amorphous drug
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Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 149
Author(s):  
Michael Choi ◽  
Stuart C. Porter ◽  
Axel Meisen

Oral solid dosage forms that contain APIs in the amorphous state have become commonplace because of many drug substances exhibiting poor water solubility, which negatively impacts their absorption in the human GI tract. While micronization, solvent spray-drying, and hot-melt extrusion can address solubility issues, spray coating of the APIs onto beads and tablets offers another option for producing amorphous drug products. High-level comparisons between bead and tablet coating technologies have the potential for simpler equipment and operation that can reduce the cost of development and manufacturing. However, spray coating directly onto tablets is not without challenges, especially with respect to meeting uniformity acceptance value (AV) criteria, comprising accuracy (mean) and precision (variance) objectives. The feasibility of meeting AV criteria is examined, based on mathematical models for accuracy and precision. The results indicate that the main difficulty in manufacturing satisfactory drug-layered tablets by spray coating is caused by the practical limitations of achieving the necessary coating precision. Despite this limitation, it is shown that AV criteria can be consistently met by appropriate materials monitoring and control as well as processing equipment setup, operation, and maintenance.


Gels ◽  
2022 ◽  
Vol 8 (1) ◽  
pp. 38
Author(s):  
Madeleine S. A. Tan ◽  
Preeti Pandey ◽  
James R. Falconer ◽  
Dan J. Siskind ◽  
Alexandra Balmanno ◽  
...  

(1) Background: Clozapine is the most effective antipsychotic. It is, however, associated with many adverse drug reactions. Nose-to-brain (N2B) delivery offers a promising approach. This study aims to develop clozapine-encapsulated thermosensitive sol–gels for N2B delivery. (2) Methods: Poloxamer 407 and hydroxypropyl methylcellulose were mixed and hydrated with water. Glycerin and carbopol solutions were added to the mixture and stirred overnight at 2–8 °C. Clozapine 0.1% w/w was stirred with polysorbate 20 (PS20) or polysorbate 80 (PS80) at RT (25 °C) before being added to the polymer solution. The final formulation was made to 10 g with water, stirred overnight at 2–8 °C and then adjusted to pH 5.5. (3) Results: Formulations F3 (3% PS20) and F4 (3% PS80) were selected for further evaluation, as their gelation temperatures were near 28 °C. The hydrodynamic particle diameter of clozapine was 18.7 ± 0.2 nm in F3 and 20.0 ± 0.4 nm in F4. The results show a crystallinity change in clozapine to amorphous. Drug release studies showed a 59.1 ± 3.0% (F3) and 53.1 ± 2.7% (F4) clozapine release after 72 h. Clozapine permeated after 8 h was 20.8 ± 3.0% (F3) and 17.8 ± 3.1% (F4). The drug deposition was higher with F4 (144.8 ± 1.4 µg/g) than F3 (110.7 ± 2.7 µg/g). Both sol–gels showed no phase separation after 3 months. (4) Conclusions: Binary PS80-P407 mixed micelles were more thermodynamically stable and rigid due to the higher synergism of both surfactants. However, binary mixed PS20-P407 micelles showed better drug permeation across the nasal mucosa tissue and may be a preferable carrier system for the intranasal administration of clozapine.


2021 ◽  
Vol 8 (3) ◽  
pp. 242
Author(s):  
Febrina Aulia Dewi ◽  
Iyan Sopyan ◽  
Taofik Rusdiana

Ko-amorf adalah suatu sistem multikomponen padat yang mengandung zat aktif dan molekul dengan berat molekul rendah lainnya (koformer) yang dapat berupa eksipien atau zat aktif yang relevan secara farmakologis. Formulasi ko-amorf yang dibuat dengan metode preparasi dan jenis koformer yang berbeda dapat menghasilkan perbedaan yang signifikan dalam stabilitas fisik dan profil disolusi suatu bentuk ko-amorf. Tujuan penulisan dari artikel review ini adalah untuk menggali informasi lebih dalam tentang sistem ko-amorf, klasifikasi ko-amorf, karakterisasi ko-amorf serta pengaruh jenis koformer dan metode preparasi ko-amorf terhadap pembentukan ko-amorf. Artikel review ini disusun dengan literature search melalui PubMed, MDPI dan Science Direct dengan memasukkan kata kunci co-amorphous, co-amorphous formulations, co-amorphous stabilizers, co-amorphous drug formulations. Dari review ini ditemukan terdapat beberapa jenis koformer yang dapat digunakan untuk pembentukan ko-amorf yaitu dapat berupa zat aktif yang relevan secara farmakologis dan eksipien seperti diantaranya yaitu asam amino, asam karboksilat, asam tanat, quercetin, sakarin dan nikotinamid. Dan untuk metode preparasi ko-amorf yang dapat digunakan diantaranya yaitu ball milling, cryomilling, melt quenching/ quench cooling, hot melt extrusion, solvent evaporation, spray drying, freeze drying hingga teknologi seperti supercritical antisolvent dan microwave technique. Keberhasilan pembentukan ko-amorf ditentukan diantaranya oleh pemilihan jenis koformer yang melibatkan berbagai sifat yang perlu dipertimbangkan, seperti Tg, potensial ikatan hidrogen, ketercampuran/ miscibility, atau perilaku kristalisasi. Sifat zat aktif dan eksipien seperti stabilitas termal, suhu leleh dan kecenderungan kristalisasi zat aktif dan eksipien, menjadi faktor yang perlu diperhatikan dalam pemilihan metode preparasi ko-amorf.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1735
Author(s):  
Sebastian Groёl ◽  
Tim Menzen ◽  
Gerhard Winter

Studying the thermal history and relaxation of solid amorphous drug product matrices by calorimetry is a well-known approach, particularly in the context of correlating the matrix parameters with the long-term stability of freeze-dried protein drug products. Such calorimetric investigations are even more relevant today, as the application of new process techniques in freeze-drying (which strongly influence the thermal history of the products) has recently gained more interest. To revive the application of calorimetric methods, the widely scattered knowledge on this matter is condensed into a review and completed with new experimental data. The calorimetric methods are applied to recent techniques in lyophilization, such as controlled nucleation and aggressive/collapse drying. Phenomena such as pre-Tg events in differential scanning calorimetry and aging shoulders in isothermal microcalorimetry are critically reviewed and supplemented with data of freeze-dried products that have not been characterized with these methods before.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1271
Author(s):  
Xin Yao ◽  
Amy Lan Neusaenger ◽  
Lian Yu

Amorphous formulations provide a general approach to improving the solubility and bioavailability of drugs. Amorphous medicines for global health should resist crystallization under the stressful tropical conditions (high temperature and humidity) and often require high drug loading. We discuss the recent progress in employing drug–polymer salts to meet these goals. Through local salt formation, an ultra-thin polyelectrolyte coating can form on the surface of amorphous drugs, immobilizing interfacial molecules and inhibiting fast crystal growth at the surface. The coated particles show improved wetting and dissolution. By forming an amorphous drug–polymer salt throughout the bulk, stability can be vastly enhanced against crystallization under tropical conditions without sacrificing the dissolution rate. Examples of these approaches are given, along with suggestions for future work.


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