Design, Formulation and Evaluation of Fexofenadine HCl Immediate Release Tablets by Solid Dispersion Method using Solvent Evaporation Technique

 

Ayanam Vasanthi1*, Ayanam Vasavi1, Miriyala Mrunalini1 G. Raveendra Babu2, M. Sowjanya3

1Department of Pharmaceutics, A.K.R.G. College of Pharmacy, Nallajerla, W.G. Dist., Andhra Pradesh.

2Department of Pharmaceutical Analysis, A.K.R.G. College of Pharmacy,

Nallajerla, W.G. Dist., Andhra Pradesh.

3Department of Chemistry, Vijaya Teja Degree College, Addanki, Andhra Pradesh.

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

 

ABSTRACT:

Currently, this study focuses on developing immediate-release Fexofenadine hydrochloride tablets. The Fexofenadine HCl tablets have super disintegrants that help to accelerate dissolution and bioavailability. Sodium lauryl sulphate, microcrystalline cellulose as filler, crospovidone, and sodium starch glycolate were used to make the tablets using a direct compression method (2-8 percent). Pre and post compressional parameters were used in the preparation of the tablets. The In-vitro disintegration study shows that as concentration of sodium starch glycolate is increased, there is an increase in the amount of time it takes for the solution to disintegrate, but at the same time, there is a decrease in the amount of time it takes for the solution to disintegrate when the crospovidone level is increased. When combined with the crospovidone tablet formulation, the test found that the resulting tablets broke down in approximately 3 to 6 minutes, with enough force to release the fragments but not to harm the friability of the product. It was found that Fexofenadine hydrochloride tablet, a fast-acting form of treatment for allergic rhinitis, could be formulated in an immediate-release form.

 

KEYWORDS: Allergic rhinitis, Crospovidone, Croscarmellose sodium.

 

 


INTRODUCTION:

This huge investment has occurred in academia and industry over the last 15 to 20 years in developing more effective drug delivery systems that target drugs to their therapeutic location. The vast majority of this work has succeeded and is described in this text. While tablets and hard gelatin capsules have been in use since the 1800s, oral solid dosage forms, such as tablets and hard gelatin capsules, are still the most commonly used dosage forms.

 

This has more to do with the widespread use of established products in the market than with the launch of new products like tablets and capsules.

 

It can be attributed to the many advantages of the solid oral dosage form. The most noninvasive method of delivering drugs is by the oral route. It offers many advantages for the manufacturer: it utilises inexpensive technology, is generally the most stable form of medication, is compact, and has the ability to be customised to further increase brand recognition. A tablet and cap sleeve can be used on many products. This chapter is not going to cover all dosage forms, but instead will summarise the basics and offer more detailed information for the dosage forms most commonly used. In order to meet the criterion of having good oral bioavailability and not causing any side effects in the GI tract, there is very little need to develop a delivery system for these types of drugs. Because it is likely, it is likely that tablets and capsules will remain a popular delivery method for future medications. This chapter is about tablets and hard gelatin capsules, particularly the underlying science. One of the most widely applied dosage forms is the solid1.

 

Immediate Release Dosage Form2,3:

A faster release dosage form allows the manufacturer to extend the exclusivity of the product in the market, while also making the dosage form or dosage regimen easier for patients to use. Now that immediate-release tablets have started to gain popularity, primarily because they are simple to administer, have rapid onset of action, and are economical, patients are becoming more compliant with their prescriptions. They also help to extend product life cycles, develop new markets, and give rise to new opportunities. When using excipients, excipient developers commonly use super disintegrants because they are highly effective at quick disintegration, release, and absorption of the drug when it is given to the body4-9.

 

MATERIALS AND METHOD:

Glenmark Generics Limited (Gujarat) provided Fexofenadine hydrochloride, which is an antihistamine drug. Sodium Lauryl Sulphate (an amphoteric agent), Microcrystalline cellulose, Croscarmellose sodium, Crosspovidone, and Sodium Saccharine were also acquired from Research-Lab Fine Chemicals and Industry (Mumbai).

 

METHODOLOGY:

Preparation of Buffers and Reagents 0.1N HCL Solution:

In a 1000ml volumetric flask, dissolve 8.5ml of concentrated HCL in distilled water and top up to the mark with distilled water.

 

Phosphate buffer solution (pH 6.8):

In a 200ml volumetric flask, 50ml of 0.2M potassium dihydrogen ortho phosphate was added to 22.4ml of 0.2 M sodium hydroxide, and the volume was made up to the mark with distilled water.

