technologies, taste-masking and clinical studies. Crit Rev Ther Drug Carrier Sys 2004; 21:433-76. 

4. www.rubicon.co.in, Rubi ODT^TM technology: Orally disintegrating tablet technology.

5. Seager H. Drug Delivery Products and the Zydis fast dissolving dosage form. J Pharm Pharmacol 1998; 50:375-82. 

6.  Habib W, Khankari RK, Hontz J. Fast dissolve drug delivery systems. Crit Rev Ther Drug Carrier Sys 2000; 17:61-72. 

7. Dobetti L. Fast disintegrating tablets. US Patent 2003; 6:596,311. 

8. Brown D. Immediate release tablets-taste over speed. Drug Del Tech 2003; 3:58-61. 

9. Behnke K, Sogaard J, Martin S, Bauml J, Ravindran AV, Agren H et al. Mirtazapine orally disintegrating tablet versus sertraline: A prospective onset of action study. J Clin Psychopharmacol 2003; 23:358-64.  

10. Jaccard TT, Leyder J. Une nouvelle forme galenique le lyoc. Ann Pharm Fr 1985; 43:123-31. 

11. Dollo G, Chevanne F, Le Corre P, Chemtob C, Le Verge R. Bioavailability of phloroglucinol in man. J Pharm Belg 1999; 54:75-82. 

12. Gafitanu E, Dumistracel I, Antochi S. Formulations and bioavailability of propyphenazone in lyophilized tablets. Rev Med Chir Soc Med Nat Iasi 1991; 95:127-8. 

13.  Clarke A, Brewer F, Johnson ES, Mallard N, Hartig F, Taylor S, et al. A new formulation of selegiline: Improved bioavailability and selectivity for MAO-B inhibition. J Neural Transm 2003; 110:124-5.

14. Dobetti L. Fast melting tablets: Developments and technologies. Pharm Technol N Am 2001; 44-50.

15. Van Scoik KG. Solid Pharmaceutical dosages in tablet triturate form and method of producing the same. US Patent 5,082,667.