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Doxycycline hydrochloride dual-release preparation and preparation method thereof

A doxycycline hydrochloride, double-release technology, applied in the direction of tetracycline active ingredients, pharmaceutical formulations, drug delivery, etc., to achieve the effects of reducing side effects and addiction, improving stability, and improving compliance

Active Publication Date: 2012-07-18
ZHONGSHUAI PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Due to the high fat solubility of doxycycline and its strong penetration into tissues, common preparations of traditional specifications (50mg, 100mg) as a broad-spectrum antibacterial drug can often cause many side effects

Method used

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  • Doxycycline hydrochloride dual-release preparation and preparation method thereof
  • Doxycycline hydrochloride dual-release preparation and preparation method thereof
  • Doxycycline hydrochloride dual-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Doxycycline hydrochloride double-release capsules and preparation method thereof

[0044] First prepare the drug-containing pellet cores according to the formula, prepare immediate-release pellets from the pellet cores, and then prepare delayed-release pellets from the immediate-release pellets, and finally fill the capsules with the immediate-release pellets and the delayed-release pellets in proportion, namely Obtain doxycycline hydrochloride double-release capsules.

[0045] (1) Ball core preparation process

[0046] Ball core prescription: microcrystalline cellulose 640g, doxycycline hydrochloride 177g, 2% (w / w) hydroxypropyl methylcellulose solution 640g.

[0047] Preparation process: pulverize doxycycline hydrochloride and filler microcrystalline cellulose to a certain particle size range, pass through an 80-mesh sieve, mix in a stirring mixer for 30 minutes, add 2% hydroxypropyl methylcellulose solution, Made of soft materials. Turn on the low-temp...

Embodiment 2

[0062] Example 2 Doxycycline hydrochloride double-release capsules and preparation method thereof

[0063] (1) Ball core composition: 640g of microcrystalline cellulose, 177g of doxycycline hydrochloride, 640g of 2% (w / w) povidone solution.

[0064] Preparation process: pulverize doxycycline hydrochloride and microcrystalline cellulose, pass through an 80-mesh sieve, mix in a stirring mixer for 30 minutes, then add povidone solution to make a soft material. Turn on the low-temperature refrigerator and control the temperature at 4-15°C. After 10 minutes, put the soft material into the low-temperature and high-pressure extruder to pass through the sieve plate with a sieve hole of 0.9-1.0mm, and adjust the extrusion speed to 40rpm to form a cylindrical shape with a moderate length. Soft materials are spheronized in a spheronizer at a speed of 1800rpm for 10 minutes to form drug-loaded pellets with uniform particle size. According to the length of the sheared cylinder, the parti...

Embodiment 3

[0072] Example 3 Doxycycline hydrochloride double-release capsules and preparation method thereof

[0073] (1) Pill core composition: 640 g of microcrystalline cellulose, 177 g of doxycycline hydrochloride, 20 g of crospovidone, and 640 g of 2% hydroxypropyl methylcellulose aqueous solution.

[0074] Preparation process: pulverize doxycycline hydrochloride, microcrystalline cellulose and crospovidone, pass through an 80-mesh sieve, mix in a stirring mixer for 30 minutes, add 640g of hydroxypropylmethylcellulose aqueous solution, and make soft material. Turn on the low-temperature refrigerator and control the temperature at 4-15°C. After 10 minutes, put the soft material into the low-temperature and high-pressure extruder and pass through the sieve plate with a size of 0.9-1.0mm. Adjust the extrusion speed to 40rpm to form a medium-length cylindrical shape. The soft material is spheronized in a spheronizer at a speed of 1800rpm for 10 minutes to form drug-loaded pellets with...

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Abstract

The invention belongs to the field of pharmaceutical science, and particularly relates to a doxycycline hydrochloride dual-release preparation and a preparation method thereof. The preparation consists of micropills with different release performance, namely the preparation is formed by mixing 50 to 85 weight percent of quick-release micropill and 50 to 15 weight percent of sustained-release micropill. The preparation method comprises the following steps of: preparing micropill cores according to a formula, and preparing the quick-release micropills by using the micropill cores; preparing thesustained-release micropills by using the quick-release micropills; and filling the quick-release micropills and the sustained-release micropills into capsules in a ratio to obtain doxycycline hydrochloride dual-release capsules. Pharmacokinetic experiments in the dual-release capsule bodies indicate that medicines in the doxycycline hydrochloride dual-release capsules can be released twice when the doxycycline hydrochloride dual-release capsules are taken once every day, and the concentration of two-time peaks is close; the concentration peak of medicines in blood plasma is reduced by a dual-release model, the possibility of side effect is reduced, and the compliance of the administration of patients is improved; and due to the adoption of a new formula and a new process, the difference among batches is reduced, and the stability of samples is improved, so the doxycycline hydrochloride dual-release preparation is suitable for industrial production.

Description

technical field [0001] The invention relates to a doxycycline hydrochloride preparation, in particular to a doxycycline hydrochloride double-release preparation and a preparation method thereof. technical background [0002] Doxycycline hydrochloride is a tetracycline antibiotic with the chemical name 6-methyl-4-(dimethylamino)-3,5,10,12,12a-pentahydroxy-1,11-dioxo-1,4 ,4a,5,5a,6,11,12a-octahydro-2-tetracenecarboxamide hydrochloride hemiethanol hemihydrate, its molecular formula is: C22H25ClN2O8.?C2H6O.?H2O, the molecular weight is 512.94, more hydrochloric acid Cycycline is light yellow or yellow crystalline powder, odorless and bitter. Soluble in water or methanol, slightly soluble in ethanol or acetone, almost insoluble in chloroform. [0003] Doxycycline hydrochloride is a tetracycline antibiotic that has been used clinically for many years. Its pharmacological action mechanism is similar to that of tetracycline, and its antibacterial effect is mainly through the comb...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/58A61K9/62A61K31/65A61P31/04
Inventor 任峰晓邬向东王军
Owner ZHONGSHUAI PHARMA SCI & TECH CO LTD
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