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In this paper, 50 batches of representative traditional Chinese medicine tablets were selected and the disintegration time was examined with the method in Chinese Pharmacopoeia. The disintegration time and disintegration phenomenon were recorded, and the dissolution behaviors of water-soluble and ultraviolet-absorbent components during the disintegration process of tablets were characterized by self-control method. The results revealed that coating type and raw material type influenced the disintegration time of tablets. It was found that only 4% of traditional Chinese medicine tablets had obvious fragmentation during the disintegration process, while 96% of traditional Chinese medicine tablets showed gradual dissolution or dispersion. Furthermore, according to the disintegration speed, disintegration phenomenon, and whether the cumulative dissolution of measured components was > 90% at complete disintegration, a disintegration behavior classification system(DBCS) was created for the regular-release traditional Chinese medicine tablets. As a result, the disintegration behaviors of 50 batches of traditional Chinese medicine tablets were classified into four categories, i.e. ⅠA_2, ⅠB_1, ⅡB_1, and ⅡB_2. traditional Chinese medicine tablets(Class I) with disintegration time ≤ 30 min were defined to be rapid in disintegration, which can be the objective of optimization or improvement of Chinese herbal extract(semi extract) tablets. Different drug release models were used to fit the dissolution curve of traditional Chinese medicine tablets with gradual dissolution or dispersion phenomenon(i.e. Type B tablets). The results showed that the dissolution curves of water-soluble components in the disintegration process conformed to the zero order kinetics and the Ritger-Peppas model. It could be inferred that the disintegration mechanisms of type B tablets were a combination of dissolution controlled and swelling controlled mechanisms. This study contributes to understanding the disintegration behavior of traditional Chinese medicine tablets, and provides a reference for the design and improvement of disintegration performance of traditional Chinese medicine tablets.
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Commerce , Medicine, Chinese Traditional , Tablets , Water , Drug CompoundingABSTRACT
Abstract Personalized medicine is gaining importance in pharmacotherapeutics as it allows tailoring the drug treatment to achieve the best patient response. Orodispersible film (ODF) is easy to formulate in hospitals, produces dose flexibility to suit an individual needs, particularly for patients suffer from swallowing issues or prohibited to take fluids. Sertraline Hydrochloride (SRT) was solubilized in several cosolvents, then different SRT ODFs based on five hydrophilic polymers namely; polyvinyl alcohol (PVA), hydroxylethyl cellulose (HEC), hydroxypropyl methylcellulose E5 LV (HPMC E5 LV), sodium alginate (NaAlg) and gelatin at two concentrations (2% and 4%) were developed and characterized. The outcomes were exposed to response surface analysis to obtain the desirability results to obtain the optimized formulation. Blended ODFs were developed from 4% PVA and 2% HEC in different blends and then potassium chloride (KCl) as a pore-forming agent was added to the best formulation to investigate its dissolution enhancement effect. F14 containing 4% PVA: 2% HEC 2:1 with 5% KCl showed best physicochemical properties of suitable pH (5.6), disintegration time (6 sec), good folding endurance which released 91 % SRT after 15 min. SRT ODF is an encouraging delivery system in the course of personalized medicine for the management of depression.
Subject(s)
Solvents , Sertraline/analysis , Precision Medicine , Excipients , Process OptimizationABSTRACT
Objective:This paper constructs a generalized regression neural network （GRNN） model to predict the disintegration time of traditional Chinese medicine （TCM） tablets. Method:Taking Astragali Radix as a model drug， the mixed Astragali Radix powders with different powder properties were prepared by mixing Astragali Radix extract powders with microcrystalline cellulose and lactose， which were made to Astragali Radix tablets by direct compression method. The powder properties of mixed Astragali Radix powders and the disintegration time of Astragali Radix tablets were determined， respectively. The correlation between the original data was eliminated by principal component analysis （PCA）. The principal component factors were used as the input layer of the GRNN model， and the disintegration time was used as the output layer for network training. Finally， the verification group data was used to predict the disintegration time， and the network prediction accuracy was calculated by comparing with the actual value. Result:Three principal component factors were obtained through PCA by analyzing the original nine variables that were correlated with each other （Hausner ratio， true density， tap density， compression degree， angle of repose， bulk density， porosity， water content and total dissolved solids）， which reduced the complexity of the network. The prediction value of the disintegration time based on this prediction method was in good agreement with the actual value， the error of disintegration time was 0.01-1.34 min and the average relative error was 3.16%. Conclusion:Based on the GRNN mathematical model， the physical properties of Astragali Radix extract powders can be used to accurately predict the disintegration time of Astragali Radix tablets， which provides a reference for studying the disintegration time of TCM tablets.
