Preparation and pharmacodynamic study of Oral Disintegration Tablets of "Hugan I" / 中草药

Objective: To optimize the prescription and preparation process of "Hugan I" Orally Disintegrating Tablets, and investigate its efficacy against acute liver injury in mice. Methods: Single factor method was used for disintegrants, lubricants, and fillers screening. Taking the appearance, hardness, friability and disintegration time of the tablets as the comprehensive evaluation index, the dosage of disintegrant, micro-silica gel and magnesium stearate was selected as the investigation factor. The Box-Behnken response surface method was used to optimize the orally disintegrating tablets. Acetaminophen (APAP, 500 mg/kg) was used to replicate acute liver injury model by one-time high-dose intragastric administration to investigate the effects of orally disintegrating tablets on the activities of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in serum, the content of glutathione (GSH) and malondialdehyde (MDA) and morphological changes in liver tissue. Results: The optimal prescription was as following: dry paste powder 22.00%, microcrystalline cellulose 18.00%, sorbitol 20.00%, mannitol 16.00%, Aspartame 0.50%, citric acid 0.50%, disintegration agent L-HPC 20.00%, micro-powder silica gel 2.50% and magnesium stearate 0.50%. The hardness of the orally disintegrating tablets was 4-7 kg, the mean disintegration time was about 50 s, and the mean friability was around 0.85%. Compared with the model group, there were significant differences (P < 0.01) in Biphenyl diester control group, "Hugan I" Decoction group and "Hugan I" Orally Disintegrating Tablets group, and the levels of ALT and AST in the serum of the mice were significantly decreased, The content of MDA in the liver tissue was decreased, which improved the damage of APAP to liver tissue. Conclusion: The formulation of the "Hugan I" Orally Disintegrating Tablet is feasible and easy to operate, which achieves the same effect with "Hugan I" Decoction that effectively prevent liver damage caused by acetaminophen with no significant differences.

Study on the Preparation of Lansoprazole Enteric-coated Pellets Orally Disintegrating Tablets / 中国药师

Objective:To prepare lansoprazole enteric-coated pellets and compress them into orally disintegrating tablets , and e-valuate the acid resistance in the acid stage and the in vitro dissolution in the buffer stage .Methods:Lansoprazole enteric-coated pel-lets were prepared by fluid bed coating technology , and the effects of the ratio of methacrylic acid copolymer dispersion to ethyl acrylate–methyl methacrylate copolymer dispersion , the concentration of triethyl citrate and the main pressure on the acid resistance in the acid stage and the in vitro dissolution in the buffer stage were evaluated .The similarity of the self-prepared orally disintegrating tablets and the reference preparation was evaluated by using f 2 similarity factor method .Results:The average particle size of microcrystalline cellulose core was 150-180 μm, the ratio of methacrylic acid copolymer dispersion to ethyl acrylate –methyl methacrylate copolymer dispersion was adjusted to 8:2, the enteric-coated weight was 30％, 20％triethyl citrate was used and the main pressure was controlled within the range of 10-16 kN.Lansoprazole enteric-coated pellets had sufficiently flexibility and stability against the compression force . The enteric coating did not break , showing good acid resistance .The dissolution similarity factor of the self-prepared orally disintegra-ting tablets and the reference preparation was greater than 50.Conclusion: Lansoprazole enteric-coated pellets orally disintegrating tablets have good acid resistance and high similarity for the in vitro dissolution, which can be further amplified .

Research Progress on orally disintegrating tablets of Chinese materia medica / 中草药

Orally disintegrating tablets is a special tablet that can disintegrate rapidly in the mouth without taking with water. It has the advantages of rapid disintegration, high bioavailability, convenient utilization and so on. The orally disintegrating tablets of Chinese materia medica (CMM) have developed rapidly in recent years, which provides a new way of thinking for the treatment of acute diseases. At the same time, the orally disintegrating tablets of CMM are faced with many problems, such as poor taste, slow disintegration, imperfect quality evaluation system and so on. In this paper, we reviewed the development status, preparation technology, main problems, and quality evaluation from the related literatures of orally disintegrating tablets in recent years, so as to provide references for further research of orally disintegrating tablets of CMM.

