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Details for Patent: 5,439,688

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Details for Patent: 5,439,688

Title: Process for preparing a pharmaceutical composition
Abstract:A pharmaceutical composition is prepared in the form of microparticles or of an implant comprising a biodegradable polymer selected from poly-1,4-butylene succinate, poly-2,3-butylene succinate, poly-1,4-butylene fumarate and poly-2,3-butylene succinate, incorporating as the active substance the pamoate, tannate, stearate or palmitate of a natural or of a synthetic peptide comprising 3 to 45 amino acids, such as LH-RH, somatostatin, GH-RH or calcitonin, or one of their synthetic analogues or homologues. The preparation comprises dry blending the ingredients in the form of powders, pre-compressing and preheating the mixture and then extruding the pre-compressed and pre-heated mixture. The product resulting from the extrusion step can then be comminuted and finally sieved.
Inventor(s): Orsolini; Piero (Martigny, CH), Heimgartner; Frederic (Villeneuve, CH)
Assignee: Debio Recherche Pharmaceutique S.A. (Martigny, CH)
Filing Date:Nov 12, 1991
Application Number:07/790,033
Claims:1. A process for preparing a pharmaceutical composition designed for the sustained and the controlled release of a drug, including a biodegradable polymer selected from the group consisting of poly-1,4-butylene succinate, poly-2,3-butylene succinate, poly-1,4-butylene fumarate and poly-2,3-butylene fumarate, and incorporating as the active substance the pamoate, tannate, stearate or palmitate salt of a natural or of a synthetic peptide, characterized in that:

a) the biodegradable polymer and the active substance selected are dry blended, both as microparticles having an average size smaller than about 500 microns;

b) the powdered mixture is compressed progressively and heated progressively to about 90.degree. C.;

c) the pre-compressed and pre-heated mixture is subjected to an extrusion at a temperature comprised between about 90.degree. and 100.degree. C., and the extruded product is cooled; and when required:

d) the product resulting from the extrusion is comminuted at a decreased temperature, and finally the microparticles obtained are selected and collected.

2. A process according to claim 1, characterized in that it includes the steps a, b and c, and in that it leads to the obtention of an implant.

3. A process according to claim 1, characterized in that it includes the steps a, b, c and d and in that it leads to the obtention of microparticles.

4. A process according to claim 3, characterized in that the microparticles of the biodegradable polymer have an average size smaller or equal to 200 microns, and preferably smaller or equal to 180 microns.

5. A process according to claim 1, characterized in that the pre-compression and the pre-heating of the mixture are carried out simultaneously, through the use of one or more endless screws.

6. A process according to claim 1, characterized in that the extrusion is carried out at a pressure comprised between 50 and 500 kg/cm.sup.2.

7. A process according to claim 1, characterized in that the comminution of the product resulting from the extrusion is a cryogenic comminution.

8. A process according to claim 1, characterized in that the selection of the microparticles resulting from the comminution, is carried out by sieving.

9. A process according to claim 1, characterized in that the active substance is the pamoate, tannate, stearate or palmitate of a natural or of a synthetic peptide comprising 3 to 45 amino acids, and in particular of LH-RH, somatostatin, GH-RH, calcitonin or synthetic peptides.

10. A process according to claim 9, characterized in that the active substance is the pamoate salt of LH-RH, of somatostatin or of one of their synthetic analogues or homologues selected from ##STR4## where R.sup.1 =lower alkyl.

11. The process of claim 1 which further comprises selecting the drug to be present in the polymer at a concentration of between about 0.1 and 15% by weight.

12. A process for preparing a pharmaceutical composition designed for the controlled release of a drug having a natural or synthetic peptide salt as an active substance from a biodegradable polymer comprising polybutylene succinates or fumarates, which comprises:

selecting the drug and polymer to both be in the form of microparticles having an average size of less than about 500 microns;

dry blending the drug and polymer microparticles to form a mixture;

compressing and heating the mixture to about 90.degree. C.;

extruding the compressed and heated mixture at a temperature of between about 90.degree. and 100.degree. C. to form an extruded product; and

comminuting the extruded product at a temperature below 90.degree. C. to obtain microparticles for use as the pharmaceutical composition.

13. The process of claim 12 which further comprises selecting the drug to be present in the polymer at a concentration of between about 0.1 and 15% by weight.

14. The process of claim 12 which further comprises selecting the drug to be in the form of a water insoluble salt.

15. The process of claim 12 which further comprises selecting the drug to be a pamoate, tannate, stearate or palmitate salt of a natural or synthetic peptide having 3 to 45 amino acids.

16. The process of claim 12 wherein the polymer microparticles are initially at a size of less than about 200 microns, and which further comprises extruding the mixture at a pressure between about 50 and 500 kg/cm.sup.2.

17. The process of claim 12 which further comprises comminuting the extruded product at cryogenic temperatures.

18. The process of claim 12 wherein the selection of the microparticles after comminution is carried out by sieving.

19. The process of claim 12 wherein the compressing and heating of the mixture is carried out simultaneously and progressively by passing the mixture through one or more endless screws.

20. The process of claim 12 which further comprises selecting the peptide to be LH-RH, somatostatin, GH-RH, or calcitonin, or synthetic peptides

21. The process of claim 12 which further comprises selecting the drug to be the pamoate salt of LH-RH, of somatostatin, or of one of their synthetic analogues or homologues selected from the group consisting of: ##STR5## where R.sup.1 consists of a lower alkyl.

22. The process of claim 12 wherein the polymer is selected from the group consisting of poly-1,4-butylene succinate, poly-2,3-butylene fumarate, poly-1,4-butylene fumarate and poly-2,3-butylene succinate.

23. The process of claim 12 wherein the extruded product before comminution comprises the pharmaceutical composition in the form of an implant.

24. A process for preparing a pharmaceutical composition designed for the controlled release of a drug, including a biodegradable polymer comprising polybutylene fumarates or polybutylene succinates, and incorporating as the active substance a pamoate, tannate, stearate or palmitate salt of LH-RH, somatostatin, GH-RH, calcitonin, or synthetic peptides comprising:

selecting the drug and polymer both to be in the form of microparticles having an average size of less than about 500 microns;

dry blending the drug and polymer microparticles to form a mixture;

compressing and heating the mixture to about 90.degree. C.;

extruding the compressed and heated mixture at a temperature of between about 90.degree. C. and 100.degree. C. to form an extruded product; and

comminuting the extruded product at a temperature below 90.degree. C. to obtain microparticles for use as the pharmaceutical composition.
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