CN1600315A - Soft capsule combination of Cloquinate/Promestriene in use for vagina - Google Patents
Soft capsule combination of Cloquinate/Promestriene in use for vagina Download PDFInfo
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- CN1600315A CN1600315A CN 03160011 CN03160011A CN1600315A CN 1600315 A CN1600315 A CN 1600315A CN 03160011 CN03160011 CN 03160011 CN 03160011 A CN03160011 A CN 03160011A CN 1600315 A CN1600315 A CN 1600315A
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- vagina
- promestriene
- chlorquinaldol
- fluid composition
- squalane
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Abstract
A clothinate/promestriene composition used to prepare the softgel for vagina contains clochinate/promestriene, solvent and surfactant.
Description
The present invention relates to contain the stable liquid capsule composition that is suitable for preparing chlorquinaldol/promestriene soft capsule for vagina.More particularly, the present invention relates to a kind of liquid content that is suitable for being mixed with soft capsule for vagina, it contains chlorquinaldol/promestriene is active component, squalane and white vaseline also relate to the soft capsule preparation that contains the aqueous content of described milkiness as cosurfactant, solvent composition and surfactant.
Chlorquinaldol has the different mechanism of action with promestriene in chlorquinaldol/promestriene vaginal tablet, is the protectant combination of a kind of broad-spectrum antibacterial agent and vaginal mucosa.Its effect has evident characteristic separately, and can not produce interaction.The mechanism of action of chlorquinaldol in prescription is: chlorquinaldol is a kind of yellow acicular crystal, slightly penetrating odor
[11]Extensive studies has been carried out to it in many pharmaceutical factories in Europe as far back as the fifties, finds that it has antimicrobial pathogen activity such as antifungal, infusorian, antibacterial (G+ and G-), clothing raw material and mycoplasma, is a kind of broad-spectrum antibacterial agent.Because it is slightly soluble in water, the pathogen microorganism generally enters pathogen cells by endocytosis, make the change of pathogen cells pH value, the metabolism of inhibition pathogen etc. finally cause the death of pathogen, and the human body epithelial cell does not have phagocytic function to chlorquinaldol, so the outer time spent of this medicine is very little to the untoward reaction of human body.The mechanism of action of promestriene in prescription is: two hydroxyls of estradiol by methyl and propyl group etherificate after, polarity weakens, make it can only enter mucous epithelium, reach the differentiation and the maturation that promote vagina epithelium mucomembranous cell in local metabolism performance estrogen function.Synthesize and secrete the effect of glycogen, and can promote DoderleinShi bacillus (vagina bacillus acidophilus's) regeneration, produce lactic acid, recover the normal sour environment of vagina
[12]But can not be by the passive interstice that diffuses through vaginal wall and rich water, can not arrive blood capillary and be absorbed, test confirms topical application promestriene absorbance less than 1%, so the topical application promestriene does not have estrogenic systemic adverse reactions.This prescription has utilized the advantage separately of the chlorquinaldol and the promestriene of different mechanism of action, for treating and preventing the infectious leucorrhoea grow in quantity of vagina to open up new way
China uses chlorquinaldol/promestriene vaginal tablet (commodity are called " Colposeptine ") beginning import in 1997, BJ Union Hospital, the Guangdong attached Second Academy of Zhongshan Medical Univ. etc. have done clinical research to chlorquinaldol/promestriene vaginal tablet treatment vaginal infection, and the result proves that it has significant curative effect to the broad-spectrum vaginal infection.
The chemical compound patent of chlorquinaldol and promestriene all lost efficacy, and chlorquinaldol/promestriene vaginal tablet is not all applied for a patent in China, also was not inconsistent the condition of incompatible China application administrative protection.By retrieval, do not see chlorquinaldol is arranged/relevant report of promestriene vagina soft gelatin capsule.
The present invention is chlorquinaldol/promestriene vagina soft capsule, wherein chlorquinaldol and promestriene and an amount of substrate and adjuvant are made the uniform emulsion of content in the preparation, this product can provide the possibility of a kind of renewal, better dosage form selection for doctor and patient as a kind of novel form.
