Poorly Water Soluble Drugs Biology Essay

Use of wetting agents: Surface active agents enhance disintegration rate by advancing wetting and incursion of disintegration fluid into solid drug atoms.Example: Steroids like Aldactone.Use of salt signifiers: Salts have improved solubility and disintegration features in comparision to the original drug.Example: Salt of basic drug like atropine is soluble than parent drug.Change of pH of the Drug Microenvironment: It is achieved in two ways insitu salt formation and add-on of buffers to the preparation.Example: Buffered Aspirin tablets.Use of metastable polymorphs: Metastable polymorphs are more soluble than the stable polymorphs of drug that exhibits polymorphism.

Example: Chloramphenicol palmitate.Solute-solvent complexation: Solvates of drugs with organic dissolvers by and large have higher aqueous solubility than the original drug.Example: 1:2 Fulvicins benzene solvate.Selective surface assimilation on indissoluble bearers: A extremely active adsorbent can heighten the disintegration rate.Example: Bentonite.

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Solid solution

Use of solid solution: Solid solution is a binary system comprising of solid solute molecularly dispersed in a solid dissolver.Use of eutectic mixtures: These systems are besides prepared by merger method. It is somewhat different from solid solution in that fused thaw of solute-solvent show complete miscibility but negligible solid-solid solubility.

Use of solid scatterings: These are by and large prepared by dissolver or co-precipitation method where both guest solute and the solid bearer dissolver are dissolved in common volatile liquid such as intoxicant.The liquid removed by vaporization under decreased force per unit area or by freezedrying which consequence in formless precipitation of invitee in crystalline bearer.Molecular encapsulation with cyclodextrins: The beta and gamma cyclodextrins and several of their derived functions are alone in holding the ability to organize molecular ivclusion with hydrophobic drugs holding hapless aqueous solubility. These cyclodextrin molecule are versatile in holding hydrophobic activity of size suited plenty to suit hydrophilic drug as a invitees ; the exterior of the host molecule is comparatively hydrophilic. Therefore, the molecularly encapsulated drug has greatly improved aqueous solubility and disintegration rate.However, among them, the technique of “ liquisolid compacts ” is one of the most promising technique.

Low cost, simple preparation technique and capableness serve to be advantages of this technique.

Liquisolid Technique:

The hapless disintegration rate of H2O indissoluble drugs is still a significant job facing the pharmaceutical industry. A great figure of new and perchance, good chemical entities do non make the populace simply because of unequal disintegration release profile. Over the old ages, assorted solid dose preparation techniques, to heighten the disintegration of ill soluble substances, have been introduced with different grades of success.

Categorization of liquisolid systems:

Liquisolid systems which are prepared by liquisolid technique are classified as follows:Categorization based on the type of liquid medicine contained.

They are divided into three subgroups of liquisolid systems are:Powdered drug solution.Powdered drug suspensions.Powdered liquid drugs.

The first two may be produced from the transition of drug solutions or drug suspensions and the latter from the preparation of liquid drugs into liquisolid systems8.Categorization based on the preparation technique used liquisolid system is divided into two classs viz. ,Liquisolid Microsystems.Liquisolid compacts.

Liquisolid Microsystems:

They are based on a new construct which employs similar methodological analysis combined with the inclusion of an linear, e.

g. , Poly vinyl pyrrolidone ( PVP ) , in the liquid medicine which is incorporated into the bearer and the coating stuffs to bring forth an tolerably streamlined alloy for encapsulation. The advantage stemming for this new technique is that the ensuing unit size of liquisolid Microsystems may be as five times less than that of liquisolid compacts.

Liquisolid compacts:

Harmonizing to Spireas et al. , the term “ liquisolid compacts “ refers to readying of immediate ( or ) sustained release tablets ( or ) capsules utilizing “ liquisolid systems ” combined with the inclusion of appropriate excipients required for tabletting ( or ) encapsulation, such as disintegrant for immediate release, binders for sustained release action.

Ideal features of constituents used in liquisolid compact preparation:

Drug – Ill soluble, indissoluble, liquid or lipotropic.Non-Volatile solvent- Water miscible.

Carrier- Coarser, farinaceous, good compatibility.Coating material- High surface country, good adsorptive belongingss.

