scholarly journals PARTIAL AMORPHIZATION OF POORLY-SOLUBLE SIMVASTATIN USP USING MEDIA MILLING IN SYNERGISM WITH SPRAY-DRYING

2020 ◽  
pp. 114-121
Author(s):  
HARITA R. DESAI ◽  
ARCHANA B. RAJADHYAX ◽  
PURNIMA D. AMIN
Keyword(s):  
Differential Scanning Calorimetry ◽  
Spray Drying ◽  
Scanning Calorimetry ◽  
Intrinsic Dissolution ◽  
X Ray ◽  
Media Milling ◽  
Rate Testing ◽  
Poorly Soluble ◽  
Spray Dried

Objective: The objective of the current study was to explore top down methods of size reduction like high speed homogenisation and media milling in synergism with spray drying in amorphization and solubility enhancement of BCS Class II antilipidemic drug Simvastatin USP. Methods: Spray-dried micronized simvastatin USP was formulated by homogenisation and media milling of drug suspension in optimized stabilizer solution. Stabilizer combination, duration of homogenisation and ball milling and drug: stabilizer ratio was optimized. The obtained dispersion was transformed into solid powder using spray drying. The obtained Spray-dried micronized Simvastatin USP was evaluated for visual morphology, Infrared spectroscopy, Differential scanning calorimetry, in vitro drug release studies, X-Ray diffractometry, Scanning electron microscopy, contact angle measurement, solubility studies, dispersibility studies and intrinsic dissolution rate testing. Results: Spray-dried micronized simvastatin USP was found to show amorphization of crystalline Simvastatin USP as confirmed by the absence of drug peak in Differential scanning calorimetry and lowered signal intensity in X-Ray diffraction studies. Spray-dried micronized Simvastatin USP was found to show enhanced drug hydrophilicity and solubility as confirmed by lowering in contact angle and increase in solubility and ease of dispersibility observations. In vitro dissolution testing and intrinsic dissolution rate testing were found to show an increase in drug release from 11% to 79% and 4 mg min-1 cm-2 to 17 mg min-1 cm-2 for drug and Spray-dried micronized Simvastatin USP respectively. Conclusion: Media milling in synergism with spray-drying was found to be a prospective solubility enhancement technique for poorly-soluble Simvastatin USP.

The preparation, characterization, structure and dissolution analysis of apremilast solvatomorphs

2017 ◽  
Vol 73 (4) ◽  
pp. 305-313 ◽  
Author(s):  
Yun-Deng Wu ◽  
Xiao-Lei Zhang ◽  
Xiao-Hong Liu ◽  
Jian Xu ◽  
Mei Zhang ◽  
...  
Keyword(s):  
Differential Scanning Calorimetry ◽  
Hydrogen Bonding ◽  
Psoriatic Arthritis ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Dissolution Rates ◽  
X Ray ◽  
Similarity Factor ◽  
Hydrogen Bonding Interactions

Apremilast (AP) {systematic name: (S)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-4-acetamidoisoindoline-1,3-dione} is an inhibitor of phosphodieasterase-4 (PDE4) and is indicated for the treatment of adult patients with active psoriatic arthritis. The ability of AP to form solvates has been investigated and three solvatomorphs of AP, namely, the AP ethyl acetate hemisolvate, C22H24N2O7S·0.5C4H8O2, the AP toluene hemisolvate, C22H24N2O7S·0.5C7H8, and the AP dichloromethane monosolvate, C22H24N2O7S·CH2Cl2, were obtained. The three AP solvatomorphs were characterized by X-ray powder diffraction, thermogravimetric analysis and differential scanning calorimetry. Single-crystal X-ray diffraction was used to analyze the structures, crystal symmetry, packing modes, stoichiometry and hydrogen-bonding interactions of the solvatomorphs. In addition, dissolution analyses were performed to study the dissolution rates of different AP solvatomorph tablets in vitro and to make comparisons with commercial apremilast tablets (produced by Celgene); all three solvatomorphs showed similar dissolution rates and similar values of the similarity factor f2 in a comparison of their dissolution profiles.

