CN103340837B - A kind of misoprostol vaginal effervescent tablets and preparation method thereof - Google Patents
A kind of misoprostol vaginal effervescent tablets and preparation method thereof Download PDFInfo
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- CN103340837B CN103340837B CN201310283193.1A CN201310283193A CN103340837B CN 103340837 B CN103340837 B CN 103340837B CN 201310283193 A CN201310283193 A CN 201310283193A CN 103340837 B CN103340837 B CN 103340837B
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- Prior art keywords
- misoprostol
- effervescent tablets
- magnesium stearate
- citric acid
- microcrystalline cellulose
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- OJLOPKGSLYJEMD-URPKTTJQSA-N methyl 7-[(1r,2r,3r)-3-hydroxy-2-[(1e)-4-hydroxy-4-methyloct-1-en-1-yl]-5-oxocyclopentyl]heptanoate Chemical compound CCCCC(C)(O)C\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC OJLOPKGSLYJEMD-URPKTTJQSA-N 0.000 title claims abstract description 60
- 229960005249 misoprostol Drugs 0.000 title claims abstract description 60
- 239000007938 effervescent tablet Substances 0.000 title claims abstract description 23
- 238000002360 preparation method Methods 0.000 title claims abstract description 20
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 53
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 40
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 20
- 235000019359 magnesium stearate Nutrition 0.000 claims description 20
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 20
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 20
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 20
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 19
- 229920000881 Modified starch Polymers 0.000 claims description 19
- 239000000203 mixture Substances 0.000 claims description 18
- 239000003826 tablet Substances 0.000 claims description 17
- 239000000843 powder Substances 0.000 claims description 15
- 238000002156 mixing Methods 0.000 claims description 14
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 14
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 claims description 13
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- 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 8
- 229930195725 Mannitol Natural products 0.000 claims description 8
- 239000000594 mannitol Substances 0.000 claims description 8
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- 239000002202 Polyethylene glycol Substances 0.000 claims description 4
- 229920001223 polyethylene glycol Polymers 0.000 claims description 4
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- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 3
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
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- 239000011734 sodium Substances 0.000 claims description 2
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- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
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- QHZLMUACJMDIAE-UHFFFAOYSA-N 1-monopalmitoylglycerol Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(O)CO QHZLMUACJMDIAE-UHFFFAOYSA-N 0.000 description 2
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 2
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- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
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- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 2
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- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 1
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 1
- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 description 1
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 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 description 1
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- 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 description 1
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 description 1
- XNOPRXBHLZRZKH-UHFFFAOYSA-N Oxytocin Natural products N1C(=O)C(N)CSSCC(C(=O)N2C(CCC2)C(=O)NC(CC(C)C)C(=O)NCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC(=O)C(C(C)CC)NC(=O)C1CC1=CC=C(O)C=C1 XNOPRXBHLZRZKH-UHFFFAOYSA-N 0.000 description 1
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- 102000016387 Pancreatic elastase Human genes 0.000 description 1
- 108010067372 Pancreatic elastase Proteins 0.000 description 1
- 208000018525 Postpartum Hemorrhage Diseases 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 208000007107 Stomach Ulcer Diseases 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 208000036029 Uterine contractions during pregnancy Diseases 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
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- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- 229960004543 anhydrous citric acid Drugs 0.000 description 1
- MSWZFWKMSRAUBD-UHFFFAOYSA-N beta-D-galactosamine Natural products NC1C(O)OC(CO)C(O)C1O MSWZFWKMSRAUBD-UHFFFAOYSA-N 0.000 description 1
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 1
- NKWPZUCBCARRDP-UHFFFAOYSA-L calcium bicarbonate Chemical compound [Ca+2].OC([O-])=O.OC([O-])=O NKWPZUCBCARRDP-UHFFFAOYSA-L 0.000 description 1
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- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 1
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- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 description 1
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 description 1
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- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
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- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
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- 150000003165 prostaglandin E1 derivatives Chemical class 0.000 description 1
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- 230000004648 relaxation of smooth muscle Effects 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 230000016160 smooth muscle contraction Effects 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- -1 sorbierite Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000002511 suppository base Substances 0.000 description 1
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Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention belongs to pharmaceutical technology field, is related to a kind of misoprostol vaginal effervescent tablets and preparation method.Misoprostol vaginal effervescent tablets of the present invention, have relaxation uterine smooth muscle, soften simultaneously cervix dilating, promote the effect of cervix maturation.Said preparation local administration, easy to use, good patient compliance, production technology is simpler, and manufacture cost is relatively low, has significant advantage.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, and in particular to a kind of misoprostol vaginal effervescent tablets and preparation method thereof.
