PATENT CLAIM ANALYSIS

Application Number: 16126799
Application Type: Utility
Filing Date: 2018-09
Publication Date: 2019-04
Patent Classification: ["424", "450000"]

Abstract:
The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL). In the preferred embodiment the drug in the solubilizing agent is mixed with the liposomes in aqueous suspension so that the concentration of solubilizing agent is lowered to below its capacity to completely solubilize the drug. This results in the drug precipitating but remote loading capability is retained. The process is scalable and, in liposomes in which the lipid composition and remote loading agent are optimized, the resulting drug-loaded liposomes are characterized by a high drug-to-lipid ratios and prolonged drug retention when the liposome encapsulated drug is administered to a subject.

Claim (Index 2):
The pharmaceutical formulation according to  claim 1 , manufactured by a method comprising:\n (a) preparing a suspension of said liposome in an aqueous solution of an ammonium salt of a carbohydrate sulfate forming a first population of said ammonium salt encapsulated within said liposome and a second population of said salt external to said liposome; (b) replacing said salt external to said liposome with an aqueous buffer, thereby forming a gradient of said carbohydrate sulfate across said lipid membrane; and (c) adding a solution of carfilzomib in an aprotic solvent to the suspension formed in (b), forming a carfilzomib precipitate allowing carfilzomib to traverse said lipid membrane, concentrating in said internal aqueous compartment, thereby encapsulating said carfilzomib.

Metadata:
- Claim Count in Document: 50.0
- Percentile: 97.0
- Lexical Diversity: 1.9845
- Patent Class: 424.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15502092', '15216416', '14879302', '14395345', '15303131']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.797828173445179
- 35 USC 102 Novelty (BERT): 0.6217565428050076
- Combined Prediction Score: 0.7802210103811619
- Mean Citation Score: 514.039696
- Max Citation Score: 753.837
- Similarity Product: 508.8320309894085

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test