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.

Formulation and evaluation of fast dissolving tablets of Granisetron hydrochloride by vacuum drying technique.

The purpose of this investigation was to develop fast dissolving tablets (FDTs) of Granisetron hydrochloride (GHCl) by vacuum drying technique using camphor as subliming agent together with croscarmellose sodium (CCS), crospovidone (CP), sodium starch glycolate (SSG) and plantago ovate (PO) as superdisintegrants. The prepared formulations were evaluated for pre-compressional and post-compressional parameters. The compatibility of drug with other ingredients was checked by FTIR studies, the results revealed that there was no interaction between dug and other excipients. The values of pre-compressional parameters were within prescribed limits and indicated good free flowing properties. In all the formulations the hardness test indicates good mechanical strength. Friability of all formulations was less than 1. Drug content was found to be high (≥ 100.44%) and uniform in all the formulations. The tablet thickness was found to be 3.11 – 3.34. The weight variation results revealed that average percentage deviation was less then ± 7.5 %, which provides good uniformity in all formulations. The disintegration time of the tablets found to be in the range of 18 to 44 sec. The formulations SBC4, SBP4, SBG4, and SBO4 50 % of drug released in 0.41, 0.48, 0.59 and 0.47 min, and 90 % of drug released in 2.01, 3.05, 4.01 and 2.51min. Stability study carried out as per ICH guidelines for three months and results revealed that upon storage disintegration time of tablets decreased significantly (p<0.05). The release of drug from the SBC4 and SBO4 formulations was quick when compared to other formulations. It was concluded that fast dissolving tablets with improved Granisetron hydrochloride dissolution could be prepared by sublimation of tablets containing suitable subliming agent.

Formulation and evaluation of fast dissolving tablets of granisetron hydrochloride.

Fast dissolving drug delivery systems offers a solution for those patients having difficulty in swallowing tablets/capsules etc. Granisetron hydrochloride was selected as the model drug. In the present study, an attempt had been made to prepare fast dissolving tablets of the drug using , plantago ovata mucilage and sodium starch glycolate as super disintegrants (2.5 to 10 % w/w) following by direct compression method. Formulations were evaluated for precompressional parameters such as angle of repose, carr’s compressibility index and hausner’s ratio. The tablets were evaluated for uniformity of weight, thickness, hardness, friability, drug content, wetting time, in-vitro dispersion time and in-vitro dissolution study. The prepared tablets were characterized by FTIR studies. No chemical interaction between drug and exciepients was confirmed by FTIR studies.

Rotating magnetic fields and granisetron treatment for preventing nausea and vomiting induced by chemo-therapy / 中华物理医学与康复杂志

Objective To observe the efficacy of a rotating magnetic field and granisetron hydrochloride in preventing nausea and vomiting caused by a eisplatin regimen, and any side effects. Methods Sixty-eight patients receiving cisplatin regimen chemotherapy were randomly assigned to two groups: a magnetic treatment group and a drug treatment group. The patients in the two groups were exposed to a rotating magnetic field or received granisetron hydrochloride, respectively. The effects of the treatments were observed. Results Both treatments could effectively prevent and treat the vomiting caused by chemotherapy. The rate of response to the rotating magnetic field was 88.2% and to the drug 91.2%. However, tardive vomiting was significantly better controlled in the rotating magnetic field group. The incidence of side effects in the magnetic field group was 20.6% , and in the drug treatment group it was 45.6%. Conclusion The efficacy of a rotating magnetic field and granisetron in treating acute vomiting were simi- lar. The rotating magnetic field was more effective in preventing tardive vomiting and had fewer side effects. Magnetic therapy should be more generally applied in clinical practice.

Preparation and Quality Control of Granisetron Hydrochloride Nasal Spray / 中国药房

OBJECTIVE:To prepare granisetron hydrochloride nasal spray and establish a method for its quality control. METHODS: Granisetron hydrochloride nasal spray was prepared using granisetron hydrochloride as chief ingredient and its content was determined by UV spectrophotometry. RESULTS: Spray appeared as colorless or yellowish supernatant liquid and it was up to the standard specified in Chinese Pharmacopeia (2005 edition). The linear range of granisetron hydrochloride was 105.9～635.4 ?g?mL-1 (r=0.999) and its average recovery rate was 100.1% (RSD=0.4%). CONCLUSION: The preparation is simple and feasible in preparation process and its quality is controllable.

Intervention Effects of Granisetron Hydrochloride on Vasovagal Syncope in Rabbits / 实用儿科临床杂志

Objective To study the effects of granisetron hydrochloride on vasovagal syncope(VVS) in rabbits.Methods Twenty-four healthy New Zealand rabbits were divided stochastically into control group and intervention group,12 in each group. The control group was injected intravenously with normal saline. The intervention group was injected intravenously with granisetron hydrchloiride.Rabbit VVS models were established,each was taken at 4 points in time in the bloodletting process:T1,T2,T3,T4,to compare the bloodletting time,the concentration of 5-hydroxytryptamine(5-HT) in T2,T3,T4 and the total blood volume between the groups,and monitor the heart rate, blood pressure during the entire process.Results 1.The time of intervention group in T2,T3,T4 was longer than the time of control group obviously(P

Clinical Study of Granisetron Against Postoperative Nausea and Vomiting Under Patient Controlled Analgesisa / 中国药房

OBJECTIVE:To study the therapeutic effect of granisetron on postoperative nausea and vomiting(PONV) under patient controlled analgesia(PCA) and to observe the influence of infusion rate of granisetron on blood circulation during operation METHODS: 90 selective surgical patients were divided into 3 groups A group(control):ondonsetron 8mg;B group:tropiestron 3mg; C group:granisetron 3mg The solutions of granisetron hydrochloride were infusied at 20,30,40,50 and 60 min before the end of operation The change of the circulation condition and the status of nausea and vomiting were observed at infusion period and 4,8,12,24hs,2d and 3d postoperatively RESULTS:Under expansion of blood volume,if infusion duration was longer than 20 min for granisetron,the circulation condition(MAP,HR) were not affected during infusion period and no headache was found There were significant differences in PONV between group A and group B(P