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Roxithromycin monohydrate crystal, its preparation method and composition dry suspension containing the combination of the crystal and ambroxol hydrochloride

A technology of roxithromycin and monohydrate, applied in the field of pharmaceutical preparations, can solve the problems of reduced drug bioavailability, inability to obtain antibacterial effect, and difficulty in achieving complete dissolution, and achieves improved bioavailability, improved drug dissolution, The effect of improving bioavailability

Active Publication Date: 2011-12-21
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Chinese patent application CN1582954A discloses a kind of compound preparation of roxithromycin and ambroxol hydrochloride, and its concrete disclosed preparation form has capsule and tablet, but the compound roxithromycin of this common capsule and tablet form, in After oral administration, the dissolution in the body is relatively slow, and it is difficult to achieve complete dissolution, resulting in a decrease in the bioavailability of the drug, and the ideal antibacterial effect cannot be achieved
[0007] CN101712707A discloses that the roxithromycin compound has three solid substance forms of crystal A type, crystal B type and crystal C type. It is found that the crystal form affects the absorption rate of the active ingredient of roxithromycin solid medicine in the organism, enhances or reduces the biological Blood drug concentration in the body thus affects the therapeutic effect of the drug in clinical practice

Method used

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  • Roxithromycin monohydrate crystal, its preparation method and composition dry suspension containing the combination of the crystal and ambroxol hydrochloride
  • Roxithromycin monohydrate crystal, its preparation method and composition dry suspension containing the combination of the crystal and ambroxol hydrochloride
  • Roxithromycin monohydrate crystal, its preparation method and composition dry suspension containing the combination of the crystal and ambroxol hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] [embodiment 1] the preparation of roxithromycin monohydrate crystal

[0064] 1) Sample dissolution: under the condition of 40-50°C, dissolve 1 kg of roxithromycin in a mixed solution of 5 kg of anhydrous methanol and 1 kg of acetone to obtain solution I, and keep the temperature of solution I at 38-42° C., wherein;

[0065] 2) Crystallization: Take solution I and press filter to remove insoluble matter to obtain solution II. Keep the temperature of solution II at 38-42°C. Under stirring, continuously add 1 / 4-2 / 5 of the volume of solution II pure water dropwise, and control it at 1 Add within ~2 hours; after crystal growth for 1~2 hours, continue to drop 3 / 5~3 / 4 of the volume of pure water of solution II under stirring, control the addition within 1~2 hours, and stir until crystallization ; After growing crystals for 1-2 hours, cool down to 15-18°C, keep warm for 1-3 hours, centrifuge, and collect the wet product of roxithromycin;

[0066] 3) Pulverization: pulverize th...

preparation Embodiment 1

[0075] [Preparation Example 1] Preparation of Roxithromycin Ambroxol Composition Dry Suspension

[0076] Prescription:

[0077]

[0078]

[0079] Preparation Process:

[0080] 1) The raw and auxiliary materials ambroxol hydrochloride, sucrose, xanthan gum and hypromellose are pulverized through an 80-mesh sieve for subsequent use;

[0081] 2) Take the roxithromycin monohydrate crystals prepared in Example 1 according to the stated amount, mix them with the crushed and sieved raw and auxiliary materials in step 1), add an appropriate amount of banana essence, mix well, and pack it have to.

preparation Embodiment 2

[0082] [Preparation Example 2] Preparation of Roxithromycin Ambroxol Composition Dry Suspension

[0083] Prescription:

[0084]

[0085] Preparation process: same as formulation example 1, the difference is that the roxithromycin monohydrate crystals used are the roxithromycin monohydrate crystals prepared in Example 2.

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Abstract

The invention relates to a roxithromycin monohydrate crystal, a preparation method thereof and a compound dry suspension containing the roxithromycin monohydrate crystal and an ambroxol hydrochloride composition. The roxithromycin monohydrate crystal provided by the invention has a molecular formula of C41H76N2O15.H2O. The preparation method comprises the steps of sample dissolving, devitrifying,smashing, water exchanging and drying. The invention also provides a composition containing the crystal, and the composition comprises 30-70 parts by weight of roxithromycin monohydrate crystals, 5-15 parts by weight of ambroxol hydrochloride, 10-30 parts by weight of xanthan gum, 10-50 parts by weight of hydroxypropyl methylcellulose, 2870-2920 parts by weight of cane sugar and a proper amount of banana essence. The crystal provided by the invention has low moisture absorption and good stability. The composition provided by the invention contains the roxithromycin monohydrate crystal, the suspension is in a good condition, the dissolution rate of medicaments is increased, and the bioavailability is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a roxithromycin monohydrate crystal, a preparation method thereof and a composition dry suspension containing the crystal and ambroxol hydrochloride. Background technique [0002] Pulmonary bacterial infection is a common and frequently-occurring disease of the respiratory system. The main clinical manifestations are cough and expectoration, and antibiotics are usually used for treatment. However, in some cases of bacterial respiratory tract infection with a large amount of sputum, although antibiotics are used reasonably, sometimes the desired curative effect cannot be obtained. The reason may be related to the unobstructed drainage of sputum. The lung is a highly perfused organ. Generally speaking, the concentration of antibacterial drugs in the lung is similar to that in plasma. However, the blood is difficult to perfuse in the abscess cavity and bronchial secretions...

Claims

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Application Information

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IPC IPC(8): C07H17/08C07H1/06A61K31/7048A61K31/137A61K9/16A61P31/04A61P11/00A61P11/06A61P11/02A61P11/08
Inventor 陈雨牛洪芬刘东昌
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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