CN1895221A - Fast-effective oral analgesic - Google Patents
Fast-effective oral analgesic Download PDFInfo
- Publication number
- CN1895221A CN1895221A CN 200610082322 CN200610082322A CN1895221A CN 1895221 A CN1895221 A CN 1895221A CN 200610082322 CN200610082322 CN 200610082322 CN 200610082322 A CN200610082322 A CN 200610082322A CN 1895221 A CN1895221 A CN 1895221A
- Authority
- CN
- China
- Prior art keywords
- oil
- hydrogenated
- oral liquid
- lecithin
- lornoxicam
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 230000000202 analgesic effect Effects 0.000 title abstract description 5
- OXROWJKCGCOJDO-JLHYYAGUSA-N lornoxicam Chemical compound O=C1C=2SC(Cl)=CC=2S(=O)(=O)N(C)\C1=C(\O)NC1=CC=CC=N1 OXROWJKCGCOJDO-JLHYYAGUSA-N 0.000 claims abstract description 50
- 229960002202 lornoxicam Drugs 0.000 claims abstract description 50
- 239000007788 liquid Substances 0.000 claims abstract description 19
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 33
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 27
- 239000007901 soft capsule Substances 0.000 claims description 22
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims description 20
- 235000010445 lecithin Nutrition 0.000 claims description 20
- 239000000787 lecithin Substances 0.000 claims description 20
- 229940067606 lecithin Drugs 0.000 claims description 20
- 239000003921 oil Substances 0.000 claims description 19
- 235000019198 oils Nutrition 0.000 claims description 19
- -1 Oleum sesami Substances 0.000 claims description 18
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 14
- 239000007766 cera flava Substances 0.000 claims description 14
- 210000000582 semen Anatomy 0.000 claims description 14
- 235000011187 glycerol Nutrition 0.000 claims description 12
- 238000002360 preparation method Methods 0.000 claims description 11
- 235000019482 Palm oil Nutrition 0.000 claims description 10
- 239000002540 palm oil Substances 0.000 claims description 10
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 10
- 229920000053 polysorbate 80 Polymers 0.000 claims description 10
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 8
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 8
- ZEMPKEQAKRGZGQ-AAKVHIHISA-N 2,3-bis[[(z)-12-hydroxyoctadec-9-enoyl]oxy]propyl (z)-12-hydroxyoctadec-9-enoate Chemical class CCCCCCC(O)C\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/CC(O)CCCCCC)COC(=O)CCCCCCC\C=C/CC(O)CCCCCC ZEMPKEQAKRGZGQ-AAKVHIHISA-N 0.000 claims description 8
- 229920001983 poloxamer Polymers 0.000 claims description 8
- 239000003240 coconut oil Substances 0.000 claims description 7
- 235000019864 coconut oil Nutrition 0.000 claims description 7
- JLPULHDHAOZNQI-ZTIMHPMXSA-N 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine Chemical class CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/C\C=C/CCCCC JLPULHDHAOZNQI-ZTIMHPMXSA-N 0.000 claims description 6
- 240000008415 Lactuca sativa Species 0.000 claims description 6
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- 235000019438 castor oil Nutrition 0.000 claims description 6
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 6
- 235000012045 salad Nutrition 0.000 claims description 6
- 239000003549 soybean oil Substances 0.000 claims description 6
- 235000012424 soybean oil Nutrition 0.000 claims description 6
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 4
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 claims description 4
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- 239000003963 antioxidant agent Substances 0.000 claims description 4
- 230000003078 antioxidant effect Effects 0.000 claims description 4
- 235000006708 antioxidants Nutrition 0.000 claims description 4
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims description 4
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- 229940075507 glyceryl monostearate Drugs 0.000 claims description 4
- 229940099578 hydrogenated soybean lecithin Drugs 0.000 claims description 4
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims description 4
- 229960000502 poloxamer Drugs 0.000 claims description 4
- 239000003760 tallow Substances 0.000 claims description 4
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- 235000019165 vitamin E Nutrition 0.000 claims description 4
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- 239000001993 wax Substances 0.000 claims description 4
- 239000003381 stabilizer Substances 0.000 claims description 3
- 244000068988 Glycine max Species 0.000 claims description 2
- 235000010469 Glycine max Nutrition 0.000 claims description 2
- 241000238631 Hexapoda Species 0.000 claims description 2
- 240000000111 Saccharum officinarum Species 0.000 claims description 2
- 235000007201 Saccharum officinarum Nutrition 0.000 claims description 2
- 239000006184 cosolvent Substances 0.000 claims description 2
- 239000003995 emulsifying agent Substances 0.000 claims description 2