Optimization of prescriptions for Yuanhu Zhitong Orally Disintegrating Tablets based on central composite design-response surface methodology / 中草药

Objective To optimize the best prescription of Yuanhu Zhitong Oral Disintegrating Tablets (YZODT). Methods Using the single factor test, the prescription of the tablets was optimized by central composite design-response surface methodology (CCD-RSM) with the tablet wetting time and the disintegration time limit as evaluation index, so as to determine the best preparation process. Results The dosages of the optimized prescription of MCC, L-HPC, and PVPP were 30%, 15%, and 5%, respectively. The average disintegration time of the optimized YZODT was 42.89 s, and the deviation from the predicted value was 3.27%. Conclusion The optimized YZODT has the advantages of fast disintegration, moderate hardness, convenient use, and simple process.

Preparation of Dexzopiclone Orally Disintegrating Tablets and Formulation Optimization / 中国药房

OBJECTIVE:To prepare Dexzopiclone orally disintegrating tablets (DODT),and to optimize its formulation.METHODS:Direct powder compression method was used to prepare DODT.Using repose angle of material,disintegration time and taste evaluation as indexes,single factor test was used to screen the types or amount of bulking agent,disintegrating agent,glidant and flavoring agent;using disintegration time as index,orthogonal experiment was applied to optimize the proportion of bulking agent,the amount of disintegrating agent,glidant and flavoring agent.Then the hardness and main component contents of DODT prepared by optimal formulation were determined.RESULTS:The optimal formulation was as follows as the ratio of mannitol-MCC 1 ∶ 4,the amount of disintegrating agent PVPP was 15％,the amount of glidant magnesium stearate was 1.0％,the amount of flavoring agent stevia was 3.0％.Three batches of prepared DODT were smooth in surface and good in taste;their disintegration time were(26.7 ± 1.2),(26.7 ± 0.6),(27.6 ± 0.9)s,hardness were (3.59 ± 0.19),(3.49 ± 0.18),(3.27 ± 0.16) kg,and contents were (99.47 ± 0.15) ％,(99.53 ± 0.05)％,(99.46 ± 0.20) ％,respectively (all RSDs≤0.87％,n=3).CONCLUSIONS:Prepared DODT are all in line with the quality requirements of orally disintegrating tablets.

Preparation and Quality Evaluation of Vardenafil Hydrochloride Orally Disintegrating Tablets / 医药导报

Objective To prepare vardenafil hydrochloride orally disintegrating tablets and evaluate their quality. Methods The tablets were prepared by direct power compression method, using crosslinking povidone ( PVPP ) as disintegrants. The preparation method was optimized by response surface test using amount of PVPP, menthol and taste-masking agents as factors with disintegrating time and distance of bitterness as index. The results of taste of orally disintegrating tablets were determined by electronic tongue, comparing to the results of taste tests. At the same time, the properties of the tablets were evaluated using appearance, content uniformity, disintegrating time, et al. as index. Results The optimal formula was as follows:PVPP 13. 26%, menthol 0. 43%, taste-masking agent SGxj 1. 26%. The results on evaluation of electronic tongue were consistent with the results of taste tests. The quality of the prepared tablets was in line with standard. The disintegrating time was (22. 34 ± 0. 34 ) s. Conclusion The preparation technology of orally disintegrating tablets is simple, and controllable in quality.

Observation efficacy and side effects of risperidone orally disintegrating tablets combined with oxazepam in schizophrenia / 中国生化药物杂志

