DEPARTEMENT OF PHARMACEUTICS

CHAPTER IV

LITERATURE REVIEW

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Somchai Sawatdee et.al1 comparitive and design studies fond that the prepared albendazole

self-microemulsion chewable tablets (F1 and F2) yielded significantly higher dissolution of

98&99 than the market product, within the 60-min timeframe. The commercial product in

this study used Zentel in this formulation albendazole formulated as SMEDDS based on

eithersesame oil + PEG400 + Tween80 or soybean oil + Cremophor RH40 + Tween80, in

order to increase the solubility, stability, and bioavailability of albendazole.

Ramachandra M. Koli.et.al2 Found that F5 batch has optimized formulation showed rapid

disintegration and maximum drug release 97% of Albendazole fast dissolving tablets

prepared by direct compression technique using different superdisintegrants, namely

croscarmellose sodium, crospovidone and sodium starch glycolate.

N.Kanaka Durga Devi.et.al3 Conducted design and comparative studies found that 99% of

drug was released for the trial ‘A3’ at 30 min compared to other trials ‘A1’& ‘A2 had shown

93% & 85% drug release at 30 min respectively of drug albendazole the dissolution profile

of batches of tablets prepared by direct compression method has shown better results

compared to the tablets prepared by other methods as well as marketed product.

Cherogony et.al4 Conducted pre-formulation studies on enhancing the dissolution and

solubulity of albendazole found thatPVP K90:

ABZ solid dispersions showed the highest increase in dissolution rate as compared to solid

dispersions of ABZ with HPMC and CMC polymers Polyethylene Glycol 8000 (PEG).

Ahmad shuaib et.al5 Found that F5 have a recorded drug release 97.48% at the end of 40

min when compared to other four formulations Albendazole fast dissolving tablets of were

prepared by directcompression method by using superdisintegrants like Crospovidone,

Croscarmellose sodium and Microcrystalline Cellulose.

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Salunkhe et.al6 Formulated albendazole tablets by wet granulation technique using

Surfactant and superdisintegrants the formulation of F6 shows the drug release of 96% when

compared to the F1-F4 formulations.

A.k. Azad et.al7 Found that formulation code CSF5 showed better result where carrier was

HMPC K 100 LV at 1:10 ratio in solvent evaporation method.Studies are conducted to

improve the dissolution profile of Albendazole using HPMC K 100 LV, Kollidon VA64 and

Mannitol as carriers by solid dispersion techniques the prepared solid dispersions were

evaluated.

Md.Habibur.Rahman et.al8 expiremental study found that ABZ:PEG:AVICLE was found to

most promising among the other polymer drug ratios analysed the effect of polyethylene

glycol - 6000 and avicel on poorly water soluble drug Albendazole by solid dispersion

method was performed to improve the % release of drug to increase polymers ratio, which

found to be prepared solid dispersion by using fusion method, the polymer ratio Albendazole:

PEG 6000: Avicel of 1:4:4 gave more drug release 65.10% within 1 hour than the other

polymer ratio 4:1:1, 2:1:1, 1:1:1,1:2:2 & the physical mixture & pure drug of Albendazole.

Samar elsamagily et.al9 Expiremental results found that that results showed an improvement

in solubility and dissolution rate of abz for all prepared sds. sd containing (Abz: pvp k30: p

407) (50%: 48%: 2%) w/w achieved the highest dissolution rate.,Worked on ternary solid

dispersion (sd) system developed for the enhancement of the solubility and dissolution rate

of albendazole (abz), a bcs class ii drug, the effect of different ratios of one of two

proloxamer grades (p 188 and p 407) in combination with pvp k30 was investigated .

Pravin.kumar.kara et.al10 studies found that the physical mixture showed the highest

dissolution improvement, a 7.76 fold increase incumulative dissolution profile than that of

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pure Albendazole. The studies are conducted to Improve the dissolution profile of

Albendazole(ABZ) using solid dispersions technique with nicotinamide (NIC) as the carrier,

All the soliddispersions prepared by kneading method showed an enhanced dissolution

profile ofAlbendazole, as compared to that of pure drug alone, concentration dependently.

Seti. Anupama et.al11 worked out to Design, Optimization, Preparation and Evaluation of

Solid dispersions of Albendazole using Factorial Design,The dispersion granules were

prepared using a hot melting technique which involved preparation of a homogenous

dispersion of albendazole in gelucire 44/14 and PEG 8000 A two-factor, four-level (4*2)

statistical design was implemented to quantitate the influence of gelucire 44/14 and PEG

8000 on the dissolution profile, where gelucire 44/14 and PEG 8000 were chosen as

independent variables, while T10min (cumulative drug release in 10 minutes) and T60 min

(cumulative drug release in 60minutes) were chosen as dependent variables In conclusion the

statistical model enabled us to understand the effects of formulation variables on the

dispersion.

