scholarly journals Enhancement of Solubility BCS Class II and IV Pharmaceuticals by Liqusolid Technique: A review

2020 ◽  
Vol 2 (2) ◽  
pp. 77
Author(s):  
Dwi Retno Sari ◽  
Yoga Windhu Wardhana ◽  
Taofik Rusdiana
Keyword(s):  
Contact Angle ◽  
Drug Release ◽  
Manufacturing Industry ◽  
Fourier Transforms ◽  
Class Ii ◽  
Production Costs ◽  
Active Pharmaceutical Ingredients ◽  
Scanning Calorimetry ◽  
Pharmaceutical Ingredients ◽  
Volatile Solvents

Many techniques can be used to improve drug solubility, which is the development of the liquisolid technique. This technique has a mechanism for increasing the surface area of the drug as well as wetting from the addition of non-volatile solvents resulting in a lower surface tension and contact angle, so the solubility and drug release very increases. Liquisolid tablets show a lower contact angle compared to the conventional tablets. The liquisolid technique approach is also promising because the process is simple in making low production costs and allows the manufacturing industry, including non-volatile solvents, fillers, dryers, and disintegrants. Liquisolid characterized by specific instruments such as powder x-ray diffraction (PXRD), Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and scanning electron microscope (SEM). Several liquisolid techniques are described in this review. The liquisolid technique is proven and able to change the physicochemical properties of active pharmaceutical ingredients, especially the solubility, drug release, and stability of the formula so that this technique can be a solution for class II and IV BCS pharmaceutical active drug classes.Keywords: Active Pharmaceutical Ingredients, Contact Angle, Solubility, Drug Release, Stability, Liquisolid Technique

scholarly journals Self-assembled sorbitol-derived supramolecular hydrogels for the controlled encapsulation and release of active pharmaceutical ingredients

2015 ◽  
Vol 51 (35) ◽  
pp. 7451-7454 ◽  
Author(s):  
Edward J. Howe ◽  
Babatunde O. Okesola ◽  
David K. Smith
Keyword(s):  
Drug Release ◽  
Controlled Drug Release ◽  
The Self ◽  
Active Pharmaceutical Ingredients ◽  
Supramolecular Hydrogel ◽  
Pharmaceutical Ingredients ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Self Assembled ◽  
Ph Controlled

A simple supramolecular hydrogel is able to extract acid-functionalised anti-inflammatory drugs via directed interactions with the self-assembled gel nanofibres and exhibits pH-controlled drug release.

scholarly journals Study of the Biodegradation of PLA/PBAT Films after Biodegradation Tests in Soil and the Aqueous Medium

2021 ◽  
Vol 12 (1) ◽  
pp. 833-846
Keyword(s):  
Contact Angle ◽  
Aqueous Medium ◽  
Visual Analysis ◽  
Fourier Transforms ◽  
Scanning Calorimetry ◽  
Thermal Compression ◽  
Hydrophilic Character ◽  
Ft Ir ◽  
Fourier Transforms Infrared Spectroscopy ◽  
Biodegradation In Soil

The intense consumption of conventional plastics has been generating a series of problems for nature due to the accumulation of municipal solid waste because of its difficult degradation. Therefore, the use of biodegradable polymers becomes a good option to minimize these effects. Poly (lactide acid)/poly(butylene adipate-co-terephthalate) (PLA/PBAT) is a biodegradable blend that can be used mainly in applications that have a short shelf life. So, it is important to know the total biodegradation time of this blend. For this reason, PLA/PBAT films (1.5 x 1.5 x 0.15 cm) were produced by thermal compression molding to be subjected to biodegradation tests in soil and aqueous medium for 180 days. The films were characterized by visual analysis, weight loss measurements, differential scanning calorimetry (DSC), Fourier transforms infrared spectroscopy (FT-IR), contact angle, and scanning electron microscopy (SEM). DSC showed an increase of 0.7% in PLA crystallinity subjected to the aqueous medium, while FT-IR showed a reduction in the bands at 1710 cm-1 and 1100 cm-1, as a result of hydrolysis for both methodologies. The blend's hydrophilic character was increased after both degradation processes, presenting a reduction of 34.5% in the contact angle after biodegradation in soil. From the results, it was possible to conclude that PLA/PBAT films did not degrade completely, as expected, but showed signs that indicated the beginning of the degradation. The degradation was more effective in the aqueous medium.

scholarly journals Interconvertible Hydrochlorothiazide–Caffeine Multicomponent Pharmaceutical Materials: A Solvent Issue

Crystals ◽  
2020 ◽  
Vol 10 (12) ◽  
pp. 1088
Author(s):  
Cristóbal Verdugo-Escamilla ◽  
Carolina Alarcón-Payer ◽  
Antonio Frontera ◽  
Francisco Javier Acebedo-Martínez ◽  
Alicia Domínguez-Martín ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Intermolecular Forces ◽  
Active Pharmaceutical Ingredients ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Great Stability ◽  
X Ray ◽  
Pharmaceutical Ingredients ◽  
Interesting Approach ◽  
Pharmaceutical Materials