Objective To investigate the efficacy and adverse reactions of risperidone orally disintegrating tablets joint oxazepam in the treatment of schizophrenia.Methods 63 patients with schizophrenia were selected and divided into two groups according to the order of admission Divided into the control group ( 31 cases ) and observation group ( 32 cases ) , were treated with chlorpromazine +alprazolam and risperidone orally disintegrating tablets+oxazepam.The two groups after treatment PANSS score, quality of life SF-36 health questionnaire score and ADL score before and after treatment, curative effect and adverse reactions were recorded and compared.Results The different PANSS score after treatment and compared, the observation group with different symptoms score and general psychopathology scores are significantly lower than the control group , the difference was statistically significant (P<0.05), the two groups after treatment ADL score compared with those before treatment were significantly increased, and the score of the observation group after treatment was significantly higher than the control group, the difference was statistically significant (P<0.05), the curative effect of observation group was 93.75%, significantly higher than the control group 77.42%, the difference was statistically significant ( P<0.05), quality of life questionnaire SF-36 score and one months after treatment, observation group scores were significantly higher than those in control group, the difference was statistically significant ( P <0.05), there were some adverse reactions in the two groups, the adverse reaction rate of observation group was 9.38%, significantly lower than 45.15%of the control group, the difference was statistically significant ( P <0.05 ) . Conclusion The implementation of schizophrenia risperidone orally disintegrating tablets oxazepam effect significantly , can better improve the clinical symptoms of patients, improve the patient's ability of daily life and quality of life.It can effectively reduce the occurrence of adverse reactions, and is a safe and effective treatment.

Development and evaluation of mosapride citrate orally disintegrating tablets for dogs / Desenvolvimento e avaliação de comprimidos de desintegrados de citrato demosaprida para cães por via oral

ABSTRACT: The purpose of the study was to prepare orally disintegrating tablets (ODTs) of mosapride citrate for dogs with fast disintegration and low cost. The ODTs were developed by varying the components and the ratio of excipients. A direct compression method was used. The properties of the ODTs, including hardness, friability, active ingredient content, and in vitro disintegration time, were investigated, and an economic analysis of the formulations was performed. For all formulations, friability was less than 1%, and the hardness varied from 37.69±4.08 to 48.73±5.62 N, which indicated that the tablets had sufficient mechanical integrity to withstand packaging and carrying. Results showed that Formulation (F) 2, containing 5% sodium carboxymethyl starch; F3, containing 5% low-substituted hydroxypropylcellulose; and F5 had not only shorter disintegration times but also lower costs, which were suitable for mosapride citrate ODTs. Although F1, contained 5% croscarmellose sodium, and F4, contained 5% crospovidone, with shorter disintegration times, the costs of F1 and F4 were 25.8% and 22.6% higher than that of F5, respectively. Results also revealed that the disintegration time of F5 was not significantly different from those of F1, F2, F3, and F4 (p>0.05), all of which contained superdisintegrants. Without superdisintegrants, F5, which contained a mixture of microcrystalline cellulose, mannitol, and lactose, was also able to achieve a short disintegration time and to meet the requirements of ODTs for dogs.

RESUMO: O objetivo do estudo foi o de preparar os comprimidos por via oral de desintegração (ODTs) de citrato de mosaprida para cães com desintegração rápida e de baixo custo. Os ODTs foram desenvolvidos através da variação dos componentes e proporção de excipientes. Um método de compressão direta foi utilizado. As propriedades dos ODTs, incluindo dureza, friabilidade, o teor de ingrediente ativo e no tempo de desintegração in vitro foram investigados e, adicionalmente, uma análise econômica das formulações foi realizada. Para todas as formulações, friabilidade foi inferior a 1%, a dureza e variou de 37,69 ± 4,08-48,73 ± 5,62 N, o que indica que os comprimidos tinham integridade mecânica suficiente para suportar a embalagem e transporte. Os resultados mostraram que a formulação (F) 2, contendo 5% de amido de carboximetilo de sódio, F3, contendo 5% de hidroxipropil celulose de baixa substituição, e F5 não só tiveram menores tempos de desintegração mas também preços mais baixos, que foram adequados para ODTs de citrato de mosapride. Embora F1, continha 5% de croscarmelose de sódio, e F4, continha 5% de crospovidona, com tempos de desintegração mais curtos, os custos de F1 e F4 eram 25,8% e 22,6% mais elevado do que a F5, respectivamente.. Os resultados também revelam que o tempo de desintegração de F5 não foi significativamente diferente do de F1, F2, F3, e F4 (P> 0.05), todas as quais contêm superdesintegrantes. Sem superdesintegrantes, F5, que contêm uma mistura de celulose microcristalina, manitol e lactose também foi capaz de conseguir um curto tempo de desintegração e satisfaz os requisitos de ODTs para cães.

