CN101347406A - Injection with high-content praziquantel and method of preparing the same - Google Patents
Injection with high-content praziquantel and method of preparing the same Download PDFInfo
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- CN101347406A CN101347406A CNA2008100459040A CN200810045904A CN101347406A CN 101347406 A CN101347406 A CN 101347406A CN A2008100459040 A CNA2008100459040 A CN A2008100459040A CN 200810045904 A CN200810045904 A CN 200810045904A CN 101347406 A CN101347406 A CN 101347406A
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Abstract
The invention discloses a high-content praziquantel injection and a preparation method thereof. The high-content praziquantel injection is prepared by using the following components with the percentages: 20-30% (W/V) of praziquantel, 10-15% (V/V) of benzyl alcohol, 20-70% (V/V) of vegetable oil or ethyl oleate, 20-70% (V/V) of benzyl benzoate or ethyl lactate, and respectively 0.02%-0.5% (W/V) of antioxidants BHA (butylhydroxytoluene) and BHT (butylated hydroxytoluene). The preparation method comprises the following steps: a certain amount of the benzyl alcohol is weighed, put into a liquid preparation tank, heated to the temperature of 60-80 DEG C, and added with the BHA and the BHT, stirred for dissolution; after the praziquantel is added and stirred until dissolution, the temperature of the solution in the liquid preparation tank is kept at 60-80 DEG C, and then one or two solvents of vegetable oil, ethyl oleate, benzyl benzoate and ethyl lactate are added, stirred, dissolved to fixed extent, after that, the solution is stirred for 20 minutes, filtrated by a 0.8mum filtration membrane, and filled in a 10ml ampoule and sterilized for 30 minutes under the condition of 100 DEG C, thus the high-content praziquantel injection is prepared. When the high-content praziquantel injection is clinically used for preventing and treating sheep coenosis and other taeniasis, the effect is good. The high-content praziquantel injection solves the disavantages of large dose in clinical use, inconvenient injection and great irritation at muscles existing in low-content praziquantel injection.
Description
Technical field
The invention belongs to the veterinary medicine technical field, relate generally to the anti-parasite medicine for animal use thing, is a kind of veterinary antiparasitic injection that contains high-content praziquantel and preparation method thereof.
Background technology
Praziquantel chemistry 2-cyclohexyl formoxyl-1,2,3,6,7 by name, 11b-six hydrogen-4H-pyrazine is [2,1-α] isoquinolin-4-ketone, English name PRAZIQUANTEL, CAS No.55268-74-, molecular formula C19H24N202, molecular weight 312.41 also.Its character of praziquantel is colourless, odorless, flavor bitter in the mouth, and outward appearance is a crystalline powder, and character is very stable under normal condition, and is slightly water-soluble, dissolves in ethapon.
The mechanism of action: what explain at present is that this medicine can hinder the picked-up of polypide to glucose, lactic acid is produced reduce, and has increased the consumption of polypide to glycogen simultaneously, makes paralysis after the rapid spasm of polypide muscle and excretes, and curative effect is rapid.Be a New-type wide-spectrum, efficient, lower toxicity anti-parasite medicine.Be mainly used in the treatment and the prevention of parasitic infection such as multiple trematodiasis, cestode and proscolex.To schistosomiasis japanica, clonorchiasis sinensis, paragonimiasis westermani and various taeniasiss etc. all has good effect.Because praziquantel also has killing effect to cercaria, miracidium, so also be used to prevent schistosomicide and treatment cerebral cysticercosis.China is synthetic and begin test and be applied to clinically in 1977, and nineteen eighty-two formally puts on market.Since the praziquantel listing,, become the main medicine of treatment schistosomicide and multiple parasitic disease very soon because of characteristics such as it are efficient, low toxicity, parasiticide spectrum are wide.