Differential scanning calorimetry of human blood serum exposed in vitro to X-ray radiation

2019 ◽  
Vol 680 ◽  
pp. 178358 ◽  
Author(s):  
Agnieszka Kiełboń ◽  
Anna Michnik ◽  
Kinga Polaczek Grelik ◽  
Klaudia Duch ◽  
Ewa Sadowska-Krępa
Keyword(s):  
Differential Scanning Calorimetry ◽  
Blood Serum ◽  
Human Blood ◽  
Human Blood Serum ◽  
Scanning Calorimetry ◽  
X Ray

scholarly journals Two Novel Palbociclib-Resorcinol and Palbociclib-Orcinol Cocrystals with Enhanced Solubility and Dissolution Rate

Pharmaceutics ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 23
Author(s):  
Chenxin Duan ◽  
Wenwen Liu ◽  
Yunwen Tao ◽  
Feifei Liang ◽  
Yanming Chen ◽  
...  
Keyword(s):  
Water Solubility ◽  
Cancer Drug ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Dissolution Rates ◽  
Intrinsic Dissolution ◽  
X Ray ◽  
Enhanced Solubility

Palbociclib (PAL) is an effective anti-breast cancer drug, but its use has been partly restricted due to poor bioavailability (resulting from extremely low water solubility) and serious adverse reactions. In this study, two cocrystals of PAL with resorcinol (RES) or orcinol (ORC) were prepared by evaporation crystallization to enhance their solubility. The cocrystals were characterized by single crystal X-ray diffraction, Hirshfeld surface analysis, powder X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared and scanning electron microscopy. The intrinsic dissolution rates of the PAL cocrystals were determined in three different dissolution media (pH 1.0, pH 4.5 and pH 6.8), and both cocrystals showed improved dissolution rates at pH 1.0 and pH 6.8 in comparison to the parent drug. In addition, the cocrystals increased the solubility of PAL at pH 6.8 by 2–3 times and showed good stabilities in both the accelerated stability testing and stress testing. The PAL-RES cocrystal also exhibited an improved relative bioavailability (1.24 times) than PAL in vivo pharmacokinetics in rats. Moreover, the in vitro cytotoxicity assay of PAL-RES showed an increased IC50 value for normal cells, suggesting a better biosafety profile than PAL. Co-crystallization may represent a promising strategy for improving the physicochemical properties of PAL with better pharmacokinetics.

A Comparative Study of Acyclovir icroencapsulation by Novel Solvent Evaporation-Matrix Erosion and Spray Drying Techniques

2012 ◽  
Vol 5 (1) ◽  
pp. 1627-1637
Author(s):  
J P Raval ◽  
D R Naik
Keyword(s):  
Spray Drying ◽  
Ethyl Cellulose ◽  
Drug Loading ◽  
In Vitro Release ◽  
Spherical Geometry ◽  
Solvent Evaporation ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Spray Dried

Designing and evaluating a multiparticulate controlled release dosage form, to increase the efficacy of acyclovir (a selective antiherpes agent). Spray drying technique for microsphere production is compared with novel solvent evaporation-matrix erosion technique for variable drug loading in different concentration of ethyl cellulose. The microspheres were characterized for physicochemical properties. The microspheres sizes were ranged from 7-25 μm. The spray dried microspheres had better encapsulation efficiency (up to 91%) compared to that of novel solvent evaporation-matrix erosion technique microspheres. Scanning electron microscopy confirmed spherical geometry due to high cross-linking density. Differential scanning calorimetry, Fourier-transform infrared spectroscopy and x-ray diffraction studies showed chemical stability and intactness of entrapped drug in the microspheres. In vitro release of acyclovir from spray dried microspheres continued for longer period compared to novel solvent evaporation-matrix erosion method. Overall, the release studies depended on the concentration of ethyl cellulose, extent of drug loading, and the technique used to prepare microspheres. Thus, marked retardation of drug release may provide a useful effective anti-retroviral drug therapy.  

