Novel formulation of pyridoxal 5'-phosphate and method of preparation

A technology of pyridoxal phosphate and preparations, which can be applied in the directions of pill delivery, pharmaceutical formulations, and medical preparations of non-active ingredients, and can solve problems such as low doses

Inactive Publication Date: 2008-01-23
MEDICURE INT INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, currently available supplements generally deliver lower doses of pyridoxal 5'-phosphate, whic...

Method used

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  • Novel formulation of pyridoxal 5'-phosphate and method of preparation
  • Novel formulation of pyridoxal 5'-phosphate and method of preparation
  • Novel formulation of pyridoxal 5'-phosphate and method of preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-5

[0118] Embodiment 1-5'-pyridoxal phosphate enteric-coated tablet formulation and preparation method thereof

[0119] Table 1 lists the ingredients and relative amounts (265 mg per tablet) of pyridoxal 5'-phosphate enteric-coated tablet preparations. As shown in Table 1, 20,000 tablets were produced in one batch. The batch size can be scaled up or down by proportionally increasing or decreasing the relative amounts.

[0120] Table 1: Pyridoxal 5′-phosphate enteric-coated tablet formulations

[0121] Element

％

mg / tablet

g / batch

Granulation stage

Pyridoxal 5′-phosphate

66.3

265

5300

Microcrystalline Cellulose (Avicel PH102)

11.9

47.5

950

Croscarmellose Sodium

2.0

8

160

Povidone (K-30)

4.7

18.75

375

Subtotal:

84.8

339.25

6785

Purified water (for PVP granule solution)

Other purified water (fo...

Embodiment 3-5

[0138] Dissolution test of embodiment 3-5'-pyridoxal phosphate enteric-coated tablet

[0139] The dissolution characteristics of 250 mg pyridoxal 5'-phosphate enteric-coated tablets were determined by conventional test methods.

[0140] Disintegration time was determined in artificial gastric juice (without pepsin) and artificial intestinal juice (without pancreatin) using USP method .

[0141] In artificial gastric juice, the tablets remained intact after 1 hour. Complete tablet disintegration was observed between 5:46 and 14:52 minutes in artificial intestinal fluid.

[0142] Dissolution times were determined using USP and USP method B for enteric-coated tablets. The paddle speed of the dissolution apparatus was set at 100 rpm, and the sampling points were set at 30 and 45 minutes. The concentration of pyridoxal 5'-phosphate in the dissolution buffer was determined by LCMS.

[0143] Dissolution data for enteric coated tablets were observed to be within the following sp...

Embodiment 4-5

[0147] Safety, tolerance and pharmacokinetic test of embodiment 4-5'-pyridoxal phosphate enteric-coated tablets

[0148] A single-centre, phase 1, open-label trial was conducted to evaluate the safety, tolerability, and pharmacokinetics of pyridoxal-5'-phosphate (p5p) enteric-coated tablets.

[0149] Subjects - Each test group consisted of 6 subjects (3 males, 3 females) consisting of:

[0150] ●Male or female, smoker or non-smoker, age ≥18 and ≤55.

[0151] ●Able to agree to participate in the trial.

[0152] ●BMI≥19.0 and 2 .

[0153] Subjects who meet any of the following conditions are excluded from this trial:

[0154] ●With clinically significant disease within 4 weeks prior to administration of study drug.

[0155] ●Clinically significant surgical procedure within 4 weeks prior to administration of study drug.

[0156] ●Any clinically significant abnormality found during drug screening.

[0157] ●Any reason for exclusion of the subject from the trial in the opinio...

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Abstract

A pyridoxal-5'-phosphate pharmaceutical formulation suitable for oral administration is provided comprising a dissolution profile, when measured in a standard dissolution apparatus, according to the United States Pharmacopoeia dissolution test, at 37 DEG C. in a 0.05M phosphate buffered solution having a pH of 6.8 at 75 rpm, as follows: (a) greater than about 30% at 15 minutes, (b) greater than about 85% at 30 minutes, (c), greater than about 90% at 45 minutes, or (d) greater than about 95% at 60 minutes. Additionally, in vivo oral intake of between 15 and 60 mg/kg of a pyridoxal-5'-phosphate pharmaceutical formulation can produce a maximum plasma level (Cmax) of between about 1 mg/L and 8 mg/L. A pharmaceutical formulation provided comprises (a) a core, wherein said core comprises pyridoxal-5'-phosphate or a pharmaceutically acceptable salt thereof; (b) a sub-coat surrounding the core; and (c) an enteric coat surrounding the sub-coat.

Description

technical field [0001] The invention relates to a pharmaceutical preparation of 5'-pyridoxal phosphate and a preparation method thereof. Background technique [0002] 5'-Pyridoxal phosphate can be used for the treatment and prevention of various diseases such as hypertension, cerebrovascular disease, cardiovascular disease and diabetes. See, eg, US Pat. Pyridoxal 5'-phosphate is commercially available in various dosages. However, currently available supplements generally deliver lower doses of pyridoxal 5'-phosphate, which are too low for the treatment of hypertension, cerebrovascular disease, cardiovascular disease and diabetes. Therefore, multiple daily doses of the supplement are usually required in order to obtain adequate therapeutic levels. [0003] The present invention provides novel oral pharmaceutical compositions capable of releasing increased amounts of pyridoxal 5'-phosphate compared to prior art formulations. The present invention also provides novel pharma...

Claims

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Application Information

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IPC IPC(8): A61K31/675A61K9/28A61K9/48A61K47/02A61K47/12A61K47/30A61K47/38
Inventor A·弗里森J·卡特
Owner MEDICURE INT INC
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