Preparation of disintegration tablet using Cucurbita maxima pulp powder as disintegration

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Lactose: Lactose is a carbohydrate, and as such a disaccharide. One Molecule of lactose consists of one molecule each of two other carbohydrates, i.e. galactose and glucose. These galactose and glucose moieties, as they are called, are linked together by means of what is known as a beta-(1,4) glucosidic linkage. The molecular structure of lactose is depicted below.

The official chemical name of lactose, as frequently encountered in regulatory documents such as the Pharmacopoeia is:
4-O-β-D-galactopyranosyl, D-glucopyranose.

A number of natural or partially modified polymers was screened for mucoadhesive properties by routinely measuring the force of detachment for swollen polymer films from pig intestinal mucosa in a saline medium. Suprisingly, hydroxypropyl- and carboxymethylcellulose showed almost no mucoadhesion, whereas the cationic polymer chitosan was fairly mucoadhesive in comparison to Polycarbophil as a reference substance. It is suggested that a strict difference be made between mucoadhesion of dry polymers on a wet tissue in air, and mucoadhesion of a swollen hydrogel in the presence of a third liquid phase. Cationic polymers should be further investigated with respect to possibly improved mucoadhesive properties in a neutral or slightly alkaline environment.Lactose is very stable from a chemical point of view. Except for some special cases, it has no tendency to react with the active ingredient or other components of a formulation. Some remarks on the chemical properties of lactose are useful, however
The low hygroscopicity of lactose supports its virtual chemical inertness. Most chemical reactions of lactose occur noticeably only in aqueous environments. Because lactose has no tendency to attract moisture, water in dry lactose preparations is normally not present in amounts sufficient for chemical reactions to proceed at a noticeable speed. The water of crystallisation is bound so tightly in the crystal lattice of the lactose that it is chemically inert.                    

α / β-isomer: In milk, lactose is present in two isomeric forms called α- and β-lactose. The molecular structures of α- and β-lactose differ in the orientation of a hydrogen and a hydroxyl group on carbon atom no. 1 in the glucose moiety. Both forms change into one another continuously. This phenomenon is called mutarotation. The velocity of mutarotation is determined by factors such as temperature, concentration, and pH (acidity) of the solution.
Lactose solutions seek a state of equilibrium between α and β form. At room temperature, the equilibrium results in a ratio of about 40% α-lactose and 60% β-lactose. The fact that two forms of lactose exist that differs in molecular structure has profound effects on various properties of lactose, such as its solid state properties, crystal morphology and solubility. [33-35]

 List of Materials Used

Materials

Suppliers

Polyvinyl Pyrrolidone K30

Central Drug House, New Delhi

Magnesium stearate

Central Drug House, New Delhi

Talc

Central Drug House, New Delhi

Lactose

Central Drug House, New Delhi

Sodium hydroxide

Central Drug House, New Delhi

Hydrochloric acid

Central Drug House, New Delhi

List of Equipments used

Equipment

Model, Manufacturer & Country

UV-Visible Spectrophotometer

Pharmaspec-1700, Shimadzu, Japan

FTIR- Spectrophotometer

8400s, Shimadzu, Japan

Dissolution Apparatus

Lab India Disso Test Appartus, India

Magnetic Starrier

5MLH DX, Remi, India

pH meter

SE946-P, Systronics

Electric Oven

Ambassadar® Laboratory Electric Oven, New Delhi, India

Friability Test Apparatus

Electrolab- EF-2 Friability (USP)

Hardness Tester

Model:EL=500N, Electrolab

Table: Formulations of matrix tablet: [36]

Excipient

Formulation

Batch 1

Batch 2

Batch 3

Drug

500mg

500mg

500mg

Polymer

41.2mg

82.4mg

123.6mg

Lactose

1500mg

1417.6mg

1376.4mg

Polyvinyl Pyrrolidone

50mg

50mg

50mg

Talc

10mg

10mg

10mg

PHYSIOCHEMICAL PROPERTIES:

Bulk density: Apparent bulk density (g/ml) was determined by placing pre-sieved bulk powder blend into a graduated cylinder via a large cylinder and measuring the volume and weight of powder blend.

Bulk density =weight of powder blend / volume of powder blend

Tapped density: It was determined by placing a graduated cylinder, containing a known mass of powder on mechanical tapping apparatus, which was operated for fixed number of taps (around 50). Using the weight of powder in a cylinder and its tapped volume, the tapped density was computed.

Tapped density =weight of powder blend/ tapped volume of powder blend

Carr’s index: It is an important parameter to study compressibility behavior of powder blend. Carr’s index was calculated, from the results of bulk density and tapped density.

Carr’s index = (bulk density-tapped density)/ tapped density

Bulkiness: It is reciprocal of bulk density, and calculated as follows-

Bulkiness= 1/bulk density

Angle of repose: For the measurement of angle of repose, a glass funnel was taken with its tip at a given height (H), above a piece of graph paper placed on a horizontal surface. Powder was poured through the funnel until the apex of the conical pile touched the tip of the funnel. The angle of repose was calculated with the formula; tan θ= H/R, where θ is the angle of repose and R is the radius of the conical pile.

Swelling index: The swelling index is defined as the volume (in milliliters) taken up by the swelling of 1 g of powder material under specified conditions. 1 gm of the pulp powder was introduced into a 25 ml glass-stoppered measuring cylinder. Twenty five milliliters of water was added and mixture was shaken thoroughly for 10 min. It was then allowed to stand for 24 h at room temperature. Then the volume occupied by the pulp powder was noted.

 Weight variation: All prepared matrix tablets were evaluated for weight variation as per USP XXIV monograph. Twenty tablets of each batch were used to evaluate weight variation among tablets and standarddeviation was calculated.

 Friability: Tablets of all batches were used to evaluate friability as per USP XXIV monograph. Friability testing was done by Roche friabilator with triplicate readings.

Hardness: Hardness of all batches was determined using Digital Force Gauge (Model:EL=500, Electrolab). The test was carried out in triplicate for all batches as per USP XXIV monograph for uncoated tablets.

 Thickness: Thickness was measured by vernier caliper as per USP XXIV monograph. The readings were carried out in triplicate and average value was noted.

Drug content: The tablets were powdered, and 50 mg equivalent weight of Diclofenac Sodium in tablet powder was accurately weighted and transferred into a 100 ml volumetric flask. Initially, 10 ml of phosphate buffer (pH6.6) was added and shaken for 10 min. then, the volume was made up to 100 ml with buffer. Subsequently, the solution in volumetric flask was filtered and 1 ml of the filtrate was diluted and analyzed at 276 nm using ultraviolet/visible variable wavelength spectrophotometer at 276 nm (Shimadzu UV-2450, Japan). The drug content of the each sample was estimated from their standard curve.

In vitro dissolution study: Dissolution test was performed at 37°C using the paddle method at 100 rpm with    900phosphatebuffer (pH6.6) as a dissolutionIndia Disso 2000, India) was used. At predetermined intervals, 5 ml of the medium was sampled and filtered. The filtrate was analyzed by ultraviolet/visible variable wavelength spectrophotometer at 276 nm.

 Charcterization parameters of cucurbita maxima pulp powder

Beta vulgarispulp powder was characterized as a pharmaceutical excipient in terms of micromeritic properties and flow behavior. Bulk density, tapped density, bulkiness and angle of repose all are found to be good to use this plant based material as a pharmaceutical excipient. Bulk density, tapped density, cars index, hausner’s ratio porosity  and flow behavior (angle of repose) were found to be  0.51to.052,  0.52 to 0.053 ,0.84 to 0.045, 1.05 to 0.076,0.052 t0 0.02, 38.65 to 0.089 respectively .his pulp powder can be act as a good candidate for pharmaceutical preparations . Relative study of physical parameters of tablets of each batch of Beta vulgaris pulp powder reveals that the tablets compressed using pulp powder as disintegrant are quite harder, so can be easily handled. The variation in the hardness, weight variation, friability and thickness values of all the fabricated tablets were found to be 21.8 to 0.06, 211 to 0.03,0.62 to 0.82%,2.46 to 0.06 respectively in reference to average values for each parameter, were found within the official limits. Friability of tablets ranged from 0.62 to 0.82%, easily predict the fact that tablets were less friable and so provide ease of handling. Less weight variation and uniform drug content easily elicit the fact that this process of tablet formulation is reproducible and so easily adopted at industrial level. Findings of the results showed that as the concentration of pulp powder increases wetting time of tablets decreases in same proportion and so disintegrating time also go down in same manner.

Bulk density

(mg/ml)

 

Tapped density

(mg/ml)

 

Carr’s

Index

Hausner’s ratio

Porosity

Bulkiness

(ml/mg)

 

Angle of repose (º)

0.51

±0.052

0.52

±0.053

0.84

±0.045

1.05

±0.076

0.52

±0.02

1.99

±0.08

38.65

±0.089

Evaluation parameters of tablet containing Diclofenac sodium as a model

Evaluation

Batch1

Batch2

Batch3

Hardness(kg/cm^2)

21.8

±0.065

20.6

±0.088

20.1

±0.067

Friability (%)

0.67

±0.065

0.59

±0.054

0.68

±0.044

Thickness (mm)

1.65

±0.078

2.16

±0.065

2.460

±0.054

Diameter (mm)

9.24

±0.065

9.52

±0.023

9.51

±0.045

Disintegration (min)

10.2

±0.023

7.0

±0.021

6.0

±0.019

Weight Variation (mg)

211

± 0.067

210

± 0.059

208

±0.054

CONCLUSION
The comparative study of various parameters clearly states the fact that the naturally obtained Beta vulgaris pulp powder stands as a good candidate to act as disintegrant and it is possible to design promising Fast disintegrating tablet using this polymer. On the basis of results obtained it can be concluded that this polymer having good micromeritic properties and flow behavior and so may act as a pharmaceutical excipient.

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