International Journal of Current Pharmaceutical Research
International Journal of Current Pharmaceutical Research
International Journal of Current Pharmaceutical Research
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<strong>Research</strong> Article<br />
FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF SOME AYURVEDIC<br />
CHURNAS BY VACUUM DRYING TECHNIQUE<br />
N. G. RAGHAVENDRA RAO 1 , UPENDRA KULKARNI 2 , BASAWARAJ S. PATIL 2 , GURURAJ V. WADAGERI 2<br />
1Department <strong>of</strong> Pharmaceutics. Luqman College <strong>of</strong> Pharmacy, Gulbarga585102, Karnataka, India, 2Department <strong>of</strong> Pharmaceutics. RME’s<br />
College <strong>of</strong> Pharmacy 585102, Karnatka, India. E mail: nraghu@rediffmail.com<br />
Received 17 Dec 2009, Revised and Accepted 06 Jan 2010<br />
ABSTRACT<br />
Patient compliance can be increased and adulteration can be decreased in ayurvedic powders by formulating them into tablets. An attempt has<br />
been made for the development <strong>of</strong> fast dissolving tablets <strong>of</strong> the ayurvedic powders like Sudarshan churna and Bhaskar lavan churna. Sudarshan<br />
churna was indicated for fever, and Bhaskar lavan churna is used in the gastrointestinal disorders like digestive impairment, dyspepsia and<br />
constipation. In the present work, fast dissolving tablets <strong>of</strong> Sudarshan churna and Bhaskar lavan churna were designed with a view to enhance<br />
patient compliance employing vacuum drying technique. The blend was examined for the pre‐compressional parameters. The prepared<br />
formulations were evaluated for hardness, weight variation, tablet thickness, friability, disintegration time, wetting time, and stability studies.<br />
Stability studies were carried out as per ICH guidelines for three months. The values <strong>of</strong> pre‐compression parameters evaluated were within<br />
prescribed limits and indicated good free flowing property. In all the formulations, friability is less than 1%, indicated that tablets had a good<br />
mechanical resistance. Hardness <strong>of</strong> the tablets was found to be in the range <strong>of</strong> 4.00‐4.50 kg/cm2 which is within acceptable limits. The wetting time<br />
<strong>of</strong> the formulations BLC3 and SC3 were shows 20 sec and 18 sec respectively. The formulation BLC3 shows less in vitro dispersion time 18 sec and<br />
formulation SC3 shows less in vitro dispersion time 20 sec. In vitro dispersion time decreases with increase in concentration <strong>of</strong> ammonium<br />
bicarbonate. The stability studies results revealed that disintegration time and wetting time <strong>of</strong> all tablets decreased significantly (p
MATERIALS AND METHODS<br />
Sudarshan churna (SC) and Bhaskar lavan churna (BLC) were<br />
procured from local market. Crospovidone was gift sample from<br />
MAPLE biotech Pvt. Ltd. Pune, India and other substances used in<br />
the study ammonium bicarbonate, spray dried lactose, talc, poly<br />
vinyl pyrrolidone (PVP), and sodium lauryl sulphate (SLS) were<br />
purchased from S.D. Fine Chemicals, Mumbai. Aspartame was<br />
obtained from Cipla Pharma. Ltd. Vikroli, Mumbai. Other reagents<br />
were <strong>of</strong> analytical grade.<br />
Methods<br />
Preparation <strong>of</strong> fast dissolving tablets <strong>of</strong> sudarshan and bhaskar<br />
lavan churnas by vacuum drying technique: The fast dissolving<br />
tablets <strong>of</strong> sudarshan and Bhaskar lavan churnas were prepared by<br />
wet granulation method using aqueous solution <strong>of</strong> 1% w/w PVP as<br />
binder for all formulation. The granules are prepared by passing the<br />
damp mass through sieves # 16. The wet granules were then dried<br />
at 60 0C in hot air oven. Dried granules (22/44) were taken and<br />
mixed with spray dried lactose, aspartame, superdisintegrant and<br />
different concentration <strong>of</strong> ammonium bicarbonate in a plastic<br />
container followed by compression <strong>of</strong> blend on a 10‐station rotary<br />
punch‐tabletting machine (Rimek mini Press‐1) using 12mm<br />
concave punches at hardness <strong>of</strong> 4 to 4.50 kg/cm 2 prior to<br />
compression <strong>of</strong> granules in to tablets, tabletting properties such as<br />
