CN1220501C - Eye drop of double rhizoma coptidis - Google Patents

Eye drop of double rhizoma coptidis Download PDF

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Publication number
CN1220501C
CN1220501C CN 02117620 CN02117620A CN1220501C CN 1220501 C CN1220501 C CN 1220501C CN 02117620 CN02117620 CN 02117620 CN 02117620 A CN02117620 A CN 02117620A CN 1220501 C CN1220501 C CN 1220501C
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add
minutes
ethanol
water
stir
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CN1456186A (en
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刘继东
姚东民
高峨
宋长海
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Abstract

The present invention relates to double coptis eye drop, which can be applied to the treatment of ophthalmological viral infection. The double coptis eye drop is composed of two parts: double coptis aseptic powder and eye drop solvent. The medicine components referred in the present invention are made into the eye drop to apply to the treatment of ophthalmological diseases for the first time. The biological availability of the medicine components is improved, and therapeutic effect and medication safety are strengthened. The effective medicine components are baicalin and chlorogenic acid, and the solvent is isoosmotic solution composed of sodium chloride and ethylparaben.

Description

A kind of medicine eye drop of double rhizoma coptidis that is applied to the ophthalmology treatment of viral infections
Affiliated technical field
The middle pharmaceutically active ingredient---SHUANGHUANLIAN---that the present invention relates to is made eye drop first, is applied to the treatment of ophthalmology viral infection, is intended to improve the bioavailability of effective ingredient, increases curative effect and drug safety.
Background technology
At traditional tcm field, before the applicating history of SHUANGHUANLIAN can be traced back to the centuries; In modern age, SHUANGHUANLIAN is first Chinese medicinal formulae of making injectable powder; Its excellent therapeutic effect is extensively confirmed and is approved.But in the application of SHUANGHUANLIAN, following defective is arranged simultaneously: the degeneration of the easy moisture absorption caking of (1), SHUANGHUANLIAN medicated powder influences curative effect and the bioavailability and the drug safety of medicine, so that lose therapeutical effect.(2), apparent therapeutic effect is slow.(3), substep is inhomogeneous in the medicine body, during the ophthalmology illness treatment, adopts injection or oral administration mode, its topical therapeutic DeGrain.Consider from the pharmacokinetics aspect, when ophthalmology illness is treated, injection (comprising quiet notes) and oral administration mode, drug absorption enters behind the blood with blood circulation to the whole body substep, also must see through blood-eye barrier, could arrive the site of action of eye focus, and medicine is circulation time in vivo, also can cause structural change in various degree owing to modes such as oxidation, reduction, decomposition, combinations, finally reaching lesions position, to show bioavailability lower; Adopt the mode that strengthens dosage for reaching comparatively ideal therapeutic effect, the hidden danger of drug safety is then arranged.
Summary of the invention
The present invention makes eye drop with SHUANGHUANLIAN by the method for double pack first, has not only solved the rotten problem of SHUANGHUANLIAN moisture absorption caking, and, solved the unfavorable problem of whole body drug treatment effect.
The medicine eye drop of double rhizoma coptidis that is applied to the ophthalmology treatment of viral infections of the present invention is characterized in that being the double pack form, is made up of with solvent two parts SHUANGHUANLIAN aseptic powder and eye drip respectively, and wherein the SHUANGHUANLIAN aseptic powder contains Flos Lonicerae [with chlorogenic acid (C 16H 18O 9) meter] be 14.0-25.0 milligram/gram; Contain Radix Scutellariae [with baicalin (C 21H 18O 11) meter] be 220.0-292.0 milligram/gram; The eye drip solvent is the aqueous solution that sodium chloride and ethyl hydroxybenzoate are made into, wherein sodium chloride-containing 9.0 mg/ml, contain ethyl hydroxybenzoate 0.5 mg/ml.
The technical solution adopted for the present invention to solve the technical problems is:
One, extract to concentrate the SHUANGHUANLIAN effective ingredient of back preparation, behind low temperature sterilization, cold drying is prepared into sterilized powder, is sub-packed in the plastic bottle that dry heat sterilization and cold wind dry up, and adds a cover the bottle cap of liner sealing gasket, is first moisture preventive measure; The moistureproof aluminium foil bag of outer plastic packaging is second moisture preventive measure.Among the above-mentioned preparation technology, its core technology is: (1) cold drying prepares aseptic fine powder, the dried packing plastic bottle of (2) dry heat sterilization cold wind, the moistureproof bottle cap of (3) sealing gasket, the moistureproof aluminium foil bag of (4) plastic packaging.
