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Objective To optimize the formulation and preparation of diphenhydramine hydrochloride and caffeine orally disintegrating tablet. Methods Melt granulation technology of steric acid and API was used to mask the unpleasant tasting of diphenhydramine hydrochloride. The tablets were prepared by direct pressing the dry powder with CCMC-Na as disintegrating agent. The formulation was optimized by orthogonal experiments to achieve the shortest disintegration time and the best taste correction. Results The optimized formula of orally disintegrating tablet was as follows： diphenhydramine hydrochloride 25 mg, caffeine 60 mg, stearic acid 25 mg, aspatan 40 mg, blueberry essence 7 mg, mannitol 45 mg, MCC 210 mg, CCMC-NA 25 mg, SDS 8 mg and magnesium stearate 5 mg. Conclusion This preparation method for orally disintegrating tablet of diphenhydramine hydrochloride and caffeine is practical and easy for quality control.
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OBJECTIVE: To investigate the taste-masking effect of montelukast sodium orally disintegrating tablets using electronic tongue technology and human sensory evaluation and determine the optimum formulation. METHODS: Orally disintegrating tablets were prepared with five different concentrations of flavoring agents or without flavoring agent.The tastes of those tablets were determined by electronic tongue, and principal component analysis and linear discriminant analysis were used to evaluate differences of different formulations. The taste-masking effect of the tablets was investigated combined with electronic tongue analysis and sensory evaluation of subjects. RESULTS: The taste of orally disintegrating tablet was the best when the total amount of flavoring agent was 1.6 mg, and the ratio of sweetening agent to aromatic agent was 5∶3. CONCLUSION: The combination of electronic tongue and human sensory assess can evaluate the taste-masking effect of orally disintegrating tablets and provide the basis for determining the optimum formulation.
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Objective: Chlorpheneramine maleate is a first-generation antihistamine drug used in the treatment of allergic conditions like rhinitis, urticaria, and cough cold, etc. In present work, the challenge has been made to develop an orally disintegrating tablet of chlorpheneramine maleate with an increase in bioavailability and patient compliance. Methods: The sublimation technique was used to prepare orally disintegrating tablets. Porous tablet prepared after sublimation of camphor at 60 °C in a hot air oven for 60 min. In the research work, 32full factorial design used to find out the effect of two variables like the amount of Crospovidone and Croscarmellose sodium. Results: All prepared formulations were analyzed for various parameters. DSC of pure drug and optimized formulation A (9) showed purity of sample and compatibility of all ingredients with each other. In FTIR study of pure drug and optimized formulation A (9) no major shifts were seen. An optimized formulation (A9) was found to have good hardness (3.2 kg/cm2), friability (<1%), disintegration time (26 s), % drug release (99.77 %) within 6 min. Conclusion: The result obtained showed that orally disintegrating tablet of chlorpheneramine maleate enhances dissolution rate, improves bioavailability which will improve patient compliance.
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There is no single-component excipient fulfills all the requisite performance to allow an active pharmaceutical ingredient to be formulated into a specific dosage form. Co-processed excipient has received much more attention in the formulation development of various dosage forms, specially for tablet preparation by direct compression method. The objective of this review is to discuss the emergence of co-processed excipients as a current and future trend of excipient technology in pharmaceutical manufacturing. Co-processing is a novel concept of combining two or more excipients that possess specific advantages that cannot be achieved using a physical admixture of the same combination of excipients. This review article discusses the advantages of co-processing, the need of co-processed excipient, general steps in developing co-processed excipient, limitation of co-processed excipient, technologies used in developing co-processing excipients, co-processed excipients in the literature, marketed products and future trends. With advantages offered by the upcoming newer combination of excipients and newer methods of co-processing, co-processed excipients are for sure going to gain attraction both from academia and pharmaceutical industry. Furthermore, it opens the opportunity for development and use of single multifunctional excipient rather than multiple excipients in the formulation.
