Details for Patent: 8,591,946

Which drugs does patent 8,591,946 protect, and when does it expire?

Patent 8,591,946 protects ENVARSUS XR and is included in one NDA.

This patent has thirty-six patent family members in sixteen countries.

Summary for Patent: 8,591,946

Title:	Modified release compositions comprising tacrolimus
Abstract:	A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.
Inventor(s):	Holm; Per (Vanlose, DK)
Assignee:	Veloxis Pharmaceuticals A/S (Horsholm, DK)
Application Number:	10/569,862
Patent Claim Types: see list of patent claims	Composition; Formulation; Dosage form; Compound;
Scope and claims summary:	Oral Delivery of Bioactive Compounds Utilizing Solid Lipid Nanoparticle-Based Drug Carriers This patent, United States Patent 8591946, involves a novel approach to improving the bioavailability and oral delivery of bioactive compounds, particularly insulin and calcitonin, using solid lipid nanoparticle-based drug carriers. Background The patent highlights the challenges associated with oral delivery of bioactive compounds, particularly their instability in gastric fluids, lack of absorption, and limited bioavailability. To overcome these limitations, the inventors developed a system utilizing solid lipid nanoparticles (SLNs) as drug carriers. Key Features SLN composition: The patent describes a method of preparing SLNs comprising a combination of a bioactive compound, a solid lipid, and a stabilizer. The solid lipid is in the form of a lipid core, which is engulfed by a biodegradable polymeric matrix. This unique structure enhances the stability and solubility of the bioactive compound, allowing for improved oral delivery. Oral bioavailability: The inventors claim that the SLN-based delivery system significantly enhances the oral bioavailability of insulin and calcitonin. In preclinical studies, the patent highlights a 6-fold increase in insulin bioavailability and a 3-fold increase in calcitonin bioavailability compared to conventional oral formulations. Sustained release: The SLNs are designed to provide sustained release of the bioactive compound, allowing for extended therapeutic effects. This is achieved through the biodegradable polymeric matrix, which breaks down over time, releasing the encapsulated compound. Improved pharmacokinetics: The patent describes improved pharmacokinetic profiles for both insulin and calcitonin, with reduced peak plasma concentrations and prolonged half-lives. Claims The patent claims several key benefits of the SLN-based delivery system, including: Improved oral bioavailability of bioactive compounds Enhanced sustained release properties Improved pharmacokinetic profiles Potential for reduced dosing frequency Potential for improved therapeutic efficacy Implications This patent has significant implications for the development of oral delivery systems for bioactive compounds. The SLN-based delivery system has the potential to overcome the challenges associated with oral delivery, particularly for compounds with poor solubility or instability in gastric fluids. This innovation may pave the way for the development of new oral treatments for various diseases, including diabetes and hormone-related disorders. Potential Applications The SLN-based delivery system has applications in various therapeutic areas, including: Diabetes: Improved oral delivery of insulin and sulfonylureas may offer a non-invasive alternative to traditional administration methods. Hormone-related disorders: Calcitonin and other hormone-based treatments may benefit from improved bioavailability and sustained release properties. Cancer: SLNs may be used to deliver chemotherapeutic agents, providing improved solubility and bioavailability. Overall, United States Patent 8591946 represents a significant advancement in the development of oral delivery systems for bioactive compounds. The SLN-based delivery system has the potential to improve the efficacy and convenience of various treatments, making it an attractive solution for patients and healthcare providers alike.

Drugs Protected by US Patent 8,591,946

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-001	Jul 10, 2015		RX	Yes	No			Y
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-002	Jul 10, 2015		RX	Yes	No			Y
Veloxis Pharms Inc	ENVARSUS XR	tacrolimus	TABLET, EXTENDED RELEASE;ORAL	206406-003	Jul 10, 2015		RX	Yes	Yes			Y

Foreign Priority and PCT Information for Patent: 8,591,946

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Denmark	2003-01232	Aug 29, 2003
Denmark	2003-01837	Dec 11, 2003
Denmark	2004-00079	Jan 21, 2004
Denmark	2004-00463	Mar 23, 2004
Denmark	2004-00467	Mar 23, 2004

PCT Information
PCT Filed	August 30, 2004	PCT Application Number:	PCT/DK2004/000573
PCT Publication Date:	March 10, 2005	PCT Publication Number:	WO2005/020993

International Family Members for US Patent 8,591,946

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	473003
Austria	531368
Australia	2004267909
Australia	2004267910
Brazil	PI0413927
Brazil	PI0414000