Two, medicine and solvent are packed the preparation eye drop respectively, and in ophthalmic remedy, if treat the eye virus infectious disease in the mode of oral or other whole body administrations with SHUANGHUANLIAN, not only dosage is big, and medicine is difficult to pass through blood-eye barrier with the SHUANGHUANLIAN first Application.Make eye drop, topical, amount of application is few, has increased curative effect and drug safety.Among the above-mentioned preparation technology, its core technology is: SHUANGHUANLIAN effective ingredient and eye drip solvent are packed respectively, have guaranteed the stability of effective ingredient.
Three, the useful result of this product is: when solving SHUANGHUANLIAN powder moisture absorption problem, adopt the method for two dose packages to prepare eye drop, when having demonstrated fully the treatment ophthalmology illness, adopt bioavailability height that the local application administering mode of direct eye drip embodied, reduce use amount, increase the advantageous feature of curative effect and drug safety.And, reduce the financial burden that use amount has also reduced the patient.
Embodiment
Eye drop of double rhizoma coptidis
[prescription] Fructus Forsythiae 100g
Flos Lonicerae 50g
Radix Scutellariae 50g
—————————————————
Make 200
Eye drip solvent sodium chloride 9.0g
Ethyl hydroxybenzoate 0.5g
——————————————————
Make 1000ml
[method for making] gets Radix Scutellariae, decocts with water each 1 hour of secondary (8,6 times of amounts), merging filtrate, and filtrate uses 2mol/L hydrochloric acid solution adjust pH to 1.0-2.0.80 ℃ of insulations 30 minutes, left standstill 24 hours, filter, precipitation adds 8 times of amounts of water, stir, with 40% sodium hydroxide solution adjust pH to 6.0-7.0, add equivalent ethanol, stir and make dissolving, filter, filtrate transfers pH to 2.0 in 80 ℃ of insulations 30 minutes with the 2mol/L hydrochloric acid solution, left standstill 12 hours, and filtered, precipitation is washed till pH value to 4.0 with ethanol, add 10 times of amounts of water, stir, to 6.0-7.0, add 0.5% active carbon with 40% sodium hydroxide solution adjust pH, fully stir, 50 ℃ of insulations 30 minutes add after 1-2 doubly measures ethanol and stir, and filter immediately, filtrate is used 2mol/L hydrochloric acid solution adjust pH to 2.0, in 80 ℃ of insulations 30 minutes, left standstill 12 hours, filter, after precipitation is washed with small amount of ethanol, in dry below 60 ℃.
Flos Lonicerae, Fructus Forsythiae extract: Flos Lonicerae, Fructus Forsythiae adds 10 times in water respectively, 8 times of amounts, dipping is after 30 minutes earlier, decoct secondary, each 1 hour, merging filtrate, be concentrated into the clear paste of relative density 1.20-1.25 (70 ℃), be chilled to 40 ℃ and slowly add ethanol, make to contain alcohol amount and reach 75%, fully stir, left standstill 12 hours, the leaching supernatant reclaims ethanol to there not being the alcohol flavor, adds water 3-4 and doubly measures, left standstill 12 hours, the leaching supernatant, being concentrated into relative density is the clear paste of 1.10-1.15 (80 ℃), is chilled to 40 ℃, add ethanol, make the alcohol amount of containing reach 85% and leave standstill more than 12 hours, the leaching supernatant reclaims ethanol to there not being the alcohol flavor.
Get Radix Scutellariae extract, add suitable quantity of water, heating and with 40% caustic lye of soda adjust pH to 7.0 makes dissolving, add above-mentioned Flos Lonicerae, Fructus Forsythiae extract, add water to 200ml, add 0.5% active carbon, keep pH7.0, heat little boiling 15 minutes, cooling filters, and adds to the full amount of water for injection, in 115 ℃ of sterilizations 30 minutes, in 1 week of cold preservation, filter with microporous filter membrane, filtrate concentrates, and lyophilization is distributed into 200, every 60mg tightly seals, promptly.
The preparation of eye drip solvent adds water 1000ml with sodium chloride and ethyl hydroxybenzoate, stirs to make it dissolving, filters with microporous filter membrane, sterilizes 30 minutes for 115 ℃, and cooling is distributed into 200, promptly.
Creativeness of the present invention realizes by clinical, toxicology and pharmacology data, provides in the lump during examination as to substances.
Fig. 1 is an eye drop of double rhizoma coptidis preparation technology flow chart.

