CN1390550A - Freeze-dried minocycline hydrochloride powder injection and its preparing process - Google Patents
Freeze-dried minocycline hydrochloride powder injection and its preparing process Download PDFInfo
- Publication number
- CN1390550A CN1390550A CN 02132673 CN02132673A CN1390550A CN 1390550 A CN1390550 A CN 1390550A CN 02132673 CN02132673 CN 02132673 CN 02132673 A CN02132673 A CN 02132673A CN 1390550 A CN1390550 A CN 1390550A
- Authority
- CN
- China
- Prior art keywords
- minocycline hydrochloride
- freeze
- dried
- powder injection
- injection
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- WTJXVDPDEQKTCV-UHFFFAOYSA-N 4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide;hydron;chloride Chemical compound Cl.C1C2=C(N(C)C)C=CC(O)=C2C(O)=C2C1CC1C(N(C)C)C(=O)C(C(N)=O)=C(O)C1(O)C2=O WTJXVDPDEQKTCV-UHFFFAOYSA-N 0.000 title claims abstract description 25
- 229960002421 minocycline hydrochloride Drugs 0.000 title claims abstract description 25
- 239000000843 powder Substances 0.000 title claims abstract description 18
- 238000002347 injection Methods 0.000 title claims abstract description 16
- 239000007924 injection Substances 0.000 title claims abstract description 16
- 238000000034 method Methods 0.000 title description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 15
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 7
- 238000002360 preparation method Methods 0.000 claims description 16
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 9
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 8
- 239000008176 lyophilized powder Substances 0.000 claims description 8
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 6
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 6
- 239000008215 water for injection Substances 0.000 claims description 6
- 229910052799 carbon Inorganic materials 0.000 claims description 5
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 4
- 229930195725 Mannitol Natural products 0.000 claims description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 4
- 239000000594 mannitol Substances 0.000 claims description 4
- 235000010355 mannitol Nutrition 0.000 claims description 4
- 238000003756 stirring Methods 0.000 claims description 4
- 108010010803 Gelatin Proteins 0.000 claims description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 3
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 3
- 229920000159 gelatin Polymers 0.000 claims description 3
- 239000008273 gelatin Substances 0.000 claims description 3
- 235000019322 gelatine Nutrition 0.000 claims description 3
- 235000011852 gelatine desserts Nutrition 0.000 claims description 3
- 239000000413 hydrolysate Substances 0.000 claims description 3
- 239000012528 membrane Substances 0.000 claims description 3
- 229920002307 Dextran Polymers 0.000 claims description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- 150000007513 acids Chemical class 0.000 claims description 2
- 239000004599 antimicrobial Substances 0.000 claims description 2
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 210000004907 gland Anatomy 0.000 claims description 2
- 239000008103 glucose Substances 0.000 claims description 2
- 229910052500 inorganic mineral Inorganic materials 0.000 claims description 2
- FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 claims description 2
- 239000004310 lactic acid Substances 0.000 claims description 2
- 235000014655 lactic acid Nutrition 0.000 claims description 2
- 239000011707 mineral Substances 0.000 claims description 2
- 150000007524 organic acids Chemical class 0.000 claims description 2
- 239000011780 sodium chloride Substances 0.000 claims description 2
- 239000001117 sulphuric acid Substances 0.000 claims description 2
- 235000011149 sulphuric acid Nutrition 0.000 claims description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 230000000844 anti-bacterial effect Effects 0.000 abstract description 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract description 2
- 239000001301 oxygen Substances 0.000 abstract description 2
- 229910052760 oxygen Inorganic materials 0.000 abstract description 2
- 238000005516 engineering process Methods 0.000 description 4
- 241000606161 Chlamydia Species 0.000 description 2
- 241000191940 Staphylococcus Species 0.000 description 2
- 230000003115 biocidal effect Effects 0.000 description 2
- 238000011031 large-scale manufacturing process Methods 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- 241000588624 Acinetobacter calcoaceticus Species 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 241000192125 Firmicutes Species 0.000 description 1
- 241000589565 Flavobacterium Species 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 206010048723 Multiple-drug resistance Diseases 0.000 description 1
- 241000589540 Pseudomonas fluorescens Species 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000035622 drinking Effects 0.000 description 1
- 239000003651 drinking water Substances 0.000 description 1
- 235000020188 drinking water Nutrition 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 210000003238 esophagus Anatomy 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000010792 warming Methods 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
A freeze dried minocycline hydrochloride powder as antibacterial injection is prepared from minocycline hydrochloride (0.05-10 wt.portions), freeze dried power supporting agent (10-100) and pH regulator. Its advantages are broad antibacterial sprectrum, high stability to light, heat, oxygen and water, and no pollution.