- 239000004006 olive oil Substances 0.000 claims description 2
- 235000008390 olive oil Nutrition 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 235000019384 rice bran wax Nutrition 0.000 claims description 2
- 239000004170 rice bran wax Substances 0.000 claims description 2
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- 239000012177 spermaceti Substances 0.000 claims description 2
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- 239000008158 vegetable oil Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 abstract description 4
- 239000002775 capsule Substances 0.000 description 12
- 238000003756 stirring Methods 0.000 description 12
- 238000005516 engineering process Methods 0.000 description 10
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical group [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 8
- 235000013339 cereals Nutrition 0.000 description 8
- 239000000470 constituent Substances 0.000 description 8
- 239000000463 material Substances 0.000 description 8
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 8
- 235000010262 sodium metabisulphite Nutrition 0.000 description 8
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- 229920002472 Starch Polymers 0.000 description 6
- 235000019698 starch Nutrition 0.000 description 6
- 239000008107 starch Substances 0.000 description 6
- 239000004255 Butylated hydroxyanisole Substances 0.000 description 5
- 235000019282 butylated hydroxyanisole Nutrition 0.000 description 5
- 239000002552 dosage form Substances 0.000 description 5
- 239000000203 mixture Substances 0.000 description 5
- 108010010803 Gelatin Proteins 0.000 description 4
- QZUDBNBUXVUHMW-UHFFFAOYSA-N clozapine Chemical compound C1CN(C)CCN1C1=NC2=CC(Cl)=CC=C2NC2=CC=CC=C12 QZUDBNBUXVUHMW-UHFFFAOYSA-N 0.000 description 4
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- 235000011852 gelatine desserts Nutrition 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 239000002202 Polyethylene glycol Substances 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
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- 229920001223 polyethylene glycol Polymers 0.000 description 3
- 238000012216 screening Methods 0.000 description 3
- 238000004513 sizing Methods 0.000 description 3
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
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- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
- 210000002469 basement membrane Anatomy 0.000 description 2
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 description 2
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- TVYLLZQTGLZFBW-ZBFHGGJFSA-N (R,R)-tramadol Chemical compound COC1=CC=CC([C@]2(O)[C@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-ZBFHGGJFSA-N 0.000 description 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 description 1
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 1
- 229920000858 Cyclodextrin Polymers 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 description 1
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 description 1
- XADCESSVHJOZHK-UHFFFAOYSA-N Meperidine Chemical compound C=1C=CC=CC=1C1(C(=O)OCC)CCN(C)CC1 XADCESSVHJOZHK-UHFFFAOYSA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
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- 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
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- ZPEIMTDSQAKGNT-UHFFFAOYSA-N chlorpromazine Chemical compound C1=C(Cl)C=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZPEIMTDSQAKGNT-UHFFFAOYSA-N 0.000 description 1
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- 238000001727 in vivo Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
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- XELXKCKNPPSFNN-BJWPBXOKSA-N morphine hydrochloride trihydrate Chemical compound O.O.O.Cl.O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O XELXKCKNPPSFNN-BJWPBXOKSA-N 0.000 description 1
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
An orally taken analgetic able to quickly take its effect is disclosed, which is the liquid lornoxicam.
Description
Technical field
The present invention relates to comprise the oral formulations of lornoxicam medicine, specifically provide a kind of oral, stable liquid lornoxicam preparation of specializing in gastrointestinal administration.
Background technology
Lornoxicam is by the non_steroidal anti_inflammatory drug of Nycomed company exploitation, goes on the market in Denmark first in October, 1997.It suppresses the synthetic of prostaglandin (PGs) by the activity that suppresses Cycloxygenase.Analgesic such as the alternative morphine hydrochloride of clinical trial demonstration lornoxicam, pethidine hydrochloride and salt love song are many alleviate surgical patient's postoperative pain, can alleviate the pain of diseases such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis effectively.