angle <strong>of</strong> repose, % compressibility were determined for all the<br />
formulations. After compression the tablet were collected and<br />
vacuum dried at 60 0 C until a constant weight was obtained to ensure<br />
the compete removal <strong>of</strong> sublimable compound to make the tablet<br />
porous. Schematics figure <strong>of</strong> Vacuum drying method for designing <strong>of</strong><br />
fast dissolving tablets is shown in Fig 1. Different formulations were<br />
prepared by vacuum drying technique compositions <strong>of</strong> which are<br />
given in Table 1.<br />
Table 1: Formulae used in the preparation <strong>of</strong> tablets containing sudarshan churna (sc) and bhaskar lavan churna (blc).<br />
Ingredients (mg/tab) SC1 SC2 SC3 BLC1 BLC2 BLC3<br />
SC/BLC 500 500 500 500 500 500<br />
Crospovidone 32.5 32.5 32.5 32.5 32.5 32.5<br />
Spray dried Lactose 75.25 62.25 36.25 75.25 62.25 36.25<br />
Ammonium bicarbonate 13 26 52 13 26 52<br />
PVP 6.5 6.5 6.5 6.5 6.5 6.5<br />
Talc 6.5 6.5 6.5 6.5 6.5 6.5<br />
Aspartame 13 13 13 13 13 13<br />
SLS. 3.25 3.25 3.25 3.25 3.25 3.25<br />
Total weight 650 650 650 650 650 650<br />
Evaluation <strong>of</strong> tablets<br />
All the formulated tablets were evaluated for weight variation,<br />
hardness, thickness, friability, wetting time, disintegration time and<br />
stability study. In the weight variation test, 20 tablets were selected<br />
at random and the average weight was calculated. Then, individual<br />
tablets were weighed and the weight was compared with an average<br />
weight. Pfizer hardness tester was used for the determination <strong>of</strong><br />
hardness <strong>of</strong> the tablet. The tablet was placed in contact b/w the<br />
plungers and the handle pressed. The force <strong>of</strong> fracture was recorded.<br />
The thickness <strong>of</strong> the tablet was recorded during the process <strong>of</strong><br />
compression using calipers (Mitotoyo Japan). The friability <strong>of</strong> tablets<br />
was determined using a Roche friabilator (Electrolab, EF2<br />
friabilator). Two tablets from each batch takened and placed in the<br />
friabilator then operated for 100 revolutions. Then the tablets were<br />
dedusted and reweighed. Percentage friability was calculated using<br />
the formula,<br />
F = (1‐W0 / W) X 100<br />
In the disintegration time study, the tablets were taken and<br />
introduced in each tube <strong>of</strong> disintegration apparatus and the tablet<br />
rack <strong>of</strong> the disintegration apparatus was positioned in to a 1 liter<br />
beaker containing 900ml <strong>of</strong> distilled water and time <strong>of</strong><br />
disintegration was recorded at 37±20C. internal diameter 6.5cm) containing 5ml <strong>of</strong> distilled water. A tablet<br />
was placed on the paper and time for complete wetting <strong>of</strong> the tablets<br />
was measured in seconds. The stability study <strong>of</strong> the tablets was<br />
carried out according to ICH guidelines, by storing the tablets in<br />
stability chamber (Lab‐Care, Mumbai) at 40±2<br />
In the wetting time study, a<br />
piece <strong>of</strong> tissue paper folded twice was placed in a petridish (with<br />
0C/75 ± 5%RH for<br />
three months. At the end <strong>of</strong> each month tablets were tested for<br />
disintegration time and wetting time.<br />
RESULTS AND DISCUSSION<br />
Flow properties <strong>of</strong> sudarshan and bhaskar lavan powders were<br />
analyzed before compression to tablets. The high values <strong>of</strong> angle <strong>of</strong><br />
repose (SC≥42.22 and BLC≥41.17) and % compressibility (SC≥55.66<br />
and BLC≥52.48) clearly indicates that both churnas were not free<br />
flowing powders. So in order to improve flow properties <strong>of</strong> powders<br />
a lubricant (talc) and glident (SLS) were incorporated into the<br />
churna powders. Even after addition <strong>of</strong> lubricant and glident also,<br />
there was no improvement in flow property <strong>of</strong> churnas. That is why,<br />
the powder blends <strong>of</strong> sudarshan and bhaskar lavan churnas were<br />
converted into the granules by using aqueous solution <strong>of</strong> 1% w/w<br />
PVP. The values <strong>of</strong> pre‐compression parameters <strong>of</strong> both churnas<br />