The design of new multicomponent pharmaceutical materials that involve different active pharmaceutical ingredients (APIs), e.g., drug-drug cocrystals, is a novel and interesting approach to address new therapeutic challenges. In this work, the hydrochlorothiazide-caffeine (HCT–CAF) codrug and its methanol solvate have been synthesized by mechanochemical methods and thoroughly characterized in the solid state by powder and single crystal X-ray diffraction, respectively, as well as differential scanning calorimetry, thermogravimetric analyses and infrared spectroscopy. In addition, solubility and stability studies have also been performed looking for improved physicochemical properties of the codrug. Interestingly, the two reported structures show great similarity, which allows conversion between them. The desolvated HCT–CAF cocrystal shows great stability at 24 h and an enhancement of solubility with respect to the reference HCT API. Furthermore, the contribution of intermolecular forces on the improved physicochemical properties was evaluated by computational methods showing strong and diverse H-bond and π–π stacking interactions.

scholarly journals Supersaturation Potential of Amorphous Active Pharmaceutical Ingredients after Long-Term Storage

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2731 ◽  
Author(s):  
Khadijah Edueng ◽  
Denny Mahlin ◽  
Johan Gråsjö ◽  
Olivia Nylander ◽  
Manish Thakrani ◽  
...  
Keyword(s):  
Solid State ◽  
Crystallization Kinetics ◽  
Physical Aging ◽  
Area Under The Curve ◽  
Crystallization Rate ◽  
Active Pharmaceutical Ingredients ◽  
Scanning Calorimetry ◽  
Supersaturation Ratio ◽  
Pharmaceutical Ingredients ◽  
Spray Dried

This study explores the effect of physical aging and/or crystallization on the supersaturation potential and crystallization kinetics of amorphous active pharmaceutical ingredients (APIs). Spray-dried, fully amorphous indapamide, metolazone, glibenclamide, hydrocortisone, hydrochlorothiazide, ketoconazole, and sulfathiazole were used as model APIs. The parameters used to assess the supersaturation potential and crystallization kinetics were the maximum supersaturation concentration (Cmax,app), the area under the curve (AUC), and the crystallization rate constant (k). These were compared for freshly spray-dried and aged/crystallized samples. Aged samples were stored at 75% relative humidity for 168 days (6 months) or until they were completely crystallized, whichever came first. The solid-state changes were monitored with differential scanning calorimetry, Raman spectroscopy, and powder X-ray diffraction. Supersaturation potential and crystallization kinetics were investigated using a tenfold supersaturation ratio compared to the thermodynamic solubility using the µDISS Profiler. The physically aged indapamide and metolazone and the minimally crystallized glibenclamide and hydrocortisone did not show significant differences in their Cmax,app and AUC when compared to the freshly spray-dried samples. Ketoconazole, with a crystalline content of 23%, reduced its Cmax,app and AUC by 50%, with Cmax,app being the same as the crystalline solubility. The AUC of aged metolazone, one of the two compounds that remained completely amorphous after storage, significantly improved as the crystallization kinetics significantly decreased. Glibenclamide improved the most in its supersaturation potential from amorphization. The study also revealed that, besides solid-state crystallization during storage, crystallization during dissolution and its corresponding pathway may significantly compromise the supersaturation potential of fully amorphous APIs.

scholarly journals Potential ecological footprints of active pharmaceutical ingredients: an examination of risk factors in low-, middle- and high-income countries

2014 ◽  
Vol 369 (1656) ◽  
pp. 20130586 ◽  
Author(s):  
Rai S. Kookana ◽  
Mike Williams ◽  
Alistair B. A. Boxall ◽  
D. G. Joakim Larsson ◽  
Sally Gaw ◽  
...  
Keyword(s):  
Manufacturing Sector ◽  
Developed Countries ◽  
High Income ◽  
Production Costs ◽  
Septic Systems ◽  
Human Consumption ◽  
Active Pharmaceutical Ingredients ◽  
Middle Income ◽  
Pharmaceutical Ingredients ◽  
Middle Income Countries

