A REVIEW ON: FORMULATION AND EVALUATION OF FAST DISSOLVING TABLET
It is the easiest way to manufacture tablets. Conventional equipment, commonly available excipients and a limited number of processing steps are involved in direct compression. Also high doses can be accommodated and final weight of tablet can easily exceed that of other production methods. This technique can now be applied to fast dissolving tablets because of the availability of improved tablet excipients, especially tablet disintegrants and sugar-based excipients.In this method, tablets are compressed directly from the mixture of the drug and excipients without anycan be directly compressed into tablets of acceptable quality. A type of disintegrant and its proportion are of prime importance. The other factors to be considered are particle size distribution, contact angle, pore size distribution, tablet hardness and water absorption capacity. All these factors determine the disintegration. The disintegrant addition technology is cost preliminary treatment. The mixture to be compressed must have adequate flow properties and cohere under pressure thus making pretreatment as wet granulation unnecessary. Few drugs effective and easy to implement at industrial level
Taste masking is an essential requirement for fast dissolving tablets for commercial success. Taste masking ingredients can be achieved by various techniques; Drugs with unacceptable bitter taste can be microencapsulated into PH sensitive acrylic polymers. Cefuroxime axetile is microencapsulated in various types of acrylic polymers (e.g eudragit E eudragit L-55 and eudragit RL) by solvent evaporation and solvent extraction techniques. These polymer microspheres showed efficient taste masking and complete dissolution in a short period. Fine granules of drug and disintegrant (e.g. low substituted hydroxypropyl cellulose) when coated with a water insoluble polymer (e.g. ethyl cellulose) masked the bitter taste of sparfloxacin. The addition of low substituted hydroxypropyl cellulose as disintegrant to the drug in cores resulted in increased dissolution rate and bioavailability of sparfloxacin compared to its conventional tablets. A novel micro encapsulation process combined with wet spherical agglomeration techniques was also developed by using a modified phase separation method to mask the bitter taste of the drugs. The spherical agglomerates containing enoxacin and other additives including disintegrants were produced in acetone-n-hexane-ammonia water or acetone-n-hexane-distilled water system by wet spherical agglomeration, applying the phenomena of flocculation of particles in liquid. The agglomerates obtained could be microencapsulated with eudragit RS by phase separation technique. The resulting microcapsules were free from bitter taste and were found bioequivalent to the commercial enoxacin tablets.
A polymer carrier system developed by Lu et al was used to reduce the bitter taste of macrolides (e.g. erythromycin and clarithromycin) by complexation to carbopol. The ionic bonding of amine macrolide to the high molecular weight polyacrylic acid results in macrolide-carbopol complex with reduced bitter taste. These complexes are prepared by dissolving or dispersing the drug and polymer in water or hydro alcoholic mixtures. Further taste masking of the complex is achieved with polymer coatings [e.g., hydroxypropyl methyl cellulose (hp-55)] despite which it exhibits good bioavailability.Formulation testing is to generate information useful to the formulator in developing stable and bio available dosage forms that can be man produced.
Characteristics of Fast-Dissolving Tablets:
ZYDIS (R.P. Scherer, Inc.)
Zydis, the best known of the fast-dissolving/disintegrating tablet preparations, was the first marketed new technology tablet. The tablet dissolves in the mouth within seconds after placement on the tongue. Thirteen products are currently available using Zydis technology. In the U.S., they include: Claritin Reditab, Dimetapp Quick Dissolve, Feldene Melt, Maxalt-MLT, Pepcid RPD, Zofran ODT and Zyprexa Zydis. On the worldwide market, other Zydis formulations are available for oxazepam, lorazepam, loperamide, and enalapril.
There are some disadvantages to the Zydis technology. The process of freeze-drying is a relatively expensive manufacturing process. As mentioned earlier, the Zydis formulation is very lightweight and fragile, and therefore should not be stored in backpacks or the bottom of purses. Finally, the Zydis formulation has poor stability at higher temperatures and humidities. It readily absorbs water, and is very sensitive to degradation at humidities greater than 65%. If there is any pinhole or minor damage to the package, the patient may find the lyophilized product has collapsed due to absorption of moisture. As with most other drugs, patients should be advised to avoid storing the Zydis technology in the medicine cabinet in the bathroom. Patients should use their Zydis formulation within six months of opening the laminated foil pouch and immediately after opening its individual blister packaging.
ORASOLV (Cima Labs, Inc.)
OraSolv was Cima's first fast-dissolving/disintegrating dosage form. The OraSolv technology, unlike Zydis, disperses in the saliva with the aid of almost imperceptible effervescence. The OraSolv technology is best described as a fast-disintegrating tablet; the tablet matrix dissolves in less than one minute, leaving coated drug powder. The taste-masking associated with the OraSolv formulation is two-fold. The unpleasant flavor of a drug is not merely counteracted by sweeteners or flavors; both coating the drug powder and effervescence are means of taste-masking in OraSolv. This technology is frequently used to develop over-the-counter formulations. The major disadvantage of the OraSolv formulations is its mechanical strength. The OraSolv tablet has the appearance of a traditional compressed tablet. However, the OraSolv tablets are only lightly compressed, yielding a weaker and more brittle tablet in comparison with conventional tablets. For that reason, Cima developed a special handling and packaging system for OraSolv. An advantage that goes along with the low degree of compaction of OraSolv is that the particle coating used for taste masking is not compromised by fracture during processing. Lyophilization and high degrees of compression, as utilized in OraSolv's primary competitors, may disrupt such a taste masking approach. The OraSolv technology is utilized in six marketed products: four Triaminic Softchew formulations, Tempra FirsTabs, and Remeron SolTab.
