CN104042585B - A kind of oral formulations of Tinidazole - Google Patents
A kind of oral formulations of Tinidazole Download PDFInfo
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- CN104042585B CN104042585B CN201410222517.5A CN201410222517A CN104042585B CN 104042585 B CN104042585 B CN 104042585B CN 201410222517 A CN201410222517 A CN 201410222517A CN 104042585 B CN104042585 B CN 104042585B
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- tinidazole
- controlled release
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- oral formulations
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Abstract
The present invention provides and can reduce medicining times, maintenance blood concentration is steady, extend effective bacteriocidal concentration to hold time, reduce side effect and compare existing sustained release preparation and can faster reach effective blood drug concentration and release rule more reappearance and uniformity and can reduce to take food and affect, realize a kind of Tinidazole oral formulations that segmentation is taken, this oral formulations is that the controlled release micro pill and plain particles component being made up of controlled release Tinidazole component is mixed with in prescription ratio and forms, described is 60: 40～75: 25 for Tinidazole mass ratio in Tinidazole in nitre oral formulations azoles component and common Tinidazole component.
Description
Technical field
The present invention relates to medicine and preparation method thereof, particularly relate to a kind of Tinidazole oral formulations and preparation method thereof.
Background technology
Tinidazole is white or pale yellow crystals or crystalline powder；Mildly bitter flavor.This product is dissolved in acetone or chloroform,
Slightly soluble in water or ethanol.The fusing point of fusing point this product is 125～129 DEG C.
Tinidazole is often and other anti-aerobic bacterias are medication combined in order to treat the microbial septicemia of various anaerobism, respiratory tract sense
Dye, abdominal cavity pelvic infection, unclean miscarriage, cellulitis etc. can obtain promising result.Tinidazole also can be anti-with aminoglycosides etc.
Raw element combines the POI for preventing Tinidazole surgery colon, operation on rectum, oral surgery and gynemetrics etc..Tinidazole is controlled
Treat the cure rates such as trichomoniasis, giardiasis, amcbiasis up to more than 90%.Drip for treating men and women's urogenital tract hair
Parasitosis；Caused by sensitive anaerobic bacteria (such as other bacteroid of bacteroides fragilis, peptococcus, clostruidium, fusiform bacilarmature etc.)
Infection, such as the respiratory tract infection such as pneumonia, pulmonary abscess, the gynecological infections such as intraperitoneal infects, endometritis, abscess of fallopian tube,
Periodontitis, mouth infection such as pericoronitis etc..For system and the local infection of anaerobic bacteria, as abdominal cavity, gynaecology, surgical wound,
Site infection and septicemia, enteron aisle or urogenital tract trichomoniasis, the giardiasis such as skin soft tissue, lung, thoracic cavity
And enteron aisle and hepatic amebiasis.
Summary of the invention
The present invention provide can reduce medicining times, maintain blood concentration steadily, extend effective bacteriocidal concentration and hold time, drop
Low side effect and compare existing sustained release preparation and can faster reach effective blood drug concentration and release rule more reappearance with consistent
Property and can reduce feed impact, realize a kind of Tinidazole oral formulations of taking of segmentation, special one Tinidazole controlled release preparation
And preparation method thereof.
The present invention solves the technical scheme that above-mentioned technical problem used: a kind of Tinidazole oral formulations, this oral system
Agent is that the controlled release micro pill and plain particles component being made up of controlled release Tinidazole component is mixed with in prescription ratio and forms；
In above-mentioned Tinidazole oral formulations component in Tinidazole and common Tinidazole component Tinidazole mass ratio be 60: 40～
75∶25；
By mass percentage, Tinidazole is 69.4% to above-mentioned controlled release Tinidazole component, filler is 14.2%, live in surface
Property agent is 0.35%, pH adjusting agent is 1.5%, adhesive is 0.5%, separation layer coating material is 0.9%, release controlling coating material
Be 8.3%, pore-foaming agent be 0.3%, plasticizer be 0%, protective layer coating material be 1.4%, antiplastering aid be 3.1%；
By mass percentage, Tinidazole is 44.0% to above-mentioned plain particles Tinidazole component, filler is 48.8%, table
Face activating agent is 0.6%, pH adjusting agent is 2.1%, disintegrant is 4.2%, lubricant is 0.3%.
For optimizing technique scheme, the measure taked also includes:
Above-mentioned Tinidazole controlled release preparation, the controlled release micro pill being made up of controlled release Tinidazole component and plain particles Both tinidazole
Dividing mass ratio is 35: 65～50: 50.