Orally disintegrating tablets based on lyophillization technology:research advances / 国际药学研究杂志

The orally disintegrating tablets(ODT)are the kinds of novel oral dosage forms which begin to gain popularity and acceptance since they can disintegrate/dissolve quickly in the oral cavity upon contact with saliva ,resulting in solutions or suspensions form of the administered medicine. The ODTs are perfect alternative for pediatric and geriatric patients with difficulty in swallowing , and uncooperative patients because of their convenience of self-administration and compactness. This communication reviews the appli?cations and technologies involved in formulation feature,lyophillization process,excipients selection,fast dissolving mechanism,and determination of disintegration time.

Preparation and quality evaluation of resveratrol orally disintegrating tablets / 中草药

Objective: The process of preparing resveratrol orally disintegrating tablets was researched, the best prescription was determined and the quality of resveratrol orally disintegrating tablets about dissolution and micromeritics were evaluated. Methods: The optimal prescription of direct powder compression method was determined by adopting Box-Benhnken center combination experiment design, with universal evaluation indexes, including disintegration time, mouthfeel, and hardness. The accumulative dissolution was tested by using dissolution test. The micromeritics about the angle of repose, loose density, tap density, and compressibility index were evaluated. Results: The optimal prescription were 50 mg resveratrol (22.5%), 63.5 mg MCC (28.6%), 18.6 mg PVPP (8.4%), 10 mg L-HPC (4.5%), 78 mg (35.1%), and 2 mg magnesium stearate (0.9%). The disintegration time of resveratrol orally disintegrating tablets prepared with the optimized prescription was qualified. More than 90% resveratrol was dissoluted within 10 min. The micromeritics showed that the powder had good fluidity and filling property. Conclusion: The process of preparation for orally disintegrating tablets by using direct compression method is feasible, it is easy to operate, and this method can meet the requirement in industry.

Orally disintegrating tablets based on lyophillization technology : Research advances / 国际药学研究杂志

The orally disintegrating tablets (ODT) are the kinds of novel oral dosage forms which begin to gain popularity and acceptance since they can disintegrate/dissolve quickly in the oral cavity upon contact with saliva, resulting in solutions or suspensions form of the administered medicine. The ODTs are perfect alternative for pediatric and geriatric patients with difficulty in swallowing, and uncooperative patients because of their convenience of self-administration and compactness. This communication reviews the applications and technologies involved in formulation feature, lyophillization process, excipients selection, fast dissolving mechanism, and determination of disintegration time.

Preparation of Stemoninine Orally Disintegrating Tablets / 中国药房

OBJECTIVE:To prepare Stemoninine orally disintegrating tablets,and to optimize its formulation and preparation technology. METHODS:Direct powder compression method was used to prepare Stemoninine orally disintegrating tablets. Using material angle of repose,disintegration time and taste evaluation as index,single factor test was used to screen several factors as bulking agent,disintegrating agent,glidant and flavoring agent;using disintegration time as index,L9(34) orthogonal test was used to optimize the formulation with ratio of MCC+mannitol,PVPP,silica powder and aspartame+stevia as factors. Validation test was also conducted. RESULTS:Optimized formulation was that MCC+mannitol(1∶1)was 50%,PVPP was 20%,silica powder was 2% and aspartame+stevia(10∶1)was 7%. 3 batches of prepared Stemoninine orally disintegrating tablets were smooth in sur-face and good in taste;their disintegrating time was(22.6±2.1)s,and weight variation,hardness,contents were within the speci-fied range (all RSD≤0.97%,n=3). CONCLUSIONS:The formulation and technology of Stemoninine orally disintegrating tab-lets are reasonable,and the quality indexes are all in line with the requirements of orally disintegrating tablets.