The Droncit that uses at present on the veterinary clinic mainly contains tablet, slow release rod etc., and tablet oral administration post-absorption is rapid, but duration of efficacy is shorter, only is 2-4 hour, the clinical repetitively administered that needs.About the development of its injection, Liu Enyong (2001) report, the toxicity size of praziquantel injection has much relations with its choice of Solvent, and the clinical using dosage of low content praziquantel injection is bigger, and inconvenience during injection is also big to the zest of muscle.Therefore, seek good to the praziquantel dissolubility, the bland solvent of muscular tissue is prepared the praziquantel injection will have crucial meaning clinical treatment.On documents, immediate with the technology of the present invention is Chinese patent CN200810017374.9 number " a kind of long-acting praziquantel slow releasing injection and preparation method thereof " document; But the disclosed purpose of this documents, proportioning component all have distinctive different with the present invention.
Summary of the invention
According to above-mentioned technical deficiency and the defective that veterinary clinic occurs, the purpose of this invention is to provide a kind of good to the praziquantel dissolubility, be a kind of injection with high-content praziquantel and preparation method thereof to little, the clinical solvent easy to use of muscular tissue zest.
The technology solution that reaches the said purpose of the present invention is as follows:
A kind of injection with high-content praziquantel and preparation method thereof, it is characterized in that injection is formulated by following percentage ratio component: concrete component content is praziquantel 20-30% (W/V), benzyl alcohol is 10-15% (V/V), vegetable oil or ethyl oleate 20%-70% (V/V), benzyl benzoate or ethyl lactate are 20%-70% (V/V), and antioxidant BHA (butylated hydroxyarisol), BHT (di-tert-butyl hydroxy-methylbenzene) are respectively 0.02%-0.5% (W/V).
Described a kind of injection with high-content praziquantel and preparation method thereof is characterized in that with the solvent more than 2 kinds or 2 kinds in the vegetable oil, ethyl oleate, benzyl benzoate, ethyl lactate, benzyl alcohol as the injection solvent, wherein benzyl alcohol be must solvent.
Described a kind of injection with high-content praziquantel and preparation method thereof is characterized in that selected vegetable oil can be any one of Semen Maydis oil, Oleum Arachidis hypogaeae semen, Oleum Brassicae campestris, Oleum sesami, soybean oil, Oleum Gossypii semen.
Described a kind of injection with high-content praziquantel and preparation method thereof, its feature also comprises the steps: to take by weighing a certain amount of benzyl alcohol in the dosing cylinder, by being steam heated to 60-80 ℃, add BHA (butylated hydroxyarisol) and BHT (di-tert-butyl hydroxy-methylbenzene), with 300-500r/min speed stirring and dissolving, after adding the praziquantel stirring and dissolving again, keep the interior solution temperature of its dosing cylinder at 60-80 ℃, and then adding vegetable oil (Semen Maydis oil, Oleum Arachidis hypogaeae semen, Oleum Brassicae campestris, Oleum sesami, soybean oil, Oleum Gossypii semen any one), ethyl oleate, benzyl benzoate, a kind of or two kinds of stirring solvent dissolvings and fixed molten in the ethyl lactate, 20 minutes postcooling are continued to stir to room temperature in fixed molten back, solution is by plate filter and with behind the 0.8um membrane filtration, adopt the packing of 10ml peace bottle with wire drawing potting machine, by flowing steam sterilization 30min under 100 ℃ of conditions of high-pressure steam sterilizing pan, cooling back packing.
Best component proportioning: praziquantel 25% (W/V), benzyl alcohol are 13% (V/V), and vegetable oil 30% (V/V), benzyl benzoate are 30% (V/V); Antioxidant is BHA and BHT mixture, is respectively 0.02% (W/V) and 0.05% (W/V).
In order to solve foregoing problems and to reach the present invention's purpose, according to the research to the praziquantel pharmaceutical properties, the present invention adopts benzyl alcohol, vegetable oil and benzyl benzoate etc. to prepare the high concentrate formulation of praziquantel as solvent.Experimental result shows that this injection is without any side effects and zest in clinical regulation dosage scope, clinical prevention and treatment Medulla caprae seuovis coenurosis and other taeniasis of being used for, and it is respond well.