 

Scanning of λmax of Fexofenadine HCL:

Stock solution preparation: A 10ml volumetric flask was used with 10mg of fexofenadine HCL. In order to dissolve the medication 2 ml of methanol were added and well stirred. The solution was developed with a mark of 0.1N HCL for a concentration of 1000μg/ml.

 

Take 1ml from the above solution and add a concentration of 100μg/ml at a concentration of 10ml with 0.1 N HCL. The solution was prepared, i.e., the UV/Visible spectrophotometer for a concentration of 100 μg/mm for μmax of 200 - 400nm.

 

Calibration curve of Fexofenadine HCl in 0.1N HCl

Stock solution preparation:

A 10ml volumetric flask of Fexofenadine HCL was taken. To The solution with 0.1N HCL was designed with a concentration of 1000μg/ml. The above-mentioned solution consists of diluting to 10ml with 0,1 N HCL 1ml, 2ml, 3ml, 4ml, 5ml and 6ml, giving concentration of 100, 200, 300, 400, 500 and μg/ml.

 

At μmax i.e. 267nms of Fexofenadine HCL, the absorption of each test solution was measured in UV/Visible blank spectroscopy.

 

Prepare solid Fexofenadine HCl dispersions:

Several carriers are reported to use β Cyclodextrin, HP β Cyclodextrin using a solvent evaporation method to prepare solid dispersions.

 

a. Solvent evaporation method:

The medicines and transporters were mixed in 1:0.25 and 1:0.5 ratios in methanol using the solvent evaporation method. Evaporation under decreased pressure removed the solvent. The weight was pulverised by the screen #100. And now the product obtained has been collected and stored in dryers.

 

Evaluation of Solid Dispersions10-30:

Estimation of Drug Content:

A quantity equal to 10mg of drug was precisely weighed to a 100ml volumetric bottle. The volume was then buffered by 0.1 N HCL and shaken or 10 min, to make the drug totally soluble. Then it filtered the solution. Dissolving 10mg of standard drug in the buffer of 0.1 N HCL produced the same concentration of standard solution. The absorption at 267nm for Fexofenadine HCL was measured in UV-Visible spectrophotometer for the sample and standard solutions both.

 

Entrapment efficacy:

Before the study of the conduct of this trapped drug in physical and biological systems, the capture efficiency of the solid disperses was an important characteristic to evaluate the amount of the substance trapped in solid dispersions since the experimental effects are usually related to doses. Solid drug formulation can be developed only if a reasonable quantity of the drug can be provided for the encapsulation efficiency of therapeutic doses since lipids can be toxic and lead to non-linear pharmacokinetics of the formulation in higher doses. An optimised loading procedure would achieve 90 percent and more trapping efficiencies. This eliminates the need to remove the untraped material, since free medicine can usually be tolerated with loading doses of 10 percent or less. Procedures like dialysis, and the removal of uncaught material through the exclusion column often take time, are tedious, expensive and uncaught material usually difficult to recover. The effectiveness of the entrapment was calculated using the formula following:

 

%Entrapment efficiency = Drug content *100/Drug added in each formulation.

 

In vitro dissolution study:

The solid dispersions prepared were dissolved in vitro. The USP type 2 paddle test [apparatus 2] was performed. The rate of revolving was 50rpm, 0.1 N HCL tampon was used to maintain dissolution and dissolution medium at 37±1°C. 5ml samples were removed at regular time intervals, filtered and replaced by 5ml of fresh dissolution medium, diluted where needed and tested using a UV-visible spectrometer for Fexofenadine HCL of 267nm.

 

Kinetics of Drug Release:

A zero order and first order determination of the drug release mechanism for the solid dispersions of the Fexofenadine HCL. In the following modes of data processing the results of the In-vitro release profile obtained for all formulations were presented:

 

Zero Order Kinetic:

It describes the system in which the drug release rate is independent of its concentration.

 

Qt = Qo + Ko t

 

Where,

Qt= Amount of drug dissolved in time t

Qo = Initial amount of drug in the solution, which is often zero Ko = zero order release constant.

If the zero order drug release kinetic is obeyed, then a plot of Qt versus t will give a straight line with a slope of Ko and an intercept at zero.

 

First Order Kinetic:

It describes the drug release from the systems in which the release rate is concentration dependent.

 

Log Qt = log Qo + kt/ 2.303

Where,

Qt = amount of drug released in time t.

Qo = initial amount of drug in the solution k = first order release constant If the first order drug release kinetic is obeyed, then a plot of log (Qo- Qt) versus t will be straight line with a slope of kt/ 2.303 and an intercept at t=0 of log Qo.