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OBJECTIVE: To prepare montelukast sodium orally disintegrating tablets and investigate the bioequivalence in Beagle dogs. METHODS: The orally disintegrating tablets were prepared by direct compression method,and the optimal formulation was screened by orthogonal test.HPLC-fluorescence method was developed for determination of montelukast sodium plasma concentration in Beagle dogs. RESULTS: The optimized formulation(1 000 tablets) was montelukast sodium 10.4 g, microcrystalline cellulose 60 g, cross linked povidone 30 g, mannitol 15 g, magnesium stearate 2 g, aerosil 1 g, aspartame 1 g, flavor 0.6 g. CONCLUSION: Montelukast sodium orally disintegrating tablets made of the optimized formulation could disintegrate rapidly. Relatively bioavailability of montelukast sodium orally disintegrating tablets is 90.7%.
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ABSTRACT: Orally disintegrating tablets (ODTs) disintegrate rapidly in the mouth in seconds when placed at the tongue. The introduction of ODTs for dogs can address many needs, ranging from convenient dosing for dogs with dysphagia to extending life cycle of drugs. Now, different technologies are widely combined for developing ODTs. The combination makes ODTs have more properties, obtaining orally disintegrating sustained release tablets or orally disintegrating enteric tablets or enhancing the dissolution rate and bioavailability of poorly water-soluble drugs and so on. The aim of this article is to give a comprehensive prospect to the application of ODTs to dogs, including ideal properties of drugs, indications of ODTs, considerations in developing ODTs and development trends of ODTs for dogs.
RESUMO: Os comprimidos de desintegração oral (ODTs) se desintegram rapidamente na boca em questão de segundos, quando colocados na língua. A introdução de ODTs para cães pode resolver muitas necessidades, que vão desde a dosagem conveniente para cães com disfagia à extensão do ciclo de vida de drogas. Hoje, diferentes tecnologias são amplamente usadas para desenvolver ODTs. A combinação torna ODTs com mais propriedades e obter comprimidos de desintegração oral de libertação sustentada ou comprimidos de desintegração oral entéricos ou melhorar a velocidade de dissolução e biodisponibilidade de drogas pouco solúveis em água e assim por diante. O objetivo deste artigo é dar uma perspectiva abrangente para a aplicação de ODTs para cães, incluindo a indicação das ODTs, considerações em ODTs em desenvolvimento, desenvolvimentos de ODTs para cães.
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OBJECTIVE: To evaluate the properties of co-processed excipient of mannitol and polyplasdone (Man-Cro) and apply it in direct compression of orally disintegrating tablets. METHODS: The physical and micromeritic properties of the co-processed excipient were compared with those of mannitol, polyplasdone, and physical mixture of the two compounds. The interaction between the two components was studied by using FT-IR, SEM, DSC and X-RD. The flowability and compressibility of the Man-Cro co-processed excipient were also compared with the two components by determining the angle of repose, bulk density, tap-density, Carl index and Kawakita's equation. The co-processed excipient was applied to prepare ibuprofen orally disintegrating tablets. The in vitro dissolution and bioavailability of the tablets were evaluated. RESULTS: The co-processed excipient of mannitol and polyplasdone formed novel aspheric particles after cocrystallization. The excipient showed good flowability, compressibility, filling ability and disintegrability. Compared with commercially available ibuprofen tablets, the ibuprofen orally disintegrating tablets prepared with the co-processed excipient had more rapid in vitro dissolution. And the homemade and commercially available preparations were bioequivalent in rats. CONCLUSION: The co-processed excipient is superior to physical mixture as drug carrier and suitable for preparation of orally disintegrating tablets by direct compression.
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OBJECTIVE:To prepare Lipoic acid orally disintegrating tablets,and to evaluate its quality. METHODS:Lipoic acid orally disintegrating tablets were prepared with direct compression after wet granulation. With disintegration time and dissolu-tion as index,the constituents of disintegrating agent,filler and lubricant were screened by single factor test combined with orthogo-nal test. The tablet weight,hardness,disintegration time,accumulative rate and percentage content were investigated. RESULTS:The optimal formulation was MCC 167.58 mg,L-HPC 23.94 mg,PVPP 47.88 mg,mannitol 60 mg,lipoic acid 300 mg and mag-nesium stearate 0.6 mg. The parameters of prepared disintegrating tablets was as follows as (0.59 ± 0.05) g in weight,(20.32 ± 0.16)kg in solidity and(23.5±0.4)s in disintegration time,101.49% in 3 min accumulative dissolution rate,96.34% of labeled content. CONCLUSIONS:Lipoic acid orally disintegrating tablets are prepared successfully and controllable in quality.