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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.
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Objective:To prepare Lycii Fructus polysaccharide buccal tablets and investigate its immunomodulatory effect. Method:Taking the appearance, taste, hardness and disintegration time of the tablets as comprehensive evaluation index, based on single factor tests, central composite design-response surface methodology was adopted to optimize the prescription of Lycii Fructus polysaccharide buccal tablets with mass ratio of dextrin to mannitol, mass ratio of cyclamate to malic acid and dosage of sodium carboxymethyl starch (CMS-Na) as factors. Kunming mice were randomly divided into 5 groups, namely the Lycii Fructus polysaccharide buccal tablets low (100 mg·kg-1·d-1), medium (200 mg·kg-1·d-1) and high (300 mg·kg-1·d-1) dose groups, the normal group (0.9% normal saline, 300 mg·kg-1·d-1) and the positive medicine group (Cinengsu group, 300 mg·kg-1·d-1). The immunomodulatory effect of the buccal tablets were investigated by calculating immune organ index, monocyte-macrophage phagocytic index, serum hemolysin antibody level, and the voix pedis thickness difference of delayed hypersensitivity (DTH) of mice. Result:Optimal prescription for the buccal tablets was 80% of Lycii Fructus extract, 11.5% of dextrin-mannitol (1.2:1), 1% of cyclamate-malic acid (1:1), 0.5% of cream essence, 6.5% of CMS-Na, 0.5% of magnesium stearate, and appropriate amount of 80% ethanol. Under the optimal condition, the hardness of the buccal tablets was 11.83 kg, its disintegration time was 13.21 min, both of which were in line with the relevant provisions of the 2015 edition of Chinese Pharmacopoeia, and the buccal tablets had good appearance and taste. Compared with the normal group, medium and high dose groups of Lycii Fructus polysaccharide buccal tablets significantly increased thymus index, spleen index and phagocytic index of mice (PPPPPConclusion:The formulation process of the buccal tablets optimized by central composite design-response surface methodology is stable and feasible, and Lycii Fructus polysaccharide buccal tablets can improve the immune regulation function of normal mice, and this study can provide experimental basis for the development, utilization and clinical application of Lycii Fructus and Lycii Fructus polysaccharides.
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Objective:To prepare aripiprazole oral disintegrating tablets , investigate the formula and evaluate the quality .Meth-ods:The formula of aripiprazole oral disintegrating tablets was investigated by a factorial experiment design .The aripiprazole particle size distribution ( X1 , D90/μm) , the ratio of mannitol to microcrystalline cellulose ( X2 ,％) and the amount of disintegration ( X3 ,％) were selected as the independent variables , and the tablet hardness ( Y1 , N) , the disintegration time ( Y2 , s) and the dissolution in 30 min ( Y3 ,％) were used as the dependent variables to ultimately determine the optimal formula .The dissolution profile of aripiprazole oral disintegrating tablets and the reference preparation in four dissolution media were compared by f2 similarity factor, and the stability of aripiprazole oral disintegrating tablets was investigated by accelerated stability testing .Results: The results of factorial experiment design of variance analysis showed that the filler ratio had significant effect on the tablet hardness (P<0.05), the amount of disinte-grant and the filler ratio had significant effect on the disintegration time (P<0.05), and the aripiprazole particle size had significant effect on the drug dissolution ( P<0.05 ) .The optimal formula of aripiprazole oral disintegrating tablets was as follows: the particle size D90 of aripiprazole was 20-40μm, the amount ratio of mannitol to microcrystalline cellulose was 2.5:1, and the amount of disinte-gration was 5.0％.Aripiprazole oral disintegrating tablets prepared with the optimal formula had higher hardness , shorter disintegration time and faster drug dissolution , and the dissolution profiles were similar with those of the reference preparation .The relevant sub-stances showed no significant increase during the accelerated stability testing , and the quality was satisfactory .Conclusion:The formu-la of aripiprazole oral disintegrating tablets is reasonable , the preparation process is feasible and the quality is controllable .
