Formulation and In Vitro Evaluation of Fast Dissolving Tablets for Albendazole

The present work is to study the effect of various superdisintegrants on drug (Albendazole) by direct compression methods. The tablets were prepared by four super disintegrants, e.g; sodium starch glycolate, cross carmellose, cross povidone and L- subsituated hydroxyl propyl cellulose. The blend was examined for angle of repose, bulk density, tapped density, compressibility index, and hausner ratio. The tablets were evaluated for hardness, drug content and friability were found satisfactory. Albendazole is a bitter in taste. To prevent bitter taste of the drug formulated with a sweetener (Aspartame), a mannitol-based diluent. Taste evaluation was done by panel tasting.

Majoritydrugs are delivered are by oral drug delivery.It offers benefitsof ease of administration and considerable manufacturing cost savings. Today drug delivery companies focused on solid oral drug delivery systems with higher patient compliance and efficient dosages. Tablet is the most popular among all dosageforms available now a day due to its ease of self-administration Majority medicines are delivered are by oral medicine delivery. It offers benefits of ease of administration and considerable manufacturing cost savings. moment medicine delivery companies concentrated on solid oral medicine delivery systems with advanced patient compliance and effective tablets. Tablet is the most popular among all lozengeforms available now a day due to its ease of tone administration, conciseness, and ease of manufacture.1

An ideal lozenge authority is the one, which incontinently gives the needed remedial attentionof medicine at the point of action and constantly maintains until durationof treatment. This would be possibleby administration of conventional lozengeform in a particular cure andat a particular frequence.2

medicines are veritably frequently given orally. Although a veritably less medicine products are taken orally is intended to be dissolved in mouth, utmost of them were taken orally and swallowed. Compared with other routes, oral medicine delivery is the veritably popular and has been used veritablyfrequently for conventional medicine delivery. It was veritablynatural, uncomplicated, accessible, safe means of administering medicines, further flexibile in lozenge form design, ease of product and costeffective.3

Yoshio etal.( 2008) estimated the effect of lubricants on the characteristics of orally disintegrating( OD) tablets manufactured using the phase transition of sugar alcohol. OD tablets were produced by directly compressing an admixture containing lactose – xylitolgrains, disintegrant, glidant and lubricant, and posterior heating. The effect of the type of lubricant on the tablet characteristics was estimatedusing magnesium stearate(mg- st), sodiumstearyl fumarate (SSF),and talc as lubricants. the hardness of the tabletsincreased toca. 6 kp because of heating, anyhow of the kind of lubricant. the oral decomposition time of the tablets containing mg- st or ssf increased with an increasein the hardness. In discrepancy, the oral decomposition time of the tablets’ containing talc wasn't changeddespite of an increase in hardness. The water immersionrate of the tablets’ containing talc was important faster than that of the tablets containing other lubricants. The water immersion rate of the tablets’ containing talc was also increased by heating.

Yoshio etal., (2008) estimated the effect of medication system on the parcels of orally disintegrating (OD) tablets, OD tablets were prepared by compressing a admixture of high meltingpoint sugar alcohol(HMP- SA) and low melting point sugar alcohol (LMP- SA) and posterior heating. In the direct contraction system (DCM) where the LMP- SA was added as a greasepaint, both hardness and decomposition time were increased by dwindling the flyspeck size of the LMP- SA. In the wet scrap contraction system (WGCM), where the LMP- SA was added as a waterless binder result, the tablets came harder with lower heating compared to tablets prepared by DCM. Using 1 xylitol as the LMP- SA handed tablets with sufficient hardness when prepared by WGCM, as opposed to DCM where 5 xylitol was necessary to prepare tablets with analogous hardness. These results suggest that slightly distributed LMP- SA on the face of HMP- SA patches in WGCM might diffuse more fluentlyduring the heatingprocess compared to mechanically mixed LMP- SA in DCM, performing in an increase in tablet hardness indeed with a short heating time and low content of LMP- SA. In addition,decomposition and hardnessstability of the tablets were affected by the LMP- SA contentwhen prepared by WGCM, suggesting that the LMP- SA content should be regulated to assure the stability of OD tabletcharacteristics.

The FDTs surfaced with an ideal to ameliorate case’s compliance. These lozenge forms fleetly disintegrate and/ or dissolveto release the medicine as soon as they come in contactwith slaver, thereforepreventing the need for water during administration, an trait that makes them largely seductive for pediatric and senior cases. Difficulty in swallowing conventional tablets and capsules is common among all age groups, especially in senior and dysphagic cases.

This complaint of dysphagia is associated with numerous medical conditions including stroke, Parkinson’s complaint, AIDS, thyroidectomy, head and neck radiationremedy and other neurological diseases including cerebral paralysis. One study showed that 26 out of 1576 cases endured difficulty in swallowing tablets due to their large size, followed by their face, shape and taste. Rapid- breakdown or presto disintegrating tablet of the type of those intended to suffer dis- aggregation in the mouth in contact with the slaver in lower than 60 seconds, ratherin lower than 40 seconds,forming a suspensewhich is easy to swallow.