Clinical test results shows: be used for the infection and the treatment of monesiosis, clinical recommended dose is the intramuscular injection of 20mg/kg body weight, and clinical cure rate is 100%; The clinical recommended dose of goat natural infection cenurus cerebralis is the intramuscular injection of 40mg/kg body weight, and clinical cure rate is 89.7%; Effective percentage 100%.
The specific embodiment
Provide specific embodiment and test routine below to further specify component of injection with high-content praziquantel disclosed by the invention and preparation method thereof.
Symbol description: W/V mass/volume percentage concentration %, V/V concentration expressed in percentage by volume %, BHA butylated hydroxyarisol, BHT di-tert-butyl hydroxy-methylbenzene.
Example 1: get benzyl alcohol 13L and join in the dosing cylinder, be steam heated to 60-80 ℃, add BHA (butylated hydroxyarisol) 0.02kg and BHT (di-tert-butyl hydroxy-methylbenzene) 0.03kg respectively, with 300-500r/min speed stirring and dissolving, add praziquantel 20kg again, after the stirring and dissolving, keep the interior solution temperature of its dosing cylinder at 60-80 ℃, and then adding benzyl benzoate 40L, stirring and dissolving adds ethyl lactate 20L, stirring and dissolving again, fixed molten with ethyl lactate at last to 100L, 20 minutes postcooling are continued to stir to room temperature in fixed molten back, and solution adopts the packing of 10ml peace bottle by plate filter and with behind the 0.8um membrane filtration with wire drawing potting machine, by flowing steam sterilization 30min under 100 ℃ of conditions of high-pressure steam sterilizing pan, cooling back packing.
Example 2: get benzyl alcohol 15L and join in the dosing cylinder, be steam heated to 60-80 ℃, add BHA (butylated hydroxyarisol) 0.02kg and BHT (di-tert-butyl hydroxy-methylbenzene) 0.03kg respectively, with 300-500r/min speed stirring and dissolving, add praziquantel 25kg again, after the stirring and dissolving, keep the interior solution temperature of its dosing cylinder at 60-80 ℃, and then adding benzyl benzoate 35L, stirring and dissolving adds soybean oil 20L, stirring and dissolving again, fixed molten with soybean oil at last to 100L, 20 minutes postcooling are continued to stir to room temperature in fixed molten back, and solution adopts the packing of 10ml peace bottle by plate filter and with behind the 0.8um membrane filtration with wire drawing potting machine, by flowing steam sterilization 30min under 100 ℃ of conditions of high-pressure steam sterilizing pan, cooling back packing.
Example 3: get benzyl alcohol 15L and join in the dosing cylinder, be steam heated to 60-80 ℃, add BHA (butylated hydroxyarisol) 0.05kg and BHT (di-tert-butyl hydroxy-methylbenzene) 0.03kg respectively, with 300-500r/min speed stirring and dissolving, add praziquantel 30kg again, after the stirring and dissolving, keep the interior solution temperature of its dosing cylinder at 60-80 ℃, and then adding benzyl benzoate 30L, stirring and dissolving adds Semen Maydis oil 20L, stirring and dissolving again, fixed molten with Semen Maydis oil at last to 100L, 20 minutes postcooling are continued to stir to room temperature in fixed molten back, and solution adopts the packing of 10ml peace bottle by plate filter and with behind the 0.8um membrane filtration with wire drawing potting machine, by flowing steam sterilization 30min under 100 ℃ of conditions of high-pressure steam sterilizing pan, cooling back packing.
