(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate
timolol maleate
CAS: 26839-77-0
Molecular Formula: C17H28N4O7S
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Names and Identifiers
| Name | timolol maleate |
| Synonyms | 248-034-7 timolol maleate d-timolol maleate (R)-(+)-Timolol maleate (R)-Timolol hydrogen maleate (+)-3-[3-(tert-butylamino)-2-hydroxypropoxy]-4-morpholino-1,2,5-thiadiazole maleate (2R)-1-[(1,1-DiMethylethyl)aMino]-3-[[4-(4-Morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]- (-)-1-(tert-Butylamino)-3-((4-morpholino-1,2,5-thiadiazol-3-yl)oxy)-2-propanol maleate (+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate 1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol (2Z)-but-2-enedioate (salt) |
| CAS | 26839-77-0 |
| EINECS | 248-034-7 |
| InChI | InChI=1/C13H24N4O3S.C4H4O4/c1-13(2,3)14-8-10(18)9-20-12-11(15-21-16-12)17-4-6-19-7-5-17;5-3(6)1-2-4(7)8/h10,14,18H,4-9H2,1-3H3;1-2H,(H,5,6)(H,7,8)/b;2-1- |
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Physico-chemical Properties
| Molecular Formula | C17H28N4O7S |
| Molar Mass | 432.49 |
| Melting Point | >194°C (dec.) |
| Boling Point | 487.2°C at 760 mmHg |
| Flash Point | 248.5°C |
| Solubility | DMSO (Slightly), Methanol (Very Slightly) |
| Vapor Presure | 2.62E-10mmHg at 25°C |
| Appearance | Solid |
| Color | White to Off-White |
| Storage Condition | -20°C Freezer |
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Risk and Safety
| HS Code | 2934990002 |
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Standard
Authoritative Data Verified Data
This product is (-)- l- (tert-butylamino)-3-[(4-morpholinyl-1, 2, 5-thiadiazol-3-yl) oxy]-2-propanol maleate. Calculated as the dried product, the content of C13H24N403S • C4H4O4 shall not be less than 99. 0%.
Last Update：2024-01-02 23:10:35
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Trait
Authoritative Data Verified Data
- This product is white crystalline powder; Odorless.
- This product is dissolved in water or methanol, slightly soluble in ethanol, slightly soluble in chloroform, almost insoluble in cyclohexane or ether.
melting point
The melting point of this product (General rule 0612) is 199~203°C, and it is decomposed at the same time during melting.
specific rotation
take this product, precision weighing, plus lmol/L hydrochloric acid solution dissolved and quantitatively diluted to make every 1ml containing about 0.lg of the solution, determined according to law (General rule 0621), the specific rotation of a 5. 7 ° to a 6.2 °.
absorption coefficient
take this product, precision weighing, and hydrochloric acid solution (9-1000) dissolved and quantitatively diluted to make a solution containing about 20ug per 1ml, the absorbance was measured at a wavelength of 0401 NM according to ultraviolet-visible spectrophotometry (General rule 199), and the absorption coefficient was 211.
Last Update：2022-01-01 11:31:54
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Differential diagnosis
Authoritative Data Verified Data
- take about 5mg of this product, add 1ml of water to dissolve, add 3 drops of potassium permanganate test solution, the purple color disappeared immediately, and heat to generate red-brown precipitate.
- take about 10mg of this product, add 1ml of water to dissolve, add 1 drop of copper sulfate test solution, 1ml of ammonia test solution and 2 drops of carbon disulfide-benzene (1:3), shake, the benzene layer was brownish yellow to brown.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 33).
Last Update：2022-01-01 11:31:55
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Exam
Authoritative Data Verified Data
acidity
take 0.50g of this product, add 25ml of water to dissolve it, and measure it according to law (General rule 0631). The pH value should be 3.8~4.3.
Related substances
take this product and add methanol to make a solution containing 25mg per lml. According to the thin layer chromatography (General 0502) test, absorb 5ul of the above solution, and point it on the silica gel G thin layer plate, with dichloromethane-methanol-concentrated ammonia solution (80:14:1) as the developing solvent, it is developed, dried, and the saturated iodine vapor is allowed to show color. No other spots are allowed except the main spots.
loss on drying
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
Last Update：2022-01-01 11:31:55
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Content determination
Authoritative Data Verified Data
take this product 0.3g, precision weighing, add glacial acetic acid 10ml dissolved, add acetic anhydride 10ml and crystal violet indicator liquid 1 drop, with perchloric acid titration solution (0.1 mol/L) titration to a blue color of the solution, and the results of the titration were corrected by a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 43 25mg of C13H24N403S • C4H404.
