Formulation and evaluation of taste mask pellets of granisetron hydrochloride as oro dispersible tablet

Orally disintegrating systems have carved a niche amongst the oral drug delivery systems due to the highest compliance of the patients, especially the geriatrics and pediatrics. In addition, patients suffering from dysphagia, motion sickness, repeated emesis and mental disorders prefer these medications because they cannot swallow large quantity of water. Further, drugs exhibiting satisfactory absorption from the oral mucosa or intended for immediate pharmacological action can be advantageously formulated in these dosage forms. However, the requirements of formulating these dosage forms with mechanical strength sufficient to withstand the rigors of handling and capable of disintegrating within a few seconds on contact with saliva are inextricable. The purpose of this research was to mask the bitter taste of granisetron hydrochloride. To mask the taste Kollicoat(r) Smartseal 30D was used as coating polymer for pellet coating. The coated pellets of the drug was directly compressed with different superdisintegrant as AC-Di-Sol, Explotab and Kollidon CL in different concentration 5.0-7.5% w/w into an ODT. The prepared tablets were evaluated for hardness, friability, weight variation, wetting time, wet absorption ratio, in-vitro disintegration time and in vitro dissolution studies. Tablets exhibited quick disintegration characteristics with Kollidon CL in concentration 7.5% w/w i.e., within 20 seconds, which is characteristic of orally disintegrating dosage forms. More than 98% of drug was released from the formulations within 15 minutes. Formulations subjected to stability testing as per the ICH guidelines for 3 months, indicated stability with no change in taste, hardness, drug content, disintegration time and dissolution profiles. Thus, the results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated dosage forms in the oral cavity.

Sistemas de desintegração oral têm um nicho entre os sistemas de administração de medicamentos por via oral devido à maior aceitação dos pacientes, especialmente os de geriatria e pediatria. Além disso, pacientes que sofrem de disfagia, enjoo de movimento, emese repetida e distúrbios mentais preferem estes medicamentos porque não podem engolir grande quantidade de água. Além disso, os fármacos que exibem absorção satisfatória a partir da mucosa oral ou que se destinam a ação farmacológica imediata podem ser vantajosamente formulados nestas formas de dosagem. No entanto, a formulação destas formas farmacêuticas exige-lhes resistência mecânica suficiente para suportar os rigores do manuseio e capacidade de desintegrar dentro de alguns segundos em contato com a saliva. O objetivo desta pesquisa foi o de mascarar o gosto amargo de cloridrato de granisetrona. Para mascarar o sabor, utilizou-se Kollicoat smartseal 30D como polímero para io revestimento dos péletes. Os péletes revestidos do fármaco foram diretamente comprimidos com superdesintegrante diferente como Ac-Di-Sol, Explotab e Kollidon CL, em diferentes concentrações 5.0-7.5% m/m em comprimidos de dispersão oral (ODT). Os comprimidos preparados foram avaliados quanto à dureza, friabilidade, variação de peso, ao tempo de umedecimento, à razão de absorção de umidade, ao tempo de desintegração in vitro e em estudos de dissolução in vitro. Os comprimidos apresentaram características de desintegração rápida com Kollidon CL, em concentração de 7,5% m/m, ou seja, dentro de 20 segundos, o que é característico para formas farmacêuticas de desintegração oral. Mais do que 98% do fármaco foi liberado a partir das formulações no prazo de 15 minutos. Formulações submetidas a testes de estabilidade de acordo com as diretrizes da ICH por 3 meses indicaram estabilidade sem alteração no sabor, dureza, teor de fármaco, tempo de desintegração e perfis de dissolução. Assim, os resultados demonstraram que o mascaramento de gosto foi bem-sucedido e atingiu-se rápida desintegração das formas de dosagem na cavidade oral.

Oral Strip Technology: A review.

Over the recent past, many of the research groups are focusing their research on this technology. Amongst Oral drug delivery system Oral Strip Technology (OST) is gaining much attention. The advantages of OST are the administration to pediatric and geriatric patient population where the difficulty of swallowing larger oral dosage forms is eliminated. This technology has been used for local action, rapid release products and for buccoadhesive systems that are retained in the oral cavity to release drug in controlled fashion. OST offers an alternate platform for molecules that undergo first pass metabolism and for delivery of peptides. An ideal OST should have the following properties: high stability, transportability, ease of handling and administration, no special packaging material and/or processing requirements, no water necessary for application, and a pleasant taste. All these requirement are fulfilled by the oral films. The OST is a good tool for product life cycle management for increasing the patent life of existing molecules or products. Compared to some of the complicated and expensive process (like lyophilization) used to manufacture ODTs(Orally Disintegrating Tablets), the OST is relatively easy to fabricate,thus reducing the overall cost of the therapy. One of the reasons is that the buccal mucosa is less permeable and is thus not able to elicit a rapid onset of absorption and hence better suited for formulations that are intended for sustained release action. Further, the buccal mucosa being relatively immobile mucosa and readily accessible, it makes it more advantageous for retentive systems used for oral trans mucosal drug delivery. The primary disadvantage associated with buccal delivery route is the low flux that in turn results in low drug bioavailability. To overcome this hurdle, various buccal penetration enhancers have been studied which improve the absorption pattern of the molecules. The article shows OST encompassing materials used in OST, method of preparation, evaluation, applications, commercial technologies and future Business prospects of this technology.

