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Peptide formulations and uses thereof

A technology for preparations and water-based preparations, applied in the field of preventive and therapeutic drugs, can solve the problems of application limitation, influence, and stability reduction of therapeutic methods

Inactive Publication Date: 2011-10-05
UNIVERSITY OF GRONINGEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Vasopressin preparations known to date are similarly affected by exposure to high ambient temperature or light
[0007] The stability of formulations comprising biologically active or therapeutic peptides (such as oxytocin or vasopressin) is known to decrease at elevated temperatures and is therefore of no use in therapeutic methods in (sub)tropical countries, including many third world countries. Apps in are restricted

Method used

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  • Peptide formulations and uses thereof
  • Peptide formulations and uses thereof
  • Peptide formulations and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Embodiment 1 (comparative example)

[0062] This comparative example demonstrates the oxytocin-stabilizing effect of divalent metal ions. Will be used as metal chloride salt (MCl 2 ) of divalent metal ions (Ca 2+ , Mg 2+ and Zn 2+ ) was added to an unbuffered formulation including oxytocin and purified water (W). Divalent metal ions were used at concentrations of 0 mM, 2 mM, 5 mM, 10 mM and 50 mM. Formulation samples were then stored at pH 4.5 at 4°C (reference control) or 55°C (test) for 4 weeks. Thereafter, all samples were stored under cooling conditions (2-8 °C) before RP-HPLC and HP-SEC analysis. Effects on stability were determined by measuring oxytocin recovery and percent oxytocin monomer. Figure 1A and 1B The results are shown in .

[0063] Figure 1A Oxytocin recovery after storage at 55° C. for 4 weeks in unbuffered pure water (W) in the absence or presence of divalent metal ions is shown. in ca 2+ or Zn 2+ Oxytocin recovery increased at 4°C in th...

Embodiment 2

[0064] Embodiment 2 (comparative example)

[0065] Citrate buffer (CB) at a concentration of 0 mM, 5 mM, 10 mM or 50 mM, acetate buffer (AC) at a concentration of 10 mM, aspartate buffer (AP) at a concentration of 10 mM or Ringer Lactate buffer (ORL) was added to the formulation including oxytocin in purified water (W). The Ringer's lactate used was Baxter Viavlo 500 mL WE2323 Ringer's lactate solution for intravenous infusion. Batch number 09B04E1P, expiration date (exp.date) 2011. The pH of the preparation was 6.4.

[0066] Composition per 100mL:

[0067]

[0068] All formulations were free of divalent metal ions (except ORL) and had a final concentration of oxytocin of 0.1 mg / ml and a pH of 4.5 (CB, AC and AP) or 6.4 (ORL). Samples of each formulation were stored at 4°C (control) or 55°C (test) for 4 weeks. Thereafter, all samples were stored under cooling (2-8° C.) prior to RP-HPLC and HP-SEC analysis. The effect on stability was determined by measuring the recove...

Embodiment 3

[0070] Embodiment 3 (comparative example)

[0071] The thermal stability of oxytocin in the presence of a combination of buffers and monovalent metal ions was investigated. Use citrate buffer (CB), acetate buffer (AC) or aspartate buffer (AP) at a concentration of 10 mM. Addition of the monovalent metal ion Na in its chloride salt form (NaCl and KCl) + and K + , using final concentrations of 10 mM and 20 mM. All formulations had a final concentration of oxytocin of 0.1 mg / ml and a pH of 4.5. Samples of each formulation were stored at 4°C (control) or 55°C (test) for 4 weeks. Thereafter, all samples were stored under cooling (2-8° C.) prior to RP-HPLC and HP-SEC analysis. The effect on stability was determined by measuring the recovery of oxytocin and the percentage of oxytocin monomer. Figure 3A and 3B The results are shown in .

[0072] exist Figure 3A In , a minor thermostability effect of oxytocin stored at 55°C was observed. Despite the presence of buffer alone...

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Abstract

The present invention relates to the field of preventive and therapeutic medicine, in particular to peptide formulations. Provided is a p H-buffered aqueous formulation comprising oxytocin, vasopressin or an analogue thereof and at least one non-toxic source of divalent metal ions in a concentration of at least 2 m M, and the use of the formulation for the manufacture of a medicament for therapeutic and / or prophylactic treatments. Also provided is a method for treating or preventing haemorrhage in a subject in need thereof, comprising administering to said subject an effective dosage amount of an oxytocin formulation according to the invention. Further provided is a method for treating or preventing diabetes insipidus or vasodilatory shock in a subject in need thereof, comprising administering to said subject an effective dosage amount of a vasopressin formulation according to the invention.

Description

technical field [0001] The present invention relates to the field of preventive and therapeutic medicine. The present invention particularly relates to therapeutic formulations comprising neurohypophysis nonapeptides containing disulfide bridges, such as oxytocin, vasopressin or analogs thereof. The present invention provides thermostable oxytocin preparations and their use in indications such as induction of labor, augmentation of labor, postpartum hemorrhage or atony of uterine contractions (or uterine atony). The present invention also provides thermostable vasopressin formulations and their use in indications such as diabetes insipidus and vasodilatory shock. Background technique [0002] Oxytocin (Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH 2 ) and vasopressin (Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Arg-Gly-NH 2 ) are peptide hormones produced in the brain of most mammals including humans, and these peptide hormones have a high degree of homology. Both nonapeptides originate from t...

Claims

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Application Information

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IPC IPC(8): A61K38/11A61K38/095
CPCA61K38/11A61P3/10A61P7/04A61P7/12A61P9/00A61K38/095
Inventor 让-皮埃尔·阿莫里克里斯蒂娜·阿瓦恩蒂亨德里克·威廉·弗里亚林克沃特·莱昂纳德斯·约瑟夫·欣里奇斯
Owner UNIVERSITY OF GRONINGEN
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