scholarly journals ENCAPSULATION OF BARBERRY FRUIT EXTRACTS BY SPRAY DRYING AND LIPOSOME ENTRAPMENT

2020 ◽  
Vol 49 (2) ◽  
pp. 125-134
Author(s):  
S. Berenji Ardestani ◽  
M. A. Sahari ◽  
M. Barzegar
Keyword(s):  
Differential Scanning Calorimetry ◽  
Spray Drying ◽  
Antioxidant Properties ◽  
Natural Food ◽  
Scanning Calorimetry ◽  
Fruit Extracts ◽  
Food Colour ◽  
Carbonated Drinks ◽  
Spray Dried ◽  
Thermal Oxidative Decomposition

Barberry is a native Iranian plant including species Berberis integerrima and B. vulgaris. Barberry fruit is used for preparing sauces, jellies, carbonated drinks, candies, food colour powders, jams, marmalades, chocolates, juices, and nectars. They are used as a natural food colorant rich in anthocyanins instead of harmful artificial ones. They contain polyphenols and antioxidants that reduce damage from free radicals and prevent chronic diseases and cancers. Barberry fruit extracts were encapsulated in maltodextrin by spray drying and Liposome Entrapment. The sizes of spray dried particles were reported 1–20 μm by SEM. Dimensions of empty and extract loaded liposomes (B. vulgaris and B. integerrima) were 18–28, 37–51, and 51–77 nm, respectively, by FE-SEM. The moist diameter of liposomes measured by dynamic light scattering (DLS) method at day 0 and after 6 months at –18 °C were as follows; empty liposomes: 163.9±2.23 and 378.90±4.98, liposomes loaded with extracts: 135.2±2.04 and 160.90±2.19 (B. vulgaris) and 113.4±1.83 and 144.20±2.01 nm (B. integerrima). Evaluation of thermal-oxidative decomposition from Differential scanning calorimetry (DSC) results at 0–45–90 days showed that the antioxidant activity and the onset temperature of the encapsulated extract was higher than the control. The extracts encapsulated in liposomes, especially B. integerrima extract, had better antioxidant properties.

scholarly journals Development and Characterization of Nanostructured Pharmacosomal Mesophases: An Innovative Delivery System for Bioactive Peptides

2018 ◽  
Vol 8 (4) ◽  
pp. 609-615 ◽  
Author(s):  
Maryam Rezvani ◽  
Javad Hesari ◽  
Seyed Hadi Peighambardoust ◽  
Maria Manconi ◽  
Hamed Hamishehkar
Keyword(s):  
Differential Scanning Calorimetry ◽  
Fourier Transform ◽  
Infrared Spectroscopy ◽  
Small Angle ◽  
Bioactive Peptides ◽  
Polarized Light ◽  
Scanning Calorimetry ◽  
X Ray ◽  
X Ray Scattering

Purpose: To potentially enhance the bioavailability and extend the bioactivity effectiveness of Isoleucine-Proline-Proline (IPP, an antihypertensive bioactive peptide of dairy origin), a novel Lyotropic Liquid Crystalline Pharmacosomal Nanoparticle (LLCPNP) was synthesized, and its physicochemical and technological characteristics were studied. Methods: LLCPNPs precursors were developed using IPP and soy phosphatidylcholine via complex formation. Polarized light microscopy, small angle X-ray scattering, differential scanning calorimetry, dynamic light scattering and Fourier transform infrared spectroscopy were employed to characterize the physicochemical properties of the nanoparticles. The in-vitro release and its related mechanisms were also studied. Results: Fourier transform infrared spectroscopy confirmed the complexation between the components of LLCPNPs. Phase behavior evaluation by polarized light microscope showed the characteristic birefringent texture. These findings along with those of small angle X-ray scattering and differential scanning calorimetry proved the formation of lamellar LLCPNPs. These particles represented nanometric size (<100 nm), high incorporation efficiency (93.72%) and proper physicochemical stability during long-term storage. In-vitro studies demonstrated a sustained release behavior fitted to non-Fickian diffusion and Higuchi kinetic models. Conclusion: The present study results emphasized that LLCPNPs could be proposed as an unrivaled carrier to promote the bioavailability, stability and shelf-life of nutraceutical and biopharmaceutical formulations containing bioactive peptides.