Description
Technical field:
The invention belongs to broad spectrum antibiotic, the preparation method of particularly a kind of freeze-dried minocycline hydrochloride powder injection and this injection.
Background technology:
Other microbial diseases such as inflammation that gram positive bacteria and gram negative bacteria cause and multiple drug resistance staphylococcus, chlamydia, pseudomonas fluorescens, Flavobacterium, health is caused very big harm, and the patient with severe symptoms often is difficult to treatment with other class antimicrobial drug, minocycline hydrochloride is powerful broad-spectrum antibiotic, and multiple fastbacteria is had good antibacterial ability.This product preparation is a tablet at present, and compared following shortcoming with injectable powder: 1, onset is slow in the tablet use; 2, has extremely strong gastrointestinal reaction; 3, require great quantity of water drinking; 4, range of application is narrow, and tablet is difficult to swallow to having swallowed the obstacle patient, is difficult for treatment in time.
Summary of the invention;
The object of the present invention is to provide a kind ofly to stable performances such as light, heat, oxygen, water, pollution-free, and be convenient to operation, transportation and storage, applied range, be fit to the freeze-dried minocycline hydrochloride powder injection of large-scale production.
Another object of the present invention is to provide the preparation method of this injection.
The object of the present invention is achieved like this: the present invention forms and comprises minocycline hydrochloride, lyophilized powder proppant and pH regulator agent, and parts by weight are: minocycline hydrochloride 0.05-10 part; Lyophilized powder proppant 0-100 part; The pH regulator agent is an amount of.
The present invention is a lyophilized injectable powder, pH value between 0-7.5, between the optimum pH 2-3.5, its purposes widen into: to how sharp drug resistance staphylococcus, chlamydia, the infection that acinetobacter calcoaceticus etc. cause has fine therapeutical effect, but the feeder vessels external administration.Wherein the lyophilized powder proppant is the water solublity proppant, and is soluble in water, and dissolving rapidly is selected from mannitol, glucose, NaCl, dextran, gelatin hydrolysate in clinical use.Osmotic pressure regulator refers to mineral acids such as hydrochloric acid, sulphuric acid, phosphoric acid, organic acid such as acetic acid, lactic acid.
The preparation method of freeze-dried minocycline hydrochloride powder injection provided by the invention is: get recipe quantity minocycline hydrochloride and lyophilized powder proppant and add water for injection, stirring makes dissolving, transfer pH to proper range with the pH regulator agent, the pin activated carbon that adds 0.1%～1% (W/V), filter de-carbon, degerming, after-teeming is penetrated water to capacity, crosses the 0.2um microporous filter membrane, after measuring content, fill; At first pre-freeze is incubated 1～5 hour to-50 ℃～-35 ℃, and evacuation in 15～30 hours, rises to temperature-10～-3 ℃, at 2～10 hours temperature is risen 15～50 ℃ again, continues to keep 3～10 hours, and gland promptly.
The present invention is with the injectable sterile powder of lyophilization principle preparation compared with prior art, is lyophilized injectable powder, and pH value has the following advantages between 0～7: be convenient to operation, be fit to large-scale production; The north and extremely frigid zones transportation in winter and storage problem have been solved; Solved esophagus by obstacle person medication.Shortened drug effect onset time.Reduced amount of drinking water.Reduced volume and weight, reduced the cost of transportation of process of operation greatly with dose product.Applied range, but feeder vessels external administration.
The specific embodiment: be described in further detail the present invention below by embodiment
Embodiment 1:
(1) preparation prescription:
Minocycline hydrochloride 108g
Mannitol 210g
0.1mol/l hydrochloric acid is an amount of
Water for injection adds to 3000ml
Make 1000
(2) preparation technology: get recipe quantity minocycline hydrochloride and mannitol and add water for injection 2500ml, stirring and dissolving, transfer pH2.0～3.5 with 0.1ml/l hydrochloric acid, add solution amount 0.1% pin activated carbon, stirring at room 15min filters after-teeming and penetrates water to 3000ml, cross the 0.2um microporous filter membrane, after measuring content, fill in the 7ml glass tube vial, every 3ml.After fill is good, insert in the freezer dryer, reduce earlier temperature, be incubated 2 hours to-45 ℃, evacuation then, and, after temperature reaches-5 ℃, be warming up to 25 ℃ by 5 ℃/hour by about 2 ℃ of/hour intensifications, and be incubated 2 hours, add plug, Zha Gai, quality inspection is cased.