Silvina.g.castro et.al12 worked to Improved Albendazole Dissolution Rate in Pluronic 188

Solid Dispersions, SDs containing albendazole 5, 10, 25, and 50% w/w and Pluronic 188(P

188) as hydrophilic carrier were formulated The systems with the lowest P 188 percentages

(SD4, SD3; PM4, PM3) tended to be more effective in increasing the ABZ dissolution rate.

J. Salomon et.al13 The results showed albendazole–PEG 6000solid dispersions would be

effective. In vitro and in vivo investigations conducted in mice to determine whether

albendazole–PEG 6000solid dispersion with pure drug alone for efficacy in the treatment of

Toxocara canis larva migrans. Albendazole-PEG6000 (1:1, 1:5 and 1:9 ratios) solid

dispersions were prepared by the solvent evaporation method. The anthelmintic effect was

examined at 28 days post-infection ( p.i.). The number of larvae recovered from mice treated

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with albendazole alone and those treated with albendazole–PEG 6000 were compared with

the numbers from the placebo group.

M.A.bhat et.al14 Physical mixtures showed enhanced dissolution compared with the pure

drug.Researched to study the mechanism of drug re,ease from solid dispersions of

albendazole, giving special emphasis to particle size of the drug in solid dispersions were

prepared using three different carriers, mixing ratios and methods to improve the solubility

and dissolution rate of albendazole The solubility of albendazole was greater with

albendazole-poloxamer 407 system, while polyethylene glycol dispersions showed

predominant wettability.

Alaiselvan.r et.al15 Studied for the Solid-phase preparation and characterization of

albendazole solid dispersion ,The Albendazole (ABZ) was prepared by powder mixing

method using Eudragit E-100 (EGT) as a carrier, Phase solubility study showed a linear

increase in the solubility with the polymer concentration, The enhancement of dissolution

rate and the dissolution efficiency depended on the heat of fusion value as well as mixing

ratio of the polymer,The stored mixture showed a significantly enhanced bioavailability in

rabbits compared to the freshly prepared one.

R.kaliaselvan et.al16 Investigation found that Onset of crystallization and extent of inhibition

increased with concentration and molecular weight of the homo-polymer having a higher

molecular weight, replacement of about 40% of vinyl-pyrrolidone monomers with vinyl-

acetate groups (as in the copolymer) resulted in reduced inhibition of crystallization. on the

“INHIBITION OF CRYSTALLIZATION OF AMORPHOUS FORM OF ALBENDAZOLE

BY SOLID DISPERSION USING POLYMER AND CO-POLYMER OF PVP AND PVA”

prepared by solvent casting mechanism to find the crystallization inhibition was studied.

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Dan liua et.al17 Solubility and dissolution studies in various media were conducted with pure

itraconazole, a physical mixture and solid dispersions. The eutectic mixture showed increase

in drug dissolution rate ,studies were aimed to increase dissolution rate of a poorly water-

soluble drug as solid dispersions itraconazole. Cooling curve method was used to determine

the eutectic point of drug-poloxamer 188 mixture and the phase diagram of the binary system

was constructed. Solid dispersions of itraconazole were prepared by the hot melt method and

characterized by differential scanning calorimetry (DSC).

18
Muralidhar.S et.al It was found that solvent evaporation method exhibited higher

dissolution rate than the corresponding solid dispersion of etoricoxib.formulated solid

dispersions of etoricoxib using PEG 6000 as carrier at various proportions by using different

techniques like physical mixtures, kneading method and solvent evaporation method were

studied.

Muralidhar S et.al 19 It was found that all the solid dispersions exhibited superior dissolution

than pure drug. Solvent evaporation method was found to be superior to other

method.formulated solid dispersions using PEG 6000 as carrier at various proportions. The

solid dispersions were prepared with different techniques like physical mixtures, kneading

method and solvent evaporation method. The drug release profile was studied in water

containing 2% SLS.

Bobe.K.R et.al20prepared atorvastatin solid dispersion by solvent evaporation and fusion

methods by using mannitol, PEG 4000 and PVP K30. Solid dispersion of drug with PEG

4000 had shown enhanced solubility with improved dissolution rate. The study also shows

that dissolution rate of atorvastatin can be enhanced to considerable extent by solid dispersion

technique with PEG.