Above-mentioned controlled release Tinidazole component, described filler is microcrystalline cellulose, Macrogol 6000, lactose, phosphoric acid
One or more mixing in hydrogen calcium, sucrose, Icing Sugar, dextrin, mannitol, sorbierite, xylitol；
Described surfactant is in double phenmethylol, lauryl sodium sulfate, dodecyl sodium sulfate, perfluorooctane sulfonate
One or more mixing；
Described pH adjusting agent is citric acid, tartaric acid, fumaric acid, malic acid, butanedioic acid, maleic acid, glutamic acid, almond
One or more combination in acid；
Described adhesive is PVP, HPMC, starch, hydroxypropyl cellulose, hydroxy ethyl cellulose
In one or more mixing；
Described separation layer coating material be the one in hydroxypropyl methyl cellulose, hydroxypropyl cellulose, PVP or
More than one mixing；
Described release controlling coating material is that polyacrylic resin, ethyl cellulose, cellulose acetate, ethylene-vinyl acetate are common
One or more mixing in polymers；
Described pore-foaming agent be in lactose, polyethylene glycol, PVP, hydroxypropyl cellulose one or more mix
Close；
Described plasticizer be in triethyl citrate, triacetyl glycerine, polyethylene glycol one or more mix
Close；
Described protective layer coating material be the one in hydroxypropyl methyl cellulose, hydroxypropyl cellulose, PVP or
More than one mixing；
Described antiplastering aid is one or more mixing in talcum powder, magnesium stearate, glycerin monostearate.
Above-mentioned plain particles Tinidazole component, described filler is starch milk saccharide complex, pregelatinized starch, crystallite
One or more mixing in cellulose, lactose, sorbierite, calcium monohydrogen phosphate；
Described surfactant is in double phenmethylol, lauryl sodium sulfate, dodecyl sodium sulfate, perfluorooctane sulfonate
One or more mixing；
Described pH adjusting agent is citric acid, tartaric acid, fumaric acid, malic acid, butanedioic acid, maleic acid, glutamic acid, almond
One or more combination in acid；
Described disintegrant is Ac-Di-Sol, PVPP, sodium carboxymethyl starch, superfine silica gel powder, low
Replace one or more mixing in HPMC；
Described lubricant be the one in magnesium stearate, zinc stearate, talcum powder, lauryl sodium sulfate or one with
Upper mixing.
Above-mentioned Tinidazole controlled release preparation, a diameter of 200 μm of controlled release micro pill～the diameter of 800 μm, preferably controlled release micro pill
It is 300 μm～a diameter of 400 μm of 700 μm, more preferably controlled release micro pill～600 μm；In plain particles Tinidazole component at least
The mixture of powders granularity of 65% is 100 μm～300 μm, and the mixture of powders granularity of preferably at least 80% is 100 μm～300 μ
m。
Present invention also offers the preparation method of a kind of Tinidazole controlled release preparation, the method comprises the following steps:
1), by controlled release Tinidazole constituent mass percentages, by Tinidazole be 69.4%, filler be 14.2%, surface
Activating agent is 0.35%, pH adjusting agent is 1.5%, adhesive is 0.5% to mix, and adds suitable quantity of water and prepares softwood；
2) the extrusion spheronization pellet processing machine of 0.4 millimeter of extrusion orifice plate, is used by described 1) the softwood extrusion spheronization system prepared
Standby micropill, and by micropill drying, sieve after to collect 35-60 mesh micropill standby；
3), respectively separation layer coating material, release controlling coating material, protective layer coating material dissolved with suitable quantity of water or divide
Dissipate, carry out separation layer the most successively with fluid bed, controlled release layer, protective layer are coated to obtain Tinidazole controlled release micro pill；
4), by plain particles Tinidazole constituent mass percentages, weigh Tinidazole be 44.0%, filler be
48.8%, surfactant be 0.6%, pH adjusting agent be 2.1%, disintegrant be 4.2%, lubricant be 0.3%, add for nitre
Azoles controlled release micro pill, mixes, tabletted, optionally with tablet thin film coating agent attractive in appearance, tablet is carried out film coating, to obtain final product
Tinidazole controlled release preparation.
Compared with prior art, the Tinidazole controlled release preparation of the present invention is the controlled release micro pill being made up of controlled release Tinidazole component
With plain particles Tinidazole component in the tablet of prescription ratio mixing compacting, in controlled release Tinidazole component, Tinidazole is with common
In particle Tinidazole component, Tinidazole mass ratio is 60: 40～75: 25；In the acetate buffer of pH5.5,15 minutes interior
Release is not less than 25%.And this controlled release preparation release rule more reappearance and uniformity, can reduce medicining times, maintenance
Blood concentration is steady, extend effective bacteriocidal concentration holds time, reduce side effect and compare existing sustained release preparation energy can faster reach
To effective blood drug concentration, and feed impact can be reduced, it is achieved segmentation is taken.