Example 4: get benzyl alcohol 15L and join in the dosing cylinder, be steam heated to 60-80 ℃, add BHA (butylated hydroxyarisol) 0.02kg and BHT (di-tert-butyl hydroxy-methylbenzene) 0.03kg respectively, with 300-500r/min speed stirring and dissolving, add praziquantel 25kg again, after the stirring and dissolving, keep the interior solution temperature of its dosing cylinder at 60-80 ℃, and then adding ethyl oleate 50L, stirring and dissolving, fixed molten with ethyl oleate at last to 100L, 20 minutes postcooling are continued to stir to room temperature in fixed molten back, and solution adopts the packing of 10ml peace bottle by plate filter and with behind the 0.8um membrane filtration with wire drawing potting machine, by flowing steam sterilization 30min under 100 ℃ of conditions of high-pressure steam sterilizing pan, cooling back packing.
Example 5: get benzyl alcohol 15L and join in the dosing cylinder, be steam heated to 60-80 ℃, add BHA (butylated hydroxyarisol) 0.05kg and BHT (di-tert-butyl hydroxy-methylbenzene) 0.02kg respectively, with 300-500r/min speed stirring and dissolving, add praziquantel 30kg again, after the stirring and dissolving, keep the interior solution temperature of its dosing cylinder at 60-80 ℃, and then adding ethyl oleate 50L, stirring and dissolving, fixed molten with ethyl oleate at last to 100L, 20 minutes postcooling are continued to stir to room temperature in fixed molten back, and solution adopts the packing of 10ml peace bottle by plate filter and with behind the 0.8um membrane filtration with wire drawing potting machine, by flowing steam sterilization 30min under 100 ℃ of conditions of high-pressure steam sterilizing pan, cooling back packing.
Embodiment 6: best component and proportioning.Getting benzyl alcohol 13L joins in the dosing cylinder, be steam heated to 60-80 ℃, add BHA (butylated hydroxyarisol) 0.02kg and BHT (di-tert-butyl hydroxy-methylbenzene) 0.05kg respectively, with 300-500r/min speed stirring and dissolving, add praziquantel 25kg again, after the stirring and dissolving, keep the interior solution temperature of its dosing cylinder at 60-80 ℃, and then adding benzyl benzoate 30L, stirring and dissolving adds soybean oil 30L, stirring and dissolving again, fixed molten with soybean oil at last to 100L, 20 minutes postcooling are continued to stir to room temperature in fixed molten back, and solution adopts the packing of 10ml peace bottle by plate filter and with behind the 0.8um membrane filtration with wire drawing potting machine, by flowing steam sterilization 30min under 100 ℃ of conditions of high-pressure steam sterilizing pan, cooling back packing.
Clinical experiment 1: choose by ELISA method early diagnosis and go out 264 of clinical natural infection cenurus cerebralis goat cases, be divided into 3 groups, 88 every group, press 30mg/kg, 40mg/kg, 50mg/kg body weight intramuscular injection 25% praziquantel injection respectively, injected once logotype 2 times in per 3 days.The result shows, is respectively 67.0%, 88.6%, 89.7% by the clinical cure rate after the various dose administration; Effective percentage is respectively 96.6%, 100%, 100%.3 kinds of using dosages are clinical all not to be had any toxicity and takes place, and cures the back and observes clinical no recurrent cases 2 months; Therefore, its clinical recommended dose is the intramuscular injection of 40mg/kg body weight, injects once logotype 2-3 time in per 3 days.
Clinical experiment 2: choose 500 of the goat cases of the clinical natural infection moniezia by microscope inspection diagnosis, be divided into 2 groups, 250 every group, press 20mg/kg, 30mg/kg body weight intramuscular injection 25% praziquantel injection respectively 1 time.Experimental result shows, is 100% by the clinical cure rate after the various dose administration.2 months post-sampling microscopies of administration, clinical no moniezia infects; Therefore, be used for the infection and the treatment of taeniasis, clinical recommended dose is the intramuscular injection of 20mg/kg body weight.
