Implant preparations for delivery of bioactive macromolecules

Claim 2

(2) A process of making a bioerodible preparation of Claim 1 with sustained action which is capable of reducing diabetic hyperglycemia continuously and promoting growth, wherein said bioactive macromolecule is insulin.

Claim 3

(3) A process of Claim 2 wherein the amount of insulin comprises about 11% to about 40% by weight with the balance being lipid material which includes glycerides selected from glyceryl esters of lauric, myristic, palmitic, stearic, oleic, linoleic acids or combination thereof; long-chain fatty acids or derivatives selected from lauric, myristic, palmitic, stearic, oleic, linoleic acids, their simple esters, salts, amides, anhydrides, or combination thereof; and non-hormonal steroids - selected from coprostanol, cholesterol, cholic acid, their esters, simple glycosides or combination thereof.

Claim 4

( 4 ) A process of Claim 1 with sustained action wherein said bioactive macromolecule is somatotropin.

Claim 5

( 5 ) A process of Claim 4 wherein the amount of somatotropin comprises about 1% to about 50% by weight, with the balance being the lipid material which includes glycerides selected from glyceryl esters of lauric, myristic, palmitic, stearic, oleic, linoleic acids or combination thereof; long-chain fatty acids or derivative selected from lauric, myristic, palmitic, stearic, oleic, linoleic acids, their simple esters, salts, amides, anhydrides, or combination thereof; and non-hormonal steroids selected from coprostanol, cholesterol, cholic acid, their esters, simple glycosides or combination thereof.

Claim 6

(6) A bioerodibe preparation suitable as implant with sustained action which comprises a compressed admixture of an effective amount of bioactive macromolecule and lipid powder with the said lipid powder being selected from glycerides, waxes, long-chain fatty acids or derivatives, sphingolipids, cerebrosides, terpenes, non-hormonal steroids or a combination thereof.

Claim 7

(7) A bioerodible preparation of Claim 6 with sustained action capable of continuously reducing diabetic hyperglycemia for a prolonged period of time and promoting growth upon implantation wherein said bioactive macromolecule is insulin.

Claim 8

(8) A bioerodible preparation of Claim 7 wherein the amount of insulin comprises about 11% to about 40% by weight with the balance being the lipid materials which includes glycerides selected from glyceryl esters of lauric, myristic, palmitic, stearic, oleic, linoleic acids or combination thereof; long-chain fatty acids or derivatives selected from lauric, myristic, palmitic, stearic, oleic, linoleic acids, their simple esters, salts, amides, anhydrides, or combination thereof; and non-hormonal steroids selected from coprostanol, cholesterol, cholic acid, their esters, simple glycosides or combination thereof.

Claim 9

(9) A bioerodible preparation of Claim 6 with sustained action wherein said bioactive macromolecule is somatotropin.

Claim 10

(10) A bioerodible preparation of Claim 9 wherein the amount of somatotropin comprises about 1% to about 50% by weight with the balance being the lipid materials which includes glycerides selected from glyceryl esters of lauric, myristic, palmitic, stearic, oleic, linoleic acids or combination thereof; long-chain fatty acids or derivatives selected from lauric, myristic, palmitic, stearic, oleic, linoleic acids, their simple esters, salts, amides, anhydrides, or combination thereof; and non-hormonal steroids selected from coprostanol, cholesterol, cholic acid, their esters, simple- glycosides or combination thereof.

Claim 11

(11) A bioerodible preparation of Claim 8 and Claim 10 which comprises pellet, disc or fractions thereof, rods, chips, spheres or flakes.

Claim 12

( 12 ) A kit for preparing a bioerodible preparation as claimed in Claim 8 and Claim 10 which comprises the bioactive macromolecule and the lipid material.

Claim 13

( 13 ) A method of sustaining the action of bioactive macromolecule preparation which comprises of compressing powder admixture of effective amount of bioactive macromolecule and lipid material selected from glycerides, waxes, long-chain fatty acids or derivatives, phospholipids, sphingolipids, cerebrosides, terpenes, nonhormonal steroids or combination thereof.

Claim 14

(14) A method of sustaining the action of bioactive macromolecule preparation as claimed in Claim 13 wherein the bioactive macromolecule is insulin.

Claim 15

(15) A method of sustaining the action of bioactive macromolecule preparation as claimed in Claim 14 wherein the amount of insulin is about 11% to about 40% by weight with the balance being the lipid material including glycerides selected from glyceryl esters of lauric, myristic, palmitic, stearic, oleic, linoleic acids or combination thereof; long-chain fatty acids or derivatives selected from lauric, myristic, palmitic, stearic, oleic, linoleic acids, their simple esters, salts, amides, anhydrides or combination thereof.

Claim 16

(16) A method of sustaining the action of bioactive macromolecule preparation as claimed in Claim 13 wherein the bioactive macromolecule is somatotropin.

Claim 17

(17) A method of sustaining the action of bioactive macromolecule preparation as claimed in Claim 16 wherein the , amount of somatotropin is about 1% to about 50% by weight with the balance being the lipid material' including glycerides selected from glyceryl esters of lauric, myristic, palmitic, stearic, oleic, linoleic acids or combination thereof; long-chain fatty acids or derivatives selected from lauric, myristic, palmitic, stearic, oleic, linoleic acids, their simple esters, salts, amides, anhydrides, or combination thereof; and non-hormonal steroids selected from coprostanol, cholesterol, cholic acids, their esters, simple glycosides or combination thereof.

Claim 18

(18) A method of treating diabetes mellitus which comprises continuously reducing hyperglycemia by implanting a . compressed powder admixture of effective amount of insulin and lipid materials selected from glycerides, waxes, long-chain fatty acids or derivatives, phospholipids, sphingolipids, cerebrosides, terpenes, non-hormonal steroids or combination thereof.

Claim 19

(19) A method of treating diabetes as claimed in Claim 18 wherein the amount of insulin comprises about 11% to about 40 % by weight with the balance being the lipid material which includes glycerides selected from glyceryl esters of lauric, myristic, palmitic, stearic, oleic, linoleic acids or combination thereof; long-chain fatty acids or derivatives selected from lauric, myristic, palmitic, stearic, oleic, linoleic acids, their simple esters, salts, amides, anhydirdes or combination thereof; and non-hormonal steroids selected from coprostanol, cholesterol, cholic acid, their esters, simple glycosides or combination thereof.

Claim 20

(20) A method of promoting growth which comprises implanting a compressed powder admixture of effective amount of the growth hormone somatotropin in lipid materials selected from glycerides, waxes, long-chain fatty acids or derivatives, phospholipids, sphingolipids, cerebrosides, terpenes, non-hormonal steroids or combination thereof.

Claim 21

(21) A method of promoting growth as claimed in Claim 20 wherein the amount of somtotropin comprises about 1% to about 50% by weight with the balance being the lipid material which includes glycerides selected from glyceryl esters of lauric, myristic, palmitic, stearic, oleic, linoleic acids or combination thereof; long-chain fatty acids or derivatives selected from lauric, myristic, palmitic, stearic, oleic, linoleic acids, their simple esters, salts, amides, anhydrides, or combination thereof; and non-hormonal steroids selected from coprostanol, cholesterol, cholic acid, their esters, simple glycosides or combination thereof.