The object of the present invention is to provide a kind of novel formulation of chlorquinaldol/promestriene, said preparation is guaranteeing under the suitable prerequisite of principal agent dosage, by selecting adjuvant and formulation method for use, chlorquinaldol/promestriene is dispersed in makes aqueous being wrapped in of milkiness in the substrate and make soft capsule in the rubber, help the local absorption effect of medicine, thereby reach high bioavailability.Simultaneously, also be clinical a kind of renewal, the better dosage form selection of providing.
Be described more specifically the present invention by the following example.But these embodiment should not be construed as the restriction to any aspect of the present invention.
Embodiment 1
1. take by weighing white vaseline and the part squalane heating for dissolving of putting together respectively, be incubated about 60 ℃, standby, be I liquid.2. the squalane that takes by weighing promestriene and surplus is in the same place, stir, promestriene is dissolved fully, add again after chlorquinaldol stirs it, add sorbitan sesquioleate, methyl parahydroxybenzoate and the propyl p-hydroxybenzoate of having weighed then, after the stirring and dissolving, mix with I liquid, fully mix with the high speed dispersing emulsification machine, promptly make content.3. add gelatin, glycerol, water, simethicone, methyl parahydroxybenzoate and propyl p-hydroxybenzoate according to the prescription of determining, in about 60 ℃, change glue, and glue is carried out vacuum outgas handle, for using on the soft gelatin capsule press machine.4. medicinal liquid and glue are incorporated in the machine of preparation soft capsule, regulate this machine and make the medicinal liquid that injects recipe quantity in each soft capsule, preparation contains the soft capsule of chlorquinaldol/promestriene in gelatin shell.
Embodiment 2
Preparing the soft capsule with following composition according to same steps as among the embodiment 1, is the consumption difference as adjuvant.
2-A constituent content (mg/ grain)
Promestriene 10
White vaseline 400
Squalane 1000
Sorbitan sesquioleate 210
Methyl parahydroxybenzoate 160
Propyl p-hydroxybenzoate 95
Amount to 2075mg
2-B constituent content (mg/ grain)
Chlorquinaldol 200
Promestriene 10
White vaseline 400
Squalane 1200
Sorbitan sesquioleate 180
Methyl parahydroxybenzoate 120
Amount to 2140mg
2-C constituent content (mg/ grain)
Chlorquinaldol 200
Promestriene 10
White vaseline 480
Squalane 1000
Sorbitan sesquioleate 180
Methyl parahydroxybenzoate 120
Amount to 2155mg
Embodiment 3
Prepare soft capsule according to embodiment 1 identical step, just increase the composition of surfactant with following composition.
3-A constituent content (mg/ grain)
Chlorquinaldol 200
Promestriene 10
White vaseline 400
Squalane 1000
Sorbitan sesquioleate 250
Methyl parahydroxybenzoate 160
Propyl p-hydroxybenzoate 95
Amount to 1915mg
3-B constituent content (mg/ grain)
Chlorquinaldol 200
Promestriene 10
White vaseline 400
Squalane 1000
Sorbitan sesquioleate 100
Sorbitan monooleate 150
Methyl parahydroxybenzoate 160
Propyl p-hydroxybenzoate 95
Amount to 1915mg
3-C constituent content (mg/ grain)
Chlorquinaldol 200
Promestriene 10
White vaseline 400
Squalane 1000
Sorbitan monooleate 200
Methyl parahydroxybenzoate 160
Propyl p-hydroxybenzoate 95
Amount to 1905mg
Embodiment 4
Same steps as preparation according to embodiment 1 has following soft capsule, just the composition of solvent and its changes of contents.
4-A constituent content (mg/ grain)
Chlorquinaldol 200
Promestriene 10
Tween-60 150
Macrogol 600 800
Sorbitan sesquioleate 210
Methyl parahydroxybenzoate 160
Propyl p-hydroxybenzoate 95
Amount to 1625mg
4-B constituent content (mg/ grain)
Chlorquinaldol 200
Promestriene 10
Tween-65 200
PEG400 1000
Sorbitan sesquioleate 210
Methyl parahydroxybenzoate 160
Propyl p-hydroxybenzoate 95
Amount to 1875mg
4-C constituent content (mg/ grain)
Chlorquinaldol 200
Promestriene 10
Hydrogenated cottonseed oil 1000
Cera Flava 50
Sorbitan sesquioleate 210
Methyl parahydroxybenzoate 160
Propyl p-hydroxybenzoate 95
Amount to 1725mg
4-D constituent content (mg/ grain)
Chlorquinaldol 200
Promestriene 10
White vaseline 400
Hydrogenated cottonseed oil 800
Sorbitan sesquioleate 210
Methyl parahydroxybenzoate 160
Propyl p-hydroxybenzoate 95
Amount to 1675mg
Claims (10)
1. the present invention relates to prepare the stable liquid composition that contains chlorquinaldol/promestriene.More particularly, the present invention relates to a kind of liquid content that can be used for being mixed with the soft capsule that vagina uses, comprise an amount of solvent such as squalane, white vaseline, surfactant of principal agent chlorquinaldol/promestriene and capacity etc., also relate to contain the aqueous content of described milkiness be fit to the soft capsule preparation that vagina is used to form.