It can be in gynemetrics's multiple fields application, including drug abortion, induced labor uterine neck accelerate the ripening and preoperative softening and cervix dilating.
Background technology
Misoprostol was synthesized in 1973 by Searle companies of Britain, belonged to artificial synthesized active prostate
Plain derivative.In initially listing in 1985, the clinical indication of Misoprostol was only to prevent non-steroid anti-inflammatory drug to cause
Duodenal ulcer and gastric ulcer, find that it triggers the function well of uterine contraction and cervix maturation-stimulating afterwards, since the nineteen ninety by
Gradually it is applied to gynemetrics.Misoprostol makes clostridiopetidase A and elastoser to uterine neck glue by stimulating uterine neck fibrocyte
Former accelerated decomposition, or the variation due to elastin laminin and Glucosamine polymerase, change arrangement of collagen fibers and increase with matrix
Add；Uterine neck and uterine smooth muscle can be influenced, makes smooth muscle relaxation, cervical dilatation, palace body smooth muscle contraction, pulls uterine neck；May be used also
The formation that gap connects between promotion Uterine Smooth Cell；Reach uterus softening, expansion, promote the purpose of cervix maturation.At present
Misoprostol in gynemetrics's multiple fields extensive use, including drug abortion, induced labor uterine neck accelerate the ripening and preoperative softening and
Cervix dilating.
Application Misoprostol in early abortion is different from oxytocin, has significant excitement to each phase gravid uterus
Effect, increase uterine leio Muscle tensility, makes in utero pressure increase, promotes embryo villi to be kept well with uterus during the stripping of palace wall
Contraction state, while the reaction of opening of the cervix nerve ending is also blocked, vagal excitatory is reduced, so as to reduce induced abortion synthesis
The generation of sign.
In late pregnancy induced labor application cervix maturation whether be that late pregnancy induced labor is successfully crucial.Misso
Forefront alcohol, which is used for late pregnancy induced labor, has obvious cervix maturation-stimulating to act on, and the time of induced labor is substantially reduced, so as to mitigate pregnant
The pain of woman.In terms of termination has mid-term or the late pregnancy of fetal abnormality or intrauterine fetal death, drug effect is obvious, success rate
It is high.
Being mainly made of using uterine neck connective tissue in hysteroscopy or other gynecological surgeries, its main component
It is collagenous fibres.Misoprostol makes in uterine neck connective tissue collagenous fibres degrade, by the Collagenase stored in cell and
Elastase discharges, and activation uterine neck collagenous fibres enzyme makes uterus softening, and relaxation uterine neck, makes cervix voluntarily expand, can keep away
Exempt from laceration of cervix, reduce patient suffering.
China's listing at present is oral conventional tablet for the Misoprostol product of gynemetrics.Since conventional tablet must
Competence exertion drug effect must be absorbed by pipe intestinal digesting, bioavilability is low, works slow, side effect is obvious.It is of the present invention
Vagina effervescence, the difference with conventional tablet, it is local application to be it, and contains effervescent agent, have disintegration it is fast,
Work the features such as rapid, bioavilability is high, and the contact surface of medicine and agents area can also be increased by producing a large amount of foams by disintegration
Product, so as to preferably play curative effect.By vagina administration, permucosal absorption, directly acts on misoprostol vaginal effervescent tablets
Target organ, long action time, higher drug concentration, sustainable performance drug effect are kept in agents area, and overcome liver head mistakes
Effect, reduces the generation of side effect.
Patent CN102939085A introduces Intravaginal administration of misoprostol, specific insert is pessary, pessary,
The form of tampon, sponge or ring；Before patent CN101010066A is introduced containing the synthesis in solid polyurethane ester hydrogel
The suppository or pessary of row parathyrine PGE1 analogs.Above-mentioned patent drug release rate is slow, it is impossible to all cloudy chambers of covering, drug utilization
It is not thorough, and easily causes drug wastage and pollution clothing.United States Patent (USP) US6664290B1 narrations take orally or vagina misso forefront
Alcohol treats postpartum haemorrhage, but wherein vaginal tablets, that is, conventional tablet, and drug release is slow, and dissolution rate is low, and bioavilability is not high, and effect is slow
It is slow.Vagina effervescence of the present invention improves formulation on external application suppository bases, and combines vagina, uterine cervix mucous membrane
Feature, gives full play to the formulation advantage of effervescent tablet.It is rapid that this product meets wet disintegration, and produces a large amount of foams, make in piece it is effective into
Part sends out effervescent effect by medicine and is rapidly dispersed into vagina, especially gauffer deep, and be evenly distributed to vagina and palace
Each position of neck stick film, fully contacts with site of action, so as to play the therapeutic effect of medicine.
