Insoluble Erythromycin Salts

Jones, P. H.; Rowley, Elizabeth K.; Weiss, Arlene L.; Bishop, Dorothy L.; Chun, Alexander

doi:10.1002/jps.2600580311

Cited by 16 publications

(9 citation statements)

References 9 publications

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“…The studies carried out on the relationships between the nature of the salt forming agent and the resulting salt cannot be reliable, from this point of view. For instance, increasing hydrophilicity of the counterion can easily be suggested as a simple remedy to increase the solubility in water of the resultant salt and was proposed in the case of erythromycin salts [10]. Also in the case of diclofenac, the need for a soluble salt opened the large field of the aliphatic amines as salt forming agents, different from the usual sodium or potassium hydroxides and, particularly, of those carrying hydroxy groups: with the hypothesis that the higher the hydrophilicity of the counterion, the higher the hydrophilicity of the resulting salt could be [1,3,11,12].…”

Section: Resultsmentioning

confidence: 99%

Diclofenac Salts. V. Examples of Polymorphism among Diclofenac Salts with Alkyl-hydroxy Amines Studied by DSC and HSM

2010

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Nine diclofenac salts prepared with alkyl-hydroxy amines were analyzed for their properties to form polymorphs by DSC and HSM techniques. Thermograms of the forms prepared from water or acetone are different in most cases, suggesting frequent examples of polymorphism among these salts. Polymorph transition can be better highlighted when analysis is carried out by thermo-microscopy, which in most cases made it possible to observe the processes of melting of the metastable form and re-crystallization of the stable one. Solubility values were qualitatively related to the crystal structure of the salts and the molecular structure of the cation.

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Section: Resultsmentioning

confidence: 99%

Diclofenac Salts. V. Examples of Polymorphism among Diclofenac Salts with Alkyl-hydroxy Amines Studied by DSC and HSM

2010

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“…The reported melting points of adipic and succinic acids are approximately 151°C–154°C and approximately 185°C–187°C, respectively11; hence, it may be hypothesized that the succinate would have a lower solubility than the adipate. On the contrary, increasing the hydrophilicity of the counterion as a means of increasing the water solubility of the resultant salt has been proposed and investigated for a series of erythromycin salts 12. The calculated log P s of adipic and succinic acid are 0.356 and −0.655 respectively,13 indicating that a salt of adipic acid may be less soluble than that of succinic acid.…”

Section: Introductionmentioning

confidence: 99%

Solid‐state characterization of novel active pharmaceutical ingredients: Cocrystal of a salbutamol hemiadipate salt with adipic acid (2:1:1) and salbutamol hemisuccinate salt

Paluch

Tajber

Elcoate

et al. 2011

Journal of Pharmaceutical Sciences

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“…Many pharmaceutical drugs on the market are salts employing counterions such as hydrochloride, mesylate, citrate, acetate, tosylate, maleate, chloride, bromide, etc. (19)(20)(21)(22). The main concern for salt formation is salt disproportion which is reversion of the salt to its unionized form.…”

Section: Conventional Approachesmentioning

confidence: 99%

Preclinical Formulations: Insight, Strategies, and Practical Considerations

et al. 2014

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Abstract. A lot of resources and efforts have been directed to synthesizing potentially useful new chemical entities (NCEs) by pharmaceutical scientists globally. Detailed physicochemical characterization of NCEs in an industrial setup begins almost simultaneously with preclinical testing. Most NCEs possess poor water solubility posing bioavailability issues during initial preclinical screening, sometimes resulting in dropping out of an NCE with promising therapeutic activity. Selection of right formulation approach for an NCE, based on its physicochemical properties, can aid in improving its solubility-related absorption and bioavailability issues. The review focuses on preclinical formulations stressing upon different preclinical formulation strategies and deciphers the understanding of formulation approaches that could be employed. It also provides detailed information related to a vast pool of excipients available today, which is of immense help in designing preclinical formulations. Few examples mentioned, throw light on key aspects of preclinical formulation development. The review will serve as an important guide for selecting the right strategy to improve bioavailability of NCEs for academic as well as industrial formulation scientists.

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Insoluble Erythromycin Salts

Cited by 16 publications

References 9 publications

Diclofenac Salts. V. Examples of Polymorphism among Diclofenac Salts with Alkyl-hydroxy Amines Studied by DSC and HSM

Diclofenac Salts. V. Examples of Polymorphism among Diclofenac Salts with Alkyl-hydroxy Amines Studied by DSC and HSM

Solid‐state characterization of novel active pharmaceutical ingredients: Cocrystal of a salbutamol hemiadipate salt with adipic acid (2:1:1) and salbutamol hemisuccinate salt

Preclinical Formulations: Insight, Strategies, and Practical Considerations

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