So far, have only the lornoxicam preparation of solid form to exist clinically, for example: tablet, freeze-dried powder.Because the character of lornoxicam is extremely unstable, comprise heat, light and oxygen.It is a kind of that CN97197619 provides, and lornoxicam and EDTA-2Na form salt, to increase its dissolubility, stability, reduces the method for turbidity.And CN02129254 forms complex to lornoxicam and nicotiamide, so that increase its dissolubility and stability.Though they can be prepared into the solution form, the two has emphasized it is aqueous solution simultaneously, and route of administration is " pharmaceutical composition that intestinal is outer or eye is suitable for ", illustrates that this class preparation is not suitable for oral.The two all fixes on acid-base value more than 7.5 in order to improve the stability of lornoxicam in aqueous solution, if it is oral to adopt this solution to be used for, the stimulating gastrointestinal road significantly reduces patient's toleration greatly.
Summary of the invention
The invention provides a kind of lornoxicam preparation of specializing in the liquid oral of gastrointestinal administration, it can significantly strengthen the beneficial effect of lornoxicam, than present commercially available prod remarkable stability and treatment advantage is arranged.Simultaneously, the invention provides a kind of selection, it provides a kind of new safety product as the substituting of prior art, and this dosage form will be that the doctor highly approves and puts forth effort and recommends.
The present invention has following characteristic: the invention provides the lornoxicam oral liquid, this liquid contains a large amount of edible oil.With oil is basement membrane, with unsettled, easily oxidized lornoxicam wraps up, and can avoid contacting of lornoxicam and oxygen; Contain a large amount of easily oxidation compositions in the oily substance simultaneously, play the effect of natural inhibitor, improve its stability greatly.And the medicine of this outer wrap oiliness basement membrane, have lipotropy, can pass fast in vivo and be fat-soluble cell membrane and enter cell interior, reach the purpose of quick inhibition of pain.Simultaneously, the employing oleaginous base is a carrier, can significantly improve the bioavailability of oral lornoxicam.The dispersibility of its height, good storing stability, the instability and the deterioration of preparation are suppressed.More advantageously be to have significantly improved the compliance of patient to treatment.
This product can select at present known any can be for oral liquid preparation form, as oral liquid (comprising oral solution, oral suspensions, Orally taken emulsion), drop, liquid hard capsule, soft capsule, spray, preferred soft capsule, this dosage form not only can have many advantages of soft capsule dosage form self, simultaneously for lornoxicam itself, also have than the more significant advantage of other oral liquids: compare with other dosage forms, soft capsule have bioavailability height, good airproof performance, content accurately, characteristics such as good looking appearance; For the patient, carry, take all very convenient; Can in capsule shell, add light screening material, overcome the shortcoming of lornoxicam photo-labile; Whole process of preparation need not heating, has overcome the instability of lornoxicam to heat.
Employing is that substrate also relatively is fit to the soft capsule dosage form among the present invention with the Polyethylene Glycol, comprises enclose.
To further make non restrictive description below to the present invention.
Active component:
By lornoxicam weight, every contains 0.5～50mg, preferred 1～25mg, more preferably 2～16mg.For the more effective dissolution rate that improves preparation that reaches, more advantageously active component is carried out pretreatment, it is crushed to more than 100 orders, more than preferred 120 orders, more preferably more than 180 orders, even micronization.
Substrate:
Through a large amount of experiment screenings, soft capsule mesostroma of the present invention is preferably vegetable oil, comprise pharmaceutical grade salad oil, soybean oil, oil with hydrogenated soybean, Oleum Arachidis hypogaeae semen, Semen Maydis oil, Oleum sesami, olive oil or their mixed system, to account for the total restatement of content, its consumption is 50-99%, preferred 70-97%, more preferably 80-95%.