Formulation and evaluation of orally disintegrating clopidogrel tablets

ABSTRACT Recent advances in drug delivery systems have aimed to achieve better patient compliance. One of these advances is the formulation of orally disintegrating tablets (ODTs) that dissolve instantaneously, releasing drugs within a few seconds without the need of water. The main objective of this paper was to prepare and develop ODTs of clopidogrel. The ODTs were prepared by direct compression. The effect of three superdisintegrants, namely crospovidone, croscarmellose sodium, and sodium starch glycolate, using three different disintegration times on the dissolution rate was investigated. The prepared tablets were evaluated for hardness, friability, disintegration time and in vitro drug release. Furthermore, the interaction of clopidogrel with the formulation excipients was studied using differential scanning calorimetry (DSC). DSC studies revealed that there were no interactions between the drug and the excipients used. All tablets had hardness values in the range 4.0-5.2 kp and friability lower than 1%. The weight and drug content uniformity of all formulations was within official limits according to BP. In vitro drug release studies of the ODTs showed that more than 90% of the drug was released within ten minutes. A palatability test in human volunteers showed acceptable taste and mouth feel. Thus, the obtained results conclusively demonstrated successful rapid disintegration of the formulated tablets and acceptable palatability.

RESUMO Recentes avanC'os em sistemas de liberaC'C#o de fC!rmacos novos visam C obtenC'C#o de melhor adesC#o do paciente. Um destes avanC'os C) a formulaC'C#o de comprimidos de desintegraC'C#o oral (ODTs), que se dissolvem instantaneamente, liberando o fC!rmaco, em alguns segundos, sem a necessidade de C!gua. O principal objetivo deste trabalho foi preparar e desenvolver ODTs de clopidogrel. Os ODTs foram preparados pelo mC)todo de compressC#o direta. Estudou-se o efeito de vC!rias concentraC'C5es de diferentes agentes de desintegraC'C#o, tais como super-crospovidona, croscarmelose de sC3dio, glicolato de amido de sC3dio no tempo de desintegraC'C#o e velocidade de dissoluC'C#o. Os comprimidos preparados foram avaliados quanto C dureza, C friabilidade, ao tempo de desintegraC'C#o e C liberaC'C#o do fC!rmaco in vitro. AlC)m disso, estudou-se a interaC'C#o de clopidogrel com os excipientes de formulaC'C#o, utilizando calorimetria de varredura diferencial (DSC). Estudos de DSC revelaram nC#o haver interaC'C#o entre o fC!rmaco e os excipientes utilizados. Todos os comprimidos possuC-am dureza na faixa de 4,0-5,2 kp e a friabilidade inferior a 1%. A variaC'C#o de peso e o teor de fC!rmaco de todas as formulaC'C5es mostraram-se dentro do limite oficial, de acordo com a BP. O estudo de liberaC'C#o do fC!rmaco in vitro de comprimidos ODTs mostrou que mais de 90% do fC!rmaco foram liberados em10 minutos. O teste de palatabilidade em voluntC!rios humanos mostrou sabor e sensaC'C#o na boca aceitC!veis. Assim, os resultados obtidos demonstraram, conclusivamente, a rC!pida e bem-sucedida desintegraC'C#o dos comprimidos formulados e a palatabilidade aceitC!vel.

Preparation and in vitro Release of Metoclopramide Orally Disintegrating Tablets / 中国药师

Objective:To prepare and optimize the formula of metoclopramide orally disintegrating tablets, and investigate the in vitro drug dissolution behavior. Methods:The formula was optimized by full-factorial experiment design, the ratio of mannotil to micro-crystalline cellulose ( X1 ) and the amount of disintegrating agent ( X2 ,%) were selected as the independent variables, and the friabili-ty ( Y1 ,%) , disintegration time ( Y2 , s) and metoclopramide dissolution ( Y3 ,%) were used as the dependent variables. The release rate of metoclopramide orally disintegrating tablets in different dissolution media was studied. Results:The optimum formula of meto-clopramide orally disintegrating tablets was as follows:the ratio of mannotil to microcrystalline cellulose was 2. 5∶ 1, and the amount of disintegrating agent was 6. 5%. The dissolution of metoclopramide orally disintegrating tablets in the different dissolution media was o-ver 80%. Conclusion:The formula design is reasonable, the preparation process is feasible and the quality can be controlled.