Embodiment 2:
(1) preparation prescription:
Minocycline hydrochloride 108g
The intoxicated 210g of dextrose
Acetic acid is an amount of
Water for injection adds to 3000ml
Make 1000
(2) preparation technology: with embodiment 1.
Embodiment 3:
Minocycline hydrochloride 108g
Gelatin hydrolysate 210g
Phosphoric acid is an amount of
Water for injection adds to 3000ml
Prepare 1000
Preparation technology: with embodiment 1.
Claims (7)
1, a kind of freeze-dried minocycline hydrochloride powder injection is characterized in that: this lyophilized injectable powder is formed and is comprised minocycline hydrochloride, lyophilized powder proppant and pH regulator agent, and parts by weight are: minocycline hydrochloride 0.05-10 part; Lyophilized powder proppant 0-100 part; The pH regulator agent is an amount of.
2, freeze-dried minocycline hydrochloride powder injection according to claim 1 is characterized in that this injection belongs to the broad-spectrum antimicrobial drug, but the feeder vessels medicine for external use.
3, according to the preparation method of the described freeze-dried minocycline hydrochloride powder injection of claim 1, it is characterized in that: get recipe quantity minocycline hydrochloride and lyophilized powder proppant and add water for injection 2000ml, stirring makes dissolving, transfer pH to proper range with the pH regulator agent, add the pin activated carbon of 0.1%～1% (W/V), filter de-carbon, degerming, after-teeming is penetrated water to capacity, cross the 0.2um microporous filter membrane, behind the mensuration content, fill; At first pre-freeze is incubated 1～5 hour to-50 ℃～-35 ℃, and evacuation in 15～30 hours, rises to temperature-10～-3 ℃, at 2～10 hours temperature is risen 15～50 ℃ again, continues to keep 3～10 hours, and gland promptly.
4,, it is characterized in that its pH value is between 0.1～7.5 according to claim 1 or 3 described freeze-dried minocycline hydrochloride powder injection and preparation methoies.
5, according to claim 1 or 3 described freeze-dried minocycline hydrochloride powder injection and preparation methoies, it is characterized in that: described lyophilized powder proppant is the water solublity proppant, is selected from mannitol, glucose, NaCl, dextran, lactose, gelatin hydrolysate.
6, freeze-dried minocycline hydrochloride powder injection according to claim 1 and preparation method is characterized in that: described PH regulator is meant mineral acids such as hydrochloric acid, sulphuric acid, phosphoric acid, organic acid such as acetic acid, lactic acid.
7, freeze-dried minocycline hydrochloride powder injection according to claim 4 and preparation method is characterized in that: its optimum pH is between 2.0-3.5.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02132673 CN1390550A (en) | 2002-07-25 | 2002-07-25 | Freeze-dried minocycline hydrochloride powder injection and its preparing process |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02132673 CN1390550A (en) | 2002-07-25 | 2002-07-25 | Freeze-dried minocycline hydrochloride powder injection and its preparing process |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1390550A true CN1390550A (en) | 2003-01-15 |
Family
ID=4746879
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02132673 Pending CN1390550A (en) | 2002-07-25 | 2002-07-25 | Freeze-dried minocycline hydrochloride powder injection and its preparing process |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1390550A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1858488A1 (en) | 2005-03-14 | 2007-11-28 | Wyeth a Corporation of the State of Delaware | Tigecycline compositions and methods of preparation |
| JP2013529201A (en) * | 2010-05-12 | 2013-07-18 | レンペックス・ファーマシューティカルズ・インコーポレイテッド | Tetracycline composition |
| US20160279151A1 (en) * | 2008-03-28 | 2016-09-29 | Paratek Pharmaceuticals, Inc. | Oral and injectable formulations of tetracycline compounds |
-
2002
- 2002-07-25 CN CN 02132673 patent/CN1390550A/en active Pending
Cited By (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9694078B2 (en) | 2005-03-14 | 2017-07-04 | Wyeth Llc | Tigecycline compositions and methods of preparation |
| EP1858488A1 (en) | 2005-03-14 | 2007-11-28 | Wyeth a Corporation of the State of Delaware | Tigecycline compositions and methods of preparation |
| US7879828B2 (en) | 2005-03-14 | 2011-02-01 | Wyeth Llc | Tigecycline compositions and methods of preparation |
| RU2428190C2 (en) * | 2005-03-14 | 2011-09-10 | Вайет | Tigecycline composition and methods for preparing |
