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Orlistat and organic acid calcium eutectic crystal body and medicine composition containing eutectic crystal body

A technology of orlistat and organic acid calcium, which is applied in the field of medicine, can solve the problems of low melting point, achieve full dissolution, shorten drying time, and improve the effect of inhibition

Active Publication Date: 2018-08-24
ZHONGSHAN WANHAN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, there is no report on the use of orlistat and calcium supplement organic acid calcium to prepare co-crystal formers to overcome the shortcomings of orlistat's low melting point and improve its effect of inhibiting fat absorption

Method used

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  • Orlistat and organic acid calcium eutectic crystal body and medicine composition containing eutectic crystal body
  • Orlistat and organic acid calcium eutectic crystal body and medicine composition containing eutectic crystal body
  • Orlistat and organic acid calcium eutectic crystal body and medicine composition containing eutectic crystal body

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Study on the preparation method of orlistat and calcium supplement organic acid calcium co-crystal

[0044] (1) Study on the preparation of orlistat and calcium gluconate co-crystal

[0045] Take type II orlistat 0.497g (1.003×10 -3 mol), placed in a 100mL three-neck flask in an ultrasonic water bath (40°C), slowly added methanol / water mixed solvent (30:1, v / v) dropwise under stirring until the solid was completely dissolved to obtain liquid A, Leave in an ultrasonic water bath (40° C.) with stirring. Another calcium gluconate monohydrate (molecular formula: Ca[C 6 h 11 o 7 ] 2 ·H 2 O, molecular weight 448.40) 4.483g (containing calcium ions 9.998×10 -3 mol, gluconate ion 19.996×10 -3 mol), placed in a 500mL three-neck flask in an ultrasonic water bath (40°C), slowly added methanol / water mixed solvent (30:1, v / v) dropwise under stirring until the solid was completely dissolved to obtain liquid B, Leave in an ultrasonic water bath (40° C.) with stirrin...

Embodiment 2

[0052] Example 2 Determination of Melting Point of Orlistat and Calcium Supplement Organic Acid Calcium Cocrystal

[0053] Orlistat-calcium gluconate co-crystal, orlistat-vitamin C calcium co-crystal, orlistat-citrate prepared respectively in Example 1 were processed according to the melting point automatic measuring instrument method recorded in the 2015 edition of "Chinese Pharmacopoeia". Calcium citrate co-crystal and orlistat calcium aspartate co-crystal were measured for melting point and melting range, and the results are shown in Table 1.

[0054] Table 1 Melting point determination results of orlistat and calcium supplement organic acid calcium cocrystal

[0055] Co-crystal former (CCF)

Orlistat: CCF (molecule ratio / molar ratio)

Eutectic melting point (°C)

Eutectic melting range (°C)

calcium gluconate

1:5

253.52

＜1

vitamin c calcium

1:4

170.91

＜1

calcium citrate

2:7

220.27

＜1

calcium a...

Embodiment 3

[0058] Example 3 Determination of the Molecular Ratio / Molar Ratio of Orlistat and Cocrystal Former (CCF) in Orlistat and Calcium Supplement Organic Acid Calcium Cocrystal

[0059] Using nuclear magnetic resonance ( 1 H-NMR, solution proton NMR) Determination of the molecular ratio / molar ratio of orlistat and co-crystal former (CFF) in orlistat and calcium supplement organic acid calcium co-crystal prepared in Example 1.

[0060] Method: Recorded on a Bruker-400MHz wavelength spectrometer equipped with an autosampler and controlled by a DRX400 console 1 H-NMR spectrum. Samples were dissolved in d6-DMSO for analysis. Data were acquired using standard Bruker load experiments with ICON-NMR v4.0.4 (construct 1) running with Topsin v1.3 (patch level 8).

[0061] Result: orlistat 1 H-NMR spectrum such as figure 1As shown, the integrated areas of all peaks are 4.33 times of the integrated areas of the peaks in the range of 0.88-0.94 ppm.

[0062] Orlistat and calcium gluconate c...

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to an orlistat and calcium supplementing agent type organic acid calcium eutectic crystal body and a medicine composition containing the eutectic crystal body. The eutectic crystal body is prepared from orlistat and calcium supplementing agent type organic acid calcium. The eutectic crystal body has higher melting point; the requirements on the drying conditions in the raw material medicine and preparation preparing process can be reduced; the effect of inhibiting the fat absorption by the orlistat can be improved. In addition, the obtained eutectic crystal is used as raw materials for preparing an oral solid preparation; the solubility of the eutectic crystal in the oral solid preparation in water is obviously higher than that of type II orlistat in commercially available orlistat capsules; the effect taking is higher than that of the type II orlistat in commercially available orlistat capsules.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a co-crystal of orlistat and a calcium supplement organic acid calcium and a pharmaceutical composition containing the co-crystal. Background technique [0002] Orlistat (orlistat) is a lipase inhibitor weight loss drug developed by Roche Pharmaceuticals. The trade name is Xenical. It was first launched in Europe and the United States in the late 1990s. Approved by the Food and Drug Administration to switch to an over-the-counter drug. Its chemical name is N-formyl-L-leucine (s)-1-[(2s,3s)-3-hexyl-4-oxyl-2-epoxypropylmethyl]dodecyl ester, also It is called Tetrahydrolipstatin (Tetrahydrolipstatin, THL), which is a semi-synthetic lipstatin derivative, and its chemical structure is as follows: [0003] [0004] Orlistat is available in capsules and tablets of its Ⅱ crystal form. It is also the only chemical weight-loss drug at home and abroad that does not affect ...

Claims

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Application Information

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IPC IPC(8): C07D305/12C07D307/62C07C59/105C07C59/265C07C229/24C07C59/08C07C59/84C07C59/347C07C229/08A61K31/365A61K31/191A61K31/19A61K31/375A61K31/198A61P3/04A61P3/06
CPCA61K31/19A61K31/191A61K31/198A61K31/365A61K31/375A61P3/04A61P3/06C07B2200/13C07C59/08C07C59/105C07C59/265C07C59/347C07C59/84C07C229/08C07C229/24C07D305/12C07D307/62A61K2300/00
Inventor 向飞杜志博彭韪
Owner ZHONGSHAN WANHAN PHARM CO LTD
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