scholarly journals PENGEMBANGAN SISTEM PEMBAWA ALBUMIN NANOPARTIKEL UNTUK SILIMARIN DAN KAJIAN SIFAT FISIK SERTA PROFIL PELEPASANNYA SECARA IN VITRO

2017 ◽  
Vol 7 (2) ◽  
pp. 23-29
Author(s):  
Rini Ambarwati ◽  
Heni Rachmawati
Keyword(s):  
Differential Scanning Calorimetry ◽  
Bovine Serum Albumin ◽  
Serum Albumin ◽  
Loading Capacity ◽  
X Ray Diffraction ◽  
Silybum Marianum ◽  
Scanning Calorimetry ◽  
X Ray

Silimarin merupakan senyawa flavonolignan yang berasal dari tumbuhan Silybum marianum (Asteraceae). Silimarin memiliki efek farmakologi sebagai antikanker dan hepatoprotektor, tetapi senyawa ini memiliki kelarutan yang rendah dalam air. Tujuan penelitian ini adalah mengembangkan formulasi silimarin dalam sistem pembawa nano dengan teknik desolvasi. Pembawa yang digunakan adalah serum albumin (bovine serum albumin/BSA). Kombinasi silimarin dalam BSA diharapkan dapat meningkatkan efikasi silimarin sebagai anti kanker karena permeabilitas BSA yang lebih baik pada sel kanker. Evaluasi standar terhadap nanopartikel silimarin-BSA meliputi ukuran dan distribusi ukuran partikel, zeta potensial, morfologi nanopartikel, kristalinitas, sifat termal, spektroskopi inframerah, efisiensi penjeratan serta profil pelepasan silimarin dari BSA nanopartikel pada 2 media berbeda (HCl 0,1 N & PBS pH 7,4). Nanopartikel BSA- silimarin memiliki ukuran partikel 174,23 13,94 nm; distribusi ukuran partikel 0,185 0,052; efisiensi penjeratan 90,54 0,098 %; loading capacity 30,18 0,036 % dan zeta potensial -1,62 mV. Hasil analisis menggunakan DSC (differential scanning calorimetry), XRD (X-ray diffraction) dan spektroskopi inframerah menunjukan bahwa nanopartikel silimarin berhasil terenkapsulasi di dalam nanopartikel BSA, dan BSA-silimarin memiliki bentuk amorf. Setelah 1 jam uji pelepasan, terdapat sebanyak 21,89% silimarin terlepas dalam HCl 0,1 N dan 54,84% silimarin terlepas dalam PBS pH 7,4 sehingga dapat disimpulkan bahwa silimarin-BSA memiliki kelarutan yang baik dalam air. Oleh karena itu, perlu dilakukan pengujian lebih lanjut untuk mengkaji akt ivitas serta perilaku silimarin-BSA in vivo untuk mengkonfirmasi data in vitro.

scholarly journals ENHANCEMENT OF DISSOLUTION AND STABILITY OF CANDESARTAN CILEXETIL–LOADED SILICA POLYMERS

2019 ◽  
pp. 64-70
Author(s):  
Mai Khanfar ◽  
Bashar Al Taani ◽  
Eman Mohammad
Keyword(s):  
Spray Drying ◽  
Solid Dispersion ◽  
Candesartan Cilexetil ◽  
Solid Dispersions ◽  
Porous Silica ◽  
Amorphous Solid ◽  
Silica Particles ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Spray Dried

