Unlock instant, AI-driven research and patent intelligence for your innovation.

Octreotide injection

a technology of octreotide and injection, which is applied in the direction of peptide/protein ingredients, cyclic peptide ingredients, non-active ingredients of pharmaceuticals, etc., can solve the problems of poor bioavailability of peptide drugs after oral or parenteral administration, and achieve the effect of improving the bioavailability of peptide drugs

Inactive Publication Date: 2018-11-15
SUN PHARMA INDS
View PDF1 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a sterile solution of octreotide or its pharmaceutically acceptable salt thereof, which has a higher concentration of octreotide base (2.0 to 2.5 mg / ml) compared to prior known diluate solutions (1.0 mg / ml). This results in a significantly reduced amount of preservative being injected per dose in the body, as compared to prior art known octreotide products like Sandostatin™ (4.0 mg / ml preservative per dose). The amount of preservative injected per dose using the injection device according to the present invention is therefore significantly reduced. This has the advantage of reducing the risk of potential adverse side effects caused by the preservative. The concentration of octreotide base in the present invention is also higher, which provides a more potent solution for injection.

Problems solved by technology

Typically it is known that peptide drugs, after oral or parenteral administration, show a poor bioavailability in the blood, e.g. due to their short biological half-lives in turn caused by their metabolic instability (see the disclosure in U.S. Pat. No. 5,538,739).

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Octreotide injection
  • Octreotide injection
  • Octreotide injection

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0055]Sterile solution of octreotide acetate according to one embodiment of the present invention is described below.

TABLE 1Sterile solution of the present inventionSr.No.Ingredientsmg / ml1Octreotide acetate equivalent to2.5octreotide base2Lactic acid3.43Mannitol22.54Phenol5.05Sodium bicarbonateq.s. to pH 4.2 ± 0.36Water for injectionq.s to 1 ml

[0056]Procedure: Specified volume of water for injection was collected in suitable container at a temperature of 20° C. to 25° C. To this octreotide acetate was added under stirring to form a clear solution. Specified quantity of lactic acid was dissolved in above solution under stirring until the clear solution was obtained. Specified quantity of mannitol was dissolved in the above solution under stirring until the clear solution was obtained. Separately phenol was dissolved in the specified quantity of water and added to the above bulk solution. Further, the pH of the solution was adjusted to about 4.20±0.30 with sufficient quantity of sodiu...

example 2

[0060]The aqueous solution of octreotide acetate having concentration equivalent to 2.5 mg / ml of octreotide base filled in a pen injection device according to example 1 of the present invention, referred to herein as test product A, was subjected to in-vivo plasma pharmacokinetic study in healthy human volunteers, whereby a given dose of octreotide acetate solution (equivalent to 100 μg octreotide base) was delivered sub-cutaneously through the multiple dose pen injection device to the human volunteer and plasma pharmacokinetic profile of octreotide was studied. The bioavailability i.e. AUC0-∞, AUC0-t, Cmax, Tmax, and other pharmacokinetic parameters were determined. The study was a randomized, open label, two treatment, two period, two sequence, single dose, cross-over study, under fasting conditions and involving twelve healthy adult human volunteers, with a washout period of 7 days between dosages. The marketed product Sandostatin™ 1.0 mg / ml solution in multi-dose vial was taken ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Concentrationaaaaaaaaaa
Concentrationaaaaaaaaaa
Densityaaaaaaaaaa
Login to View More

Abstract

The present invention relates to a sterile solution comprising: octreotide in the form of a pharmaceutically acceptable salt, present at a concentration equivalent to 2.0 mg / ml to 2.5 mg / ml of octreotide base, and at least one preservative in a pharmaceutically acceptable vehicle, wherein the sterile solution is present in an injection device.

Description

FIELD OF INVENTION[0001]The present invention relates to a sterile solution of octreotide in the form of a pharmaceutically acceptable salt filled in an injection device, wherein the octreotide salt is present at a concentration equivalent to 2.0 mg / ml to 2.5 mg / ml of octreotide base.BACKGROUND OF INVENTION[0002]Octreotide is commercially available under the brand name Sandostatin™ as a preserved solution filled in sterile 5 ml multidose vials in two strengths, 200 μg / ml and 1000 μg / ml. The present inventors had previously developed a multiple dose pen injection device containing solution of octreotide acetate that allowed self-administration of octreotide dose to the patients, as disclosed in the US Pat. Appl. Publ. No. 20140213984A1. During this time, the present inventors worked towards the development of an injection device, such as a pen injection device, having multiple doses that supply daily doses of octreotide for about a month or so. In particular, attempts were made to de...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K38/12A61K9/00A61K9/08A61K47/26A61K47/12A61K47/14A61K47/10
CPCA61K38/12A61K9/0019A61K9/08A61K47/26A61K47/12A61K47/14A61K47/10A61K38/08
Inventor RANA, AMARTHUMMAR, RAKESHAGRAWAL, SUDEEPBHOWMICK, SUBHAS BALARAMTHENNATI, RAJAMANNAR
Owner SUN PHARMA INDS