This liquid exists with the solution situation, also can be suspension, emulsion etc.According to the existence form difference, should add suitable cosolvent, suspending agent and emulsifying agent, be selected from tween 80, Arlacel-60, polyoxyethylene castor oil, polyoxyethylene hydrogenated Oleum Ricini, pluronic, poloxamer, MCT Oil, tristerin, Cera Flava, haze tallow, spermaceti, insect wax, Cera Flava, rice bran wax, sugarcane wax, hydrogenated palm oil, Oleum Cocois, hydrogenated coconut oil, lecithin, hydrolecithin, fabaceous lecithin, hydrogenated soybean lecithin or their mixed system, preferred tween 80, Arlacel-60, polyoxyethylene castor oil, polyoxyethylene hydrogenated Oleum Ricini, pluronic, poloxamer, glyceryl monostearate, Cera Flava, haze tallow, Cera Flava, the hydrogenation brown tung oil, Oleum Cocois, hydrogenated coconut oil, lecithin, hydrolecithin, fabaceous lecithin, hydrogenated soybean lecithin or their mixed system, more preferably tween 80, polyoxyethylene castor oil, polyoxyethylene hydrogenated Oleum Ricini, Cera Flava, hydrogenated palm oil, hydrogenated coconut oil, lecithin, fabaceous lecithin or their mixed system; To account for the total restatement of content, its consumption is 2-30%, preferred 3-15%, more preferably 4-10%.
For further improving the quality of products, add stabilizing agent, antioxidant and antiseptic again in the solution; Stabilizing agent comprises glycerol, propylene glycol, triglyceride, or their mixed system.Preferably glycerine, propylene glycol or their mixed system.To account for the total restatement of content, its consumption is 2-30%, preferred 3-15%, more preferably 4-10%.
Antioxidant comprises various vitriolic sodium salts, BHA, and vitamin E, EDTA-2Na, EDTA-CaNa, to account for the total restatement of content, its consumption is 0.05-15%, preferred 0.5-10%, more preferably 1-5%.。
The present oral soft capsule that the someone hints or clearly instruction comprises lornoxicam and other active component simultaneously as yet clinically.The invention provides this technology, successfully in the lornoxicam soft capsule, added other active component, for example tiopronin, tranquilizer (stable, clozapine, chlorpromazine etc.), other nonsteroidal anti-inflammatory drugs, analgesic (as: morphine, tramadol, caffeine, lignocaine, tetracaine), aspirin, antibacterial-anti-inflammatory drug, Chinese medicine extract or its extract active component etc., to improve the curative effect of lornoxicam, and/or overcome untoward reaction behind the oral lornoxicam, and/or reach synergism.
Soft capsule material of the present invention is advisable with suitable elasticity, comprise sizing material and solvent, sizing material comprises plant gum and animal glue, as: arabic gum, carrageenin, xanthan gum, Algin, starch (derivant that comprises starch deep processed product or starch) glue, glutinous rice foxtail millet (Oryza glutinosa), foxtail millet corn, gelatin etc., preferred gelatin; General selection water is solvent;
For solving soft capsule poor stability, leakage and the slow shortcoming of disintegrate, the present invention takes selected sizing material control viscosity, iron-holder and kinetic parameter reached the purpose of strict screening capsule material.
In addition, aldehyde material and gelatin autoxidation process all can make gelatin take place crosslinked and influence disintegrate, for overcoming these influence factors, adopt to add an amount of plasticizer in the capsule material, through a large amount of tests, have successfully overcome the defective of above-mentioned soft capsule.Wherein plasticizer comprises glycerol, xylitol, sorbitol (acid anhydride), dimethicone, propylene glycol, Polyethylene Glycol, cyclodextrin, starch (derivant that comprises starch deep processed product or starch) class, various acid etc., preferably glycerine, Polyethylene Glycol, sorbitol (acid anhydride), tartaric acid, glycine.For making capsule more stable and sensation is better, can in glue, add an amount of antiseptic, antioxidant, opacifier, aromatic and pigment etc.
The present invention does not make specific limited to the preparation method of soft capsule, can adopt this area conventional method, for example pressing or dropping preparation method (drop pill method).The face shaping of described soft capsule is not made specific limited, can be existing arbitrary shape.
Following examples are intended to further specify the present invention, scope of the present invention are not limited.Those skilled in the art can not depart from the improvement and the variation of category of the present invention and spirit to embodiment disclosed herein.
Embodiment 1
Prescription
Constituent content (mg/ capsule/grain)
Lornoxicam 5
Propylene glycol 20
Oleum Arachidis hypogaeae semen 150
Fabaceous lecithin 20
Vitamin E 5
Amount to 200
Technology:
Get the lornoxicam raw material, pulverize, behind 200 mesh sieves, standby excessively.