Claims (2)

1. a medicine eye drop of double rhizoma coptidis that is applied to the ophthalmology treatment of viral infections is characterized in that being the double pack form, is made up of with solvent two parts SHUANGHUANLIAN aseptic powder and eye drip respectively, and wherein the SHUANGHUANLIAN aseptic powder contains Flos Lonicerae [with chlorogenic acid (C 16H 8O 9) meter] be 14.0-25.0 milligram/gram; Contain Radix Scutellariae [with baicalin (C 21H 18O 11) meter] be 220.0-292.0 milligram/gram; The eye drip solvent is the aqueous solution that sodium chloride and ethyl hydroxybenzoate are made into, wherein sodium chloride-containing 9.0 mg/ml, contain ethyl hydroxybenzoate 0.5 mg/ml.
2. according to the described eye drop of double rhizoma coptidis of claim 1, it is characterized in that SHUANGHUANLIAN aseptic powder wherein prepares by following method: at first get Radix Scutellariae 50 grams, decoct with water secondary, each 1 hour, merging filtrate, filtrate use 2mol/L hydrochloric acid solution adjust pH to 1.0-2.0; 80 ℃ of insulations 30 minutes, left standstill 24 hours, filter, precipitation adds 8 times of amounts of water, stir, with 40% sodium hydroxide solution adjust pH to 6.0-7.0, add equivalent ethanol, stir and make dissolving, filter, filtrate transfers pH to 2.0 in 80 ℃ of insulations 30 minutes with the 2mol/L hydrochloric acid solution, left standstill 12 hours, and filtered, precipitation is washed till pH value to 4.0 with ethanol, add 10 times of amounts of water, stir, to 6.0-7.0, add 0.5% active carbon with 40% sodium hydroxide solution adjust pH, fully stir, 50 ℃ of insulations 30 minutes add after 1-2 doubly measures ethanol and stir, and filter immediately, filtrate is used 2mol/L hydrochloric acid solution adjust pH to 2.0, in 80 ℃ of insulations 30 minutes, left standstill 12 hours, filter, after precipitation is washed with small amount of ethanol, in dry below 60 ℃; Secondly extracting honeysuckle 50 restrains, Fructus Forsythiae 100 grams add 10 times in water respectively, 8 times of amounts, dipping is after 30 minutes earlier, decoct secondary, each 1 hour, merging filtrate, be concentrated into the clear paste of relative density 1.20-1.25, be chilled to 40 ℃ and slowly add ethanol, make to contain alcohol amount and reach 75%, fully stir, left standstill 12 hours, the leaching supernatant reclaims ethanol to there not being the alcohol flavor, adds water 3-4 and doubly measures, left standstill 12 hours, the leaching supernatant is concentrated into the clear paste that relative density is 1.10-1.15, is chilled to 40 ℃, add ethanol, make the alcohol amount of containing reach 85% and leave standstill more than 12 hours, the leaching supernatant reclaims ethanol to there not being the alcohol flavor; Get Radix Scutellariae extract once more, add entry, the heating and with 40% caustic lye of soda adjust pH to 7.0, make dissolving, add above-mentioned Flos Lonicerae, Fructus Forsythiae extract, add water to 200ml, add 0.5% active carbon, keep pH7.0, heat little boiling 15 minutes, cooling, filter, add to the full amount of water for injection, in 115 ℃ of sterilizations 30 minutes, 1 week of cold preservation filters with microporous filter membrane, and filtrate concentrates, lyophilization is distributed into 200, every 60mg; Wherein the eye drip solvent prepares by following method: sodium chloride 9.0 gram and ethyl hydroxybenzoate 0.5 gram are added water 1000ml, stir and make it dissolving, filter with microporous filter membrane, 115 ℃ of sterilizations 30 minutes are cooled off, and are distributed into 200, promptly.
CN 02117620 2002-05-10 2002-05-10 Eye drop of double rhizoma coptidis Expired - Lifetime CN1220501C (en)

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CN 02117620 CN1220501C (en) 2002-05-10 2002-05-10 Eye drop of double rhizoma coptidis

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Application Number Priority Date Filing Date Title
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CN1220501C true CN1220501C (en) 2005-09-28

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Publication number Priority date Publication date Assignee Title
CN109350683A (en) * 2018-10-15 2019-02-19 吴迪 A kind of eyedrops and preparation method thereof can be relieved the swelling and pain of eyes red heat
CN115569160A (en) * 2022-10-08 2023-01-06 沈阳兴齐眼药股份有限公司 Shuanghuanglian eye drops and its preparation method, stability improvement method and extract extraction method

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Assignee: Shenyang Sinqi Pharmaceutical Co., Ltd.

Assignor: Liu Jidong

Contract fulfillment period: 2005.10.26 to 2010.10.26

Contract record no.: 2008210000060

Denomination of invention: Eye drop of double rhizoma coptidis

Granted publication date: 20050928

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Address after: 110027 No. 12, 4, three street, Shenyang economic and Technological Development Zone, Liaoning, China

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Patentee after: Shenyang Sinqi Pharmaceutical Co., Ltd.

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