granules evaluated were within prescribed limits and indicated good<br />
free flowing property (Table 2). Then granules were compressed<br />
into tablets on a 10‐station rotary punching machine (Rimek mini<br />
Press‐1) using 12mm concave punch.<br />
Table 2: Precmpressional parameters <strong>of</strong> granules<br />
Formulation Angle <strong>of</strong> repose<br />
Compressibility<br />
Bulk density Tapped density Hausner’s Ratio<br />
Code<br />
(Ө) (±SD), n=3<br />
(%) (±SD), n=3<br />
(gm/cc) ± SD, n=3 (gm/cc) ± SD, n=3 ± SD, n=3<br />
SC 1 23.65 (0.22) 16.66 (0.72) 0.43 (0.006) 0.55 (0.02) 1.27 (0.03)<br />
SC 2 24.22 (0.52) 17.72 (0.52) 0.44 (0.007) 0.52 (0.02) 1.18 (0.04)<br />
SC 3 23.70 (0.62) 19.54 (0.55) 0.45 (0.004) 0.51 (0.01) 1.13 (0.03)<br />
BLC 1 22.49 (0.92) 18.59 (1.22) 0.44 (0.006) 0.54 (0.02) 1.22 (0.03)<br />
BLC 2 23.52 (0.72) 18.33 (0.92) 0.42 (0.004) 0.53 (0.01) 1.26 (0.03)<br />
BLC 3 21.58 (0.55) 19.22 (0.99) 0.44 (0.002) 0.55 (0.02) 1.25 (0.04)<br />
Note: Values in parenthesis are standard deviation (±SD)<br />
In all formulations, the hardness test indicates good mechanical<br />
strength. Hardness <strong>of</strong> tablets decreased with increase in the amount<br />
<strong>of</strong> volatile component 14 (Fig 2‐3). Friability <strong>of</strong> all the formulations<br />
less than 1%, it indicates that the tablets had good mechanical<br />
resistance. The wetting time and disintegration time values<br />
decreased with increase in the concentration <strong>of</strong> volatile component<br />
(Fig 2‐3). It may be due to their lowest hardness and the maximum<br />
porous structure was responsible for faster water uptake, hence it<br />
facilitates wicking action <strong>of</strong> crospovidone in bringing about faster<br />
disintegration 15 (Table 3). Vacuum drying techniques use to prepare<br />
highly porous compressed tablets (mentioned in Fig 1) that were<br />
rapidly soluble in saliva. Crospovidone containing tablets rapidly<br />
exhibit high capillary activity and pronounced hydration with a little<br />
tendency to gel formation 16 and thus disintegrate tablets rapidly.<br />
37
Hardness(kg/cm)<br />
5<br />
4<br />
3<br />
2<br />
1<br />
0<br />
SC1 SC2 SC3<br />
Formulation Code<br />
Fig 2: Graphical representation <strong>of</strong> hardness and disintegration whiletablets containing sudarshan churna<br />
Hardness(kg/cm)<br />
5<br />
4<br />
3<br />
2<br />
1<br />
0<br />
BLC1 BLC2 BLC3<br />
Formulation Code<br />
Fig. 3: graphical representation <strong>of</strong> hardness and disintegration while tablets containing bhaskar lavan churna.<br />
Table 3: postcompression parameters <strong>of</strong> fast dissolving tablets<br />
Formulation code Weight variation<br />
(%)<br />
(±SD), n=20<br />
Hardness<br />
(kg/cm 2) (±SD),<br />
n=6<br />
Friability<br />
(%)<br />
(±SD), n=10<br />
SC1 0.7 (2.22) 4.50 (0.00) 0.12 (0.06) 55 (0.35) 30 (0.03)<br />
SC2 0.3 (1.00) 4.25 (0.40) 0.16 (0.01) 48 (0.05) 28 (0.22)<br />
SC3 0.9 (0.92) 4.00 (0.50) 0.24 (0.04) 20 (0.18) 18 (0.25)<br />
BLC1 0.3 (0.52) 4.55 (0.19) 0.29 (0.01) 45 (0.44) 40 (0.30)<br />
BLC2 0.7 (1.50) 4.50 (0.25) 0.32 (0.06) 37 (0.40) 38 (0.40)<br />
BLC3 0.8 (2.25) 4.00 (0.70) 0.50 (0.10) 18 (0.03) 20 (0.50)<br />
Note: Values in parenthesis are standard deviation (±SD)<br />
Table 4: Weight <strong>of</strong> tablet before and after vacuum drying<br />
Formulation Before vacuum drying(mg) After vacuum drying(mg)<br />
SC1 650 638<br />
SC2 650 625<br />
SC3 650 600<br />
BLC1 650 639<br />
BLC2 650 622<br />
BLC3 650 601<br />
70<br />
60<br />
50<br />
40<br />
30<br />
20<br />
10<br />
0<br />
60<br />
50<br />
40<br />
30<br />
20<br />
10<br />
0<br />
Disintegration<br />
time(sec)<br />
(±SD), n=6<br />
Disinegration time(sec)<br />
Disinegration time(sec)<br />
Wetting time<br />
(sec)<br />
(±SD), n=3<br />
38
The prepared tablets were subjected for weighing before and after<br />
vacuum drying the weight may be slightly decreased with increase<br />
in the concentration <strong>of</strong> volatile component after vacuum drying<br />
results are shown in Table 4. Stability studies results (Table 5)<br />
revealed that the disintegration time <strong>of</strong> all the formulations were<br />
decreased (P