Evaluation of spironolactone compatibility with magnesium stearate and other lubricants in paediatric formulation using thermal and nonthermal techniques

The objective of the present study is to develop chewable tablets containing different pharmaceutical compositions with simple manufacturing procedures using different excipients. Mannitols, L-HPC 11, Aspartame, Crospovidone, Crospovidone, Aerosil, and Magnesium Stearate are used as excipients for effective formulation of anti-asthmatic drug Montelukast. Montelukast is a selective, orally acting leukotriene receptor antagonist that is used for the treatment of asthma and seasonal allergic rhinitis. Montelukast chewable tablets were prepared by Direct Compression methods using suitable excipients. The chewable tablets were better presented using artificial sweetener Aspartame as flavouring agent. A total of forteen formulations were prepared and the granules were evaluated for pre-compression parameters. The formulated tablets were evaluated for post-compression parameters .The results showed that all the physical parameters were within the acceptable limits. The in vitro release study of all the formulations showed good release. The study concludes that aforementioned excipients can be used to design chewable montelukast sodium tablets.

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Formulation and Evaluation of Nelfinavir Extended Release Trilayer Matrix Tablets by Design of Experiment

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2018.11.5.6 ◽

2018 ◽

Vol 11 (5) ◽

pp. 4259-4268

Author(s):

Nirmala Rangu ◽

Gande Suresh

Keyword(s):

Controlled Release ◽

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Magnesium Stearate ◽

Zero Order ◽

Matrix Tablets ◽

Drug Dissolution ◽

Crystalline Cellulose ◽

Dissolution Profile ◽

Release Formulation

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.

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Crystal Transition and Drug-excipient Compatibility of Clarithromycin in Sustained Release Tablets

Current Pharmaceutical Analysis ◽

10.2174/1573412915666190328234326 ◽

2020 ◽

Vol 16 (7) ◽

pp. 950-959

Author(s):

Yu Li ◽

Xiangwen Kong ◽

Fan Hu

Keyword(s):

Sustained Release ◽

Powder Diffraction ◽

Magnesium Stearate ◽

Influential Factor ◽

High Concentration ◽

Scanning Calorimetry ◽

X Ray ◽

Sustained Release Tablets ◽

Crystal Transition ◽

Excipient Compatibility

Background: Clarithromycin is widely used for infections of helicobacter pylori. Clarithromycin belongs to polymorphic drug. Crystalline state changes of clarithromycin in sustained release tablets were found. Objective: The aim of this study was to find the influential factor of the crystal transition of clarithromycin in preparation process of sustained-release tablets and to investigate the possible interactions between the clarithromycin and pharmaceutical excipients. Methods and Results: The crystal transition of active pharmaceuticals ingredients from form II to form I in portion in clarithromycin sustained release tablets were confirmed by x-ray powder diffraction. The techniques including differential scanning calorimetry and infrared spectroscopy, x-ray powder diffraction were used for assessing the compatibility between clarithromycin and several excipients as magnesium stearate, lactose, sodium carboxymethyl cellulose, polyvinyl-pyrrolidone K-30 and microcrystalline cellulose. All of these methods showed compatibilities between clarithromycin and the selected excipients. Alcohol prescription simulation was also done, which showed incompatibility between clarithromycin and concentration alcohol. Conclusion: It was confirmed that the reason for the incompatibility of clarithromycin with high concentration of alcohol was crystal transition.

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In-Depth Comparison of Dry Particle Coating Processes Used in DPI Particle Engineering

Pharmaceutics ◽

10.3390/pharmaceutics13040580 ◽

2021 ◽

Vol 13 (4) ◽

pp. 580

Author(s):

Nicholas Bungert ◽

Mirjam Kobler ◽

Regina Scherließ

Keyword(s):

Drug Carrier ◽

Magnesium Stearate ◽

High Shear ◽

Particle Engineering ◽

Dry Powder Inhalation ◽

Particle Coating ◽

Lower Drug ◽

Dry Particle Coating ◽

Coarse Model ◽

Carrier Systems

High-shear mixer coatings as well as mechanofusion processes are used in the particle-engineering of dry powder inhalation carrier systems. The aim of coating the carrier particle is usually to decrease carrier–drug adhesion. This study comprises the in-depth comparison of two established dry particle coating options. Both processes were conducted with and without a model additive (magnesium stearate). In doing so, changes in the behaviour of the processed particles can be traced back to either the process or the additive. It can be stated that the coarse model carrier showed no significant changes when processed without additives. By coating the particles with magnesium stearate, the surface energy decreased significantly. This leads to a significant enhancement of the aerodynamic performance of the respective carrier-based blends. Comparing the engineered carriers with each other, the high-shear mixer coating shows significant benefits, namely, lower drug–carrier adhesion and the higher efficiency of the coating process.

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The Influence of Temperature and Viscosity of Polyethylene Glycol on the Rate of Microwave-Induced In Situ Amorphization of Celecoxib

Molecules ◽

10.3390/molecules26010110 ◽

2020 ◽

Vol 26 (1) ◽

pp. 110

Author(s):

Nele-Johanna Hempel ◽

Tra Dao ◽

Matthias M. Knopp ◽

Ragna Berthelsen ◽

Korbinian Löbmann

Keyword(s):

Polyethylene Glycol ◽

Microwave Radiation ◽

Magnesium Stearate ◽

Einstein Equations ◽

Dissolution Process ◽

Target Temperature ◽

Peg 4000 ◽

Lower Viscosity ◽

Model Drug

Microwaved-induced in situ amorphization of a drug in a polymer has been suggested to follow a dissolution process, with the drug dissolving into the mobile polymer at temperatures above the glass transition temperature (Tg) of the polymer. Thus, based on the Noyes–Whitney and the Stoke–Einstein equations, the temperature and the viscosity are expected to directly impact the rate and degree of drug amorphization. By investigating two different viscosity grades of polyethylene glycol (PEG), i.e., PEG 3000 and PEG 4000, and controlling the temperature of the microwave oven, it was possible to study the influence of both, temperature and viscosity, on the in situ amorphization of the model drug celecoxib (CCX) during exposure to microwave radiation. In this study, compacts containing 30 wt% CCX, 69 wt% PEG 3000 or PEG 4000 and 1 wt% lubricant (magnesium stearate) were exposed to microwave radiation at (i) a target temperature, or (ii) a target viscosity. It was found that at the target temperature, compacts containing PEG 3000 displayed a faster rate of amorphization as compared to compacts containing PEG 4000, due to the lower viscosity of PEG 3000 compared to PEG 4000. Furthermore, at the target viscosity, which was achieved by setting different temperatures for compacts containing PEG 3000 and PEG 4000, respectively, the compacts containing PEG 3000 displayed a slower rate of amorphization, due to a lower target temperature, than compacts containing PEG 4000. In conclusion, with lower viscosity of the polymer, at temperatures above its Tg, and with higher temperatures, both increasing the diffusion coefficient of the drug into the polymer, the rate of amorphization was increased allowing a faster in situ amorphization during exposure to microwave radiation. Hereby, the theory that the microwave-induced in situ amorphization process can be described as a dissolution process of the drug into the polymer, at temperatures above the Tg, is further strengthened.

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Physical and Lubrication Properties of Magnesium Stearate

Journal of Pharmaceutical Sciences ◽

10.1002/jps.2600811214 ◽

1992 ◽

Vol 81 (12) ◽

pp. 1194-1198 ◽

Cited By ~ 39

Author(s):

U.I. Leinonen ◽

H.U. Jalonen ◽

P.A. Vihervaara ◽

E.S.U. Laine

Keyword(s):

Magnesium Stearate ◽

Lubrication Properties

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Efficacy and safety of a magnesium stearate paclitaxel coated balloon catheter in the porcine coronary model

International Journal of Cardiology ◽

10.1016/j.ijcard.2020.12.071 ◽

2021 ◽

Author(s):

Stephanie Bettink ◽

Melanie Löchel ◽

Daniel Peters ◽

Wolfram Haider ◽

Ulrich Speck ◽

...

Keyword(s):

Balloon Catheter ◽

Magnesium Stearate ◽

Efficacy And Safety

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Predictive evaluation of multicomponent direct compress model tablets by integrating sphere UV-Vis spectroscopy and chemometrics

Bio-Medical Materials and Engineering ◽

10.3233/bme-211269 ◽

2021 ◽

pp. 1-12

Author(s):

Yuta Otsuka ◽

Suvra Pal

Keyword(s):

Regression Models ◽

Process Analytical Technology ◽

Compaction Pressure ◽

Principal Component ◽

Magnesium Stearate ◽

Dicalcium Phosphate ◽

Integrating Sphere ◽

Pls Regression ◽

Standard Normal Variate ◽

Vis Spectroscopy

BACKGROUND: Control of the pharmaceutical manufacturing process and active pharmaceutical ingredients (API) is essential to product formulation and bioavailability. OBJECTIVE: The aim of this study is to predict tablet surface API concentration by chemometrics using integrating sphere UV-Vis spectroscopy, a non-destructive and contact-free measurement method. METHODS: Riboflavin, pyridoxine hydrochloride, dicalcium phosphate anhydrate, and magnesium stearate were mixed and ground with a mortar and pestle, and 100 mg samples were subjected to direct compression at a compaction pressure of 6 MPa at 7 mm diameter. The flat surface tablets were then analyzed by integrating sphere UV-Vis spectrometry. Standard normal variate (SNV) normalization and principal component analysis were applied to evaluate the measured spectral dataset. The spectral ranges were prepared at 300–800 nm and 500–700 nm with SNV normalization. Partial least squares (PLS) regression models were constructed to predict the API concentrations based on two previous datasets. RESULTS: The regression vector of constructed PLS regression models for each API was evaluated. API concentration prediction depends on riboflavin absorbance at 550 nm and the excipient dicalcium phosphate anhydrate. CONCLUSION: Integrating sphere UV-Vis spectrometry is a useful tool to process analytical technology.

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Difference in the Dissolution Behaviors of Tablets Containing Polyvinylpolypyrrolidone (PVPP) Depending on Pharmaceutical Formulation After Storage Under High Temperature and Humid Conditions

Journal of Pharmacy & Pharmaceutical Sciences ◽

10.18433/j3hw3q ◽

2016 ◽

Vol 19 (4) ◽

pp. 511 ◽

Cited By ~ 2

Author(s):

Yoh Takekuma ◽

Haruka Ishizaka ◽

Masato Sumi ◽

Yuki Sato ◽

Mitsuru Sugawara

Keyword(s):

High Temperature ◽

Benzoic Acid ◽

Dissolution Rate ◽

Simple Structure ◽

Pharmaceutical Formulations ◽

Magnesium Stearate ◽

Principal Agent ◽

Amino Groups ◽

Dissolution Tests ◽

Rosuvastatin Calcium

PURPOSE. Storage under high temperature and humid conditions has been reported to decrease the dissolution rate for some kinds of tablets containing polyvinylpolypyrrolidone (PVPP) as a disintegrant. The aim of this study was to elucidate the properties of pharmaceutical formulations with PVPP that cause a decrease in the dissolution rate after storage under high temperature and humid conditions by using model tablets with a simple composition. METHODS. Model tablets, which consisted of rosuvastatin calcium or 5 simple structure compounds, salicylic acid, 2-aminodiphenylmethane, 2-aminobiphenyl, 2-(p-tolyl)benzoic acid or 4.4’-biphenol as principal agents, cellulose, lactose hydrate, PVPP and magnesium stearate as additives, were made by direct compression. The model tables were wrapped in paraffin papers and stored for 2 weeks at 40°C/75% relative humidity (RH). Dissolution tests were carried out by the paddle method in the Japanese Pharmacopoeia 16th edition. RESULTS. Model tablets with a simple composition were able to reproduce a decreased dissolution rate after storage at 40°C/75% RH. These tablets showed significantly decreased water absorption activities after storage. In the case of tablets without lactose hydrate by replacing with cellulose, a decreased dissolution rate was not observed. Carboxyl and amino groups in the structure of the principal agent were not directly involved in the decreased dissolution. 2-Benzylaniline tablets showed a remarkably decreased dissolution rate and 2-aminobiphenyl and 2-(p-tolyl)benzoic acid tablets showed slightly decreased dissolution rates, though 4,4’-biphenol tablets did not show a decrease dissolution rate. CONCLUSIONS. We demonstrated that additives and structure of the principal agent were involved in the decreased in dissolution rate for tablets with PVPP. The results suggested that one of the reasons for a decreased dissolution rate was the inclusion of lactose hydrate in tablets. The results also indicated that compounds as principal agents with low affinity for PVPP may be easily affected by airborne water under high temperature and humid conditions. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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FORMULATION AND EVALUATION OF ORAL FAST DISINTEGRATING TABLET OF IBUPROFEN USING TWO SUPER DISINTEGRANTS

International Journal of Current Pharmaceutical Research ◽

10.22159/20966 ◽

2017 ◽

Vol 9 (4) ◽

pp. 92

Author(s):

Hrishav Das Purkayastha ◽

Bipul Nath

Keyword(s):

Drug Release ◽

Magnesium Stearate ◽

Direct Compression ◽

Compression Method ◽

Disintegration Time ◽

Orally Disintegrating Tablet ◽

Rapid Release ◽

Weight Variation ◽

Fast Disintegrating Tablet

Objective: The aim of the present investigation was to design and evaluate orally disintegrating tablet (ODT) of Ibuprofen, a NSAID drug used for the treatment of arthritis with a view to improve its oral bioavailability. The focus of the current study was to develop ODT of Ibuprofen using super disintegrants for ease of administration and its physicochemical characterization.Methods: Tablets were made from blends by direct compression method. All the ingredients were passed through mesh no. 80. All the ingredients were co-ground in a pestle motor. The resulting blend was lubricated with magnesium stearate and compressed into tablets using the Cadmach single punch (round shaped, 8 mm thick) machine.Results: Physicals parameters of the prepared tablets like Hardness, Weight variation, Friability, thickness, drug content etc. found within the limits. The disintegration time of prepared ODTs was in the range of 45 to 55 seconds. In vitro dispersion time was found to be 22 to 52 seconds which may be attributed to faster uptake of water due to the porous structure formed by super disintegrants. Short disintegration and faster release of ibuprofen were observed with Cross carmellose sodium as compared to sodium starch glycollate.Conclusion: It is concluded that F3 offered the relatively rapid release of Ibuprofen when compared with other formulations. The increase in the concentrations of super disintegrants may lead to increase in the drug release. The formulation prepared with cross carmellose sodium was offered the relatively rapid release of Ibuprofen when compared with other concentrations of both the super disintegrant.

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