 

Formulation of Fexofenadine Hcl Tablets:

Fexofenadine HCL was added to its equivalent weight with the suitable excipients and the tablets were formulated with the formulae specified in the table as direct compression. Every ingredient was separately transmitted to #60 mesh sieve. By adding a small portion of each drug and mixing it to obtain a single combination, the medicine and mannitol were mixed together. Then, geometrically, the other ingredients were mixed and coarse (#44 mesh) sieve passed, and the tablets were compressed with hydraulic presses. The machine was adjusted to compress strength for all batches in the range of 3-4 kg/cm2. For all F1 to F9 formulations, the weight of the tablets was consistent (210mg).

 

Table 1: Formulation of ORD tablets by using super disintegrants

Ingredients

F1

F2

F3

F4

F5

F6

Solid Dispersion

SF4 (equivalent to 60 mg drug)

 

90

 

90

 

90

 

90

 

90

 

90

Lycoat (mg)

3

5

7

-

-

-

SSG (mg)

-

-

-

3

5

7

Aspartame(mg)

60

60

60

60

60

60

Lactose(mg)

Q.S.

Q.S.

Q.S.

Q.S.

Q.S.

Q.S.

Magnesium Stearate (%)

3

3

3

3

3

3

Talc (%)

3

3

3

3

3

3

Total (mg)

200

200

200

200

200

200

 

Method preparation of mixed blend of drug and excipients:

They all passed through 780 no. All materials. For each specified formulation (Table) the required quantity of each ingredient has been taken and all the ingredients have been grinded to the required fineness level (except magnesium stearate and talc). The flow properties of the powdered blend were assessed below.

 

Angle of repose:

The angle of repose can be used to calculate the frictional force in a loose powder. It is defined as the greatest possible angle between the surface of the powder pile and the horizontal plane. When more powder is added to the pile, it slides down the sides until the mutual friction of the particles, which produces a surface angle, equals the gravitational force. The angle of repose was measured using the fixed funnel method. A funnel was secured with its tip at a specific height (h) above graph paper placed on a flat horizontal surface. The mixture was carefully poured through the funnel until the apex of the conical pile was just touching the funnel's tip. The radius (r) of the conical pile's base was measured. The following formula was used to calculate the angle of repose:

 

Tan is equal to h/r.

Tan = Repose Angle

H    = the cone's height,

r        denotes the radius of the cone's base.

 

Bulk density:

Weight per unit volume is the definition of density. Bulk density is defined as the mass of the powder divided by the bulk volume and is expressed in grammes per cubic centimetre (gm/cm3). The bulk density of a powder is determined primarily by particle size distribution, particle shape, and particle adhesion. Bulk density is critical in determining the size of containers required for raw material and blend handling, shipping, and storage. It's also important in size blending machines. Without compacting, a 10gm powder blend was sieved and introduced into a dry 20ml cylinder. The powder was levelled carefully without compacting, and the unsettled apartment volume, Vo, was read.

 

The following formula was used to calculate the bulk density:

M/Vo = Bulk Density

Where,

M denotes sample weight.

Vo denotes the apparent volume of powder.

 

Tapped Density:

Following the bulk density measurement procedure, the cylinder containing the sample was tapped using a suitable mechanical tapped density tester capable of 100 drops per minute, and this was repeated until the difference between succeeding measurements was less than 2%, and then tapped volume, V Measured, to the nearest graduated unit. The tapped density was calculated in grammes per litre using the following formula:

 

M/V = Tap

Where Tap denotes the density of taps.

M denotes the sample's weight.

V=Powder-tapped volume

 

Powder compressibility is measured in the following ways:

The compressibility index (Carr's index) is a measure of a powder's proclivity to be compressed. It is calculated using the bulk and tapped densities. The less compressible a material is, in theory, the more flowable it is. As such, it quantifies the relative importance of inter-particulate interactions. Such interactions are generally less significant in a free-flowing powder, and the bulk tapped densities will be closer in value.

 

Poorer flowing materials frequently have greater inter particle interactions, resulting in a larger difference between bulk and tapped densities. The compressibility index, which is calculated using the following formulas, reflects these differences:

 

Carr's index = [(tap-b/tap)100]

Where,

B stands for bulk density.

Tapped density = tap

 

Floating tablet formulation development:

Granules were prepared using the direct compression method 10-15 to optimise sodium bicarbonate concentration.