Micromeritic evaluation of the direct compression excipient Parteck® ODT for orally disintegrating tablets / 中国药学杂志

OBJECTIVE: To evaluate the micromeritic properties of Parteck® ODT to provide preliminary theoretical basis for the direct compression technology of orally disintegrating tablets (ODTs).

Formulation and Evaluation of Oral Disintegrating Tablets of Lornoxicam by 3² Factorial Design.

Oral disintegrating dosage form provides an opportunity to manufacturers to extend product life cycle and to expand market. Oral disintegrating tablets (ODT) have this opportunity over conventional tablets. Lornoxicam is non steroidal anti-inflammatory drug and used in treatment of post traumatic pains, muscular and skeletal pains, joint disorder and rheumatic arthritis. Fast onset of action is required in these indications. Therefore it was thought to prepare ODT of Lornoxicam which would help to avoid first pass metabolism and to improve bioavailability as well. ODT were prepared by direct compression method by using crospovidone as superdisintegrating agent and optimized by 32 factorial design. Independent variables were concentration of crospovidone (X1) and hydroxypropyl cellulose (X2) while dependent variables were disintegration time and percent drug released. Optimised formulation, F4, showed drug content (97.90±0.37%), disintegration time (20.33±0.317 sec), percent drug released (101.5±0.59%), water absorption ratio (113.5±1.26%). This formulation was stable at 400C ±20C and RH 75%±5% for three months. Present study demonstrated potential for rapid absorption, improved bioavailability, effective therapy and patient compliance.

Formulation Development and Evaluation of Acyclovir Orally Disintegrating Tablets.

Orally disintegrating systems have an edge amongst the oral drug delivery systems due to the highest component of compliance they enjoy in patients especially the geriatrics and pediatrics. In addition, patients suffering from dysphagia, motion sickness, repeated emesis and mental disorders prefer these medications because they cannot swallow large quantity of water. Further, drugs exhibiting satisfactory absorption from the oral mucosa or intended for immediate pharmacological action can be advantageously formulated in these dosage forms. However, the requirements of formulating these dosage forms with mechanical strength sufficient to withstand the rigors of handling and capable of disintegrating within a few seconds on contact with saliva are inextricable. Therefore, research in developing orally disintegrating systems has been aimed at investigating different excipients as well as techniques to meet these challenges. Acyclovir is an antiviral drug used for the treatment of herpes simplex virus (HSV), mainly HSV-1 and HSV-2 and varicella zoster virus. It is a BCS class III drug. Hence an orally disintegrating tablet formulation of acyclovir was prepared by direct compression and wet granulation techniques after incorporating superdisintegrants croscarmellose sodium and sodium starch glycolate. Seven formulations were prepared. Tablet containing sodium starch glycolate showed excellent in vitro dispersion time and drug release as compared to other formulation. After study of seven formulations DT3 showed short dispersion time with maximum drug release in 10 min. It is concluded that fast disintegrating acyclovir tablets could be prepared by direct compression using superdisintegrants.

An unlimited scope for novel formulations as orally disintegrating systems: Present and future prospects.

An orally disintegrating tablet or orodispersible tablet (ODT) is a drug dosage form available for a limited amount of over-the-counter (OTC) and prescription medications. ODTs differ from traditional tablets in that they are designed to be dissolved on the tongue rather than swallowed whole. The ODT serves as an alternative dosage form for patients who experience dysphasia (difficulty in swallowing) or for where compliance is a known issue and therefore an easier dosage form to take ensures that medication is taken. Common among all age groups, dysphasia is observed in about 35% of the general population, as well as up to 60% of the elderly institutionalized population and 18-22% of all patients in long-term care facilities. During the last decade, ODTs have become available in a variety of therapeutic markets, both OTC and by prescription. An additional reason to use ODTs is the convenience of a tablet that can be taken without water.