DURASOLV (Cima Labs, Inc.)
DuraSolv is Cima's second-generation fast-dissolving/disintegrating tablet formulation. Produced in a fashion similar to OraSolv, DuraSolv has much higher mechanical strength than its predecessor due to the use of higher compaction pressures during tableting. The DuraSolv product is thus produced in a faster and more cost-effective manner. DuraSolv is so durable that it can be packaged in either traditional blister packaging or vials.
The newest DuraSolv formulation, NuLev, is actually dispensed in a conventional stock bottle. Pharmacists are advised to take care when dispensing such DuraSolv formulations from stock bottles to ensure they are not exposed to high levels of moisture or humidity. Excess handling of tablets can introduce enough moisture to initiate dissolution of the tablet matrix. One disadvantage of DuraSolv is that the technology is not compatible with larger doses of active ingredients, because the formulation is subjected to such high pressures on compaction. Unlike OraSolv, the structural integrity of any taste masking may be compromised with high drug doses. The drug powder coating in DuraSolv may become fractured during compaction, exposing the bitter-tasting drug to a patient's taste buds. Therefore, the DuraSolv technology is best suited for formulations including relatively small doses of active compound.10 DuraSolv is currently available in two products: NuLev and Zomig ZMT.
WOWTAB (Yamanouchi Pharma Technologies, Inc.)
The WOWTAB fast-dissolving/disintegrating tablet formulation has been on the Japanese market for a number of years. It has just recently been introduced into the U.S. The WOWTAB technology utilizes sugar and sugar-like (e.g., mannitol) excipients. The two different types of saccharides are combined to obtain a tablet formulation with adequate hardness and fast dissolution rate. Due to its significant hardness, the WOWTAB formulation is a bit more stable to the environment than the Zydis or OraSolv. It is suitable for both conventional bottle and blister packaging. The taste masking technology utilized in the WOWTAB is proprietary, but claims to offer superior mouthfeel due to the patented SMOOTHMELT action.8
The WOWTAB product dissolves quickly in 15 seconds or less.8 The WOW in WOWTAB signifies the tablet is to be given With Out Water. Two WOWTAB formulations currently on the U.S. market are Benadryl Allergy & Sinus FASTMELT and Children's Benadryl Allergy & Cold FASTMELT.
FLASHDOSE (Fuisz Technologies, Ltd.)
Fuisz Technologies has three oral drug delivery systems that are related to fast dissolution. The first two generations of quick-dissolving tablets, Soft Chew and EZ Chew, require some chewing. However, these paved the way for Fuisz's most recent development, FlashDose. The FlashDose technology utilizes a unique spinning mechanism to produce a floss-like crystalline structure, much like cotton candy. This crystalline sugar can then incorporate the active drug and be compressed into a tablet. This procedure has been patented by Fuisz and is known as Shearform. The final product has a very high surface area for dissolution. It disperses and dissolves quickly once placed onto the tongue.
Interestingly, by changing the temperature and other conditions during production, the characteristics of the product can be altered greatly. Instead of a floss-like material, small spheres of saccharides can be produced to carry the drug. The process of making microspheres has been patented by Fuisz, and is known as CEFORM and serves as an alternative method of taste masking.
FLASHTAB (Prographarm Group)
The Flashtab technology is yet another fast-dissolving/disintegrating oral tablet formulation. It utilizes most of the same excipients as in conventional compressed tablets. A disintegrating agent and a swelling agent are used in combination with coated drug particles in this formulation to produce a tablet that disintegrates in the mouth in under one minute.
ORAQUICK (KV Pharmaceutical Co., Inc.)
The OraQuick fast-dissolving/disintegrating tablet formulation utilizes a patented taste masking technology. KV Pharmaceutical claims its microsphere technology, known as MicroMask, has superior mouthfeel over taste-masking alternatives. The taste masking process does not utilize solvents of any kind, and therefore leads to faster and more efficient production. Also, lower heat of production than alternative fast-dissolving/disinte-grating technologies makes OraQuick appropriate for heat-sensitive drugs. KV Pharmaceutical also claims that the matrix that surrounds and protects the drug powder in microencapsulated particles is more pliable, meaning tablets can be compressed to achieve significant mechanical strength without disrupting taste-masking. OraQuick claims quick dissolution in a matter of seconds, with good taste-masking. There are no products using the OraQuick technology currently on the market, but KV Pharmaceutical has products in development such as analgesics, scheduled drugs, cough and cold, psychotropics, and anti-infectives.
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