The content of the invention
It is an object of the present invention to providing a kind of misoprostol vaginal effervescent tablets, it is general to solve current Misoprostol
Logical tablet bioavailability is low, works the problems such as slow.
Another object of the present invention is to provide the preparation method of this misoprostol vaginal effervescent tablets.
Misoprostol vaginal effervescent tablets provided by the invention are by bulk pharmaceutical chemicals and pharmaceutically acceptable filler, effervesce
Agent, disintegrant and lubricant composition.
The bulk pharmaceutical chemicals may be selected from Misoprostol and Misoprostol-hydroxypropyl methylcellulose mixture, preferably before misso
Row alcohol-hydroxypropyl methylcellulose mixture.Dosage can be containing 25,50,200,600 μ g/ pieces of Misoprostol, preferably 200 μ g/ pieces.
The filler is selected from microcrystalline cellulose, pregelatinized starch, mannitol, sorbierite, lactose, xylitol, maltose
One kind or its mixture in alcohol, low-substituted hydroxypropyl cellulose and starch；Preferably microcrystalline cellulose, pregelatinized starch and sweet dew
Alcohol.
The effervescent agent is selected from citric acid, tartaric acid, dextrotartaric acid, fumaric acid, malic acid, anhydrous citric acid, lemon
One or more in sour sodium；Alkaline agent may be selected from sodium acid carbonate, sodium carbonate, potassium carbonate, saleratus, calcium carbonate, calcium bicarbonate
In one or more；Preferably citric acid is 1: 1.75 with sodium acid carbonate weight ratio.
The lubricant may be selected from magnesium stearate, Macrogol 6000, stearic acid, talcum powder, paraffin, glycerol monostearate
One kind or its mixture in ester, monopalmitin and superfine silica gel powder；It is preferred that magnesium stearate and Macrogol 6000.
Misoprostol vaginal effervescent tablets preparation method provided by the invention is dry powder vertical compression, and concrete technology is：Weigh suitable
The side that the Misoprostol of amount-hydroxypropyl methylcellulose mixture progressively increases with appropriate filler, effervescent agent and lubricant according to equivalent
Formula, sieve direct tablet compressing after mixing, to obtain the final product.
Misoprostol vaginal effervescent tablets of the present invention have following advantage：1. pharmaceutical preparation is simple, suitably
Industrialized production.2. medicine is disintegrated rapidly in vagina, drug solubility is high.3. due to a large amount of foams that disintegration produces, medicine point
Cloth is uniform, is fully combined with site of action, works rapid.4. vagina administration, avoids systemic medication side effect, adverse reaction
It is relatively low.5. solid pharmaceutical preparation, easy to carry and transport, storage period length.
Embodiment
The misoprostol vaginal effervescent tablets of the present invention are further elaborated with by following embodiments.But this hair
Bright to be not limited in following embodiments, simple modifications or modification under the premise of the method for the present invention to the present invention belong to the present invention will
Seek protection domain.
Embodiment 1
Specification：Containing 200 μ g/ pieces of Misoprostol
Preparation process is as follows：Weigh Misoprostol powder, microcrystalline cellulose, pregelatinized starch, citric acid, bicarbonate
Sodium, polyethylene glycol-6000, magnesium stearate etc. are in the way of equivalent is progressively increased, and sieve direct tablet compressing after mixing.
Evaluation：Smooth in appearance, hardness is moderate, disintegration time limited within 5min, gas release 5ml.
Embodiment 2
Specification：Containing 200 μ g/ pieces of Misoprostol
Preparation process is as follows：Weigh Misoprostol powder, microcrystalline cellulose, pregelatinized starch, citric acid, bicarbonate
Sodium, polyethylene glycol-6000, magnesium stearate etc. are in the way of equivalent is progressively increased, and sieve direct tablet compressing after mixing.