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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.
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Objective:To optimize the formula of adefovir dipivoxil tablets and investigate the dissolution in vitro. Methods:The formula was optimized by the D-optimal mixture design, the effects of the amount of filler ( X1 ,%) , the amount of disintegrant agent ( X2 ,%) and the amount of binder ( X3 ,%) were selected as the independent variables, and the friability ( Y1 ,%) , disintegration time ( Y2 , min) and dissolution of adefovir dipivoxil ( Y3 ,%) were the dependent variables. The similarity of the self-prepared prepa-ration and the reference preparation was obtained by using f2 similarity factor. The stability of adefovir dipivoxil tablets was evaluated preliminarily by high temperature, high humidity and strong light testing. Results:The optimal formula of adefovir dipivoxil tablets was as follows:the amount of lactose monohydrate was 67. 0%, the weight of croscarmellose sodium was 8. 0% and the amount of pregelati-nized starch was 12. 0%. The prepared tablets had lower friability, shorter disintegration time and higher drug dissolution rate. The dissolution similarity factors of the self-prepared tablets and the reference preparation in four dissolution media were all greater than 50. The results of influencing factor tests showed that the product should be moisture preservation. Conclusion:The formula of adefovir dip-ivoxil tablets optimized by the D-optimal mixture design is similar to that of the reference preparation, and the preparation process is feasible, which can meet the requirements of large production.
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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.
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Drug counterfeiting and production of substandard drug is a global problem. Substandard or counterfeit drugs are threat for the effective treatment of diseases and highly worsen the quality of life of patients. This study was aimed to assess the pharmaceutical quality of ranitidine hydrochloride tablets manufactured in Bangladesh. Tablets were collected from different parts of Bangladesh and quality parameters were evaluated according to the United States Pharmacopoeia and the British Pharmacopoeial methods. The potency of tablets was measured spectrophotometrically. Weight variation and disintegration time were performed according to pharmaceutical monographs. Among 43 brands tested, 8 failed to comply with the USP specification (active ingredient: 90±10%) due to containing of less amount of ranitidine of which 6 brands were spurious and 2 were substandard in nature. Two brands did not comply with the specification for weight variation of tablets whereas all brands passed disintegration time test. The findings clearly demonstrate the production of substandard ranitidine tablets in Bangladesh. The drug control authority of Bangladesh should take effective steps to prevent the production of substandard drugs to secure public health.
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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.
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Specific values of technological properties of excipients allow the establishment of numerical parameters to define and compare their functionality. This study investigates the functionality of Polyplasdones XL and XL10. Parameters studied included tablet disintegration profiles, compactibility profiles and powder flow. The results allowed the establishment of quantitative surrogate functionalities of technological performance, such as absolute number, and as a value relative to the known microcrystalline cellulose type 102. Moreover, the establishment of an explicit functionality to improve the technological performance of two diluents and a model drug was investigated, as was setting up of these functionalities, as quantitative values, to determine the input variables of each material and its probable functionality in a drug product. Disintegration times of pure Polyplasdone XL and its admixtures were around half that of Polyplasdone XL10. The improvement in tablet compactibility was 25-50% greater for Polyplasdone XL10 than Polyplasdone XL. Crospovidones proportions of up to 10% have little effect on the flow properties of other powders, although pure Polyplasdone XL10 and its admixtures display compressibility indexes about 20% greater than Polyplasdone XL. The observed results are in line with a smaller particle size of Polyplasdone XL10 compared to Polyplasdone XL.