| CN102512429A (en) * | 2005-03-14 | 2012-06-27 | 惠氏公司 | Tigecycline compositions and methods of preparation |
| US10588975B2 (en) | 2005-03-14 | 2020-03-17 | Wyeth Llc | Tigecycline compositions and methods of preparation |
| KR101354093B1 (en) * | 2005-03-14 | 2014-01-24 | 와이어쓰 엘엘씨 | Tigecycline compositions and methods of preparation |
| US8975242B2 (en) | 2005-03-14 | 2015-03-10 | Wyeth Llc | Tigecycline compositions and methods of preparation |
| JP2008533146A (en) * | 2005-03-14 | 2008-08-21 | ワイス | Tigecycline composition and method of preparation |
| US9254328B2 (en) | 2005-03-14 | 2016-02-09 | Wyeth Llc | Tigecycline compositions and methods of preparation |
| EP3348258A1 (en) * | 2008-03-28 | 2018-07-18 | Paratek Pharmaceuticals, Inc. | Oral and injectable formulations of tetracycline compounds |
| US20160279151A1 (en) * | 2008-03-28 | 2016-09-29 | Paratek Pharmaceuticals, Inc. | Oral and injectable formulations of tetracycline compounds |
| US9278105B2 (en) | 2010-05-12 | 2016-03-08 | Rempex Pharmaceuticals, Inc. | Tetracycline compositions |
| US9744179B2 (en) | 2010-05-12 | 2017-08-29 | Rempex Pharmaceuticals, Inc. | Tetracycline compositions |
| US9084802B2 (en) | 2010-05-12 | 2015-07-21 | Rempex Pharmaceuticals, Inc. | Tetracycline compositions |
| JP2013529201A (en) * | 2010-05-12 | 2013-07-18 | レンペックス・ファーマシューティカルズ・インコーポレイテッド | Tetracycline composition |
| US11944634B2 (en) | 2010-05-12 | 2024-04-02 | Melinta Subsidiary Corp. | Tetracycline compositions |
| US12161656B2 (en) | 2010-05-12 | 2024-12-10 | Melinta Subsidiary Corp. | Tetracycline compositions |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN100560061C (en) | A kind of lornoxicam freeze-dried powder injection and preparation method thereof | |
| CN101654529A (en) | Preparation method and application of chitosan and/or metal composite of chitosan derivative | |
| CN101472560B (en) | Medicinal composition for treating burns and preparation method thereof | |
| JP2006516988A (en) | Pharmaceutical composition comprising an active agent and chitosan for sustained drug release or mucoadhesion | |
| CN112980003A (en) | Natural polysaccharide based antibacterial hydrogel, preparation method and application | |
| CN1593385A (en) | Gel capable of injecting temperature sensitive complex and its preparation method | |
| CN105837837B (en) | A kind of preparation method of the medical chitosan temperature-sensitive hydrogel containing nano silver | |
| CN114478834A (en) | A kind of guanidine-based hyaluronic acid antibacterial polymer and its preparation method and application | |
| CN112386572B (en) | Gamithromycin injection and preparation method thereof | |
| CN1390550A (en) | Freeze-dried minocycline hydrochloride powder injection and its preparing process | |
| CN103585109A (en) | Cefquinome liposome and preparation method thereof | |
| CN104586899B (en) | A kind of aerosol and preparation method thereof for treating bedsore | |
| CN115926200A (en) | Preparation method and application of enzyme-catalyzed double-crosslinked polymer composite hydrogel material | |
| CN107441494B (en) | Chitosan oligosaccharide and antibiotic with antibacterial film activity and application thereof | |
| CN114456239A (en) | Shengtaisu and external antibacterial peptide gel preparation and application prepared therefrom | |
| CN1569366A (en) | Nano-silver aqueous solution preparation and its preparation method, use and using method | |
| CN1439629A (en) | Laevo potassium aspartate material and preparation therefrom and preparing method thereof | |
| CN1919170A (en) | Colloid pectin bismuth dry suspensoid and its preparing process | |
| WO2021169075A1 (en) | Injectable and antibacterial bifunctional hydrogel, preparation method therefor, and application thereof | |
| CN101744776A (en) | Minocycline hydrochloride freeze-drying powder injection and preparation method thereof | |
| CN1111411C (en) | Antibacterial clindamycin phosphate powder injection and its preparing process | |
| CN111905058A (en) | Pharmaceutical composition for skin mucosa nursing and wound repair and preparation method thereof | |
| CN1843358A (en) | Ketoconazole eye drops and fabricating method thereof | |
| CN100493610C (en) | Composition of sodium fusidafe for injection and preparing method thereof | |
| CN1732975A (en) | Prescription of compound electrolyte drug for injection and method for preparing the same |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |