scholarly journals Preparation of pellets containing a standardized Artemisia annua L. extract by extrusion-spheronization

Revista Fitos ◽  
2021 ◽  
Vol 15 (1) ◽  
pp. 84-92
Author(s):  
Elviscley de Oliveira Silva ◽  
Ricardo Neves Marreto ◽  
Edemilson Cardoso da Conceição ◽  
Maria Teresa Bara
Keyword(s):  
Artemisia Annua ◽  
Antimalarial Activity ◽  
Hplc Method ◽  
Water Soluble ◽  
Solid Ratio ◽  
Solid Dosage ◽  
Artemisia Annua L ◽  
Water Soluble Drug ◽  
Average Size ◽  
Extrusion Spheronization

Artemisinin, the major substance with antimalarial activity of Artemisia annua L., is a poorly water-soluble drug. The development of pellets containing a standardized hydroethanolic extract of A. annua may overcome these drawbacks while offer an intermediate product with good technological properties for subsequent tablet manufacture. This work aimed to obtain and characterize A. annua pellets using the extrusion-spheronization technique. The extract was prepared by percolation and artemisinin content was determined using a validated HPLC method. The standardized extract was then used as a liquid binder in the preparation of pellets with different liquid: solid ratio. The formulation PF5 containing microcrystalline cellulose: A. annua extract (40:58) resulted in pellets with 1.49 ± 0.02 % (w/w) artemisinin, average size of approximately 500 µm and sphericity of 0.82 ± 0.08. These pellets were encapsulated in hard gelatin capsules and the percentage released was higher than 80% in 10 min using 0.1N HCl and phosphate buffer media. These data allow to suggest that the pelletizing strategy used made it possible to achieve the desired artemisinin dissolution and generates perspectives for the potential further use of the A. annua pellets as a solid dosage form for malaria treatment.

Formulation development and characterization of highly water-soluble drug-loaded extended-release pellets prepared by extrusion–spheronization technique

2019 ◽  
Vol 16 (5) ◽  
pp. 1351-1365
Author(s):  
Muhammad Iqbal Nasiri ◽  
Rabia Ismail Yousuf ◽  
Muhammad Harris Shoaib ◽  
Kamran Zaheer ◽  
Tariq Ali ◽  
...  
Keyword(s):  
Extended Release ◽  
Water Soluble ◽  
Formulation Development ◽  
Water Soluble Drug ◽  
Extrusion Spheronization

scholarly journals Systematic and Model-Assisted Process Design for the Extraction and Purification of Artemisinin from Artemisia annua L.—Part III: Chromatographic Purification

Processes ◽  
2018 ◽  
Vol 6 (10) ◽  
pp. 180 ◽  
Author(s):  
Fabian Mestmäcker ◽  
Axel Schmidt ◽  
Maximilian Huter ◽  
Maximilian Sixt ◽  
Jochen Strube
Keyword(s):  
High Performance ◽  
Artemisia Annua ◽  
Batch Process ◽  
Pilot Scale ◽  
Hplc Method ◽  
Artemisia Annua L ◽  
Reproducibility Study ◽  
Extraction And Purification ◽  
Layer Chromatography ◽  
Characteristic Process

In this study, the purification of an extract from Artemisia annua L. using chromatographic methods is studied. In a first step, a screening of different phases and solvents using thin-layer chromatography (TLC) was performed. Then, a laboratory-scale high performance liquid chromatography (HPLC) method was developed and transferred to a pilot scale. A reproducibility study based on 120 injections was carried out. The batch process that was developed and the results from a designed continuous simulated moving bed (SMB) chromatography were compared based on characteristic process numbers and economy.

Investigation on release of highly water soluble drug from matrix-coated pellets prepared by extrusion–spheronization technique

2016 ◽  
Vol 13 (2) ◽  
pp. 333-344 ◽  
Author(s):  
Muhammad Iqbal Nasiri ◽  
Rabia Ismail Yousuf ◽  
Muhammad Harris Shoaib ◽  
Muhammad Fayyaz ◽  
Faaiza Qazi ◽  
...  
Keyword(s):  
Water Soluble ◽  
Water Soluble Drug ◽  
Extrusion Spheronization

scholarly journals SYSTEMATIC REVIEW: COCRYSTAL AS EFFORTS TO IMPROVE PHYSICOCHEMICAL AND BIOAVAILABILITY PROPERTIES OF ORAL SOLID DOSAGE FORM

2021 ◽  
pp. 43-52
Author(s):  
IYAN SOPYAN ◽  
ALVIN B. ◽  
INSAN SUNAN K. S. ◽  
CIKRA IKHDA N. H. S.
Keyword(s):  
Physicochemical Properties ◽  
Dosage Form ◽  
Water Solubility ◽  
Drug Stability ◽  
Water Soluble ◽  
New Drugs ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Water Soluble Drug ◽  
Biopharmaceutical Properties

Water solubility and low bioavailability of active pharmaceutical ingredients are some of the main challenges in the process of developing new drugs, especially drugs in oral solid dosage forms. One way to improve drug solubility is the principle of cocrystallization. Cocristallyzation itself is the process of combining the active ingredients of a less water-soluble drug with a coformer so that it becomes more soluble. Pharmaceutical cocrystal provides benefits to improve physicochemical properties without affecting its pharmacological properties. In this review, we have reviewed literature discussions and research that discuss co-crystallization as an aid to improve the physicochemical and bioavailability of drugs and also discuss some drugs in the form of cocrystal and their improvement in physicochemical-biopharmaceutical properties. The main references data used in this review are research journals published in the past 10 y (2010-2020) using keywords: cocrystal, physicochemistry, bioavailability, and solid dosage form, and using google scholar as a database. Discussion on the effect of cocrystal on physicochemical properties and bioavailability of drugs was produced. The method of producing cocrystal and its characterization was also discussed. Cocrystal offers a promising approach to improve the physicochemical properties of API. The benefits of cocrystal can be observed through increased solubility, dissolution rate, permeability, bioavailability, drug stability, and tabletability.

