CN1602859A - Dripping pills of methoxsalen and its preparation method - Google Patents
Dripping pills of methoxsalen and its preparation method Download PDFInfo
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- CN1602859A CN1602859A CNA200410055335XA CN200410055335A CN1602859A CN 1602859 A CN1602859 A CN 1602859A CN A200410055335X A CNA200410055335X A CN A200410055335XA CN 200410055335 A CN200410055335 A CN 200410055335A CN 1602859 A CN1602859 A CN 1602859A
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- methoxsalen
- coolant
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- polyethylene glycol
- dissolution
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Abstract
The invention uses super micro shattering and drop pills producing the technology to produce fenfluramine drop pills, reaching the purposes such as increasing speed, and dissolution of disintegration, increasing the medicine stability, reducing the dose of auxiliary materials and decreasing cost, with rapid effect and convenient use. It can be buccal as well as deglutition, has remarkable conformity, and is especially suitable for children, older man, sicker in bed or with difficulty of swallowing.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically methoxsalen drop pill and preparation method thereof.
Background technology
Methoxsalen is a photosensitizer, can be activated by the long wave ultraviolet of wavelength at 320～400nm with the bonded 8-MOP of epidermis cell, and the maximum effect wavelength is 365nm.Under the effect of long wave ultraviolet, the thymus pyrimidine generation photochemical reaction on 8-MOP and the epidermal dna Double helix forms photoadduct, produce phototoxic reaction, synthetic and the mitoschisis of epidermal dna is suppressed, and the epidermis cell renewal speed is slowed down, thereby psoriasis is played therapeutical effect.The result of photosensitivity reaction also makes the tryrosinase vigor in the melanocyte increase, and impels melanocyte to form; Impel the melanocyte in the hair follicle in epidermis, to move, occur pigmentation on the skin thereby make.
Methoxsalen oral about 95% combines with plasma albumin from gastrointestinal absorption, with epidermis cell stronger adhesion is arranged.Photosensitization peaked in the back of taking medicine in 1.5～3 hours, and sustainable 8 hours, at liver metabolism, 95% metabolite was discharged from kidney in 24 hours.Methoxsalen needs to share (being called the PUVA therapy) with long wave ultraviolet (UVA), and treatment psoriasis, vitiligo, cutaneous T cell lymphoma also can be used for the treatment of palmoplantar pustulosis, eczema, atoipc dermatitis, lichen planus etc.
Methoxsalen is insoluble in water, and its disintegration of tablet time is long, and dissolution and dissolution rate are low, absorption difference, bioavailability is low, and the supplementary product consumption ratio is big, child, old people, bed patient and dysphagia patients are taken inconvenience, and compliance is poor, have influenced the performance of methoxsalen therapeutical effect.
The present invention makes the methoxsalen drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of methoxsalen sheet, and the therapeutical effect of methoxsalen is given full play to.
Summary of the invention
The methoxsalen drop pill of making by using ultramicro communication technique and dropping pill formulation Technology not only have disintegrate molten loose fast, dissolution and dissolution rate improve, steady quality, the pill volume is little, both can swallow also can buccal, easy to carry and use, onset is rapid, compliance is good, be particularly suitable for the characteristics that child, old people, bed patient and dysphagia patients are taken, but also have working condition and production equipment is simple, production cost is low, compare the advantage that supplementary product consumption reduces with tablet, demonstrated fully the new drug research exploitation spirit that people-oriented.
For achieving the above object, the present invention by the following technical solutions: the methoxsalen fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
The chemical name of methoxsalen is 9-methoxyl group-7-hydrogen-furan a pair of horses going side by side (3.2-g) (1) benzene a pair of horses going side by side pyrans-7-ketone among the present invention, and structural formula is
Molecular formula is C
12H
8O
4, molecular weight is 216.19.
Substrate among the present invention includes but not limited to polyethylene glycol 6000, Macrogol 4000, polyethylene glycol 1500, cetomacrogol 1000, sodium stearate, glycerin gelatine, poloxamer, stearic acid, glycerol monostearate acid, insect wax etc.
Coolant among the present invention includes but not limited to dimethicone, liquid paraffin, vegetable oil, water, alcoholic solution etc.
Below through detecting to beneficial effect of the present invention as directed
One, detects index and method
1. disintegrate (molten loosing) time limit: check according to inspection technique disintegration (two appendix XA of Chinese Pharmacopoeia version in 2000).
