scholarly journals Biopharmacotechnical and physical properties of solid pharmaceutical forms containing rutin commercially acquired in Juiz de Fora city, Brazil

2020 ◽  
Vol 42 ◽  
pp. e52212
Author(s):  
Thiago Maurício de Souza Pinto ◽  
Fabrini Luiz Alves Almeida ◽  
Julianna Oliveira de Lucas Xavier ◽  
Glauciemar Del-Vechio-Vieira ◽  
Ana Lúcia Santos de Matos Araújo ◽  
...  
Keyword(s):  
Clinical Practice ◽  
Physical Properties ◽  
Therapeutic Efficacy ◽  
Average Weight ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Anti Inflammatory ◽  
Kinetics Of

Rutin is a flavonoid used in clinical practice to treat capillary fragility and prevent bleeding due to its wide variety of pharmacological actions, including antioxidant, anti-inflammatory, anti-allergic, antiproliferative, and anticarcinogenic activities. In this study, the biopharmacotechnical and physical properties of film-coated tablets containing rutin marketed in drugstores were evaluated. Using samples from three batches called A, B and C, we determined the average weight, disintegration time, hardness, content and dissolution profile, and kinetics of the tablets. The samples demonstrated average weight of 457.45 ± 12.32 to 449.15 ± 8.95 mg; disintegration time, 30.17 ± 2.14 to 15.17 ± 2.14 min; hardness, 1.92 ± 0.55 to 1.69 ± 0.36 Kgf; and rutin content, 18.34 ± 1.21 to 15.66 ± 1.29 mg. After 90 min, the dissolution profile showed 52.65, 41.80, and 79.2% for A, B, and C, respectively. The results imply that the non-conformities of the tested products can significantly compromise the drug’s therapeutic efficacy.

Physicochemical Evaluation of Brands of Amlodipine Besylate Tablets.

2020 ◽  
Vol 1 (5) ◽  
pp. 24-33
Author(s):  
C.A. Anyanwu-Ndulewe ◽  
◽  
L.E. Mogbolu ◽  
M.A. Oladunni ◽  
A.A. Adepoju-Bello
Keyword(s):  
Hardness Test ◽  
Drug Market ◽  
The United States ◽  
Financial Strain ◽  
Average Weight ◽  
Dissolution Profile ◽  
Amlodipine Besylate ◽  
Disintegration Time ◽  
Physicochemical Evaluation ◽  
Dissolution Efficiency

Background: Hypertension is a chronic condition, and the cost of filling prescriptions has a potential of putting a financial strain on patients, hence the need for lower priced but bioequivalent generics. The Nigerian drug market is awash with generics of Amlodipine besylate, a first line drug in the treatment of hypertension, therefore, any prescribed alternative must be bioequivalent to the originator. Objectives: This study assessed the physicochemical properties of some brands in order to predict pharmaceutical and bioequivalence and invariably, the interchangeability with the innovator brand. Methods: Compendial parameters of average weight, friability, disintegration, drug content and dissolution profile of ten generic brands were evaluated using the United States Pharmacopeia (USP) as well as the non-official hardness test. Results: Two brands failed the test for hardness, while still keeping to the stipulated friability limit. All the brands met the required disintegration time, irrespective of the discordance of some brands in the breaking force and friability values. All brands were found to contain between 92.00 and 103.57% (w/w) of Amlodipine besylate. Two brands failed to achieve ≥75% dissolution expected at 30 minutes and this was reflected in the low f2 values of 35.06% and 28.73%. The dissolution curves displayed a similarity for two brands, which was also corroborated by the high percentage dissolution efficiency (DE) of 92.00%, as well as the f1 and f2 values, compared to the innovator brand. Conclusion: Although the parameters used may predict therapeutic equivalence, interchangeability with the comparator brand is subject to relevant bioequivalence studies.

scholarly journals Physical characteristics of effervescent tablet probiotics in various concentration of tapioca coatings

2021 ◽  
Vol 919 (1) ◽  
pp. 012045
Author(s):  
D A Oktavia ◽  
D L Ayudiarti ◽  
D Febrianti ◽  
V Yanuar
Keyword(s):  
Physical Properties ◽  
External Environment ◽  
Shrimp Farming ◽  
Average Weight ◽  
Liquid Form ◽  
Disintegration Time ◽  
Shrimp Ponds ◽  
South Sulawesi ◽  
Coastal Aquaculture ◽  
Effervescent Tablet