Get recipe quantity propylene glycol and vitamin E, behind the mix homogeneously, add the lornoxicam of above-mentioned standby recipe quantity, dispersed with stirring evenly after, add the Oleum Arachidis hypogaeae semen of recipe quantity, after stirring, add fabaceous lecithin, after stirring, be processed into soft capsule
Embodiment 2
Prescription
Constituent content (mg/ capsule/grain)
Lornoxicam 2
Glycerol 20
Semen Maydis oil 400
Lecithin 20
Sodium sulfite 8
Amount to 450
Technology:
Get the lornoxicam raw material, pulverize, behind 120 mesh sieves, standby excessively.
Get recipe quantity glycerol and sodium sulfite, after mix homogeneously and the dissolving, add the lornoxicam of recipe quantity, after dispersed with stirring is even, add the Semen Maydis oil of standby recipe quantity, after stirring, add lecithin, after stirring, be processed into soft capsule
Embodiment 3
Prescription
Constituent content (mg/ capsule/grain)
Lornoxicam 8
Glycerol 50
Triglyceride 20
Salad oil: soybean oil=1: 1 500
Hydrogenated palm oil 15
Cera Flava 8
Sodium pyrosulfite 7
Amount to 608
Technology:
Get the lornoxicam raw material, pulverize, behind 180 mesh sieves, standby excessively.
Get recipe quantity glycerol, triglyceride and sodium pyrosulfite, after mix homogeneously and the dissolving, the lornoxicam that adds standby recipe quantity, after dispersed with stirring is even, add the salad oil of recipe quantity and the miscella of soybean oil, after stirring, add Cera Flava and hydrogenated palm oil, after stirring, be processed into soft capsule
Embodiment 4
Constituent content (mg/ capsule/grain)
Lornoxicam 4
Propylene glycol 41
Polyoxyethylene hydrogenated Oleum Ricini 20
Tween 80 30
Semen Maydis oil: Oleum Sesami=3: 1 350
EDTA-CaNa 10
Amount to 455
Technology:
Get the lornoxicam raw material, pulverize, behind 280 mesh sieves, standby excessively.
Get recipe quantity polyoxyethylene hydrogenated Oleum Ricini and EDTA-CaNa, add above-mentioned lornoxicam, after disperseing fully, add propylene glycol and tween 80, be stirred well to dissolving fully, add the prior Semen Maydis oil of synthetic recipe quantity in proportion and the miscella of Oleum Sesami, after stirring, be processed into soft capsule.
Embodiment 5:
Prescription
Constituent content (mg/ capsule/grain)
Lornoxicam 3
Clozapine 5
Tween 80 40
Glycerol 80
Oleum Arachidis hypogaeae semen 300
Hydrolecithin 30
BHA 20
Amount to 478
Technology
Get lornoxicam and clozapine raw material, pulverize, behind 200 mesh sieves, standby excessively.
Get recipe quantity glycerol, add above-mentioned lornoxicam and clozapine, after being uniformly dispersed, add tween 80, be stirred well to fully, add Oleum Arachidis hypogaeae semen, hydrogenated palm oil and BHA, after stirring, be processed into soft capsule.
Embodiment 6:
Prescription
Constituent content (mg/ capsule/grain)
Lornoxicam 4
Semen Maydis oil 300
Fabaceous lecithin 15
BHA 6
Amount to 325
Technology
Get the lornoxicam raw material, pulverize, behind 200 mesh sieves, standby excessively.
Get the recipe quantity Semen Maydis oil, lecithin, BHA is stirred well to fully and is uniformly dispersed, and adds above-mentioned lornoxicam raw material, after stirring, is processed into soft capsule.
Embodiment 7:
Prescription
Constituent content (mg/ capsule/grain)
Lornoxicam 8
Salad oil 300
Glyceryl monostearate 13
Hydrogenated coconut oil 20
Lecithin 15
EDTA-2Na 6
Sodium pyrosulfite 5
Amount to 367
Technology
Get lornoxicam, sodium pyrosulfite and EDTA-2Na supplementary material are pulverized, and be behind 200 mesh sieves, standby excessively.
Get the recipe quantity salad oil, glyceryl monostearate, hydrogenated coconut oil, lecithin adds above-mentioned lornoxicam and sodium pyrosulfite and EDTA-2Na, after being uniformly dispersed, be stirred well to fully after, be processed into soft capsule.
