Indian scientists show insoluble drugs can be taken orally in nano crystal form

Taking a big leap in how oral medicines are administered, Indian scientists have shown that producing nanoscopic crystals of a pharmaceutical product can allow the medication to be absorbed by the gut even if the drug is not soluble in water.

The study suggests that more than half of the medicinal drugs being developed by the pharmaceutical industry dissolve only very weakly in water, if at all.

This is a major problem for administering such drugs as it means they are not effective if taken by mouth.

The industry has developed many approaches to addressing this problem, such as adding a small quantity of an organic solvent, such as ethanol, to the mixture, coupling the drug with a charged ion to increase bioavailability and in more recent times using water-soluble "carriers", such as the ring-shaped cyclodextrin.

A much more effective approach would be to somehow make the drug soluble without resorting to such additives.

Scientists have, over the last decade or so, discovered that producing microscopic crystals of a pharmaceutical product can make it soluble in water even if the bulk compound is not.

The tiny particle size, means a much greater surface area to volume ratio giving access to more water molecules that can surround the particles, which is the essence of dissolving a compound.

This effect can then allow the particles to be carried across the lining of the gut wall where they would previously simply move past with no interaction.

The effect can be explained in terms of the physical chemistry and mathematics known to nineteenth century scientist Lord Kelvin, Herbert Freundlich, and Wilhelm Ostwald.

Now, R. Ravichandran of the Regional Institute of Education (NCERT), in Bhopal, India, has demonstrated that gymnemic acids derived from the herb Gymnema sylvestre , can be made more readily bioavailable by forming the active compounds as nanoscopic crystals, nanocrystals.

The compounds have medicinal activity in a range of diseases, in particular diabetes mellitus, with the native herb having been used in traditional medicine for several centuries.

Ravichandran's detailed examination of the physical and chemical properties of nanocrystals of gymnemic acids could provide important clues as to how to transfer the medical benefits of the herb to a regulated pharmaceutical product for further investigation and with a more strict profile in treating disease.

The study has been published in the International Journal of Nanoparticles.

Antares Pharma (AIS) and BioSante Pharmaceuticals (BPAX) Announce Committee Recommends Continuation of the LibiGel Phase III Clinical Program

Antares Pharma, Inc. (NYSE Amex: AIS) partner BioSante Pharmaceuticals (Nasdaq: BPAX) announced that based upon a review of study conduct and blinded data from the LibiGel Phase III Cardiovascular and Breast Cancer Safety Study, the LibiGel Safety Study External Executive Committee has recommended continuation of the LibiGel Phase III clinical program. A very low cardiovascular event rate has occurred thus far in the LibiGel Phase III clinical studies.

Under the terms of the agreement, BioSante is responsible for all development activities for LibiGel and Antares has retained international commercialization rights to LibiGel in significant territories including the European Union and Japan.

Antares President and Chief Executive Officer, Paul K. Wotton, Ph.D. said, "We are very pleased to see further and encouraging progress made with LibiGel, which uses the Antares Pharma ATD system, an FDA approved technology. A transdermal gel offers an ideal means to deliver drugs like testosterone in a controlled and reproducible way with a convenient to use dosage form. We have an advanced and deep pipeline of ATD based products, including LibiGel, where we have significant intellectual property and commercialization rights. We expect to earn additional milestone and royalty payments in the future from our multi-product agreement with BioSante."

Biosante Pharmaceuticals, Inc. is a specialty pharmaceutical company focused on developing products for female sexual health, menopause, contraception and male hypogonadism

Molecular Insight Pharmaceuticals, Inc. to Present Clinical, Preclinical Data at the Society of Nuclear Medicine 2009 Annual Meeting

CAMBRIDGE, MA - Molecular Insight Pharmaceuticals, Inc. (NASDAQ: MIPI) researchers will present data on the Company's progress in developing novel radiopharmaceuticals that may provide a promising option for molecular imaging of solid tumors, at the Society of Nuclear Medicine (SNM) annual meeting in Toronto. The presentations include clinical data on Molecular Insight's Trofex(TM), a radiolabeled, small-molecule molecular imaging pharmaceutical in development for diagnosis and staging of prostate cancer. Trofex, an internally developed compound, targets prostate specific membrane antigen (PSMA), a protein highly expressed by prostate tumor cells, and has the potential to both detect and, when labeled with a therapeutic isotope, treat metastatic prostate cancer. Data also will be presented on Molecular Insight's recent discovery research oncology projects that have focused on the development of radiolabeled small-molecule inhibitors that target the cancer-related enzymes, carbonic anhydrase IX and seprase.

Clinipace to Manage Two Phase II Clinical Trials for Inspire Pharmaceuticals

Clinipace’s Technology-Driven Service Model is Designed to Streamline Timelines and Generate Significant Clinical Trial Transparency and Cost Savings

MORRISVILLE, N.C.-Clinipace, a digital clinical research organization, announced today that Inspire Pharmaceuticals, Inc. has selected the company to manage and deploy two phase II studies for the ophthalmic prescription medicine, AzaSite®.

Currently approved by the U.S. Food and Drug Administration (FDA) for the treatment of bacterial conjunctivitis, Inspire has initiated two Phase II randomized placebo-controlled clinical trials of AzaSite as a potential treatment of blepharitis, an ocular disease characterized by the inflammation of the eyelids.

Clinipace will provide technology-driven clinical trial services to Inspire including data management (EDC), clinical monitoring, site management, regulatory document management, and biostatistical consulting. To bring increased trial visibility, the project team will utilize TEMPOTM for Clinical Trials software from Clinipace to manage site initiation, patient enrollment and randomization, clinical data capture, monitoring trip reports, site management, regulatory document tracking, and much more.

“We share a common goal with Clinipace of changing the way we approach the clinical development process – shifting away from some of the more traditional CRO processes and moving towards an integrated technology-driven model,” said Chad Ice, senior director, clinical research, Inspire.

“With Clinipace, we plan to remove unnecessary layers of management and processes,” said Ice. “We believe that Clinipace can help assure that communication with our clinical sites is much more seamless – one of the most vital links driving the success of our clinical trial process.”

“We’re hearing from the market time and time again that pharmaceutical companies are tired of having over-scaled and over-priced resources pitched to them from CROs today,” said Christopher Porter, chief operating officer, Clinipace. “That’s the driving force behind our dedication to providing innovative companies like Inspire a scalable solution with the right kind and quantity of resources to match any size clinical study and operational approach.”