Os valores específicos de propriedades tecnológicas de excipientes permitem o estabelecimento de parâmetros numéricos para definir e comparar a sua funcionalidade. Este estudo investiga a funcionalidade dos excipientes. Os parâmetros estudados foram perfis de desintegração dos comprimidos, perfis de compactação e fluxo de pó. Os resultados permitiram expressar o desempenho tecnológico através de valores absolutos e valores relativos à conhecida celulose microcristalina tipo 102. Do mesmo modo, permitiram estabelecer uma funcionalidade explícita para melhorar o desempenho tecnológico de dois diluentes e um fármaco modelo. A criação destas funcionalidades, como valores quantitativos, permite conhecer as variáveis de entrada de cada material e sua provável funcionalidade em um medicamento. Os tempos de desintegração do Poliplasdone XL e das suas misturas são cerca da metade do observado para as misturas com o Poliplasdone XL10. Melhoria da compressão de comprimidos que contêm Polyplasdone XL10 é 25-50% maior do que o Polyplasdone XL. Crospovidonas em proporções de até 10% têm pouco efeito sobre as propriedades de fluxo dos outros pós embora o Poliplasdone XL10 e suas misturas exibam índices de compressibilidade cerca de 20% maior do que o Poliplasdone XL. Os resultados observados estão em sintonia com o menor tamanho de partícula do Poliplasdone XL10, em comparação com o Poliplasdone XL.
Subject(s)
Tablets/analysis , International Classification of Functioning, Disability and Health/classification , Excipients , Stearates/analysis , Tablets/pharmacokineticsABSTRACT
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.
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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.
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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 prepare and optimize candesartan cilexetil tablets,and study the stability preliminarily. Methods:The formula was optimized by Box-Behnken experiment design,the ratio of lactose to pregelatinized starch( X1 ),the amount of disintegrant ( X2 ,%)and the amount of lubricant( X3 ,%)were selected as the independent variables,and weight difference( Y1 ,%),friability ( Y2 ,%),disintegration time( Y3 ,%)and candesartan cilexetil dissolution( Y4 ,%)were the dependent variables. The release rate of candesartan cilexetil tablets and the reference tablets were compared by similarity factor( f2 value). Preliminary stability was studied by high-temperature test,high-humidity test and illumination test. Results:The optimal formula of the tablets was as follows:the ratio of lactose to pregelatinized starch was 7:1,the amount of disintegrant was 5. 5%,and the amount of lubricant was 0. 5%. The f2 for the candesartan cilexetil tablets and the reference tablets in different dissolution meda was 60. 62,73. 34,66. 95 and 68. 60,respec-tively. Conclusion:The formula design is reasonable,the preparation process is feasible and the quality can be controlled.
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Objective:To prepare old tea buccal tablets using wet granulation method and optimize the preparation technology. Methods:The amount of each adjuvant was studied by single factor experiments, and the formula of the buccal tablets was optimized by the orthogonal experiments using taste and disintegration time as indices. Results:The optimal formula was composed of old tea ex-tract 30 g,mannitol 60g,PEG6000 20 g,aspartame 10 g,citric acid 10 g and menthol crystal 1 g. All the tested indices including ap-pearance, hardness and disintegration time met the requirements described in Chinese pharmacopeia. Conclusion: The preparation technology is reasonable and feasible for the industrial production.
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Banana starch obtained from unripe fruits of Musa sapientium L. has been evaluated as disintegrant in comparison with official corn starch. The physicochemical and material properties of the starches were evaluated and the properties of paracetamol tablet prepared by wet granulation using the starches as endo-disintegrants were determined. The results indicated that the physicochemical and material properties of banana starch varied considerably from corn starch. Scanning electron microscopy showed that banana starch granules were oval or ellipsoidal in shape while corn starch granules were angular or polyhedral in shape. The crushing strength (CS) of paracetamol tablets increased with disintegrant concentration while friability decreased. Tablets containing banana starch exhibited higher CS but lower friability than those containing corn starch. Paracetamol tablets containing banana starch had longer disintegration times than those containing corn starch although there were no significant (p >0.05) differences in the disintegration time of tablets. The results showed that banana starch compared well with corn starch as disintegrant.