Evaluation：Smooth in appearance, hardness is moderate, and disintegration time limited is more than 5 minutes, can scatter but not dissolve completely.
Embodiment 3
Specification：Containing 200 μ g/ pieces of Misoprostol
Preparation process is as follows：Weigh Misoprostol powder, microcrystalline cellulose, sorbierite, pregelatinized starch, citric acid,
Sodium acid carbonate, polyethylene glycol-6000, magnesium stearate etc. are in the way of equivalent is progressively increased, and sieve direct tablet compressing after mixing.
Evaluation：Smooth in appearance, hardness is moderate, disintegration time limited at 3-4 minutes, gas release 3ml.
Embodiment 4
Specification：Containing 200 μ g/ pieces of Misoprostol
Preparation process is as follows：Weigh Misoprostol powder, microcrystalline cellulose (102#), pregelatinized starch, mannitol, Chinese holly
In the way of equivalent is progressively increased, sieving is directly pressed after mixing for rafter acid, sodium acid carbonate, polyethylene glycol-6000, magnesium stearate etc.
Piece.
Evaluation：Smooth in appearance, hardness is moderate, disintegration time limited at 3 minutes or so, gas release 3.5ml.
Embodiment 5
Specification：Containing 200 μ g/ pieces of Misoprostol
Preparation process is as follows：Weigh Misoprostol powder, microcrystalline cellulose (102#), pregelatinized starch, mannitol, Chinese holly
In the way of equivalent is progressively increased, sieving is directly pressed after mixing for rafter acid, sodium acid carbonate, polyethylene glycol-6000, magnesium stearate etc.
Piece.
Evaluation：Smooth in appearance, hardness is moderate, disintegration time limited at 3 minutes or so, gas release 6-6.5ml.
Embodiment 6
Specification：Containing 25 μ g/ pieces of Misoprostol
Preparation process is as follows：Weigh Misoprostol powder, hydroxypropyl methylcellulose, microcrystalline cellulose, pregelatinized starch, Chinese holly
Rafter acid, sodium acid carbonate, polyethylene glycol, magnesium stearate etc. are in the way of equivalent is progressively increased, and sieve direct tablet compressing after mixing.
Evaluation：Smooth in appearance, hardness is moderate, disintegration time limited within 5min, gas release 5ml.
Embodiment 7
Specification：Containing 50 μ g/ pieces of Misoprostol
Preparation process is as follows：Weigh Misoprostol powder, microcrystalline cellulose, sorbierite, pregelatinized starch, citric acid,
Sodium acid carbonate, polyethylene glycol, magnesium stearate etc. are in the way of equivalent is progressively increased, and sieve direct tablet compressing after mixing.
Evaluation：Smooth in appearance, hardness is bigger, disintegration time limited 3-4 minute, gas release 3ml.
Embodiment 8
Specification：Containing 600 μ g/ pieces of Misoprostol
Preparation process is as follows：Weigh Misoprostol powder, microcrystalline cellulose, mannitol, pregelatinized starch, citric acid,
Sodium acid carbonate, polyethylene glycol, magnesium stearate etc. are in the way of equivalent is progressively increased, and sieve direct tablet compressing after mixing.
Evaluation：Smooth in appearance, hardness is moderate, about 4 minutes disintegration time limiteds, gas release 5ml.
Claims (5)
1. a kind of misoprostol vaginal effervescent tablets, it is characterised in that every misoprostol vaginal effervescent tablets contain Misoprostol
200 μ g, the composition of every 1000 include Misoprostol-hydroxypropyl methylcellulose mixture 20g, microcrystalline cellulose 150g, pre- glue
Change starch 50g, citric acid 29g, sodium acid carbonate 49g, polyethylene glycol-6000 3g, magnesium stearate 2g, its preparation method is：Weigh
Misoprostol powder, microcrystalline cellulose, pregelatinized starch, citric acid, sodium acid carbonate, polyethylene glycol-6000, magnesium stearate etc.
In the way of equivalent is progressively increased, sieve direct tablet compressing after mixing.
2. a kind of misoprostol vaginal effervescent tablets, it is characterised in that every misoprostol vaginal effervescent tablets contain Misoprostol
200 μ g, the composition of every 1000 include Misoprostol-hydroxypropyl methylcellulose mixture 20g, 102 50g of microcrystalline cellulose, mountain
Pears alcohol 100g, pregelatinized starch 100g, citric acid 20g, sodium acid carbonate 35g, polyethylene glycol-6000 5g, magnesium stearate 2g, its
Preparation method is：Weigh Misoprostol powder, microcrystalline cellulose, sorbierite, pregelatinized starch, citric acid, sodium acid carbonate, poly-
Ethylene glycol -6000, magnesium stearate etc. are in the way of equivalent is progressively increased, and sieve direct tablet compressing after mixing.