Detailed description of the invention
Below in conjunction with embodiment, the present invention will be further described.
Embodiment 1:
(1) controlled release Tinidazole micropill prescription
(2) common Tinidazole micropill prescription
| Component function | Ingredient names | Consumption (g) |
| Main ingredient | Tinidazole | 315 |
| Filler | Starch milk saccharide complex | 200 |
| Filler | Pregelatinized starch | 150 |
| Surfactant | Perfluorooctane sulfonate | 4 |
| PH adjusting agent | Malic acid | 15 |
| Disintegrant | Ac-Di-Sol | 20 |
| Disintegrant | Superfine silica gel powder | 10 |
| Lubricant | Magnesium stearate | 2.5 |
Prepare tablet mixing recipe quantity
| Ingredient names | Consumption (g) |
| Controlled release Tinidazole micropill | 509.4 |
| Common Tinidazole micropill | 487.2 |
| Amount to | 996.6 |
It is pressed into 1000.
By the concrete preparation method of above prescription:
1), by pastille micropill each recipe quantity mixing supplementary material in controlled release Tinidazole micropill prescription, add suitable quantity of water, prepare soft
Material；
2), use the extrusion spheronization pellet processing machine of 0.4mm extrusion orifice plate that prepared by above-mentioned softwood extrusion spheronization pastille micropill, dry
Dry, the collection 3560 mesh pastille micropills that sieve are standby；
3), weigh HPMC by separation layer recipe quantity, add water be configured to 3% solution, add talcum powder, stir；
4), the pastille micropill that fluid bed is above-mentioned is used to pack separation layer；
4), weighing each auxiliary material by controlled release layer recipe quantity, be configured to the coating solution of 25% solid content with water, use fluid bed will
It is surrounded by the pastille micropill bag controlled release layer of separation layer；
5), weigh HPMC by protective layer recipe quantity, add water be configured to 3% solution, add talcum powder, stir, make
With fluid bed by the above-mentioned pastille micropill bag protective layer being surrounded by separation layer, controlled release layer；
6), by above-mentioned being surrounded by separation layer, controlled release layer, the pastille micropill of protective layer be placed in 40 DEG C of baking ovens be dried, aging 24
Hour obtain controlled release Tinidazole micropill；
7), by plain particles Both tinidazole divide recipe quantity to weigh each supplementary material, add the controlled release Tinidazole micropill of recipe quantity,
Mix, compressing tablet, film coating, obtain Tinidazole controlled release preparation.
Use Chinese Pharmacopoeia two annex XC the first methods of version in 2010, with pH5.5 acetate buffer 1000ml as dissolution
Medium, rotating speed is 100r/min, measures release, and result is as follows:
| Time (h) | 0.25 | 2 | 4 | 6 | 8 | 12 |
| Release (%) | 40.9 | 67.3 | 82.6 | 89.5 | 93.5 | 98.6 |
The controlled release preparation of the present invention is multiple-unit preparation, in the acetate buffer of pH5.5, and 15 minutes interior releases
It is not less than 25%.This controlled release preparation release rule more reappearance and uniformity, can reduce medicining times, maintain blood concentration to put down
Surely, extend effective bacteriocidal concentration to hold time, reduce side effect and compare existing sustained release preparation faster to reach effective blood medicine dense
Degree, and feed impact can be reduced, it is achieved segmentation is taken.
The foregoing is only presently preferred embodiments of the present invention, not in order to limit the present invention, all spirit in the present invention and
Within principle, any modification, equivalent substitution and improvement etc. made, should be included within the scope of the present invention.
Embodiment 2:
Controlled release Tinidazole micropill prescription
Preparation 1000g micropill, is pressed into 1000.
