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Formulation for a viptadil

A technology of pharmaceutical preparations and preservatives, applied in the field of pharmaceutical preparations of alendidil and its derivatives

Active Publication Date: 2012-02-22
缓解疗法国际股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Any change in physical appearance such as a color change in turbidity can reduce patient or consumer confidence in the product
Second, since some products are dispensed in multi-dose containers, uniform dosing of obsolete active ingredients must be determined
[0016]Development of suitable pharmaceutical formulations for defined targets is complex

Method used

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  • Formulation for a viptadil
  • Formulation for a viptadil
  • Formulation for a viptadil

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] The stability of alendidil was determined over a pH range of 5 to 7 and at the temperatures and lengths of time shown in Tables 1-4 below.

[0113] pH values ​​for purity and assay are shown in Table 1 for peptides in 150 mM citrate buffer and 1 mM EDTA, in Table 2 for peptides in 150 mM acetate buffer, and in Table 3 for peptides in 150 mM phosphate buffer and 4.

[0114] Table 1

[0115]

[0116] Table 2

[0117]

[0118] table 3

[0119]

[0120]

[0121] Table 4

[0122]

[0123] From these tables it can be seen that alendidil is most stable at about pH 6. figure 1 The purity loss data in the table above were summarized to more clearly show the increased stability of alendidil at about pH 6.

Embodiment 2

[0125] This example describes the liquid formulation of alendidil using citrate buffer or 0.9% sodium chloride without buffer components. The pH of the sodium chloride solution is between 5.3 and 5.8. A solution with a pH value of approximately 6 was shown to increase the stability of alentidil (see Example 1).

[0126] Another important characteristic of the formulation is the amount of alendidil in solution. Surprisingly, the inventors found that alentidil in formulations comprising alentidil in amounts ranging from 0.0066% to 0.2% was more stable than formulations comprising alentidil in amounts less than 0.0066%, as measured by the percentage loss of the test (See Table 5). The purity of the samples did not show any significant change at different concentrations of alendidil. When the concentration of alendidil increased from 0.033 mg / Ml to 0.066 mg / mL, the shelf life increased approximately 3-fold.

[0127] table 5

[0128] Altidel concentration 0.033...

Embodiment 3

[0131] Based on the finding that alendidil is most stable at a pH of about 6 and an amount of alendidil of about 0.0066%, the following formulations were developed:

[0132] Formulation A

[0133] Element Weight % (w / v) Atendil 0.0066-0.5 Sodium chloride 0.9 water for injection 100mL

[0134] In formulation B, mannitol was added to the formulation to increase the stability of alentidil.

[0135] Formulation B

[0136] Element Weight % (w / v) Atendil 0.0066-1.0 Mannitol 4.0 Sodium chloride 0.16 water for injection 100mL

[0137] Formulation C

[0138] Element Weight % (w / v) Atendil 0.001-1.0 Citrate buffer (50mM, pH 5.8) citric acid 0.227 Trisodium citrate dihydrate 1.12 Mannitol 4.0 water for injection 100mL

[0139] Preparation D

[0140] Element Weight % (w / v) Atendil 0.001-1.0 Citrate buffer (120mM,...

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PUM

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Abstract

The present invention relates to pharmaceutical formulations of Aviptadil and its derivatives. The stability of the Aviptadil formulation was shown to be improved by a formulation having a defined concentration of Aviptadil prepared in a buffer having a defined pH range.

Description

technical field [0001] The present invention relates to the pharmaceutical preparations of Aviptadil and its derivatives. Background technique [0002] Altideil (Vasoactive Intestinal Peptide, VIP, vasoactive intestinal peptide) has been used for more than 20 years in the United States and in European countries in controlled trials including humans and animals. Injectable alotidil combined with fentonide has been shown to be useful in the treatment of erectile dysfunction in the United Kingdom, Denmark, and New Jersey. Since the discovery of alendidil in the early 1970s, the pharmacology and toxicology of the endogenous peptide alendidil have been described in numerous peer-reviewed journals. [0003] Endogenous alendidil, also known as vasoactive intestinal peptide (VIP), is a 28 amino acid peptide with the following amino acid sequence (from N to C terminus): [0004] His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Arg-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Ser- Il...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/00A61K38/22A61K47/00A61P7/00A61P9/00A61P9/02A61P9/10A61P25/28A61P25/16A61K47/26A61K47/02A61K47/10A61K47/30
CPCA61K9/0019A61K38/2278A61K47/02A61K47/12A61K47/26A61P3/10A61P5/16A61P7/00A61P7/06A61P9/00A61P9/02A61P9/10A61P9/12A61P11/00A61P11/06A61P17/00A61P21/04A61P25/02A61P25/16A61P25/28A61P29/00A61P35/00A61P43/00
Inventor 巴赫·吉洛德多里安·巴菲克
Owner 缓解疗法国际股份有限公司
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