 

The following is the procedure for using the direct compression method:

1.   All of the ingredients, including the drug, were individually passed through sieve no. 60.

2.   All of the ingredients were thoroughly mixed by triturating for up to 15 minutes.

3.   Talc was used to lubricate the powder mixture.

4.   The tablets were made using the direct compression method and a 6mm punch.

 

Evaluation of Tablets:

Post compression parameters Weight variation test:

The weight variation test is carried out in order to ensure uniformity in the weight of tablets in a batch. First the total weight of 20 tablets from each formulation is determined and the average is calculated. The individual weight of the each tablet is also determined to find out the weight variation.

 

Tablet hardness:

The hardness of tablet is an indication of its strength. It is the force required to break a tablet by compression in the radial direction. The force is measured in kg and the hardness of about 3-5kg/cm2 is considered to be satisfactory for uncoated tablets. Hardness of 10 tablets from each formulation is determined by Monsanto hardness tester, Pfizer hardness tester etc. Excessive hardness significantly reduces the disintegration time.

 

Tablet friability:

Friability is the loss of weight of tablet in the container due to removal of fine particles from the surface. Friability test is carried out to access the ability of the tablet to withstand abrasion in packaging, handling and transport. Roche friabilator is employed for finding the friability of the tablets. Weigh the 20 tablets from each batch and place in Roche friabilator that will rotate at 25 rpm for 4 minutes. All the tablets are dedusted and weighed again. The percentage of friability can be calculated using the formula.

 

% Friability = [(W1-W2)100]/W1

 

Where,

W1= Weight of tablet before test,

W2 = Weight of tablet after test

The pharmacopoeia limit of friability test for a tablet is not more than 1%. This test is not applicable for lyophilized and flash dose tablets, but is done for tablets prepared by direct compression and moulding. It is a difficult to achieve friability within this limit for MDT and to keep hardness to the lowest to achieve a minimum possible disintegration time.

 

In-vitro Disintegration time:

Tablet disintegration is an important step in drug absorption. The test for disintegration was carried out in Electrolab USP disintegration test apparatus. It consists of 6 glass tubes which are 3 inches long, open at the top, and held against a 10 mesh screen, at the bottom end of the basket rack assembly. To test the disintegration time of tablets, one tablet was placed in each tube and the basket rack was positioned in a 1 liter beaker containing pH 0.1N HCL buffer solution at 37°C ± 1°C such that the tablet remains 2.5 cm below the surface of the liquid. The time taken for the complete disintegration of the tablets was noted.

 

Thickness and Diameter:

Tablet thickness and diameter can be measured using a simple procedure. Five tablets are taken and their thickness is measured using Vernier calipers. The thickness and diameter is measured by placing tablet between two arms of the Vernier calipers.

 

Drug content uniformity:

The tablets were tested for their drug content uniformity. At random 20 tablets were weighed and powdered. The powder equivalent to 25 mg was weighed accurately and dissolved in 100ml of 0.1N HCL. The solution was shaken thoroughly. The undissolved matter was removed by filtration through Whatmann No.41 filter paper. Then the dilute the solution to obtain 10µg solution. The absorbance of the diluted solutions was measured at 267nm.

 

Dissolution studies In-vitro dissolution study is performed by using USP Type II Apparatus (Paddle type) at 50 rpm. 0.1N HCL buffer 900ml is used as dissolution medium which is maintained at 37±0.5°C. Aliquots of dissolution medium (10ml) are withdrawn at specific time intervals and filter. An equal amount of fresh dissolution medium is replaced immediately following withdrawal of test sample. The percentage of drug released at various intervals is calculated using beer-lamberts law.

 

Kinetics of Drug Release:

The mechanism of drug release for the Fexofenadine HCL solid dispersions was determined using zero order and first order.

 

The results of in vitro release profile obtained for all the formulations were plotted in modes of data treatment as follows:

 

Zero Order Kinetic:

It describes the system in which the drug release rate is independent of its concentration.

 

Qt = Qo + Ko t

Where,

Qt= Amount of drug dissolved in time t

Qo = Initial amount of drug in the solution, which is often zero and

Ko = zero order release constant.

If the zero order drug release kinetic is obeyed, then a plot of Qt versus t will give a straight line with a slope of Ko and an intercept at zero.

 

First Order Kinetic:

It describes the drug release from the systems in which the release rate is concentration dependent.

 

Log Qt = log Qo + kt/ 2.303

Where,

Qt = amount of drug released in time t.

Qo = initial amount of drug in the solution k = first order release constant If the first order drug release kinetic is obeyed, then a plot of log (Qo- Qt) versus t will be straight line with a slope of kt/ 2.303 and an intercept at t=0 of log Qo.