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21
Niranjan Kumar.M et al It was found that Dissolution rates and drug releases of solid

dispersions with PVP-K30 was most effective and to enhance the dissolution rate of the

drug.prepared alprazolam solid dispersions by solvent evaporation method by using PEG

6000 and PVP k-30 as carriers at different ratios were studied.

Roul lk et.al22 It was studied that the Dissolution rates and drug release of solid dispersions

prepared by using the PVP-K30 was most effective and enhanced the dissolution rate of drug

Alprazolam solid dispersion by solvent evaporation method using PEG-6000,PVP K-30, as

carriers at different ratios were studied.

K.P.R.Chowdary et.al23 It was studied that the Dissolution rate and dissolution efficacy of

the solid dispersions was enhanced, the dissolution rate of drug Aceclofenac solid dispersion

prepared by kneading method using Starch phosphate, Gelucire50/13 as carriers at different

ratios were studied.

Irin dewan et.al24 Studied that the Dissolution and Absorbption rate of solid dispersion was

enhanced ,the dissolution rate of drug Carvedilol solid dispersion prepared by solvent

evaporation method using PEG-6000,Prolaxamer407,HPMC,SSG as carriers at different

ratios were studied.

P.kumar et.al25 Studied that the dissolution rate of solid dispersion was enhanced , the

dissolution rate of Cefidinr Solid dispersion prepared by solvent evaporation method using

PVP K-30,PEG-4000 as carriers at different ratios were studied.

D.b.deshmukh et.al26 Enhanced the Solubility of the poorly soluble drug by solid dispersion

technique ,the solubility of the Diacerein increased by solid dispersion technique using PVP

k-30,HPMC E4 as carriers at different ratios were studied.

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Abhishek das et.al27 studied that the dissolution rate and solubulity of the drug was improved

by employing solid dispersion technique of the poorly water solubule drug Etoricoxib by

using solid dispersion technique using lactose, mannitol, sucrose as carriers at different ratios

were studied.

Krishnamoorthy et.al28 Studied that the dissolution rate and solubulity of the drug was

enhanced by solid dispersion technique of the poorly solubule drug Olanzapine by using solid

dispersion technique using pregelatinized starch and SSG as carriers at different ratios were

studied.

Vyas jigral et.al29 Found that the dissolution rate and solubulity of the drug was enhanced by

solid dispersion technique of the poorly solubule drug Rofecoxib by using PEG-6000,PVP K-

30 as carriers at different ratios were studied.

Averineni ranjith kumar et.al30 Found that the bioavailability and solubility rate was

increased by solvent evaporation method of the drug Gliclazide by using PEG-

4000&6000,PVP k-30as carriers at different ratios were studied.

Ch v prasad rao et.al31 Found that the dissolution rate was enhanced by solid dispersion

technique by kneading method of drug Mefenamic acid by using PEG-6000,PVP k-

30,HPMC,MCC as carriers at different ratios were studied.

Minhaz et.al32 Studied that the solubility was increased by solid dispersion technique by

solvent evapouration method of drug clonazepam using PEG-6000,HPMC,HPC,Polaxamer

407 as carriers at different ratios were studied.

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REFERENCE

1.Somchai Sawatdee et.al. Formulation Development of Albendazole-LoadedSelf-

Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability

Pharmaceutics (2019);11(134):1-20.

2. Ramachandra M. Koli.et.al FORMULATION AND EVALUATION OF MOUTH

DISSOLVING TABLETS OF ALBENDAZOLE IAJPS (2018);05 (07): 6572-6585.

3. N.Kanaka Durga Devi.et.al Design and Comparative Evaluation of Albendazole Chewable

Tablets Int. J. Pharm. Sci(2018);48(1):5-8.

4. CHEROGONY et.al. Preformulation Study on Enhancing the Solubility of Albendazole

East and Central African Journal of Pharmaceutical Sciences(2018);21(1):10-15.

5. AHMAD SHUAIB et.al. Preparation and evaluatation of Albendazole chewable

tablet International Journal of Applied Research 2016; 2(6): 327-329.

6. Salunkhe et al. FORMULATION, OPTIMIZATION AND DEVELOPMENT OF

ALBENDAZOLE TABLET FOR THE IMPROVEMENT OF ORAL BIOAVAILABILITY

World Journal of Pharmaceutical Research(2016);5(8):1170-1181.

7. A. K. Azad et.al. Improvement of dissolution propreties of albendazole from different

methods of solid dispersion ., Journal of Drug Delivery & Therapeutics. 2018; 8(5):475-480.

8. Md.Habibur.Rahman et.al.Analyze the effect of peg-6000 and avicle on poorly water

soluble drug Albendazole by solid dispersion method., UJPSR / 2 (1), 2016, 1-8.

