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Preparation method for doxycycline modified release pellet and preparation

A technology of doxycycline and doxycycline hydrochloride, which is applied in the field of preparation of doxycycline modified-release pellet preparations, can solve the problems of reduced bioavailability, stimulation of the upper digestive tract, reduced bioavailability and the like

Inactive Publication Date: 2014-09-17
天津新济复兴药业科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Doxycycline hydrochloride is bitter in taste and has a strong irritating effect on the upper digestive tract. Since the original oral dosage form of doxycycline is ordinary tablets and capsules, it has a strong irritating effect on the gastrointestinal tract, so its clinical application is limited. Therefore, it is necessary to improve the dosage form and reduce irritation, but often followed by a decrease in bioavailability
The best absorption site of doxycycline is the stomach and upper small intestine, which belongs to active absorption, and enteric-coated capsules will undoubtedly reduce its bioavailability

Method used

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  • Preparation method for doxycycline modified release pellet and preparation
  • Preparation method for doxycycline modified release pellet and preparation
  • Preparation method for doxycycline modified release pellet and preparation

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Experimental program
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Effect test

Embodiment Construction

[0022] 1. Influencing factors of modified-release doxycycline hydrochloride pellets

[0023] (1) Effect of pore-forming agent HPMC E15 on release In order to obtain a more ideal drug release rate, a pore-forming agent can be added to the coating material to increase the porosity and permeability of the coating film or matrix to facilitate the regulation of drug release . Under the condition of constant weight gain of polymer coating, the drug release rate increased with the increase of porogen dosage in the coating solution. It can be seen that when the weight gain of the polymer coating is constant, the drug release rate of the pellets can be adjusted in a wide range by adjusting the amount of the porogen.

[0024] In this experiment, HPMC E15 was used as the porogen. On the basis of fixing other prescription factors, the addition amount was 0.4%, 8%, 12%, 14%, 16% or 18% of the mass fraction of the polymer content in the coating solution formulation. , Determination of dru...

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Abstract

The invention discloses a preparation method for a doxycycline modified release pellet and preparation. The method includes the steps of: preparing a doxycycline hydrochloride drug loaded pellet, then mixing the pellet with an appropriate amount of a coating material, applying a fluidized bed to perform coating by bottom spraying, and carrying out drying to obtain the doxycycline hydrochloride modified release pellet; mixing auxiliary materials evenly, and mixing an adhesive with the auxiliary materials uniformly according to a weight ratio of 0.01-1:1; and under a molten state of the adhesive, sticking the auxiliary materials to the surface of the coated pellet prepared form doxycycline by the adhesive so as to obtain a pellet particle; and subjecting the pellet particle to direct tabletting, or mixing the pellet particle with a buffer particle prepared by a conventional method according to a weight ratio of 1:9-9:1 and then conducting tabletting, thus obtaining a pellet tablet. The preparation method provided by the invention is free of layering phenomenon in the tabletting process, and the prepared pellet tablet has uniform quality and drug content. Thus, the method is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular, the invention relates to a preparation method of doxycycline modified-release pellet preparation. Background technique [0002] Doxycycline is a semi-synthetic tetracycline antibiotic with strong and long-acting characteristics. Both in vivo and in vitro tests have shown that it has good antibacterial effects on Gram-positive and negative bacteria. It is mainly used to treat sensitive Gram-positive bacteria. Upper respiratory tract infections, tonsillitis and senile chronic bronchitis caused by cocci and gram-negative bacilli are also used to treat cholera, typhus, scrub typhus, mycoplasma pneumonia, etc., and to prevent falciparum malaria and leptospirosis infections. It is highly sensitive to mycoplasma, chlamydia and rickettsia, and has inhibitory effect on a variety of periodontal bacteria. At the same time, it can also inhibit the activity of collagenase and directly promote...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/65A61K47/38A61P31/04A61P33/06A61P33/02
Inventor 崔景柏吴传斌梁华辉张乃军
Owner 天津新济复兴药业科技有限公司
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