Solubility of Solid Solutes in HFA‐134a With a Correlation to Physico‐Chemical Properties

Hoye, Julie A.; Gupta, Abhishek; Myrdal, Paul B.

doi:10.1002/jps.21080

Cited by 9 publications

(3 citation statements)

References 19 publications

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“…Because, compounds with strong crystal lattices (high melting points) will readily crystallize in solvent hence the solubility benefit will be low[28]. Compounds with weak crystal lattices (low melting points) are less prone to crystallize and therefore amount in solution will remain high[2930]. Microscopic visual analysis infers needle shape (fig.…”

Section: Resultsmentioning

confidence: 99%

Preparation and crystallographic analysis of gliclazide polymorphs

Jayaramu¹,

Sb²,

Narode³

et al. 2015

Indian J Pharm Sci

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Since the introduction of gliclazide in the pharmaceutical industry, a large number of research groups have been engaged in various investigations aiming to enhance its biomedical application. But, very limited efforts have been made to study polymorphism of gliclazide. Therefore, this study focuses on solvent-induced polymorphism of gliclazide and its characterization by thermal methods. Three polymorphs namely, Form-I, II and III and an amorphous powder were produced from different solvents and solvent mixtures. Crystals were analyzed using infrared spectroscopy, differential scanning calorimetry, X-ray powder diffraction and single crystal x-ray diffraction. Polymorph Form-I is found to exist in centro-symmetric triclinic P-1 space group and has endothermic peak at 162.93°. Form-II has endothermic peak from 171.2° to 172.35° and exists in centro-symmetric monoclinic P21/a space group while Form-III has endothermic peak from 168.93° to 169.86° and exists in centro-symmetric monoclinic P21/n space group. The equilibrium solubility values of Form-I, II, III and the amorphous form were 0.4825±0.025, 0.2341±0.042, 0.2581±0.038 and 0.5213±0.072 mg/ml, respectively. The Form-I has relatively higher solubility and similar to that of amorphous gliclazide. Form-II and Form-III are relatively most stable and least soluble. However, there was no remarkable difference in their aqueous solubility under the conditions in which study was conducted.

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Section: Resultsmentioning

confidence: 99%

Preparation and crystallographic analysis of gliclazide polymorphs

Jayaramu¹,

Sb²,

Narode³

et al. 2015

Indian J Pharm Sci

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“…[31][32][33] Research has shown that increasing drug melting point reduces solubility in HFA 134a. 34 For example, progesterone with a melting point of 129C is soluble in HFA 134a with the concentration of approximately 1% w/w and this increases to 10% w/w with the addition of 20% ethanol. 35 Therefore, a melting point of 150C or less may be considered as a desired property for solubility in HFA based propellants.…”

Section: Potential Candidates For Ultrafine Pmdi For Treatment Of Cov...mentioning

confidence: 99%

The Potential Use of Cyclosporine Ultrafine Solution Pressurised Metered- Dose Inhaler in the Treatment of COVID-19 Patients

Ehtezazi

2022

RADDF

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Introduction: Serious COVID-19 respiratory problems start when the virus reaches the alveolar level, where type II cells get infected and die. Therefore, virus inhibition at the alveolar level would help prevent these respiratory complications. Method: A literature search was conducted to collect physicochemical properties of small molecule compounds that could be used for the COVID-19 treatment. Compounds with a low melting point were selected along with those soluble in ethanol, hydrogen-bond donors, and acceptors. Results : There are severe acute respiratory syndrome coronavirus inhibitors with physicochemical properties suitable for the formulation as an ultrafine pressurised metered-dose inhaler (pMDI). Mycophenolic acid, Debio 025, and cyclosporine A are prime candidates among these compounds. Cyclosporine A (hereafter cyclosporine) is a potent SARS-CoV-2 inhibitor, and it has been used for the treatment of COVID-19 patients, demonstrating an improved survival rate. Also, inhalation therapy of nebulised cyclosporine was tolerated, which was used for patients with lung transplants. Finally, cyclosporine has been formulated as a solution ultrafine pMDI. Although vaccine therapy has been started in most countries, inhalation therapies with non-immunological activities could minimise the spread of the disease and be used in vaccine-hesitant individuals. Conclusion: Ultrafine pMDI formulation of cyclosporine or Debio 025 should be investigated for the inhalation therapy of COVID-19.

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“…The ice bath was removed and mixture was heated under reflux for 5 h. A solid was obtained upon cooling, which was recrystallized from hot water to afford salicylic acid (3.05 g, 61%), mp 156.5˚C (lit. [14] 159˚C for SA). 1H and 13C NMR spectra were identical to a commercial sample.…”

Section: General Procedures For Synthesis Of Samentioning

confidence: 99%

Reactions with Aminobenzoic Acids via Diazonium Salts Open New Routes to Bio-Derived Aromatics

Farlow¹,

Krömer²

2016

IJOC

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Aromatics have a broad application in our everyday life ranging from plastics, coatings and fibres, to food and pharmaceuticals. To date the bulk of these aromatics is derived from naphtha-based petrochemistry. However, recent progress in the fermentative production of metabolites using renewable resources and engineered microbes has enabled the production of bio-precursors, such as 4-amino benzoic acid (pABA) and 2-amino benzoic acid (oABA). In this work we explored the feasibility of Sandmeyer reactions for the conversion of pABA to terephthalic and oABA salicylic acid, providing two very important platform chemicals for the chemical and pharmaceutical industries. We could demonstrate that both acids can be obtained from the amino benzoic acids derived from the shikimate pathway in microbes and plants. Good conversions could be achieved using Sandmeyer reactions at mild conditions with biodegradable reagents and without organic solvents.

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Solubility of Solid Solutes in HFA‐134a With a Correlation to Physico‐Chemical Properties

Cited by 9 publications

References 19 publications

Preparation and crystallographic analysis of gliclazide polymorphs

Preparation and crystallographic analysis of gliclazide polymorphs

The Potential Use of Cyclosporine Ultrafine Solution Pressurised Metered- Dose Inhaler in the Treatment of COVID-19 Patients

Reactions with Aminobenzoic Acids via Diazonium Salts Open New Routes to Bio-Derived Aromatics

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