scholarly journals The Impact of Carbon Source, Explants and Growth Regulators on Callogenesis and Organogenesis of Artemisia annua

2015 ◽  
Vol 7 (4) ◽  
pp. 475-485 ◽  
Author(s):  
Bita GHASSEMI ◽  
Fatemeh DEHGHAN NAYERI ◽  
Ramin HOSSEINI
Keyword(s):  
Carbon Source ◽  
Artemisia Annua ◽  
Antimalarial Activity ◽  
Leaf Explants ◽  
Basal Medium ◽  
Stem Explants ◽  
Root Explants ◽  
Artemisia Annua L ◽  
High Concentrations ◽  
The Impact

Artemisinin, a sesquiterpene lactone isolated from Artemisia annua L. plant is known for its antimalarial activity. The low content of artemisinin has stimulated researchers to enhance its production through biotechnological approaches such as tissue culture. The present study was initiated to study the effect of some important factors alone and in combination, on the callogenesis and organogenesis of Artemisia annua. The type of carbon source had a significant effect on NAA efficiency to callogenesis of A. annua, whereas the best callogenesis of A. absinthium was observed at 2 mg/L BAP + 30 g/L sucrose and in the absence of NAA, with root explants. Presence of BAP also had an important effect on callogenesis, especially in high concentrations. A suitable suspension culture was obtained in the MS basal medium containing 0.5 mg/L NAA and BAP, with 30 g/L glucose. Artemisinin was naturally production was at least 0.03 mg/g (w.dt) at the first day and peaked on the 16th day with 0.31 mg/g (w.dt) in the cell culture of A. annua. The maximum number of shoots (2.167 ± 1.484) was induced at 0.5 mg/L BAP + 0.1 mg/L NAA + glucose (30 g/L) with leaf explants. However, treatments containing glucose did not show a good shoot induction. Longer shoots were induced in the medium containing either 0.5 mg/l NAA + 0.5 mg/l BAP + sucrose with leaf explants (1.493 cm ± 0.342) or 0.5 mg/l NAA + sucrose with stem explants (0.697 cm ± 0.930). Medium containing 0.5 or 2 mg/l NAA and sucrose (without BAP) induced more roots though.

scholarly journals RP-HPLC method development and validation for the quantification of Efonidipine hydrochloride in HME processed solid dispersions

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Ashish S. Rajput ◽  
Durgesh K. Jha ◽  
Sharda Gurram ◽  
Devanshi S. Shah ◽  
Purnima D. Amin
Keyword(s):  
Method Development ◽  
Solid Dispersions ◽  
Hplc Method ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Intermediate Precision ◽  
Rp Hplc ◽  
Water Soluble Drug ◽  
Hplc Grade Acetonitrile ◽  
Eudragit Epo

Abstract Background Efonidipine hydrochloride (EFO) is a poorly water-soluble drug and, hence, has poor bioavailability. Solid dispersions (SDs) of EFO using Eudragit EPO were prepared using hot-melt extrusion (HME) for the first time. The current study aims at developing a simple RP-HPLC method to quantify EFO in the developed SDs. Results The chromatographic separation was carried out on an Agilent Eclipsed XDB-C18 column (4.6 × 250 mm), packed with 5 μm particles. The optimized mobile phase consisted of HPLC grade acetonitrile and 0.020 mol/L KH2PO4 (pH 2.5) buffer in the ratio of 85:15 v/v with a flow rate optimized at 1.2 ml/min. The developed method was validated for system suitability, linearity, accuracy, precision, and robustness. The linearity results showed an excellent linear relationship between the drug concentration and peak area, indicating the peak area is directly proportional to the analyte concentration within a specific range and an excellent correlation coefficient of 0.9998. Intermediate precision and repeatability confirmed that the method provides precise results with %RSD value less than 2% for EFO. The assay results of the developed formulations were in the acceptable range with RSD less than 2%. The enhanced drug dissolution from the Eudragit EPO carrier with 10% Citric Acid (CA) is attributed to the conversion of the drug from crystalline to amorphous form, and microenvironmental acidic pH provided by CA. Conclusion In a nutshell, the developed RP-HPLC method showed excellent ability to differentiate the formulations and highlights the role of the polymer and the plasticizer. Graphical abstract

Comparative phytochemical study on the phenolic compounds content of Artemisia annua L. from wild populations in Republic of Moldova

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
CP Stefanache ◽  
OC Bujor ◽  
R Necula ◽  
V Ghendov ◽  
A Trifan ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Artemisia Annua ◽  
Wild Populations ◽  
Phytochemical Study ◽  
Republic Of Moldova ◽  
Artemisia Annua L

The fixation of a water-soluble drug in calcium-induced alginate gel beads and the release profiles from the vehicle.

1997 ◽  
Vol 12 (1) ◽  
pp. 49-55 ◽  
Author(s):  
Yoshifumi Murata ◽  
Norie Katayana ◽  
Takashi Kajita ◽  
Etsuko Miyamoto ◽  
Susumu Kawashima
Keyword(s):  
Water Soluble ◽  
Alginate Gel ◽  
Gel Beads ◽  
Water Soluble Drug ◽  
Release Profiles

NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo
Keyword(s):  
Drug Release ◽  
Droplet Size ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Particle Size Reduction ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

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