 

RESULTS AND DISCUSSION:

Determination of melting point:

The melting point of Fexofenadine HCL was found to be 193-196° C which was determined by capillary method.

 

Solubility:

Solubility of Fexofenadine HCL was carried out at 250C using 0.1 N HCL, 6.8 phosphate buffer, and purified water.

 

Analytical method development by U.V. Spectroscopy:

 

Fig 1: UV Scan Spectrum of Fexofenadine HCL

Table 2: Calibration curve data of Fexofenadine HCL

Concentration(µg/ml)

Absorbance

0

0

100

0.131 ± 0.025

200

0.236 ± 0.025

300

0.342 ± 0.025

400

0.456 ± 0.025

500

0.575 ± 0.025

600

0.674 ± 0.025

 

 

Fig 2: Calibration curve of Fexofenadine HCl

 

Drug excipient compatibility:

Drug and excipient compatibility was confirmed by comparing spectra of FT-IR analysis of pure drug with that of various excipients used in the formulation.

 

 

Fig3: IR spectrum of pure Fexofenadine HCL

 

 

Fig4: IR spectrum of Fexofenadine HCl Optimised Formulation

Form the drug excipient compatibility studies we observe that there are no interactions between the pure drug (Fexofenadine HCL) and optimized formulation (Fexofenadine HCL: excipients) which indicates there are no physical changes.

 

Drug content uniformity for solid dispersions:

Table 3: Drug content uniformity for solid dispersions by solvent evaporation method.

Form.code

%drug content

SF1

69.64 ± 0.09

SF2

76.21± 0.12

SF3

85.82± 0.05

SF4

89.76± 0.21

Percentage drug content values of all the formulation (SF1-SF4) were in the range of 69.64-89.72.

 

Entrapment efficiency of solid dispersions by solvent evaporation method:

Table 4: Entrapment efficiency of solid dispersions by solvent evaporation method

Form.code

Entrapment efficiency

SF1

73.21±0.05

SF2

78.52±0.03

SF3

88.75±0.11

SF4

96.75±0.09

The entrapment efficacy of the formulated solid dispersions was found to be in the range of 73.21- 96.75%respectively.

 

In vitro Drug Release Studies of Solid Dispersions:

Solvent Evaporation Method:

Table 5: Invitro drug release studies for formulations (SF1-SF4)

S. No

Time

(Min)

Percentage drug release

1:0.25 (SF1)

1:0.5(SF2)

1:0.25(SF3)

1:0.5 (SF4)

0

0

0

0

0

0

1

15

32.78

35.12

37.26

42.86

2

30

39.92

39.98

41.22

56.85

3

45

47.36

49.82

52.82

63.28

4

60

56.28

58.22

61.21

72.48

5

75

64.86

74.86

78.36

80.21

6

90

74.16

78.21

81.16

88.96

 

Invitro drug release of Fexofenadine HCL solid dispersions with H P β Cyclodextrin and β Cyclodextrin in various ratios were observed which shows at the end of 90 mins the formulation SF1 releases 74.16, formulation SF2 releases 78.21, formulation SF3 releases 81.16, formulation SF4 releases 88.96%.

 



Fig 5: In vitro drug release profile for drug: H P β Cyclodextrin (SF1-SF2) and β Cyclodextrin (SF3-SF4)


 

Evaluation of tablets:

 


Table 6: Pre Compression parameters

Formulation

Derived properties

Flow properties

Bulk density (mean±SD)

Tapped density

(mean±SD)

Angle of repose

(mean±SD)

Carr’s index

(mean±SD)

Hausner’s ratio

(mean±SD)

F1

0.48±0.01

0.56±0.015

26.38±0.30

14.28±1.02

1.16±0.06

F2

0.46±0.01

0.52±0.02

27.42±0.39

11.53±1.26

1.13±0.03

F3

0.42±0.04

0.48±0.01

24.02±0.68

12.58±2.08

1.14±0.05

F4

0.46±0.02

0.54±0.015

26.26±0.96

14.81±1.28

1.12±0.02

F5

0.52±0.6

0.60±0.03

30.68±0.73

13.33±1.86

1.17±0.04

F6

0.49±0.2

0.58±0.006

29.26±0.36

15.51±1.96

1.18±0.05

 


The angle of repose of different formulations was ≤ 30.68 which indicates that material had good flow property. So it was confirmed that the flow property of blends were free flowing. The bulk density of blend was found between 0.42g/cm3 to 0.52g/cm3.Tapped density was found between 0.48g/cm3 to 0.60g/cm3. These values indicate that the blends had good flow property. Carr’s index for all the formulations was found to be between 11.53-15.518 and Hausner’s ratio from 1.12-1.18 which reveals that the blends have good flow character.

