scholarly journals The Effect of Particle Size on the Physical Characteristics and Drug-release Behavior of Mini-tablets

2021 ◽  
Vol 18 (21) ◽  
pp. 43
Author(s):  
Awis Sukarni Mohmad Sabere ◽  
Mohd Muzamir Mahat

This study aimed to investigate the influence of particle size of the excipients on the behavior of mini-tablets in terms of physical characteristics and drug release profiles. Material and methods: All of the mini-tablets based on HPMC, PEG 6K and PEO 8M PVP produced high quality mini-tablets from both sieve fractions while 90F was very fragile. Results: Crushing strength values were the most pronounced difference between the mini-tablets from all formulations. The PEO 8M-based mini-tablets showed the highest values and deformation behavior instead of fracture. Water absorption and drug release profiles also showed intriguing and different results between the various formulations. Conclusion: The results suggested that even though different particle size has limited effect on the physical characteristic of the product, it may have a significant effect on its drug dissolution profile. HIGHLIGHTS The particle size of powders or granules can influence the physical properties and release profiles of tablets, particularly mini-tablets PEG 6K and PEO 8M mini-tablets from the larger sieve fraction variation absorbed less moisture and released drugs faster than their counterparts, whereas HPMC and PVP 90F mini-tablets from both sieve fractions exhibited a similar pattern in terms of moisture uptake and drug release profiles PEO 8M mini-tablets of both sieve fractions displayed almost linear release profiles with the highest crushing strength than the rest of the formulations GRAPHICAL ABSTRACT

2016 ◽  
Vol 4 (03) ◽  
pp. 05-14
Author(s):  
Patil P.D ◽  
Desai S.R ◽  
Disouza J.I

Suspension is a heterogeneous mixture including solid particles that are satisfactorily bulky for sedimentation. Generally they must be larger than one micrometer. It is when particles are left floating around freely in a solvent. The inner phase (solid) is discrete all through the external phase (fluid) during mechanical stir, with utilizing of certain excipients or suspending agents. Metronidazole or 2-(2 methyl-5 nitro-1 H –imidazol-1 yl) ethanol belongs to the nitro imidazole group of antibiotics whose antimicrobial property through derive from the formation of toxic free radicals by intracellular reduction. The objective of present study was to prepare suspension of Metronidazole by using different suspending agents and stability testing was to provide evidence on how the quality of suspensions varies with the time under of influence of environmental factors such as temperature, light, oxygen, moisture, other ingredient or excipients in the dosage form, particle size of drug, microbial contamination etc. and to establish a recommended storage condition. The FTIR and DSC techniques are use for characterization of active ingredient MBZ. This suspension was evaluated for appearance, pH, sedimentation volume and dissolution study for in vitro drug release. Result of evaluation indicates 1% w/v xanthan gum give optimal characteristic suspension. Suspension containing 1% w/v was exposed for the stability studies as per ICH guidelines. The suspensions were evaluated for their physicochemical parameter, particle size, drug release, drug content and microbiological assessment. The suspension shows good stability at 25ºC ± 2 ºC /60%± 5% RH, 30 ºC ± 2 ºC /65%± 5% RH and good quantitative analysis result throughout the period of study. Suspension stored at 40 ºC ± 2 ºC /75%± 5% RH shows noncompliance with the analysis parameter after 4 week of storage. This indicate high temperature storage was shows degradation of the suspension which results in crystal growth in formulation and affect the physicochemical parameter as Appearance, pH, viscosity, specific gravity, drug dissolution profile and drug content.


Author(s):  
Nirmala Rangu ◽  
Gande Suresh

The present study was aimed to develop once-daily controlled release trilayer matrix tablets of nelfinavir to achieve zero-order drug release for sustained plasma concentration. Nelfinavir trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVP (Polyvinyl Pyrrolidine) K-30 and MCC (Micro Crystalline Cellulose). Barrier layers were prepared with Polyox WSR-303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 were found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the zero-order and best fitted to Higuchi model. FT-IR studies confirmed that there were no chemical interactions between drug and excipients used in the formulation. These results indicate that the approach used could lead to a successful development of a controlled release formulation of nelfinavir in the management of AIDS.


2020 ◽  
Vol 833 ◽  
pp. 129-133
Author(s):  
Ridwan Tobi Ayinla ◽  
John Ojur Dennis ◽  
Hasnah Bt Moh’d Zaid ◽  
Fahad Usman ◽  
Asfand Yar

The advantages of palm kernel shell (PKS) as a renewable and sustainable material for activated carbon production have been explored for various applications such as water treatment, pollutant, pesticide, and heavy metal adsorption. However, the full promises of this material for energy storage devices have not been duly studied. In this research, PKS is physically activated and the effect of particle size on the physical characteristics of the activated char was investigated. Pellet (3 mm), granules (0.4 mm), and powder (0.0075 mm) are the sizes considered in the experiment. The surface morphology, surface area, porosity and functional group at different sized was analyzed. Finally, a suitable particle size was recommended for the electrode material of supercapacitor based on the physical characteristics of the activated carbon.


Author(s):  
Harshada Anil Kasar ◽  
Asish Dev ◽  
Subhakanta Dhal

Objective: The objective of this study was to formulate and optimize a chewable formulation of lidocaine hydrochloride using a 32 factorial design for optimized the superdisintegrant concentration.Methods: Various concentrations of sodium starch glycolate (SSG) (13.33 mg, 26.66 mg, and 40 mg) of superdisintegrant and starch (50 mg, 83 mg, and 116.66 mg) were added in the formulation; nine formulations were prepared according to 32 factorial designs and evaluated. The responses were analyzed for analysis of variance using Design-Expert version 10 software. Statistical models were generated for each response parameter. The models were tested for significance. Procedure to manufacture chewable tablets by direct compression was established.Results: The results show that the presence of a superdisintegrant is desirable for chewable formulation. The best-optimized batch F7 found the batch having starch of amount 116.66 mg and SSG 13.33 mg. All the prepared batches of tablets were within the range. Optimized batch F7 showed drug content 102.46±0.0543, wetting time 18±1.7320, friability 0.65±0.0216, and drug release rate 99.97±0.0124% at the end of 30 min.Conclusion: It can be concluded that 32 full factorial design and statistical models can be successfully used to optimize the formulations, and it was concluded that the trial batch F7 is the optimized formulation which compiles official specifications of chewable tablets. The optimized batch was evaluated for thickness, weight variation, hardness, friability, drug dissolution, and stability study for 3 months. The similarity factor was calculated for comparison of dissolution profile before and after stability studies. After 30 min the drug release rate for batch F7 was 98.97% (Table 6). Hence, the results of stability studies reveal that the developed formulation has good stability.


1970 ◽  
Vol 7 (1) ◽  
pp. 27-32 ◽  
Author(s):  
Md Shaikhul Millat Ibn Razzak ◽  
Ferdous Khan ◽  
Md Ziaur Rahman Khan ◽  
Kanij Fatema ◽  
Muhammed Shahidul Islam ◽  
...  

The present study was undertaken to investigate the effect of channeling agents on the release profile of Theophylline from METHOCEL K4M based matrix systems. Matrix tablets of Theophylline using METHOCEL K4M were prepared by direct compression process. METHOCEL K4M polymer is hydrophilic in nature. NaCl and PEG 1500 were used as channeling agents. Drug release study was evaluated for eight hours using USP 22 paddletype dissolution apparatus using distilled water as the dissolution medium. The release mechanisms were explored and explained with zero order, Higuchi and Korsmeyer equations. The release rate, extent and mechanisms were found to be governed by channeling agent type and content. Higher channeling agent content (42.49%) in the matrix increased the rate and extent of the drug release because of increased porosity in the tablet matrices, at lower channeling agent (19.76%) level, the rate and extent of drug release was decreased and in absence of channeling agents these were least. NaCl ensures maximum release of drug from low viscosity grade METHOCEL K4M than PEG 1500 when other parameters were kept constant. It was found that type and amount of channeling agent significantly affect the time required for 50% of drug release (T50%), percentage drug release at 8 hours, release rate constant (K) and diffusion exponent (n). Kinetic modeling of dissolution profiles revealed drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport, which was mainly dependent on the presence of type and amount of channeling agent. These studies indicate that the proper balance between a matrix forming agent and a channeling agent can produce a drug dissolution profile similar to a theoretical dissolution profile.Key words: Channeling agent, Theophylline, Release Profile, Methocel K4MDOI = 10.3329/dujps.v7i1.1214Dhaka Univ. J. Pharm. Sci. 7(1): 27-32, 2008 (June)


Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1453
Author(s):  
Hellen Windolf ◽  
Rebecca Chamberlain ◽  
Julian Quodbach

3D printing offers the advantage of being able to modify dosage form geometry, which can be exploited to modify release characteristics. In this study, we investigated the influence of the surface area to volume ratio (SA/V) to change and predict release profiles of 3D printed dosage forms. Geometries with varying SA/V and dosages were designed and printed, and drug dissolution was investigated. Three drug substances were used: pramipexole, levodopa (both BCS I) and praziquantel (BCS II). Two polymers were chosen as matrix formers: polyvinyl alcohol (water-soluble) and ethylene vinyl acetate (inert). Drug release was characterized using the mean dissolution time (MDT) and established equations that describe complete dissolution curves were applied. Predictions were validated with previously un-printed dosage forms. Based on an identified MDT-SA/V correlation, the MDT can be predicted with a deviation of ≤5 min for a given SA/V. Using correlations of fit parameters and SA/V, RMSEP values of 0.6–2.8% and 1.6–3.4% were obtained for the BCS I formulations and RMSEP values of 1.0–3.8% were obtained for the BCS II formulation, indicating accurate prediction over a wide range of dissolution profiles. With this approach, MDT and release profiles of dosage forms with a given SA/V can be precisely predicted without performing dissolution tests and vice versa, the required SA/V can be predicted for a desired release profile.


2016 ◽  
Vol 697 ◽  
pp. 595-598
Author(s):  
Zhin An Chai ◽  
Cheng Ji Deng ◽  
Hong Xi Zhu ◽  
Xiao Jun Zhang ◽  
Liang Yi Zhou

Starting from different sizes of magnesia and bauxitewith sodium hexametaphosphate as anchoring agent, specimens obtained by suppression were sintered at 1500°C and 1550°C and heat preservation for 3h in the electric hearth furnace, respectively. The effect of particle size distribution of magnesia and bauxite on the properties of magnesia-alumina refractory materials was investigated. The composition of magnesia-alumina refractory which consists of various particle size distributions was determined, according to Andreasen packing model, with distribution coefficient (q) of 0.15, 0.20, 0.25, 0.30, 0.35, 0.40 and 0.50. The fractographs of the specimen were observed by scanning electron microscopy. The linear rate of change, apparent porosity, bulk density and crushing strength of these specimens were studied. The results showed: a crushing strength of 52.39 MPa, an apparent porosity value of 15.55% and a bulk density value of 2.91 g/cm3 were obtained via a particle size distribution coefficient of 0.30 at 1550°C. Simultaneously, the refractory materials had small linear rate of change.


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