Claims (4)
1, a kind of injection with high-content praziquantel and preparation method thereof, it is characterized in that injection is formulated by following percentage ratio component: concrete component content is praziquantel 20-30% (W/V), benzyl alcohol is 10-15% (V/V), vegetable oil or ethyl oleate are 20%-70% (V/V), benzyl benzoate or ethyl lactate are 20%-70% (V/V), and antioxidant BHA (butylated hydroxyarisol), BHT (di-tert-butyl hydroxy-methylbenzene) are respectively 0.02%-0.05% (W/V).
2, a kind of injection with high-content praziquantel according to claim 1 and preparation method thereof, it is characterized in that with the solvent more than 2 kinds or 2 kinds in the vegetable oil, ethyl oleate, benzyl benzoate, ethyl lactate, benzyl alcohol as the injection solvent, wherein benzyl alcohol be must solvent.
3, a kind of injection with high-content praziquantel according to claim 1 and preparation method thereof is characterized in that selected vegetable oil can be any of Semen Maydis oil, Oleum Arachidis hypogaeae semen, Oleum Brassicae campestris, Oleum sesami, soybean oil, Oleum Gossypii semen.
4, a kind of injection with high-content praziquantel according to claim 1 and preparation method thereof is characterized in that comprising the steps:
Take by weighing a certain amount of benzyl alcohol in the dosing cylinder, by being steam heated to 60-80 ℃, add BHA (butylated hydroxyarisol) and BHT (di-tert-butyl hydroxy-methylbenzene), with 300-500r/min speed stirring and dissolving, after adding the praziquantel stirring and dissolving again, keep the interior solution temperature of its dosing cylinder at 60-80 ℃, and then adding vegetable oil (Semen Maydis oil, Oleum Arachidis hypogaeae semen, Oleum Brassicae campestris, Oleum sesami, soybean oil, Oleum Gossypii semen any one), ethyl oleate, benzyl benzoate, a kind of or two kinds of stirring solvent dissolvings and fixed molten in the ethyl lactate, 20 minutes postcooling are continued to stir to room temperature in fixed molten back, solution is by plate filter and with behind the 0.8um membrane filtration, adopt the packing of 10ml peace bottle with wire drawing potting machine, by flowing steam sterilization 30min under 100 ℃ of conditions of high-pressure steam sterilizing pan, cooling back packing.
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103126782A (en) * | 2013-02-26 | 2013-06-05 | 内蒙古农牧业科学院 | Method for treating parasitic disease |
| WO2013143299A1 (en) * | 2012-03-31 | 2013-10-03 | 利邦德制药有限公司 | Lactate-based fulvestrant or fulvestrant derivative oily preparation and preparation method thereof |
| CN103432074A (en) * | 2013-09-09 | 2013-12-11 | 攀枝花市农林科学研究院 | Praziquantel emulsion injection and preparation technology thereof |
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2008
- 2008-08-28 CN CNA2008100459040A patent/CN101347406A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013143299A1 (en) * | 2012-03-31 | 2013-10-03 | 利邦德制药有限公司 | Lactate-based fulvestrant or fulvestrant derivative oily preparation and preparation method thereof |
| US10568890B2 (en) | 2012-03-31 | 2020-02-25 | Xi'an Libang Pharmaceutical Co., Ltd | Lactate-based fulvestrant or fulvestrant derivative oily preparation and preparation method thereof |
| CN103126782A (en) * | 2013-02-26 | 2013-06-05 | 内蒙古农牧业科学院 | Method for treating parasitic disease |
| CN103126782B (en) * | 2013-02-26 | 2016-06-29 | 内蒙古农牧业科学院 | A kind of Therapeutic Method of parasitic disease |
| CN103432074A (en) * | 2013-09-09 | 2013-12-11 | 攀枝花市农林科学研究院 | Praziquantel emulsion injection and preparation technology thereof |
| CN103432074B (en) * | 2013-09-09 | 2015-04-22 | 攀枝花市农林科学研究院 | Praziquantel emulsion injection and preparation technology thereof |
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Open date: 20090121 |