 

Characterization of tablets Post Compression parameters:

All the batches of tablet formulations were characterized for official evaluation parameters like Weight variation, Hardness, Friability, Tablet thickness and drug content and results are shown in the table-7.

 

Table 7: Characterization Fexofenadine HCL tablets

Formulation

Weight variation

Thickness

(mm)

Hardness

(kp)

Friability

(%)

Disintegrating time (sec)

F1

151.2±0.02

3.4±0.02

3.6±0.01

0.68±0.02

39.18±0.02

F2

149.3±0.06

3.5±0.04

4.2±0.03

0.62±0.06

34.16±0.05

F3

148.4±0.07

3.7±0.06

3.5±0.02

0.79±0.08

30.36±0.06

F4

151.6±0.04

3.4±0.01

3.9±0.01

0.65±0.02

36.08±0.08

F5

149.2±0.03

3.2±0.01

3.7±0.01

0.59±0.08

40.29±0.02

F6

149.8±0.02

3.5±0.02

4.1±0.06

0.48±0.06

43.12±0.07

Hardness of the tablet was acceptable and uniform from batch to batch variation, which was found to be 3.68 – 4.28kg/cm2.All the formulations passed the weight variation test as the % weight variation was within the pharmacopoeial limits of the tablet weight. Friability values were found to be less than 1% in all the formulations F1 – F6 and considered to be satisfactory ensuring that all the formulations are mechanically stable.

 

Drug content uniformity of formulations:

The prepared formulations were analysed for drug content and the data is reported in below Table. The drug content was found to be within the limits which show that the drug was uniformly distributed in all the formulations.

 

Percenatge drug content values of formulation F1 is 95.96%, F2 is 97.65 %, F3 is 99.62 %, F4 is 98.02%, F5 is 98.71%, F6 is 98.16%,. The drug content values for all the formulations (F1- F6) was found to be in the range of 95.96-99.62%.

 

Dissolution studies of the tablets:

The prepared tablets were subjected to dissolution studies in order to know the amount drug release. As the concentration of polymer increased, the drug release decreased.

 

Drug release kinetics:

The drug release from the tablets was explained by using mathematical model equations such as zero order, first order methods. Based on the regression values it was concluded that the optimized formulation F3 follows First order kinetics.

 

SUMMARY AND CONCLUSION:

The therapeutic effectiveness of a drug product intended for oral administration depends on its gastrointestinal absorption. Dissolution is often the rate limiter in the absorption of a drug from a solid dosage form by the gastrointestinal system. Poorly soluble drugs have proved unpredictable and are absorbed slowly compared to higher- solubility drugs. As a result, the development into bioavailable dosage forms presents great difficulty for these medicines. The aqueous solubility, the rate of dissolution and the bioavailability of those drugs from their oral solid dosage forms should therefore be increased. HP β cyclodextrin solid dispersion technique has been used to improve the dissolution properties of poorly soluble water medicines and bioavailability. This study showed how the dissolution performance of Fexofenadine HCL can be significantly improved using a solid dispersion technique.

 

The antihistamine medicine used in the treatment of hayfever and similar allergy symptoms is Fexofenadine hydrochloride. Their oral absoption is 33% and has a half-life of 14.4 hours and is a BCS II medication. Thus, an enhanced solubility and dissolution rate of this model medication can help in the treatment of bacterial infections. This formula is favourable. There have been studies to improve the solubility of the poorly soluble drug Fexofenadine HCL through solid dissolution technology using HP β cyclodextrin and β cyclodextrin, and therefore its efficacy and bioavailability.

 

In the introductory part, the short introduction on solid dispersions was explained. In addition, the introduction on dissolution rate and various solutions for improving the solubility was developed in this chapter, in particular on solid dispersion technology. The goal and aim were discussed as well.

 

A complete drug description of Fexofenadine HCL and its use, contraindication and side effects have been included with the drug profile and excipient profiles. Literature survey on the preparation and past research of solid dispersions with different drugs and methods.

 

Detailed explanation was provided of the methodologies as well as materials and experimental methods used in this investigation. Later introduction was explained with regard to all the assessment parameters and method of preparing physical and solid fexofenadin HCL dispersions through solvent evaporation. Solid Fexofenadine HCL dispersions were prepared in various drug and carrier ratios with different carriers (1:0.25, and 1:0.5).