Abstract RICA (Research Institute for Coastal Aquaculture) Maros in South Sulawesi has developed 5 probiotic preparations, namely RICA-1, RICA-2, Rica-3, RICA-4 and RICA-5 in liquid form to improve shrimp farming in ponds. In practice, the use of liquid probiotics has been very optimal but the distribution is constrained because of its liquid form. For this reason, microencapsulation of liquid probiotics is carried out to protect from the external environment and maintain the viability of probiotic cells in the encapsulated matrix. The purpose of this study was to determine the physical properties of probiotic effervescent tablets using tapioca coating with different concentration variants (10 and 20%) with four effervescent tablet formulas. The results showed that the pH of the probiotic effervescent tablet Formula 3 with a coating concentration of 10% tapioca had a neutral pH compared to all existing formulas. However, the pH for probiotic effervescent tablets produced by all formulas can still be applied to shrimp ponds. Formula 4 with 10% tapioca coating has a mean weight and hardness that is close to the standard as well as a disintegration time that meets the specified standard of tablet physical properties. Meanwhile, the tablet friability value was met by Formula 3 with a concentration of 10% tapioca coating. It can be concluded that the best formula that meets the standard physical properties of tablets is Formula 4 with 10% tapioca coating. The probiotic effervescent tablet with tapioca coating has a weakness in the hardness value which causes the average weight to be not uniform. These results indicate that tapioca coating is not suitable for use as a coating for probiotic effervescent tablets.

Formulation and Evaluation of Atorvastatin Calcium-Poly-ε-Caprolactone Nanoparticles Loaded Ocular Inserts for Sustained Release and Antiinflammatory Efficacy

2020 ◽  
Vol 21 (15) ◽  
pp. 1688-1698
Author(s):  
Germeen N.S. Girgis
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
In Vivo Study ◽  
Average Weight ◽  
Drug Release Profile ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory

Purpose: The work was performed to investigate the feasibility of preparing ocular inserts loaded with Poly-ε-Caprolactone (PCL) nanoparticles as a sustained ocular delivery system. Methods: First, Atorvastatin Calcium-Poly-ε-Caprolactone (ATC-PCL) nanoparticles were prepared and characterized. Then, the optimized nanoparticles were loaded within inserts formulated with Methylcellulose (MC) and Polyvinyl Alcohol (PVA) by a solvent casting technique and evaluated physically, for in-vitro drug release profile. Finally, an in-vivo study was performed on the selected formulation to prove non-irritability and sustained ocular anti-inflammatory efficacy compared with free drug-loaded ocuserts. Results: The results revealed (ATC-PCL) nanoparticles prepared with 0.5% pluronic F127 were optimized with 181.72±3.6 nm particle size, 0.12±0.02 (PDI) analysis, -27.4± 0.69 mV zeta potential and 62.41%±4.7% entrapment efficiency. Nanoparticles loaded ocuserts manifested compatibility between drug and formulation polymers. Moreover, formulations complied with average weight 0.055±0.002 to 0.143±0.023 mg, and accepted pH. ATC-PCL nanoparticles loaded inserts prepared by 5% MC showed more sustained, prolonged in-vitro release over 24h. In-vivo study emphasized non-irritability, ocular anti-inflammatory effectiveness represented by smaller lid closure scores, and statistically significant lowering in PMN count after 3h. Conclusion: These findings proposed a possibly simple, new and affordable price technique to prepare promising (ATC-PCL) nanoparticles loaded inserts to achieve sustained release with prolonged antiinflammatory efficacy.

Nanotechnological Innovations Enhancing the Topical Therapeutic Efficacy of Quercetin: A Succinct Review

2020 ◽  
Vol 17 (4) ◽  
pp. 270-278
Author(s):  
Maha Nasr ◽  
Rawan Al-Karaki
Keyword(s):  
Side Effects ◽  
Therapeutic Efficacy ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Topical Delivery ◽  
Natural Compounds ◽  
Therapeutic Activity ◽  
Dermatological Diseases ◽  
Anti Inflammatory ◽  
Topical Applications

Nanotechnology is currently a hot topic in dermatology and nutraceutical/cosmeceutical delivery, owing to the advantages it provides in terms of enhancing the skin permeation of drugs, as well as increasing their therapeutic efficacy in the treatment of different dermatological diseases. There is also a great interest in the topical delivery of nutraceuticals; which are natural compounds with both therapeutic and cosmetic benefits, in order to overcome the side effects of topically applied chemical drugs. Quercetin is a key nutraceutical with topical antioxidant and anti-inflammatory properties which was reported to be effective in the treatment of different dermatological diseases, however, its topical therapeutic activity is hindered by its poor skin penetration. This review highlights the topical applications of quercetin, and summarizes the nanocarrier-based solutions to its percutaneous delivery challenges.

Physical properties and reaction kinetics of CO2 absorption into unloaded and CO2 loaded viscous monoethanolamine (MEA) solution

2021 ◽  
Vol 329 ◽  
pp. 115569
Author(s):  
Rouzbeh Ramezani ◽  
Ida M. Bernhardsen ◽  
Renzo Di Felice ◽  
Hanna K. Knuutila
Keyword(s):  
Physical Properties ◽  
Reaction Kinetics ◽  
Co2 Absorption ◽  
Kinetics Of

scholarly journals Physical properties and water absorption kinetics of three varieties of Mucuna beans

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Ajibola B. Oyedeji ◽  
Olajide P. Sobukola ◽  
Ezekiel Green ◽  
Oluwafemi A. Adebo
Keyword(s):  
Physical Properties ◽  
Water Absorption ◽  
Rate Constant ◽  
Geometric Mean ◽  
Seed Mass ◽  
Activation Energies ◽  
Mucuna Pruriens ◽  
Absorption Kinetics ◽  
Kinetics Of ◽  
Soaking Temperature

AbstractThe physical properties and water absorption kinetics of three varieties of Mucuna beans (Mucuna pruriens, Mucuna rajada and Mucuna veracruz) were determined in this study. Physical properties including length, width, thickness, geometric mean diameter, sphericity, porosity, bulk density, area, volume and one thousand seed mass were calculated while hydration kinetics was studied by soaking Mucuna beans in water at 30 °C, 40 °C and 50 °C and measuring water uptake at 9 h interval. Peleg’s equation was used to model the hydration characteristics and Arrhenius equation was used to describe the effect of temperature on Peleg’s rate constant k1 and to obtain the activation energies for soaking. Significant variations were observed in almost all the physical properties of the different varieties, however, there were no significant differences (p < 0.05) in their thicknesses and bulk densities. The effectiveness of fit of Peleg’s model (R2) increased with increase in soaking temperature. Peleg’s rate constant k1 decreased with increase in soaking temperature while k2 increased with temperature increase. Activation energies of Mucuna pruriens, Mucuna rajada and Mucuna veracruz were 1613.24 kJ/mol, 747.95 kJ/mol and 2743.64 kJ/mol, respectively. This study provides useful information about the properties of three varieties of Mucuna beans that could be of importance to processors and engineers for process design and optimization.

scholarly journals Administration route governs the therapeutic efficacy, biodistribution and macrophage targeting of anti-inflammatory nanoparticles in the lung

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Lu Wang ◽  
Yafei Rao ◽  
Xiali Liu ◽  
Liya Sun ◽  
Jiameng Gong ◽  
...  
Keyword(s):  
Therapeutic Efficacy ◽  
Lung Inflammation ◽  
Respiratory Diseases ◽  
Inflammatory Responses ◽  
The Other ◽  
Target Cells ◽  
Administration Route ◽  
Toll Like Receptor ◽  
Administration Routes ◽  
Anti Inflammatory

Abstract Background Uncontrolled inflammation is a central problem for many respiratory diseases. The development of potent, targeted anti-inflammatory therapies to reduce lung inflammation and re-establish the homeostasis in the respiratory tract is still a challenge. Previously, we developed a unique anti-inflammatory nanodrug, P12 (made of hexapeptides and gold nanoparticles), which can attenuate Toll-like receptor-mediated inflammatory responses in macrophages. However, the effect of the administration route on its therapeutic efficacy and tissue distribution remained to be defined. Results In this study, we systematically compared the effects of three different administration routes [the intratracheal (i.t.), intravenous (i.v.) and intraperitoneal (i.p.)] on the therapeutic activity, biodistribution and pulmonary cell targeting features of P12. Using the LPS-induced ALI mouse model, we found that the local administration route via i.t. instillation was superior in reducing lung inflammation than the other two routes even treated with a lower concentration of P12. Further studies on nanoparticle biodistribution showed that the i.t. administration led to more accumulation of P12 in the lungs but less in the liver and other organs; however, the i.v. and i.p. administration resulted in more nanoparticle accumulation in the liver and lymph nodes, respectively, but less in the lungs. Such a lung favorable distribution was also determined by the unique surface chemistry of P12. Furthermore, the inflammatory condition in the lung could decrease the accumulation of nanoparticles in the lung and liver, while increasing their distribution in the spleen and heart. Interestingly, the i.t. administration route helped the nanoparticles specifically target the lung macrophages, whereas the other two administration routes did not. Conclusion The i.t. administration is better for treating ALI using nanodevices as it enhances the bioavailability and efficacy of the nanodrugs in the target cells of the lung and reduces the potential systematic side effects.

scholarly journals 3DP Printing of Oral Solid Formulations: A Systematic Review

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 358 ◽  
Author(s):  
Chiara R. M. Brambilla ◽  
Ogochukwu Lilian Okafor-Muo ◽  
Hany Hassanin ◽  
Amr ElShaer
Keyword(s):  
Systematic Review ◽  
Data Extraction ◽  
New Technology ◽  
Three Dimensional ◽  
Extraction Process ◽  
Carcinogenic Risk ◽  
Drug Dissolution ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Advantages And Disadvantages

Three-dimensional (3D) printing is a recent technology, which gives the possibility to manufacture personalised dosage forms and it has a broad range of applications. One of the most developed, it is the manufacture of oral solid dosage and the four 3DP techniques which have been more used for their manufacture are FDM, inkjet 3DP, SLA and SLS. This systematic review is carried out to statistically analyze the current 3DP techniques employed in manufacturing oral solid formulations and assess the recent trends of this new technology. The work has been organised into four steps, (1) screening of the articles, definition of the inclusion and exclusion criteria and classification of the articles in the two main groups (included/excluded); (2) quantification and characterisation of the included articles; (3) evaluation of the validity of data and data extraction process; (4) data analysis, discussion, and conclusion to define which technique offers the best properties to be applied in the manufacture of oral solid formulations. It has been observed that with SLS 3DP technique, all the characterisation tests required by the BP (drug content, drug dissolution profile, hardness, friability, disintegration time and uniformity of weight) have been performed in the majority of articles, except for the friability test. However, it is not possible to define which of the four 3DP techniques is the most suitable for the manufacture of oral solid formulations, because the selection is affected by different parameters, such as the type of formulation, the physical-mechanical properties to achieve. Moreover, each technique has its specific advantages and disadvantages, such as for FDM the biggest challenge is the degradation of the drug, due to high printing temperature process or for SLA is the toxicity of the carcinogenic risk of the photopolymerising material.

scholarly journals EVALUATION OF MUSA ACUMINATA FRUIT AS A NATURAL SUPERDISINTEGRANT FOR TABLET FORMULATION

2018 ◽  
Vol 11 (10) ◽  
pp. 167
Author(s):  
Gopinath E
Keyword(s):  
Nutritive Value ◽  
Low Cost ◽  
Cost Effective ◽  
Musa Acuminata ◽  
Tablet Formulation ◽  
Angle Of Repose ◽  
Average Weight ◽  
Disintegration Time ◽  
Solubility Study ◽  
Orodispersible Tablet

Objective: The objective of the present work was to develop and evaluate a new, low-cost effective superdisintegrant from Musa acuminata fruit for tablet formulation.Methods: The study involved collection of M. acuminata fruit powdered and evaluated for physicochemical properties. Propranolol Hcl was used as a model drug for tablet formulation. Different concentrations of M. acuminatea powder were used as superdisintegrant, and orodispersible tablet is prepared and evaluated. In the present study, sodium starch glycolate was used as synthetic superdisintegrant for comparative study.Result: The powder was dark brownish and did not change throughout the study. The percentage porosity of powder was found to be 42.88% and angle of repose of was found to be 33.69°. The solubility study shows that the powders are sparingly soluble in water and disperse into individual particles. Total ash and acid insoluble ash values of powder were found to be 2.61 and 2.11% w/w, respectively. The average weight of tablets was ranged from 101.42 to 103.52 mg and averaged hardness was found to be 3.4 kg/cm2. Moreover, the tablets exhibited acceptable friability. Disintegration time of all formulations was found to be in the range of 22–80 s and wetting time was found to be 07–18 s.Conclusion: From the study, it was concluded that M. acuminatea powder in the range of 2–12% can be used as superdisintegrant in orodispersible tablet formulation and shall be preferred as having nutritive value as well as cost profit in the development of orodispersible tablet than synthetic polymer.

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