Gliclazide Abelmoschus Esculentus Fruit Mucilage Prolonged Release Tablets Biology Essay

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The present study was aimed to develop matrix tablets of Gliclazide with Abelmoschus esculentus fruit mucilage and to study its functionality as a matrix forming agent for prolonged release tablet formulations. The dried powdered mucilage of Abelmoschus esculentus mucilage was studied for physicochemical parameters. Various formulations of Gliclazide Abelmoschus esculentus mucilage were prepared. All the formulations passed the evaluation parameters as per official and pharmacopoeial limits with low standard deviation values. The swelling behavior and release rate characteristics of formulated matrix tablets were studied. The dissolution study proved that the dried Abelmoschus esculentus fruit mucilage can be used as a matrix forming material for making prolonged release matrix tablets.

Key words: Gliclazide, Abelmoschus esculentus, matrix tablets, prolonged release.

INTRODUCTION:

Abelmoschus esculentus, (Malvaceae family) is an annual or perennial climber, growing up to 2 m tall. The fruit is a capsule up to 18 cm long1. Gliclazide is an oral hypoglycemic agent, which is a commonly prescribed drug for the treatment of patients with type II diabetes mellitus. It belongs to sulfonyl ureas drug class. Gliclazide is a weak acid (pKa = 5.98) practically insoluble in water and acidic environment but highly permeable (class 2) according to the Biopharmaceutical classification System (BCS)2. The oral absorption is uniform, rapid and complete with nearly 100% bioavailability. The usual dose of Gliclazide is 80-320 mg daily3. The pharmacokinetics and dosage schedule supports once daily prolonged release formulations for Gliclazide for better control of blood glucose levels to prevent hypoglycemia, enhance clinical efficacy and patient compliance4. The objective of present investigation is to design and evaluate prolonged release tablets of Gliclazide using Abelmoschus esculentus fruit mucilage as release retardant for making prolonged release matrix tablets.

MATERIALS AND METHODS:

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Gliclazide was obtained as a gift sample from Dr. Reddy's Laboratories, Hyderabad, India. Abelmoschus esculentus fruits were collected from plants growing in local areas of Anantapur, India. The plant was authenticated at the Botany Department of Sri Krishnadevaraya University, Anantapur, India. Ethanol (95%), Acetone, Tri chloro acetic acid, sodium hydroxide, diethyl ether, Micro crystalline cellulose (Avicel) and Magnesium stearate were procured from SD Fine chemicals (Mumbai, India). All other chemicals used were of analytical reagent grade and double distilled water was used throughout the experiments.

Extraction of mucilage5

The fresh Abelmoschus esculentus fruits were collected and washed with water. Incisions were made on the fruits, left over night. The fruits were crushed and soaked in water for 5-6 hours, boiled for 30 minutes and left to stand for 1 hour to allow complete release of the mucilage into the water. The mucilage was extracted using a multi-layer muslin cloth bag to remove the marc from the solution. Acetone (three times the volume of filtrate) was added to precipitate the mucilage. The mucilage was separated, dried in an oven at 40°C, collected, ground, passed through a # 80 sieve and stored in desiccator at 30°C & 45% relative humidity till use. The collected mucilage was tested for flow properties which were shown in Table 1. All values were found to be satisfactory.

Physical characterization of Abelmoschus esculentus fruit mucilage5

Fresh Abelmoschus esculentus fruits were procured from the local market, Anantapur, India and authenticated by the Botany department, Sri Krishnadevaraya University, Anantapur, India. The seeds do not contain any mucilage and were removed prior to extraction. The fruits were sliced, homogenized with five times its weight of water, centrifuged at 4000 rpm for 15 min and the mucilage was precipitated with three volumes of ethanol and washed with excess of ethanol followed by acetone. The mucilage so obtained was dried under vacuum (˂ 1Torr at 25°C for 12 hours).

Purification of the Mucilage5

The crude mucilage was homogenized (Potter homogenizer) with cold dilute trichloro acetic acid solution (5%). The solution was centrifuged (3500 rpm for 20 min), neutralized with sodium hydroxide by drop wise addition and then dialyzed for 30 hours against distilled water. The mucilage was precipitated with ethanol (in the quantities of three times the volumes) and washed successively with ethanol, acetone and diethyl ether.

Characterization of Mucilage 5-8

The collected mucilage was evaluated for physicochemical characteristics viz., morphological characteristics, identification by chemical tests, Solubility, melting range, pH, Swelling index, Ash values, presence of foreign organic matter, test for lead and arsenic, Loss on drying, Density, compressibility index and angle of repose etc. (Table 1) The evaluation was carried out as per procedures describe in official books.

Preparation of Prolonged release matrix tablets

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Prolonged release matrix tablets of Gliclazide with Abelmoschus esculentus fruit mucilage were prepared by using different drug: mucilage ratios. Abelmoschus esculentus fruit mucilage was used as matrix forming material while microcrystalline cellulose as a diluent and Magnesium stearate as a lubricant. All ingredients used were passed through a # 100 sieve, weighed and blended. The granules were prepared by wet granulation technique and compressed by using 10 mm flat faced punches. The compositions of formulations were showed in Table 2. These matrix tablets were evaluated for their physical properties as per I.P methods which were shown in Table 3.

Swelling behavior of prolonged release matrix tablets

The extent of swelling was measured in terms of % weight gain by the tablet. The swelling behavior of formulation GMA-1, GMA-2, GMA-3, GMA-4 and GMA-5 were studied. One tablet from each formulation was kept in a Petri dish containing phosphate buffer of pH 7.4. At the end of 2 hours, the tablet was withdrawn, kept on tissue paper and weighed then for every 2 hours, till the end of 12 hours. The % weight gain by the tablet was calculated by formula9.

S.I = {(Mt-M0) / M0} X 100

Where, S.I = Swelling Index, Mt = Weight of tablet at time't' and

Mo = Weight of tablet at time 0. Swelling behavior of prolonged release matrix tablets were represented in Fig. 4.

In vitro drug release studies 10

Release of Gliclazide from the matrix tablets was studied in phosphate buffer of pH 7.4 (900 ml) using United States Pharmacopoeia (USP) 8-station Dissolution Rate Test Apparatus (Model Electro lab, TDT- 06T, Mumbai, India) with a rotating paddle stirrer at 50 rpm and 37° ± 0.5°C. A sample of Gliclazide matrix tablets equivalent to 10 mg of Gliclazide was used in each test. Samples of dissolution fluid were withdrawn through a filter (0.45 μm) at different time intervals and were assayed at 229 nm for Gliclazide content using a UV/ visible single-beam spectrophotometer-117 (Systronics Corporation, Mumbai, India)10. The drug release experiments were conducted in triplicate (n = 3). The in- vitro release rates were showed in Fig. 5.

RESULTS AND DISCUSSION:

Infrared Spectrum of Gliclazide Pure drug, Infrared Spectrum of Abelmoschus esculentus fruit mucilage, Infrared Spectrum of Gliclazide with Abelmoschus esculentus fruit mucilage, shows the formation of matrix material without any negative interactions which were represented in Fig. 1, 2 and 3 respectively.

The Abelmoschus esculentus fruit mucilage was yellow in colour, soluble in water and forms hage viscous solution. The % yield was 23 ±2.173 g /kg with average particle size of 165.15±10.265µm and the weight loss on drying was found to be 4.20±2.573. The Swelling ratio was found to be 45±3.841, pH was found to be 7.0±0.56 and the Charring was found to be 220±4.520 C. The density of 0.5% w/v liquid was found to be 0.997±0.055 and microbial count of bacteria was 5cfu/g and Fungi were 2 cfu/g. The Angle of repose of Abelmoschus esculentus fruit mucilage were found to be 27.96±1.6840, Loose Bulk density was found to be 0.604±0.018 g/cm3, Tapped bulk density was found to be 0.866±0.021 g/cm3, Compressibility Index was found to be 0.302±0.023%, Hausner's ratio was found to be 1.434±0.047. All the above were conducted in 5 trials. The thickness of formulated tablets was uniform and ranged from 5.8±0.41 to 6.2±0.15, the hardness of formulated tablets were more than 5 kg/cm2 indicating good mechanical strength and the loss on friability was less than 1% which indicates the formulated tablets can withstand the physical stress while transportation.

In-vitro drug release profile of Gliclazide from formulated matrix tablets were studied using zero order, first order, Higuchi, Korsmeyer Peppa's and Hixson-Crowell's Models which were shown in Fig. 5, 6, 7, 8 and 9 respectively. The rate of release was faster in GMA-1 and slower in GMA-5. The kinetic plots were perfectly fitting to the formulated Abelmoschus esculentus fruit mucilage- Gliclazide matrix tablets. This result shown that as the proportion of Abelmoschus esculentus fruit mucilage increased, the overall time of release of the drug from the matrix tablet was also increased. Drug releases from matrix tablets were by drug dissolution, drug diffusion or a combination of both.

CONCLUSION:

The present study revealed that Abelmoschus esculentus fruit mucilage appears to be suitable for use as a release retardant in the manufacture of prolonged release matrix tablets because of its good swelling, good flow and suitability for matrix formulations. From the dissolution study, it was concluded that dried Abelmoschus esculentus mucilage can be used as an excipient for making prolonged release matrix tablets.

ACKNOWLEDGEMENT:

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The authors are thankful to Dr. Reddy's Laboratories, Hyderabad, India for providing the pure drug sample.

Table 1: Physicochemical characterization of Abelmoschus esculentus fruit mucilage

Properties

Abelmoschus esculentus

fruit mucilage

Description

yellow powder

Solubility

Slowly soluble in water

produces hage viscous solution

% yield (g /kg)

23 ±2.173

Ave. particle size

165.15±10.265

Wt. loss on drying

4.20±2.573

Swelling ratio

45±3.841

pH

7.0±0.56

Charring (0C)

220±4.52

Density of liquid (0.5% w/v)

0.997±0.055

Microbial count (cfu/g)

Bacteria:5 ; Fungi: 2

Angle of repose (q°)

27.96±1.684

Loose Bulk density (g/cm3)

0.604±0.018

Tapped bulk density(g/cm3)

0.866±0.021

Carr's Index

0.302±0.023

Hausner's ratio

1.434±0.047

Number of trials (n)=5

Table 2: Formulae of Abelmoschus esculentus fruit mucilage -Gliclazide matrix tablets

Ingredients

(mg)

Formulations

GMA-1

GMA-2

GMA-3

GMA-4

GMA-5

Gliclazide

160

160

160

160

160

Abelmoschus esculentus dried mucilage

5

10

15

20

25

Micro crystalline cellulose (Avicel)

80

75

70

65

60

Magnesium stearate

5

5

5

5

5

Total weight of tablet

250

250

250

250

250

Table 3: Physical properties of Abelmoschus esculentus fruit mucilage Gliclazide matrix tablets

Formulation

Thickness

(mm)

Hardness

(kg/cm2)

Friability

(%)

Drug content

(%)

GMA-1

5.9±0.21

7.70±1.25

0.80±0.02

101.2±7.08

GMA-2

6.2±0.15

8.10±1.40

0.75±0.05

100.6±6.30

GMA-3

5.8±0.41

6.90±1.35

0.46±0.03

99.8±1.80

GMA-4

6.0±0.39

6.80±1.45

0.62±0.06

99.6±2.50

GMA-5

6.1±0.58

7.20±1.30

0.72±0.07

100.8±4.45

Fig. 1: Infrared Spectrum of Gliclazide Pure drug

Fig. 2: Infrared Spectrum of Abelmoschus esculentus fruit mucilage

Fig. 3: Infrared Spectrum of formulation (GMA-5)blend

Fig. 4: Swelling Index of formulated matrix tablets

Fig. 5: Zero order release Plots formulated matrix tablets

Fig. 6: First order release Plots formulated matrix tablets

Fig. 7: Higuchi Plots formulated matrix tablets

Fig. 8: Korsmeyer Peppa's Plots formulated matrix tablets

Fig. 9: Hixson-Crowell Plots formulated matrix tablets