 

Solubility and melting point determination, drug content uniformity, encroachment efficiency, and In-vitro dissolution studies were discussed as results of prepared solid dispensations of Fexofenadine HCL by solvent evaporation. Different analytical methods such as FT-IR studies were used to characterise the solid state.

 

Finally, the better results are shown by solvent evaporation process with a drug release of 88,96 percent (KF1 - KF4) by comparing all of the formulations (SF1-SF4) (SF4) containing Fexofenadine HCL β cyclodextrin (1:0.5)), which is why it has been chosen as the best formulation.

 

The optimised formulation used different disintegrants in different concentrations to formulate immediate release tablets. The parameters pre-compression and post-compression were examined and results obtained. There is an acceptable limit to all the results. Release of the formulated tablets by In-vitro medication was done with 0.1N HCL. The Lycoat (7mg) formulation F3 shows 98.82 percent release of medicinal products in 30 minutes. The optimised formulation is based on kinetis in the first order.

 

In preparation of solid dispersions by solvent evaporation method, HP β cyclodextrin and β cyclodextrin were used. Fexofenadine HCL is observed with β cyclodextrin by observing the dissolution (1:0.5). Better release of medicine shows. And all the solid scatters prepared have been evaluated and the results have been explained in the above data.

 

REFERENCES:

1.     M.L.R. Medina, V. Kumar. Evaluation of cellulose II powders as a potential multifunctional excipient in tablet formulations, International Journal of Pharmaceutics 322, pp: 31-35 (2006).

2.     M.C. Gohel, Improving the Tablet Characteristics and Dissolution Profile of Ibuprofen by using a Novel Co processed Superdisintegrant, AAPS, Pharm SciTech, vol. 8, no.1, Article 13: E1-E6 (2007).

3.     European Pharmacopoeia Supplement, Strasbourg, France: Council of Europe. 2002

4.     A. Goran. Tablets and compaction, in Aulton, M. E., Pharmaceutics, The Science of Dosage Form Design, 2nd Edition, Churchill Livingstone, New York, , pp. 397-440. 2002

5.     A. John, M. Chris. Modified-release peroral dosage forms, in: Aulton, M.E., Pharmaceutics, The science of dosage form design, 2nd Edition, Churchill Livingstone, New York, pp. 289-305. 2002

6.     Azeem S, Sharma S. Immediate drug delivery systems: review, Int. J. Biopharm. Toxicol., vol. 1, no. 1, pp 24-46, 2011

7.     Leah E, Appel DT, Friesen JE, Byers MD, Crew BC, Hancock SJ, Schadtle. Immediate release dosage forms containing solid drug disbursion, U.S. Patent, pp 424 465; 2002.

8.     Mishra B, Shukla D, Chakraborty S, Singh S, An overview of formulation of mouth dissolving tablets, Scientia Pharmaceutica, pp 77, 309-326. 2009

9.     Menat AK, Patel MS, Patel MR, Patel NM, Fast dissolving tablets a novel approach to drug delivery. Asian J. Pharm. Sci. Res., vol. 2, no. 8, pp 13-21. 2012

10.  Garg A, Gupta MM, A review of mouth dissolving tablets. J. Drug Delivery Therapeutics, vol. 3, no.2, pp 207-214. 2013

11.  Jagani H, Patel R, Upadhyay P, Bhangale J, Kosalge S, Fast dissolving tablet on present and future prospectus. J. Advances In Pharmacy And Healthcare, vol. 2, no. 1, pp 57-69. Res. 2011

12.  Hirani JJ, Rathod DA, Vadalia KR, A review in orally disintegrating tablets. Tropical J. Pharm., vol. 8, no. 2, pp 161-172. Res. 2009

13.  Patel P, Dhanani C, Kadeval A, Patel M, Patel N‚ Patel R, A modern approach on fast dissolving tablets. Int. J. Modern Pharm., vol. 1, no.2, pp 1-17. Res. 2012

14.  Leon Lachmann, Herbert A, Liberman, Joseph L.Kaing, The theory and practice of Industrial Pharmacy: pp 293-303.

15.  Ansel‘s Pharmaceutical dosage forms and drug delivery systems, eighth edition, pp 227- 260.

16.  Snehal B. Kulkarni, M. M. Bari, S. D. Barhate, Ashutosh Tripath. Formulation and Evaluation of Immediate Release Tablet of Efavirenz by Micellar Solubilization Technique. Asian J. Pharm. Res. 2019; 9(1): 12-18.