2. the product that the present invention relates to comprises an amount of solvent such as the squalane, white vaseline of principal agent chlorquinaldol/promestriene and capacity and surfactant etc., is fit to the gelatin clathrate that vagina is used to form.Be used for the treatment of and prevent the infectious leucorrhoea grow in quantity of vagina.
3. the fluid composition used of the vagina of claim 1, it also comprises pharmaceutic adjuvant or excipient.
4. the fluid composition used of the vagina of claim 1, wherein said solvent comprises squalane, oil-soluble substrate and water-soluble base.
5. the fluid composition used of the vagina of claim 4, wherein said oil-soluble substrate comprise semi-synthetic fatty acid glyceride class, natural fatty acid ester and hydrogenated oil and fat.(as: mountain grease, cocoa butter, hydrogenated cottonseed oil etc.)
6. the fluid composition used of the vagina of claim 4, wherein said water-soluble base comprises polyethylene glycols and nonionic surfactants etc.(as: PEG400, Tweens and pluronic gram class etc.)
7. the surfactant that the fluid composition used of the vagina of claim 1, wherein said surfactant refer to use always (comprising cationic, anionic, amphoteric ion type and nonionic).
8. the fluid composition used of the vagina of claim 1, the ratio of wherein said chlorquinaldol/promestriene, described squalane, described white vaseline and described surfactant is 1: 0.05: 5～100: 2～10: 2～10 (weight).
9. the fluid composition used of the vagina of claim 8, wherein said chlorquinaldol/promestriene, described squalane, described white vaseline and described surfactant ratio be 1: 0.05: 5～10: 2～5: 2～5 (weight).
10. the fluid composition of claim 1, it is made into the soft capsule for vagina preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03160011 CN1600315A (en) | 2003-09-22 | 2003-09-22 | Soft capsule combination of Cloquinate/Promestriene in use for vagina |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03160011 CN1600315A (en) | 2003-09-22 | 2003-09-22 | Soft capsule combination of Cloquinate/Promestriene in use for vagina |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1600315A true CN1600315A (en) | 2005-03-30 |
Family
ID=34660767
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03160011 Pending CN1600315A (en) | 2003-09-22 | 2003-09-22 | Soft capsule combination of Cloquinate/Promestriene in use for vagina |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1600315A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100394919C (en) * | 2006-03-01 | 2008-06-18 | 杨军 | Medicinal composition for treating vagina disease |
| CN100402037C (en) * | 2006-04-10 | 2008-07-16 | 杨军 | Medicine composition for treating valval and/or vaginal diseases |
| CN100408041C (en) * | 2006-04-10 | 2008-08-06 | 杨军 | Medicine composition for treating valval and/or vaginal infection |
| CN102038688B (en) * | 2009-10-15 | 2013-09-25 | 沈阳沃森药物研究所 | Chlorquinaldol-promestriene vaginal emulsifiable micro-emulsion soft capsule and preparation method thereof |
-
2003
- 2003-09-22 CN CN 03160011 patent/CN1600315A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100394919C (en) * | 2006-03-01 | 2008-06-18 | 杨军 | Medicinal composition for treating vagina disease |
| CN100402037C (en) * | 2006-04-10 | 2008-07-16 | 杨军 | Medicine composition for treating valval and/or vaginal diseases |
| CN100408041C (en) * | 2006-04-10 | 2008-08-06 | 杨军 | Medicine composition for treating valval and/or vaginal infection |
| CN102038688B (en) * | 2009-10-15 | 2013-09-25 | 沈阳沃森药物研究所 | Chlorquinaldol-promestriene vaginal emulsifiable micro-emulsion soft capsule and preparation method thereof |
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