By above prescription each method the most processed:
1), by pastille micropill each recipe quantity mixing supplementary material in controlled release Tinidazole micropill prescription, add suitable quantity of water, prepare soft
Material；
2), use the extrusion spheronization pellet processing machine of 0.4mm extrusion orifice plate that prepared by above-mentioned softwood extrusion spheronization pastille micropill, dry
Dry, the collection 3560 mesh pastille micropills that sieve are standby；
3), weigh HPMC by separation layer recipe quantity, add water be configured to 3% solution, add talcum powder, stir；
4), the pastille micropill that fluid bed is above-mentioned is used to pack separation layer；
4), weighing each auxiliary material by controlled release layer recipe quantity, be configured to the coating solution of 25% solid content with water, use fluid bed will
It is surrounded by the pastille micropill bag controlled release layer of separation layer；
5), weigh HPMC by protective layer recipe quantity, add water be configured to 3% solution, add talcum powder, stir, make
With fluid bed by the above-mentioned pastille micropill bag protective layer being surrounded by separation layer, controlled release layer；
6), by above-mentioned being surrounded by separation layer, controlled release layer, the pastille micropill of protective layer be placed in 40 DEG C of baking ovens be dried, aging 24
Hour obtain controlled release Tinidazole micropill；
7), compressing tablet, film coating, obtain Tinidazole controlled release preparation.
Embodiment 3:
Below by way of verifying beneficial effects of the present invention:
Verification experimental verification: Tinidazole oral formulations embodiment 1 contrasts with embodiment 2 and 3 vitro release.
Use Chinese Pharmacopoeia two annex XC the first methods of version in 2010, with pH5.5 acetate buffer 1000ml as dissolution
Medium, rotating speed is 100r/min, at the appointed time puts sampling, is measured with high performance liquid chromatograph, measures Tinidazole respectively
Oral formulations embodiment 1 and embodiment 2 and 3 vitro release.Result is shown in table below.
| Time (h) | 0.25 | 2 | 4 | 6 | 8 | 12 |
| Embodiment 1 release (%) | 40.9 | 67.3 | 82.6 | 89.5 | 93.5 | 98.6 |
| Embodiment 2 release (%) | 12.8 | 34.3 | 67.5 | 89.4 | 94.9 | 98.3 |
Result shows: the medicine of the Tinidazole oral formulations embodiment 1 of the present invention is not less than 15 minutes interior releases
25%, and, the medicine of Tinidazole oral formulations embodiment 2 is below 10% 15 minutes interior releases, discharges the most unstable.
Claims (2)
1. a Tinidazole oral formulations, this oral formulations is the controlled release micro pill and plain particles being made up of controlled release Tinidazole component
Component is mixed with in prescription ratio and forms, and in described Tinidazole oral formulations component, Tinidazole replaces in common Tinidazole component
Nitre azoles mass ratio is 60: 40～75: 25；
Described controlled release Tinidazole component is calculated as with preparation 1000g controlled release micro pill dosage:
2. oral formulations as claimed in claim 1, it is characterised in that described plain particles Tinidazole component is by mass percentage
Meter, Tinidazole is 44.0%, filler is 48.8%, surfactant is 0.6%, pH adjusting agent is 2.1%, disintegrant is
4.2%, lubricant is 0.3%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410222517.5A CN104042585B (en) | 2014-05-21 | 2014-05-21 | A kind of oral formulations of Tinidazole |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410222517.5A CN104042585B (en) | 2014-05-21 | 2014-05-21 | A kind of oral formulations of Tinidazole |
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| Publication Number | Publication Date |
|---|---|
| CN104042585A CN104042585A (en) | 2014-09-17 |
| CN104042585B true CN104042585B (en) | 2016-08-24 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201410222517.5A Active CN104042585B (en) | 2014-05-21 | 2014-05-21 | A kind of oral formulations of Tinidazole |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN113230226A (en) * | 2021-05-28 | 2021-08-10 | 丽珠集团丽珠制药厂 | Tinidazole tablet and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1575164A (en) * | 2001-08-29 | 2005-02-02 | 兰贝克赛实验室有限公司 | Controlled release preparation of clarithromycin or tinidazole |
| CN1650972A (en) * | 2004-11-26 | 2005-08-10 | 复旦大学 | Glow release micro pill containing gingko leaf extract and its preparation method |
-
2014
- 2014-05-21 CN CN201410222517.5A patent/CN104042585B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1575164A (en) * | 2001-08-29 | 2005-02-02 | 兰贝克赛实验室有限公司 | Controlled release preparation of clarithromycin or tinidazole |
| CN1650972A (en) * | 2004-11-26 | 2005-08-10 | 复旦大学 | Glow release micro pill containing gingko leaf extract and its preparation method |
Non-Patent Citations (2)
| Title |
|---|
| 替硝唑剂型的研制;刘金虹;《天津药学》;20091231;第21卷(第1期);第50-52页 * |
| 替硝唑口腔缓释膜的研制及临床应用;唐华涛，欧阳子夜;《现代生物医学进展》;20101231;第10卷(第14期);第2735-2736页 * |
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| CN104042585A (en) | 2014-09-17 |
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