Mechanical property predictions for polymorphs of sulphathiazole and carbamazepine

Roberts, R.J.; Payne, Robin S.; Rowe, R.C.

doi:10.1016/s0928-0987(99)00065-2

Cited by 54 publications

(28 citation statements)

References 16 publications

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“…For example, polymorphs of metaprotol tartarate [104] paracetamol [105][106][107][108], sulfamerazine [109], phenobalbitone [110], carbamazepine [111,112] and phenylbutazone [113] have been shown to exhibit different mechanical properties. A common effect of polymerphism is alteration of powder flow due to the difference in particle morphology of two polymorphs.…”

Section: Mechanical Properties Of Polymorphs and Amorphous Drug Formsmentioning

confidence: 99%

Drug polymorphism: a review

Saifee¹,

Inamda²,

Dhamecha³

et al. 2010

Int J Health Res

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an online international journal allowing free unlimited access to abstract and full-text of published articles. The journal is devoted to the promotion of health sciences and related disciplines (including medicine, pharmacy, nursing, biotechnology, cell and molecular biology, and related engineering fields). It seeks particularly (but not exclusively) to encourage multidisciplinary research and collaboration among scientists, the industry and the healthcare professionals. It will also provide an international forum for the communication and evaluation of data, methods and findings in health sciences and related disciplines. The journal welcomes original research papers, reviews and case reports on current topics of special interest and relevance. All manuscripts will be subject to rapid peer review. Those of high quality (not previously published and not under consideration for publication) will be published without delay. The maximum length of manuscripts should normally be 10,000 words (20 single-spaced typewritten pages) for review, 6,000 words for research articles, 3,000 for technical notes, case reports, commentaries and short communications. Submission of Manuscript:The International Journal of Health Research uses a journal management software to allow authors track the changes to their submission. All manuscripts must be in MS Word and in English and should be submitted online at http://www.ijhr.org. Authors who do not want to submit online or cannot submit online should send their manuscript by e-mail attachment (in single file) to the editorial office below. Submission of a manuscript is an indication that the content has not been published or under consideration for publication elsewhere. Authors may submit the names of expert reviewers or those they do not want to review their papers. Enquiries AbstractFormulators are charged with the responsibility of formulating a product which is physically and chemically stable, and bioavailable. Solid-state properties including polymorphism, solvate and salt formation can have a profound impact on important properties (solubility & stability) that are essential for successful development of drug candidates. Crystallization of pharmaceutically active ingredients, particularly those that possess multiple polymorphic forms, are among the most critical and least understood pharmaceutical manufacturing processes. Many process and product failures can be traced to a poor understanding and control of crystallization processes. Most drugs exhibits structural polymorphism and it is desirable to develop the most thermodynamically stable polymorph of the drug to assure reproducible bioavailability of the product over its shelf-life under a variety of real world storage conditions. There are occasional situations in which development of a meta-stable crystalline or amorphous form is justified to achieve the desired medical benefit. Such situation includes those in which faster dissolution rates or higher concentrations are desired in order to achieve rapid absorption an...

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Section: Mechanical Properties Of Polymorphs and Amorphous Drug Formsmentioning

confidence: 99%

Drug polymorphism: a review

Saifee¹,

Inamda²,

Dhamecha³

et al. 2010

Int J Health Res

View full text Add to dashboard Cite

show abstract

“…Polymorphism can also affect the mechanical properties of drug particles impacting the manufacturability and physical attributes of tablets. For example, polymorphs of paracetamol (Di Martino et al, 1996;Nichols and Frampton, 1998;Beyer et al, 2001;Joiris et al, 1998), sulfamerazine (Sun and Grant, 2001), carbamazepine (Roberts et al, 2000;Otsuka et al, 1999), and phenylbutazone (Summers et al, 1976) have been addressed different mechanical properties. A common effect of polymorphism can be the change of powder flow due to the difference in particle morphology of polymorphs.…”

Section: Stability and Mechanical Propertiesmentioning

confidence: 99%

Drug Polymorphism and its Importance on Drug Development Process

Jeong¹,

Youn²,

Shin³

et al. 2010

Journal of Pharmaceutical Investigation

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− Polymorphism has been recognized to be a critical issue throughout the drug product development process.Most of solid phase drugs have polymorphism, which has generated a great deal of interest and the field has been evolving rapidly. Preferably, thermodynamically most stable form of a drug substance is selected to obtain consistent bioavailability over its shelf life and various storage conditions. Moreover, it has the lowest potential for conversion from one polymorphic form to another. However, metastable or amorphous forms may be used intentionally to induce faster dissolution rate for rapid drug absorption and higher efficacy. For pharmaceutical industry, polymorphism is one of the key activities in form selection process together with salt selection. This article introduces the main features in the investigation of solid form selection especially polymorphic behavior with thermodynamic backgrounds, physicochemical properties with solubility, dissolution, and mechanical properties, and characterization techniques for proper analysis. The final form can be recommended based on the physicochemical and biopharmaceutical properties and by the processability, scalability and safety considerations. Pharmaceutical scientists especially in charge of formulation need to be well aware of the above issues to assure product quality.

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“…91) The Young's modulus of aspirin has been determined from its crystal structure 92) and the mechanical properties of aspirin, sulphathiazole, carbamazepine, and polymorphs of primidone (forms A and B) can be predicted 93) by applying lattice dynamics to the atom-atom potential model while also taking into account the crystal morphology. Even though it is possible to predict the mechanical properties of a compound from its crystal structure, crystal engineering of pharmaceuticals has not yet resulted in the design of crystals with desired mechanical properties.…”

Section: Importance Of Studying the Structure Of Pharmaceutical Cr Ysmentioning

confidence: 99%

Relationship between the Structure and Properties of Pharmaceutical Crystals

Sheth

Grant

2005

KONA

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The majority of drug products are solid dosage forms, most of which contain the drug substance in the crystalline state. This review considers the forces responsible for crystal packing, the various types of pharmaceutical crystals, and the methods used to determine the structure of pharmaceutical crystals. These topics provide background for the main thrust, which focuses on the importance of studying the structure of pharmaceutical crystals with particular stress on phase changes of crystal forms of drugs during pharmaceutical processing and implications of different solid forms of drugs on its mechanical properties. The present review does not consider pharmaceutical co-crystals, which could be the subject of another review.

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Mechanical property predictions for polymorphs of sulphathiazole and carbamazepine

Cited by 54 publications

References 16 publications

Drug polymorphism: a review

Drug polymorphism: a review

Drug Polymorphism and its Importance on Drug Development Process

Relationship between the Structure and Properties of Pharmaceutical Crystals

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