Active pharmaceutical ingredients (APIs) can enter the natural environment during manufacture, use and/or disposal, and consequently public concern about their potential adverse impacts in the environment is growing. Despite the bulk of the human population living in Asia and Africa (mostly in low- or middle-income countries), limited work relating to research, development and regulations on APIs in the environment have so far been conducted in these regions. Also, the API manufacturing sector is gradually shifting to countries with lower production costs. This paper focuses mainly on APIs for human consumption and highlights key differences between the low-, middle- and high-income countries, covering factors such as population and demographics, manufacture, prescriptions, treatment, disposal and reuse of waste and wastewater. The striking differences in populations (both human and animal), urbanization, sewer connectivity and other factors have revealed that the environmental compartments receiving the bulk of API residues differ markedly between low- and high-income countries. High sewer connectivity in developed countries allows capture and treatment of the waste stream (point-source). However, in many low- or middle-income countries, sewerage connectivity is generally low and in some areas waste is collected predominantly in septic systems. Consequently, the diffuse-source impact, such as on groundwater from leaking septic systems or on land due to disposal of raw sewage or septage, may be of greater concern. A screening level assessment of potential burdens of APIs in urban and rural environments of countries representing low- and middle-income as well as high-income has been made. Implications for ecological risks of APIs used by humans in lower income countries are discussed.

Reversed-Phase High Performance Liquid Chromatographic Analysis of Three First Line Anti-Tuberculosis Drugs

2019 ◽  
Vol 69 (12) ◽  
pp. 3590-3592
Author(s):  
Nela Bibire ◽  
Romeo Iulian Olariu ◽  
Luminita Agoroaei ◽  
Madalina Vieriu ◽  
Alina Diana Panainte ◽  
...  
Keyword(s):  
High Performance ◽  
Biological Fluids ◽  
Gradient Elution ◽  
High Performance Liquid Chromatographic ◽  
Reversed Phase ◽  
Assay Method ◽  
Active Pharmaceutical Ingredients ◽  
First Line ◽  
Pharmaceutical Ingredients ◽  
Liquid Chromatographic

Active pharmaceutical ingredients such as isoniazid, pyrazinamide and rifampicin are among the most important first-line anti-tuberculosis drugs. A simple, rapid and sensitive reversed phase-high performance liquid chromatographic assay method for the simultaneous determination of isoniazid, pyrazinamide and rifampicin has been developed. Separation of the interest compounds was achieved in a 10 min chromatographic run in gradient elution mode on a Zorbax SB-C18 stainless steel column (150 � 4 mm, 5 mm) using a guard column containing the same stationary phase. The gradient elution was carried out with a mobile phase of 10% CH3CN aqueous solution for channel A and 50% CH3CN in pH = 6.8 phosphate buffer (20 mM), to which 1.5 mL triethylamine were added for channel B. Quantification of the analyzed substances was carried out spectrophotometrically at 269 nm. Detection limits of 0.48 mg/L for isoniazid, 0.52 mg/L for pyrazinamide and 0.48 mg/L for rifampicin were established for the developed assay method. The present work showed that the proposed analysis method was advantageous for simple and rapid analysis of the active pharmaceutical ingredients in pharmaceuticals and biological fluids.

The Development of Pemetrexed Diacid-Loaded Gelatin-Cloisite 30B (MMT) Nanocomposite for Improved Oral Efficacy Against Cancer: Characterization, In-Vitro and Ex-Vivo Assessment

2020 ◽  
Vol 17 (3) ◽  
pp. 246-256
Author(s):  
Kriti Soni ◽  
Ali Mujtaba ◽  
Md. Habban Akhter ◽  
Kanchan Kohli
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Confocal Laser ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Cloisite 30B ◽  
Ft Ir

Aim: The intention of this investigation was to develop Pemetrexed Diacid (PTX)-loaded gelatine-cloisite 30B (MMT) nanocomposite for the potential oral delivery of PTX and the in vitro, and ex vivo assessment. Background: Gelatin/Cloisite 30 B (MMT) nanocomposites were prepared by blending gelatin with MMT in aqueous solution. Methods: PTX was incorporated into the nanocomposite preparation. The nanocomposites were investigated by Fourier Transmission Infra Red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscope (SEM) X-Ray Diffraction (XRD) and Confocal Laser Microscopy (CLSM). FT-IR of nanocomposite showed the disappearance of all major peaks which corroborated the formation of nanocomposites. The nanocomposites were found to have a particle size of 121.9 ± 1.85 nm and zeta potential -12.1 ± 0.63 mV. DSC thermogram of drug loaded nanocomposites indicated peak at 117.165 oC and 205.816 oC, which clearly revealed that the drug has been incorporated into the nanocomposite because of cross-linking of cloisite 30 B and gelatin in the presence of glutaraldehyde. Results: SEM images of gelatin show a network like structure which disappears in the nanocomposite. The kinetics of the drug release was studied in order to ascertain the type of release mechanism. The drug release from nanocomposites was in a controlled manner, followed by first-order kinetics and the drug release mechanism was found to be of Fickian type. Conclusion: Ex vivo gut permeation studies revealed 4 times enhancement in the permeation of drug present in the nanocomposite as compared to plain drug solution and were further affirmed by CLSM. Thus, gelatin/(MMT) nanocomposite could be promising for the oral delivery of PTX in cancer therapy and future prospects for the industrial pharmacy.

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