Objective: To prepare stable amorphous solid dispersions of candesartan cilexetil (CAN) with different types of silica, including non-porous (aerosil 200) and porous silica (sylysia 350) using the spray-drying method. Methods: various ratios of candesartan cilexetil (CAN) were spray dried with aerosil and sylysia. Powder x-ray diffraction (x-ray) differential scanning calorimetry (DSC), SEM were used to characterize the spray dried powders in addition to dissolution and stability studies. Results: X-ray results showed that the spray–dried (CAN) in the prepared solid dispersion were in amorphous form irrespective of the used silica. In (DSC) analysis, the melting peak of spray-dried (CAN-silica) solid dispersion disappeared. Dissolution property of (CAN) was remarkably improved by formulating with silica particles. In comparing the effect of the type of the silica particles, the dissolution rate of (CAN) from the spray-dried (CAN-sylysia) was faster than that (CAN-aerosil 200) irrespective of the drug content. It was also shown that the spray-dried formulation with silica did not recrystallize when storing at severe storage conditions (40 °C, 75% RH) for three months, while spray-dried (CAN) without silica easily re-crystallized under the same conditions. Conclusion: Spray drying of (CAN) with sylysia 350 is an efficient method to enhance the dissolution and stability of the drug.

Optimization of Microcrystalline Cellulose PH 101, Lactose, and Kollidon® K 30 To Obtain Co-Processed Excipient Through Spray Drying

2017 ◽  
Vol 7 (2) ◽  
Author(s):  
Kusuma P. ◽  
Syukri Y ◽  
Sholehuddin F. ◽  
Fazzri N. ◽  
Romdhonah . ◽  
...  
Keyword(s):  
Spray Drying ◽  
Microcrystalline Cellulose ◽  
Chemical Change ◽  
Direct Compression ◽  
Flow Properties ◽  
Scanning Calorimetry ◽  
Compression Process ◽  
Infrared Spectrophotometer ◽  
Physical Mixtures ◽  
Spray Dried

The most efficient tablet processing method is direct compression. For this method, the filler-binder can be made by coprocessing via spray drying method. The purpose of this study was to investigate the effect of spray dried co-processing on microcrystalline cellulose (MCC) PH 101, lactose and Kollidon® K 30 as well as to define the optimum proportions. Spray dried MCC PH 101, lactose, and Kollidon® K 30 were varied in 13 different mixture design proportions to obtain compact, free-flowing filler-binder co-processed excipients (CPE). Compactibility and flow properties became the key parameters to determine the optimum proportions of CPE that would be compared to their physical mixtures. The result showed that the optimum proportion of CPE had better compactibility and flow properties than the physical mixtures. The optimum CPE, consisting of only MCC PH 101 and Kollidon® K 30 without lactose, that were characterized using infrared spectrophotometer, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscope (SEM) indicated no chemical change therein. Therefore, this study showed that spray dried MCC PH 101, lactose and Kollidon® K 30 could be one of the filler-binder alternatives for direct compression process.

Studies on the Preparation, Characterization and Solubility of -Cyclodextrin-Roxythromycin Inclusion Complexes

2009 ◽  
Vol 2 (2) ◽  
pp. 523-530
Author(s):  
D. Nagasamy Venkatesh ◽  
S. Karthick ◽  
M. Umesh ◽  
G. Vivek ◽  
R.M. Valliappan ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Phase Solubility ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Ir Studies ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

Roxythromycin/ β-cyclodextrin (Roxy/ β-CD) dispersions were prepared with a view to study the influence of β-CD on the solubility and dissolution rate of this poorly soluble drug. Phase-solubility profile indicated that the solubility of roxythromycin was significantly increased in the presence of β-cyclodextrin and was classified as AL-type, indicating the 1:1 stoichiometric inclusion complexes. Physical characterization of the prepared systems was carried out by differential scanning calorimetry (DSC), X-ray diffraction studies (XRD) and IR studies. Solid state characterization of the drug β-CD binary system using XRD, FTIR and DSC revealed distinct loss of drug crystallinity in the formulation, ostensibly accounting for enhancement of dissolution rate.

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