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Objective: Five commercial brands were analyzed with respect to their physical characters, chemical content, and drug release. Methods: The brands of metformin were randomly selected. All the groups were coded and analyzed. The tablets were examined for their shape, size, weight, and color and the tablets were tested for their friability, disintegration, drug content, and purity using standard procedures. Results and discussion: On physical inspection, Brand C 500 was is the smallest and Brand D 500 SR was the largest in size. Brand C 500 was lesser in weight while Brand E XR 500 weighed more. On purity test, all other brands passed the standard for purity. All the brands had loss in weight less than 1% after the friability test. On chemical content examination, variation was seen between the batches as well as the brands. The brands such as Brand A XL 500 and Brand D 500 SR contained the required content. But the brands like Brand C 500 and Brand E XR 500 had only lesser content and failed in the validity test. Conclusion: The physical properties of the five brands of metformin tablets were analyzed. Sustained release dosage form was mainly designed for maintaining therapeutic blood or tissue levels of the drug for extended period of time. Apart from the color and shape, the weight and size are very important to improve patients’ compliance. It is the duty of the pharmaceutical company to manufacture proper dosage forms to achieve the therapeutic goal.
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Formulation of FDT (fast dispersing tablets) of nebivolol was optimized and evaluated using simplex lattice design (SLD). The influence of type and concentration of three disintegrants viz., Ac-Di-Sol, Primojel and Polyplasdone XL on hardness, friability and disintegration time of tablet was studied. Response surface plot and the polynomial equations were used to evaluate influence of polymer on the tablet properties. Results were statistically analyzed using ANOVA, and a p < 0.05 was considered statistically significant. Results reveal that fibrous integrity and optimal degree of substitution in Primojel and Ac-Di-Sol are mainly responsible for the hardness of the tablet. Use of Polyplasdone in higher percentage in tablet formulation may result in high friability. Increase in concentration of Ac-Di-Sol increases the disintegration time but increased concentration of Primojel in the tablet formulation decreases the disintegration time. This is also evident from model terms for disintegration time with a high 'F' value of 14.69 and 'p' value of 0.0031 (<0.05). The reason could be that Primojel has higher swelling properties and an optimum hydration capacity, which favors fast disintegration of a tablet. In conclusion, careful selection of disintegrant for FDT could improve their properties. Use of Simplex Lattice Design for formulation development could simplify the formulation process and reduce the production cost.
Otimizou-se e avaliou-se formulação de comprimidos de dispersão rápida (CDR) de nebivolol, usando planejamento de grade simplex (PGS). Estudou-se a influência do tipo e da concentração de três desintegrantes viz, Ac-Di-Sol, Primojel e Poliplasdona XL, na dureza, friabilidade e tempo de desintegração do comprimido. O gráfico de superfície de resposta e as equações polinomiais foram utilizados para avaliar a influência do polímero nas propriedades do comprimido. Os resultados foram analisados estatisticamente por ANOVA, considerando-se p < 0,05 como estatisticamente significativo. Os resultados revelam que a integridade das fibras e o grau de substituição ótimo no Primojel e Ac-Di-Sol são os principais responsáveis pela dureza do comprimido. O uso de Poliplasdona em maior porcentagem na formulação pode produzir friabilidade elevada. O aumento de Ac-Di-Sol aumenta o tempo de desintegração, mas o aumento da concentração de Primojel na formulação diminui o tempo de desintegração. Isto é, também, evidente no modelo de tempo de desintegração com alto valor de "F" de 14,69 e "p" de 0,0031 (< 0,05). A razão poderia ser que o Primojel tem maiores propriedades de intumescimento e ótima capacidade de hidratação, favorecendo a desintegração rápida do comprimido. Em conclusão, a cuidadosa seleção de um desintegrante para CDR poderia aprimorar suas propriedades. O uso do PGS para o desenvolvimento da formulação poderia simplificar o processo de formulação e reduzir o custo de produção.