Hence, in the present study an attempt is made to formulate fast disintegrating tablets of Albendazole (A benzimidazole broad- diapason anthelmintic structurally related to mebendazole that's effective againstnumerous conditions.)

Fast disintegrating tablets are getting popular as one of the stoner friendlylozenge forms. Our purpose is to developan original composition of fast disintegrating tablet by using conventional tablet manufacturing process.The introductory approachused in the development of fast disintegrating tablets is the use of super disintegrants. Cross caramelize sodium, sodium bounce glycolate, and cross povidone,low- substituted hydroxylpropyl cellulose was used in the present study.

Before that, bitter taste of albendazole was masked by using sweetener.

1. Medicine Profile Albendazole Description

A benzimidazole broad- diapason anti helmintic structurally related to mebendazole that's effective againstnumerous conditions. (From Martindale, The Extra Pharmacopoeia, 30th ed, p38). Albendazole contains not lower than98.0 percent and not furtherthan102.0 percent calculated on the dried base.

Molecular FormulaC12H15N3O2S

Chemical/ IUPAC Name Methyl 5- propylthio- 1H- benzimidazol-2- ylcarbamate.

Chemical                                                                                                                Structure:

Molecular weight265.3 g/ operative Physicochemical Profile

Description Whiteor slightly unheroicgreasepaint. Melting point 250- 251 ºC

Solubility virtually undoable in water, freely answerable in anhydrous formicacid, veritably slightlyanswerable in methylenechloride, virtually undoable in ethanol (96 per cent). Trade names Albenza,Albendazole is a WHO Essentialdrug.

Routes Only oral route

Metabolism Oxidationof sulfur snippet tosulfoxide, the active metabolite

partial life About8.5- 12 hr, terminalelimination half- life ranges from 8 to 12 hours (single cure, 400 mg).

CAS number 54965-21-8 orders Anthelmintics, Anticestodal Agents, Antiprotozoal Agents, Tubulin Modulators. Description Albendazole is a benzimidazole medicine used for the treatmentof a variety of parasitic worminfestations. Although this use is wide in the United States, theU.S. Food and Drug Administration (FDA) haven't approved albendazole for this suggestion. It's retailed by Amedra Pharmaceuticals.
 

1. SODIUM bounce GLYCOLATE Nonproprietary Names

BP Sodium bounceglycollate

PhEur Carboxymethylamylum natricum USPNF Sodiumbounce glycolate

Antonyms

Carboxymethyl bounce, sodium swab; Explosol;Explotab; Glycolys; Primojel; bounce carboxymethyl ether, sodiumswab; Tablo; VivastarP.

Chemical Name and CAS Registry Number Sodium carboxymethyl bounce (9063-38-1)

Structural Formula

Functional order

Tablet and capsule disintegrant.

Preparation of standard graph of Albendazole
Standard estimation wind of Albendazole
Scanning of medicine
The pure medicine Albendazole when scrutinized over a range 200-
400 nm to determine its lmax, the peak was observed at 291 nm

Preparation of standard graph of Albendazole
Albendazole have the maximum absorbance at 291 nm. Standard
graph of Albendazole in water was colluded by taking attention
ranging from 10 to 100 μg/ ml and a good correlation was attained with
R2 value of0.9991

Table: Preparation of standard graph of Albendazole in distilledPars of tripletwere reported

R2 = 0.9991

pitch = 0.010914

Summary

Fast disintegrating tablestsof Albendazole preparedby direct contraction system

• The in vitro medicinerelease from expression containing superdisintegrant SSG was set up between87.64 ±2.36 to96.70 ±1.64 in 10 min and the maximum medicine release was set up with F2 expression.
• The in vitro medicinerelease from expression containing superdisintegrant CCS was set up between94.20 ±2.34 to95.72 ±2.14 in 10 min and the maximum medicine release with F9 expression.
• The in vitro medicinerelease from expression containing superdisintegrant CP was set up between90.75 ±2.06 to97.32 ±1.24in 10 min and the maximum medicine release with F14formulation.
• The in   vitro  medicine   release  from  expression   containing

superdisintegrant L- HPC was set up between90.75 ±1.09 to 96043

±2.32 in 30 min and the maximummedicine release with F16 expression.

Fast disintegrant tabletstransfigure into easy- to- swallowsuspense on contactwith the slaver,after ingested in mouth. Theseare particularly useful for pediatric or senior cases, can be taken withoutliquids. The developedphrasings have suitablecharacteristics. Among the four superdisintegrants, Crosspovidone (F14) showed good disintegrants property. It has also shown good water immersion rate.