Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
First Claim
1. A mixture of conjugates, wherein each conjugate consists of a calcitonin and a polyethylene glycol moiety, wherein the polyethylene glycol moiety is coupled to an amine function of the calcitonin, wherein the mixture is a monodispersed mixture, a substantially purely monodispersed mixture or a purely monodispersed mixture.
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Abstract
A mixture of conjugates in which each conjugate in the mixture comprises a calcitonin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may lower serum calcium levels in a subject by 10, 15 or even 20 percent or more. Moreover, the mixture may be more effective at surviving an in vitro model of intestinal digestion than non-conjugated calcitonin. Furthermore, the mixture may exhibit a higher bioavailability than non-conjugated calcitonin.
173 Citations
15 Claims
- 1. A mixture of conjugates, wherein each conjugate consists of a calcitonin and a polyethylene glycol moiety, wherein the polyethylene glycol moiety is coupled to an amine function of the calcitonin, wherein the mixture is a monodispersed mixture, a substantially purely monodispersed mixture or a purely monodispersed mixture.
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13. A monodispersed mixture of conjugates, wherein each conjugate consists of a calcitonin coupled to at least one polyethylene glycol moiety consisting of at least 4 polyethylene glycol subunits, wherein coupling between the calcitonin and the polyethylene glycol moiety-consists of an amine bond(s), said mixture having a molecular weight distribution with a standard deviation of less than about 22 Daltons.
- 14. A mixture of conjugates wherein each conjugate consists of a calcitonin coupled to at least one polyethylene glycol moiety, wherein coupling between the calcitonin and the polyethylene glycol moiety consists of an amine bond(s), wherein the mixture has a dispersity coefficient (DC) greater than 10,000 where
Specification