The patent's inventors are Shen, Shou-Cang (
This patent was filed on
From the background information supplied by the inventors, news correspondents obtained the following quote: "The poor solubility of active pharmaceutical ingredients (APIs) in water is one of the most challenging issues in the development of many pharmaceutical products for commercialization. More than one third of the drugs listed in the US Pharmacopoeia and half of the new chemical entities (NCEs), or new active ingredients are poorly water soluble or insoluble. The poorly water-soluble substances have a solubility of less than 10 g/L, in particular less than 5 g/L and more particularly, less than 1 g/l. Substances with aqueous solubility less than 0.1 g/L are classified as practically insoluble or an insoluble substance. When these drugs are administered, they usually have a very low bio-availability because of their poor solubility in the digestive fluid, causing erratic and incomplete absorption that may lead to a loss in therapeutic effect. Many NCEs fail to be commercialized due to their insolubility or poor solubility in water.
"Much effort has been made to enhance the dissolution rate of poorly water-soluble drugs to increase bioavailability. One strategy is to improve dissolution rates through specific formulation methods, the most common being particle size reduction (see, Jinno, J. et al.,
"Among the various approaches, solid dispersion or solution formulations have been used to improve the dissolution rate of such kinds of drugs. Solid dispersions are usually formulated with soluble organic polymers (see,
"Generally, the commercial application of solid dispersion has been very limited, primarily because of manufacturing difficulties and stability problems. These dosage forms developed often have drawbacks, such as poor product thermodynamic stability, issues with manufacturability such as poor batch-to-batch reproducibility and limitations in scaling-up for commercial production (see, Serajuddin,
"As mentioned above, another method is to reduce particle size, which is intended to increase the contact surface areas between the drug particle and the dissolution medium. The drawback of this technique lies in instability of particle size and agglomeration during post-milling storage, which causes variation in dissolution rate (see, Ng, W. K. et al.,
"An alternative approach is to produce drugs in the amorphous form by co-grinding the drugs with other additives such as porous powder (see, Yonemochi, E. et al., J. Colloid Interphase Sci. 173:186-191 (1995)). Spray drying and quench are also applied to produce amorphous pharmaceutical products as the quick drying and cooling prevents the crystal growth (see, Gupta, P. et al.,
"The discovery of a series of new ordered mesoporous material called MS41 family, having a regular pore size distribution that can be systematically varied between 2 and 10 nm, has opened up new possibilities in the field of catalysis, adsorption and pharmaceutical applications. Moreover, among the various structures of mesoporous silica materials, SBA-15 synthesized by nonionic polymer surfactant is the most extensively investigated due to its mesostructural diversity as well as the larger pore and thicker wall. The pore size is adjustable up to 30 nm. The feasibility to obtain different pore size and geometries offers wide potential for hosting molecules larger than the ones exhibited for classic microporous materials. In addition, the large surface areas of pore walls are occupied with high concentrations of silanol groups, which make the porous materials modifiable with different surface functional groups. Thus, the absorption properties are adjustable for different purposes of molecule hosting.
"In view of the foregoing, there is a need for formulating drugs and specialty chemicals that are poorly water soluble, practically insoluble or insoluble. Formulations are needed which improve the dissolution rates of these compounds in order to improve their absorption in the digestive tract and thereby improve their efficacy. It is highly desirable to develop new formulations and methods that can amorphize an API to improve dissolution rates as well as stabilize the amorphous form during subsequent extended storage. The present invention satisfies these and other needs."
Supplementing the background information on this patent, NewsRx reporters also obtained the inventors' summary information for this patent: "The present invention provides pharmaceutical and specialty chemical formulations that utilize mesoporous materials or compositions, which possess high surface areas and large pore volumes as excipients. In certain aspects, the formulations are prepared by methods of using a co-spray drying process to prepare amorphous active ingredients, which are entrapped in the nanosized mesoporous channels with high homogeneity.
"As such, in one embodiment, the present invention provides a pharmaceutical composition, comprising: a substantially water-insoluble pharmaceutical active ingredient; and a mesoporous composition having a plurality of nanopores, wherein the substantially water-insoluble pharmaceutical active ingredient is sprayed-dried together with the mesoporous composition to entrap the pharmaceutical active ingredient within the nanopores.
"In certain aspects, an amorphous form of the active ingredient is kept very stable by confinement in the nanospace. The preparation process is both reproducible and can be easily scaled. In certain aspects, the present invention overcomes product instability concerns and manufacturability issues of current solid dispersion methods.
"The present invention provides novel formulations and methods to improve the dissolution rates of poorly water-soluble active compounds, in particular active pharmaceutical ingredients (APIs). In certain aspects, a straightforward method of co-spray drying an active ingredient with a mesoporous material or composition is reproducible and can be easily scaled for commercial production as compared to other solid dispersion technologies.
"As such, in another embodiment, the present invention provides a method for preparing a pharmaceutical composition, the method comprising: admixing a substantially water-insoluble pharmaceutical active ingredient with a mesoporous composition having a plurality of nanopores in a suitable solvent or mixture of solvents; and spray-drying the substantially water-insoluble pharmaceutical active ingredient with the mesoporous composition to entrap the pharmaceutical active ingredient within said nanopores, thereby producing said pharmaceutical composition.
"In certain instances, the substantially water-insoluble pharmaceutical active ingredient is a member selected from an analgesic, an antipyretic, an anti-cholesterol or cholesterol-reducing agent, an anti-inflammatory agent, an antimicrobial, a decongestant and an antihistamine.
"These and other aspects, objects and embodiments will become more apparent when read with the figures and detailed description which follows."
For the URL and additional information on this patent, see: Shen, Shou-Cang; Ng,
Keywords for this news article include:
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