Preparation optimization of palonosetron hydrochloride oral disintegrating tablets by orthogonal test / 重庆医学

Objective To prepare optimization of palonosetron hydrochloride oral disintegrating tablets by orthogonal test. Methods Palonosetron hydrochloride oral disintegrating tablets were prepared with direct compression process.The content of pal-onosetron hydrochloride was determined by HPLC.The formulation was optimized with disintegration time as evaluation indices. Results The optimal formulation(60 mg/tablet)was as follows:L-HPC 12%,mannitol∶SMCC= 2∶1,magnesium stearate 2%, stevia glycosides 3%.The oral disintegrating tablets showed dine appearance and tested better;the disintegration time was 12 sec-onds;the tablets featured a hardness of 3 kg;4 min dissolution rate was 99%.Conclusion The preparation method is simple and reasonable,and the tablets can disintegrate rapidly.

Fast mouth dissolving disintegrating tablet and patient counseling points for FDDTs - A Review.

Recent developments in technology have presented viable dosage alternatives for patients who may have difficulty swallowing tablets or liquids. Traditional tablets and capsules administered with an 8-oz. glass of water may be inconvenient or impractical for some patients. For example, a very elderly patient may not be able to swallow a daily dose of antidepressant. An eight-year-old with allergies could use a more convenient dosage form than antihistamine syrup. A schizophrenic patient in the institutional setting can hide a conventional tablet under his or her tongue to avoid their daily dose of an atypical antipsychotic. A middle-aged woman undergoing radiation therapy for breast cancer may be too nauseous to swallow her H2-blocker. The convenience of administration and improved patient compliance are important in the design of oral drug delivery system which remains the preferred route of drug delivery inspite of various disadvantages. One such problem can be solved in the novel drug delivery system by formulating “mouth dissolving tablets” (MDTs) which disintegrates or dissolves rapidly without water within few seconds in the mouth due to the action of super-disintegrant or maximizing pore structure in the formulation. The review describes the various formulation aspects, technologies developed for MDTs, marketed formulation and drugs used in this research area.

Orally disintegrating tablets: An overview.

Orally disintegrating tablets (ODTs) have greatly increased dosage forms which have remarkable impact on the patient compliance especially for the pediatric, geriatric and psychiatric patients with deglutition disorders. Several technologies either conventional or patented based on freeze drying/lyophilization, spray drying, moulding, phase transition process, melt granulation, sublimation, mass extrusion, cotton candy process, direct compression etc. have been developed for manufacturing of ODTs. In this review brief information about ODTs including definition, ideal and desired characteristics, advantages, limitations and disadvantages, drug canditates, challenges in formulation, excipients with recent developments in superdisintegrants, tast masking, manufacturing techniques, evaluation parameters and recent patents in ODTs are presentented.

Preparation and Stability of Mirtazapine Orally Disintegrating Tablets / 中国药师

Objective:To optimize the formula of mirtazapine orally disintegrating tablets by orthogonal experiment and determine the stability preliminarily. Methods:The formula was optimized by orthogonal experiment based on 4 impacting factors:the amount of mannotil (A), microcrystalline mellulose (B), low substituted hydroxypropyl cellulose (C) and cross-linked polyvinylpyrrolidone ( D) , respectively with 2 indices of disintegration time and dissolution. The release rate of the orally disintegrating tablets and the ref-erence tablets was studied by similarity factors. The stability was respectively studied by high temperature test, high humidity test and photostability test. Results:The optimum formula of the tablets was as follows:the amount of A, B, C and D was 70, 20, 2. 5 and 10 mg, respectively. The f2 for the orally disintegrating tablets and the reference tablets in the dissolution medium was 63. 38. Conclu-sion:The formula is reasonable, the preparation process is feasible and the quality is stable.

Study on Quality Standard for Fufang Tianma Gouteng Orally Disintegrating Tablets / 中国中医药信息杂志

Objective To establish the quality standard of Fufang Tianma Gouteng Orally Disintegrating Tablets. Methods Gastrodiae Rhizoma, Uncariae Ramulus Cum Uncis, Angelicae Sinensis Radix and Paeoniae Radix Alba in the preparation were identified by TLC, the content of gastrodin in gastrodia was determined by HPLC. Results The herbs of preparation could be identified by TLC without interference. Gastrodin showed a good linear relationship in the range of 0.191 2-1.147 2 μg (r=0.999 9). The average recovery was 97.72% (RSD=1.40%, n=6). Conclusion The methods are available with a good reproducibility, and can control the quality of the preparation effectively.