2. dissolution rate: sample thief, according to dissolution method (two appendix XC second methods of Chinese Pharmacopoeia version in 2000), with 0.25% sodium dodecyl sulfate solution 900ml is solvent, rotating speed is that per minute 150 changes, operation in accordance with the law, through 10,20,30, in the time of 40 minutes, get solution 10ml, filter, precision is measured subsequent filtrate 5ml and is put in the 10ml measuring bottle, add filtered in advance 0.25% sodium dodecyl sulfate solution and be diluted to scale, shake up (unclear, can go again filtration), according to spectrophotography (two appendix IVA of Chinese Pharmacopoeia version in 2000) as solution, with filterable 0.25% sodium dodecyl sulfate solution is blank, measures trap at the wavelength place of 248nm; Precision takes by weighing the methoxsalen reference substance 12.5mg that is dried to constant weight through 105 ℃ in addition, put in the 50ml measuring bottle, add dissolve with ethanol and be diluted to scale, shake up, precision is measured 2ml, puts in the 100ml measuring bottle, add filterable 0.25% sodium dodecyl sulfate solution and be diluted to scale, shake up, measure, calculate stripping quantity with method.
Two, commercially available methoxsalen sheet testing result
1. disintegration time: 65 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 32.4 51.2 71.3 83.5
Three, example 1 sample detection result
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 64.7 93.5 98.6 99.7
Four, example 2 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 67.4 95.3 97.2 96.4
Five, example 3 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 59.8 91.2 99.5 99.8
Six, example 4 sample detection results
1. the molten diffusing time: 3 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 64.2 97.3 99.5 99.6
Seven, example 5 sample detection results
1. the molten diffusing time: 5 minutes
2. dissolution rate:
Time (minute) 10 20 30 40
Dissolution (%) 53.1 92.4 99.0 98.7
Eight, example 6 sample detection results
1. the molten diffusing time: 8 minutes
2. dissolution rate
Time (minute) 10 20 30 40
Dissolution (%) 54.0 92.3 98.5 98.0
The specific embodiment
One, example 1
Prescription:
Methoxsalen 5g
Polyethylene glycol 6000 15g
Make 1000
Method for making: the methoxsalen fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused polyethylene glycol 6000 substrate, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Two, example 2
Prescription:
Methoxsalen 5g
Macrogol 4000 15g
Make 1000
Method for making: the methoxsalen fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused Macrogol 4000 substrate, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Three, example 3
Prescription:
Methoxsalen 5g
Polyethylene glycol 6000 5g
Macrogol 4000 10g
Make 1000
Method for making: the methoxsalen fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in fused Macrogol 4000 and the polyethylene glycol 6000 mixed-matrix, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Four, example 4
Prescription:
Methoxsalen 5g
Glyceryl monostearate 15g
Make 1000
Method for making: the methoxsalen fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused glyceryl monostearate substrate, and mixing is a coolant with the frozen water, the dropping preparation method pill, and drying, promptly.
Five, example 5
Prescription:
Methoxsalen 5g
Polyethylene glycol 6000 10g
Poloxamer 5g
Make 1000
Method for making: the methoxsalen fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in fused polyethylene glycol 6000 and the poloxamer mixed-matrix, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.
Six, example 6
Prescription:
Methoxsalen 5g
Glyceryl monostearate 15g
Poloxamer 1g
Make 1000
Method for making: get the mixing fine powders that methoxsalen and poloxamer cross 200 mesh sieves through micronizing and be added in the fused glyceryl monostearate substrate, mixing is a coolant with the frozen water, the dropping preparation method pill, and drying, promptly.
Claims (4)
1. methoxsalen drop pill and preparation method thereof is characterized in that: the methoxsalen fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, and abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.
2. the chemical name of the described methoxsalen of claim 1 is 9-methoxyl group-7-hydrogen-furan a pair of horses going side by side (3.2-g) (1) benzene a pair of horses going side by side pyrans-7-ketone, and structural formula is
, molecular formula is C
12H
8O
4, molecular weight is 216.19.
3. the described substrate of claim 1 includes but not limited to polyethylene glycol 6000, Macrogol 4000, polyethylene glycol 1500, cetomacrogol 1000, sodium stearate, glycerin gelatine, poloxamer, stearic acid, glycerol monostearate acid, insect wax etc.
4. the described coolant of claim 1 includes but not limited to dimethicone, liquid paraffin, vegetable oil, water, alcoholic solution etc.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200410055335XA CN1602859A (en) | 2004-08-23 | 2004-08-23 | Dripping pills of methoxsalen and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200410055335XA CN1602859A (en) | 2004-08-23 | 2004-08-23 | Dripping pills of methoxsalen and its preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1602859A true CN1602859A (en) | 2005-04-06 |
Family
ID=34666167
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA200410055335XA Pending CN1602859A (en) | 2004-08-23 | 2004-08-23 | Dripping pills of methoxsalen and its preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1602859A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115414354A (en) * | 2022-08-29 | 2022-12-02 | 西南医科大学 | Application of xanthotoxin in preparation of medicine for treating thrombocytopenia |
-
2004
- 2004-08-23 CN CNA200410055335XA patent/CN1602859A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115414354A (en) * | 2022-08-29 | 2022-12-02 | 西南医科大学 | Application of xanthotoxin in preparation of medicine for treating thrombocytopenia |
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| WD01 | Invention patent application deemed withdrawn after publication |