9. Samar elsamagily et.al. Improvement of Albendazole solubility and dissolution rate by

ternary solid dispersion technique.,Am.J.Ph.Health research, 2014;2(10):61-78.

10. Pravin.kumar.kara .et.al .Albendazole solid dispersion in Nicotinamide(solid state

characterization and in-vitro dissolution study)., Int J Pharm Bio Sci 2013 Jan; 4(1): (P) 306 -

319 .

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11. Seti. Anupama .et.al. Design ,optimization, preparation and evaluation of solid dispersion

of albenadzole using factorial design., Der Pharmacia Sinica, 2011, 2 (5):30-42 .

12. Silvina.g.castro .et.al. Improved albendazole dissolution rate in pluronic 188 solid

dispersion., AAPS PharmSciTech, 2010,2(4):1518-1525.

13. J. Salomon .et.al.High efficacy of albendazole in PEG-6000 in the treatment of toxacara

canis lava., Journal of Antimicrobial Chemotherapy (2009) 64, 375–378 .

14. M.A.Bhat.et.al.Studies on mechanism of enhanced dissolution of albendazole solid

dispersion with crystalline carriers., Indian J. Pharm. Sci., 2006, 68 (5): 599-607 .

15. Alaiselvan.r et.al. Solid phase preparation and characterization of albendazole solid

dispersion., Ars Pharm 2006; 47 (1): 91-107.

16.Kalaiselvan et.al. Inhibition of albendazole crystallization in pvp solid molcecular

dispersion.,Pharamazie 2006;618-624.

17. Dan Liua., Increasing solubility and dissolution rate of drugs via eutectic mixtures:

Itraconazole–poloxamer188 system., Asian Journal of Pharmaceutical Sciences 2006; 1(3-4):

213-221.

18. Muralidhar S et al. Enhancement of dissolution rate of etoricoxib through solid dispersion

technique. Journal of Applied Pharmaceutical Science 2011; 1 (5): 129-132.

19. Muralidhar S et al. Enhancement of dissolution rate of celecoxib through solid dispersion

technique. Journal of Pharmaceutics and Cosmetology 2011; 1(2): 113 – 119.

20. Bobe K R et al. Formulation and evaluation of solid dispersion of atorvatstatin with

various carriers. Intl Journal of Comprehensive Pharmacy 2011; 1(2):1-6.

21. . Niranjan Kumar M and Laxmikanta Roul. Improvement of dissolution rate of poorly

soluble alprazolam by solid dispersion. Intl J Pharmaceutical Sciences and Research 2011;

2(1): 79-83.

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22.Roul lk et.al, Dissolution rate enhancement of Alprazolam by solid dispersion .IJPR

2012;46(1):50-60

23.K.P.R.Chowdary et.al.,A Factorial Study On The Enhancement Of Dissolution Rate Of

Aceclofenac By Solid Dispersion In Starch Phosphate And Gelucire, IJRPC 2012;2(4):10-11.

24.IRIN DEWAN et.al., FORMULATION AND EVALUATION OF SOLID

DISPERSIONS OF Carvedilol,IJRPC 2012,2(3):1-5.

25.P.Kumar et.al., Physico chemical charectrization of solid dispersion of cefdinir with PVP

k-30 and PEG-6000,IJPS nanotech 2010,3(2):15-20

26.D.B.Deshmukh et.al.,Dissolution enhancement of Diacerein by solid dispersion technique,

JPAR 2010;2(11):734-739

27.Abhishek Das et.al., Solubulity and dissolution enhancement of etoricoxib by solid

dispersion technique by using sugar carriers;INTERNATIONAL Scholoraly Research

Network ISrN 2011,8(1):30-40.

28.Krishnamoorthy et.al., Charectrization of Olanzapine-Solid

dispersion;IJSP:2011:10(11):13-14

29.Vyas jigral et.al.,Formulation and Evaluation of Solid dispersions of rofecoxib for

improvement of Dissolution profile IJPR 2011:5(5):577-581.

30.Avireneni .Ranjith.kumar et. al. ,Enhanced Dissolution and bioavailability of Gliclazide

Using solid dispersion technique IJPS :2010:1(2):49-57

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31.CH V Prasad Rao et.al.,Enhancement of dissolution rate of poorly soluble drug mefenamic

acid by solid dispersion technique IJPS 2011:2(3):1020-1025

32. Minhaz et.al, Enhancement of solubulity and dissolution properties of clonazepam by

solid dispersion IJP Life sciences 2012:3(3):1500-1510

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