Embodiment 8:
Prescription
Constituent content (mg/ capsule/grain)
Lornoxicam 8
Soybean oil 300
Cera Flava 11
Hydrogenated palm oil 18
Soybean phospholipid 10
EDTA-2Na 8
Sodium pyrosulfite 7
Amount to 362
Technology
Get lornoxicam, sodium pyrosulfite and EDTA-2Na supplementary material are pulverized, and be behind 120 mesh sieves, standby excessively.
Get the recipe quantity soybean oil, Cera Flava, hydrogenated palm oil, soybean phospholipid adds above-mentioned lornoxicam and sodium pyrosulfite and EDTA-2Na, after being uniformly dispersed, be stirred well to fully after, be processed into soft capsule.
Claims (9)
1, a kind of pharmaceutical composition is specialized in the oral liquid of gastrointestinal administration, comprises lornoxicam and oleaginous base or carrier.
2, the described oral liquid of claim 1, by lornoxicam weight, each preparation unit contains 0.5～50mg, preferred 1～25mg, more preferably 2～16mg;
3, the described oral liquid of claim 1, oleaginous base is preferably vegetable oil, comprises pharmaceutical grade salad oil, soybean oil, oil with hydrogenated soybean, Oleum Arachidis hypogaeae semen, Semen Maydis oil, Oleum sesami, olive oil or their mixed system;
4, the described oral liquid of claim 2, its active component is crushed to more than 100 orders at least, more than preferred 120 orders, more preferably more than 180 orders, even micronization;
5, the oleaginous base in the described oral liquid of claim 3, to account for the total restatement of content, its consumption is 50-99%, preferred 70-97%, more preferably 80-95%;
6, the described oral liquid of claim 1 also comprises cosolvent, suspending agent and emulsifying agent; Be selected from tween 80, Arlacel-60, polyoxyethylene castor oil, polyoxyethylene hydrogenated Oleum Ricini, pluronic, poloxamer, MCT Oil, tristerin, Cera Flava, haze tallow, spermaceti, insect wax, Cera Flava, rice bran wax, sugarcane wax, hydrogenated palm oil, Oleum Cocois, hydrogenated coconut oil, lecithin, hydrolecithin, fabaceous lecithin, hydrogenated soybean lecithin or their mixed system, preferred tween 80, Arlacel-60, polyoxyethylene castor oil, polyoxyethylene hydrogenated Oleum Ricini, pluronic, poloxamer, glyceryl monostearate, Cera Flava, haze tallow, Cera Flava, hydrogenated palm oil, hydrogenated coconut oil, lecithin, hydrolecithin, fabaceous lecithin, hydrogenated soybean lecithin or their mixed system, more preferably tween 80, polyoxyethylene castor oil, polyoxyethylene hydrogenated Oleum Ricini, Cera Flava, hydrogenated palm oil, lecithin, fabaceous lecithin or their mixed system; To account for the total restatement of content, its consumption is 2-30%, preferred 3-15%, more preferably 4-10%.
7, the described oral liquid of claim 1 also comprises stabilizing agent; Be selected from glycerol, propylene glycol, triglyceride, or their mixed system.Preferably glycerine, propylene glycol or their mixed system.To account for the total restatement of content, its consumption is 2-30%, preferred 3-15%, more preferably 4-10%.
8, the described oral liquid of claim 1 also comprises antioxidant, is selected from various vitriolic sodium salts, BHA, and vitamin E, to account for the total restatement of content, its consumption is 0.05-15%, preferred 0.5-10%, more preferably 1-5%;
9, the described oral liquid of claim 1, preferred soft capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100823220A CN100560058C (en) | 2006-05-23 | 2006-05-23 | A kind of analgesic of oral, quick acting |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100823220A CN100560058C (en) | 2006-05-23 | 2006-05-23 | A kind of analgesic of oral, quick acting |
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|---|---|
| CN1895221A true CN1895221A (en) | 2007-01-17 |
| CN100560058C CN100560058C (en) | 2009-11-18 |
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| CNB2006100823220A Active CN100560058C (en) | 2006-05-23 | 2006-05-23 | A kind of analgesic of oral, quick acting |
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| Country | Link |
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