Need of liquisolid compact technique is chiefly for category of drugs which are:

Ill H2O soluble, indissoluble, liquid drugs ( or ) lipotropic drugs.Ill flowable pulverization alloies.To help direct compaction.

To better efficiency of tablet fabrication.

Principle involved in preparation of liquisolid compacts:

Inert, sooner water-miscible organic dissolver systems with high boiling point such as propene ethanediol, liquid polythene ethanediols, or glycerol are best suited as liquid vehicles. Once the bearer is saturated with liquid, a liquid bed is formed on the atom surface which is immediately adsorbed by the all right coating atoms. Therefore, an seemingly dry, free flowing, and compressible pulverization is obtained. Normally, microcrystalline cellulose is used as bearer stuff and formless Si dioxide ( colloidal silicon oxide ) as surfacing stuff. Assorted excipients such as lubricators and disintegrants may be added to the liquisolid system to bring forth liquisolid compacts ( Fig. 1 ) .Solid DrugCarrier stuffDrug – Non volatile dissolver mixtureNon-volatile dissolver systemWet atomsBy add-on of adjuvantsSimple alloyConcluding preparation


Coating stuff incorporationTabletting ( or ) Encapsulation


1: Word picture of liquisolid compacts.

Liquisolid compacts of ill soluble drugs incorporating a drug solution or drug suspension in a solubilizing vehicle show enhanced drug release due to an increased surface country of drug available for release, an increased aqueous solubility of the drug, and an improved wettability of the drug particles9-14 thereby heightening the disintegration belongingss of ailing H2O soluble drugs.

Advantages of Liquisolid tablets15-19:

Liquisolid tablets have many advantages like ;Number of non-water-soluble solid drugs can be formulated into liquisolid systems.Can be applied to explicate liquid medicines such as greasy liquid drugs.Better handiness of an orally administered H2O indissoluble drug.Lower production cost than that of soft gelatin capsules.Production of liquisolid systems is similar to that of conventional tablets.

Can be used for preparation of liquid oily drugsExhibits enhanced in-vitro and in-vivo drug release as compared to commercial opposite numbers, including soft gelatin capsule readyings.Can be used in controlled drug bringing.Drug release can be modified utilizing suited preparation ingredients.Drug can be molecularly dispersed in the preparation.Capability of industrial production is besides possible.

Restrictions of liquisolid tablets15-17:

Low drug burden capacities.Requirement of high solubility of drug in non-volatile liquid vehicles.

Applications of liquisolid techniques15-19:

Rapid release rates are obtained in liquisolid preparations.These can be expeditiously used for H2O indissoluble solid drugs or liquid lipotropic drugs.Sustained release of drugs which are H2O soluble drugs such as propranolol hydrochloride has been obtained by the utilizing this technique.

Solubility and disintegration sweetening.Planing of controlled release tablets.Application in probiotics.

Anti-convulsant drug ( Clonazepam ) :

Status epileptics is a neurological upset, which requires speedy direction of ictuss in order to avoid hazard of lasting encephalon harm. Clonazepam, a benzodiazepine derived function is used widely in the intervention of position epileptics. Clonazepam is preferred over the other benzodiazepines due to its longer continuance of action ( 24h ) 20.Clonazepam, the drug of pick in suppression of myoclonic ictuss, Acts of the Apostless by increasing the effectivity of the inhibitory neurotransmitter, gamma amino butyric acid ( GABA ) , within the cardinal nervous system.Soon, Clonazepam is available in tablet and injectable dose signifiers ( Revotril, Hoffmann, LaRoche, NJ, USAhttp: //www.

fda.gov/cder/foi/nda/index.htm ) 21. These preparations release clonazepam into the peripheral circulation ensuing in limited drug consumption across the blood-brain-barrier and in drug distribution to nontargeted sites22. Although endovenous disposal provides rapid ictus suppression, the most convenient and normally employed path of drug bringing has been by unwritten consumption.Clonazepam being ill soluble in H2O its rate of unwritten soaking up is frequently controlled by the disintegration rate in the GI piece of land and by liquisolid technique the solubility and disintegration of clonazepam can be enhanced.

Table 1: List of drugs as liquisolid compacts


Drug Name

Polymers used


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