17.  Rajeshree Panigrahi, K.A. Chowdary, Gitanjali Mishra, Manas Bhowmik, Saiprasanna Behera. Formulation of fast dissolving tablets of Lisinopril using combination of synthetic superdisintegrants. Asian J. Pharm. Tech. 2(3): July-Sept. 2012; Page 94-98.

18.  S. Kumara Swamy, G. Arun, Bethi Srinivas, Agaiah Goud B. Effect of Various Super Disintegrants on the Drug Release Profile of Orally Disintegrating Tablets. Asian J. Pharm. Tech. 2016; 6(2): 99-105.

19.  Renuka S. Deshmukh, M. M. Bari, S. D. Barhate. Formulation and Evaluation of Orodispersible Tablet of Naratriptan HCl. Asian J. Pharm. Tech. 2018; 8 (3):139-144 .

20.  Design and Evaluation of the Fast Dissolving Tablets of Aceclofenac by Sublimation Technique. Sumanta Malakar, Ashok Kumar P., Suresh V. Kulkarni, Someshwara Rao B., Amit S. Yadav. Research J. Pharma. Dosage Forms and Tech. 2010; 2(3):233-236 .

21.  V. Saikishore, G. Srikanth, Ch. Pooja, Y. Mrudula, R. Pavani, Ch. Jyosthna , C. Mayuren. Design and Development of Fast Dissolving Tablets of Glibenclamide. Research J. Pharma. Dosage Forms and Tech. 2011; 3(5): 225-229.

22.  A. Pavan Kumar, V. Sai Kishore, T. E. Gopala Krishna Murthy, K. Madhu Babu,. Formulation of Valsartan Fast Dissolving Tablets Using Novel Co Processed Superdisintegrants. Research J. Pharma. Dosage Forms and Tech. 2012; 4(1): 52-55.

23.  Sharad A. More, Shrinivas K. Mohite. Formulation Development and Evaluation of Orodispersible Tablet of Omeprazole by Using Co-Processed Superdisintegrant. Research J. Pharma. Dosage Forms and Tech. 2012; 4(4): 216-220.

24.  V. Kalyani, V. Sai Kishore, U. Kartheek, S. Aruna, A. Navya Krishna. Design and Development of Olanzapine Immediate Release Tablets by using Natural Super Disintegrant. Res. J. Pharm. Dosage Form. and Tech. 6(2):April- June 2014; Page 85-90.

25.  V. Kalyani, V. Sai Kishore, U. Kartheek, S. Aruna, A. Navya Krishna. Design and Development of Olanzapine Immediate Release Tablets by using Natural Super Disintegrant. Res. J. Pharm. Dosage Form. and Tech. 6(2):April- June 2014; Page 85-90.

26.  Omprasad Nayakal, Prajakta Patil, Mangesh Bhutkar, Dheeraj Randive, Somnath Bhinge. Formulation and Evaluation of Fast Dissolving Tablets containing Clopidogrel bisulfate using holy basil seeds as a natural superdisintegrant. Res. J. Pharm. Dosage Form. and Tech. 2018; 10(4): 209-214.

27.  Ranabir Chanda, H. Padmalata 1 Venkatesh, Janmajoy Banerjee Formulation and Evaluation of Oral Disintegrating Tablets of Ondansetron Hydrochloride. Res. J. Pharma. Dosage Forms and Tech.2019; 11(1):53-63.

28.  Y. Krishna Reddy1*, Gopagoni lavanya. Formulation and In Vitro Evaluation of orally Disintegrating Tablets of Amlodipine Besylate. Res. J. Pharma. Dosage Forms and Tech.2019; 11(4):264-268.

29.  SC Jagdale, AR Chabukswar, BS Kuchekar, AN Padalkar, AU Kale. Comparative Evaluation of Superdisintegrants with Formulation Development of Orodispersible Tablets of Mosapride Citrate Dihydrate. Research J. Pharm. and Tech. 2(1): Jan.-Mar. 2009; Page 91-96.

30.  Venkatalakshmi R, Sasikala C, SP Silambarasan. Formulation and Evaluation of Loperamide Hydrochloride Mouth Dissolving Tablet by Using Super Disintegrants. Research J. Pharm. and Tech. 3(2): April- June 2010; Page 530-534.

 

 

 

 

 

 

 

Received on 15.07.2021          Modified on 18.12.2021

Accepted on 08.06.2022   ©Asian Pharma Press All Right Reserved

Asian J. Pharm. Tech. 2022; 12(4):290-298.

DOI: 10.52711/2231-5713.2022.00047