3. a kind of misoprostol vaginal effervescent tablets, it is characterised in that every misoprostol vaginal effervescent tablets contain Misoprostol
200 μ g, the composition of every 1000 include Misoprostol-hydroxypropyl methylcellulose mixture 20g, 102 100g of microcrystalline cellulose,
Pregelatinized starch 50g, mannitol 100g, citric acid 20g, sodium acid carbonate 35g, polyethylene glycol-6000 5g, magnesium stearate 2g, its
Preparation method is：Weigh Misoprostol powder, microcrystalline cellulose 102, pregelatinized starch, mannitol, citric acid, bicarbonate
Sodium, polyethylene glycol-6000, magnesium stearate etc. are in the way of equivalent is progressively increased, and sieve direct tablet compressing after mixing.
4. a kind of misoprostol vaginal effervescent tablets, it is characterised in that every misoprostol vaginal effervescent tablets contain Misoprostol
200 μ g, the composition of every 1000 include Misoprostol-hydroxypropyl methylcellulose mixture 20g, 102 100g of microcrystalline cellulose,
Pregelatinized starch 80g, mannitol 70g, citric acid 58g, sodium acid carbonate 32g, polyethylene glycol-6000 5g, magnesium stearate 2g, its
Preparation method is：Weigh Misoprostol powder, microcrystalline cellulose 102, pregelatinized starch, mannitol, citric acid, bicarbonate
Sodium, polyethylene glycol-6000, magnesium stearate etc. are in the way of equivalent is progressively increased, and sieve direct tablet compressing after mixing.
5. a kind of misoprostol vaginal effervescent tablets, it is characterised in that every misoprostol vaginal effervescent tablets contain Misoprostol
25 μ g, the composition of every 1000 include Misoprostol-hydroxypropyl methylcellulose mixture 2.5g, hydroxypropyl methylcellulose 17.5g, micro-
Crystalline cellulose 150g, pregelatinized starch 50g, citric acid 29g, sodium acid carbonate 49g, polyethylene glycol-6000 3g, magnesium stearate 2g,
Its preparation method is：Weigh Misoprostol powder, hydroxypropyl methylcellulose, microcrystalline cellulose, pregelatinized starch, citric acid, carbon
Sour hydrogen sodium, polyethylene glycol, magnesium stearate etc. are in the way of equivalent is progressively increased, and sieve direct tablet compressing after mixing.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310283193.1A CN103340837B (en) | 2013-07-08 | 2013-07-08 | A kind of misoprostol vaginal effervescent tablets and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310283193.1A CN103340837B (en) | 2013-07-08 | 2013-07-08 | A kind of misoprostol vaginal effervescent tablets and preparation method thereof |
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| CN103340837B true CN103340837B (en) | 2018-04-27 |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20160008310A1 (en) | 2014-07-11 | 2016-01-14 | Azanta A/S | Misoprostol dispersible tablet |
| RS56468B1 (en) * | 2014-07-11 | 2018-01-31 | Azanta Denmark As | Misoprostol dispersible tablet |
| WO2016004960A2 (en) | 2014-07-11 | 2016-01-14 | Azanta A/S | Misoprostol dispersible tablet |
| CN113230383A (en) * | 2021-05-10 | 2021-08-10 | 广州天恩药业科技有限公司 | Formula for repairing postpartum vagina injury and relaxation |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6664290B1 (en) * | 1994-09-27 | 2003-12-16 | University College London | Oral or vaginal administration of mesoprostol in third stage labor |
-
2013
- 2013-07-08 CN CN201310283193.1A patent/CN103340837B/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6664290B1 (en) * | 1994-09-27 | 2003-12-16 | University College London | Oral or vaginal administration of mesoprostol in third stage labor |
Non-Patent Citations (2)
| Title |
|---|
| 阴道给药系统的剂型发展;陆继伟等;《中国临床药学杂志》;20031231;第12卷(第2期);第123-126页 * |
| 阴道给药系统的研究现状及进展;吴莹等;《安徽医药》;20101231;第14卷(第7期);第754-757页 * |
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