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OBJECTIVE: To evaluate the micromeritic properties of Parteck® ODT to provide preliminary theoretical basis for the direct compression technology of orally disintegrating tablets (ODTs).
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OBJECTIVE:To compare the bioequiavailability of two simvastatin preparations in human bodies.METHODS:A total of 18 healthy male volunteers were enrolled in a randomized crossover study in which the subjects were randomly assigned to receive single dose of 40mg simvastatin orally disintegrating tablet(test) or simvastatin tablets(reference).The plasma concentrations of simvastatin were determined by LC-MS,and the pharmacokinetic parameters and bioavailability were calculated with 3p97 program.RESULTS:The pharmacokinetics of simvastatin test and reference preparations were fitted the one-compartment model.The main pharmacokinetic parameters of the two preparations were as following:Cmax:(6.73?5.22) vs.(7.08?5.41)ng?mL-1、tmax:(2.11?0.74)vs.(1.89?0.85)h,AUC0～12:(19.83?19.09)vs.(19.98?18.20)ng?h?mL-1,AUC0～∞:(22.18?20.09)vs.(22.41?21.07)ng?h?mL-1.The relative bioavailability of simvastatin orally disintegrating tabl-et as against simvastain tablet(reference) was (99.25?13.11)%.CONCLUSION:Simvastatin test and reference preparations were bioequivalent.
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OBJICTIVE: To prepare Breviscapine orally disintegrating tablet and to establish its quality control method. METHODS: The formula of the core of the tablet was optimized with disintegration time as a parameter by an orthogonal design, and the content and the related substances of Breviscapine orally disintegrating tablet were determined by HPLC. RESULTS: The prepared Breviscapine orally disintegrating tablet showed a good stability, and its characters, dissolution, content and the related substances were all in conformity with the related specifications stated in Chinese Pharmacopoeia (2005 edition). CONCLUSION: The methods of preparation and Quality control are simple and feasible.
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OBJECTIVE:To study the relative bioavailability and pharmacokinetics of salbutamol sulfate orally disinte?grating tablets.METHODS:A single dose of8mg salbutamol sulfate orally disintegrating tablets or commercial salbutamol tablets was administered in a randomized crossover design in18volunteers and the plasma concentrations of salbutamol were determined by HPLC.The pharmacokinetic parameters were calculated with3p97pharmacokinetic program and the bioequiv?alency was evaluated.RESULTS:The concentration-time curve of two preparations fitted to two-compartment model.The peak plasma levels(C max )of salbutamol sulfate orally disintegrating tablet and commercial salbutamol sulfate tablet were(17.65?6.48)ng/ml and(16.60?6.21)ng/ml,respectively.The peak time(T max )were(1.92?1.18)h and(2.03?1.17)h and AUC 0～24 were(127.23?32.41)ng/(h?ml)and(131.42?37.73)ng/(h?ml),respectively.The relative bioavailability of salbu_ tamol sulfate orally disintegrating tablet was(99.32?15.58)%.CONCLUSION:The results of two one-side tests suggests that salbutamol sulfate orally disintegrating tablet is bioequivalent to the commercial salbutamol tablet.
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Objective:To study the relative bioavailability and pharmacokinetics of salbutamol orally disintegrating tablet in 18 healthy male volunteers.Methods:A single dose of 8 mg of salbutamol orally disintegrating tablet was administered in a randomized crossover way in 18 volunteers and the plasma concentrations of salbutamol were determined by HPLC.The pharmacokinetic parameters were calculated with 3P97 pharmacokinetic program and the bioavailability was evaluated.Results:The concentration-time curve of two preparations fitted two compartment model.The peak plasma levels(cmax) of salbutamol orally disintegrating tablet and market of salbutamol were 17.48?5.52 and 16.60?6.21 ng/ml,respectively.The peak time(Tmax) were 2.47?1.04 and 2.03?1.17h and AUC(0-24) were 127.34?32.66 and 131.42?37.73 ng?h/ml,respectively,The relative bioavailability of salbutamol orally disintegrating tablet was 98.76%?12.92%.Conclusion:The results of two one-side tests suggest that salbutamol orally disintegrating tablet is bioequivalent to the market tablet of salbutamol.