Last Update：2022-01-01 11:31:56
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Category
Authoritative Data Verified Data
B adrenergic receptor blockers.
Last Update：2022-01-01 11:31:56
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 11:31:56
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Timolol maleate tablets
Authoritative Data Verified Data
This product contains timolol maleate (C13H24N4O3S • C4H404) should be 90.0% ~ 110.0% of the label amount.
trait
This product is white tablet.
identification
- take an appropriate amount of the fine powder of this product (about 5mg of timolol maleate), add water lml, shake, centrifuge, take the supernatant and add 3 drops of potassium permanganate test solution, the purple color disappears immediately, heat, that is, a red-brown precipitate was formed.
- take an appropriate amount of fine powder of this product (about 10mg of timolol maleate), add 1 ml of water, shake, centrifuge, and take the supernatant and 1 drop of copper sulfate test solution, adding 1 ml of ammonia solution and 2 drops of carbon disulfide-benzene (1:3), and shaking, the benzene layer was brownish yellow to brown.
- the solution under the content measurement was measured by ultraviolet-visible spectrophotometry (General 0401), and the maximum absorption was found at a wavelength of Nm.
examination
- Content uniformity take 1 tablet of this product, put it in a 50ml measuring flask, add 0.1 mol/L hydrochloric acid solution appropriate amount, fully shake to dissolve timolol maleate, with 0. Dilute the lmol/L hydrochloric acid solution to the scale, shake well, filter, take the appropriate amount of filtrate accurately, use 0.1 mol/L hydrochloric acid solution was quantitatively diluted to prepare a solution containing 20ug per 1 ml. Determination of content according to the method under the content determination item, should comply with the provisions (General 0941).
- dissolution of this product, according to the dissolution and release determination method (General 0931 third method), with 0.100 ml of 1 mol/L hydrochloric acid solution was used as the dissolution medium at a rotation speed of revolutions per minute, and the solution was filtered after 30 minutes, and the filtrate was used as the test solution. The absorbance was measured at a wavelength of 295mn according to UV-Vis spectrophotometry (General rule 0401), and the dissolution amount of each tablet was calculated as the absorption coefficient of C13H24N403S • C4H404 was 205. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
Take 20 tablets of this product, precision weighing, fine grinding, precision weighing an appropriate amount (equivalent to timolol maleate 5mg), put it in a 50ml measuring flask, add 0.1 mol/L hydrochloric acid solution appropriate amount, shake to dissolve timolol maleate and dilute to the scale, shake, filter, take 10ml of continuous filtrate, put it in 50ml measuring flask, add 0.lmol/L hydrochloric acid solution diluted to the scale, shake, according to UV-visible spectrophotometry (General 0401 ) , at the wavelength of 295nm absorbance, the absorption coefficient of C13H24N403S • C4H404 was calculated as 205.
category
Same as timolol maleate.
specification
(1)2.5mg (2)5mg
storage
light shielding, sealed storage.
Last Update：2022-01-01 11:31:57
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Timolol Maleate Eye Drops
Authoritative Data Verified Data
This product contains timolol maleate according to timolol (C13H24N4O3S) calculation, should be 90.0% ~ 110.0% of the label amount. This product can add an appropriate amount of bacteriostatic agent.
trait
This product is a clear colorless liquid.
identification
- take this product, according to timolol maleate under the identification (1), (2) test, showed the same reaction.
- the solution under the content measurement was measured by ultraviolet-visible spectrophotometry (General 0401), and the maximum absorption was found at a wavelength of Nm.
examination
- the pH value should be 6.5 to 7.5 (General 0631).
- osmolality the osmolality ratio shall be 0632-0.9 as determined by osmolality measurement method (General 1.3).
- others shall comply with the relevant provisions under Ophthalmic Preparations (General rule 0105).
Content determination
precision: take an appropriate amount of this product and quantitatively dilute it with hydrochloric acid solution (9-1000) to a solution containing 20ug of timolol per 1 ml, according to UV-visible spectrophotometry (General rule 0401), the absorbance is measured at the wavelength of 295nm, calculated as the absorption coefficient of C13H24N403S- C4H404 is 205, and the result is multiplied by 0.7316, that is, the content of C13H24N403S.
category
Same as timolol maleate.
specification
Based on timolol (l)5ml:12.5mg (2)5ml:25Mg
storage
light shielding, sealed storage.
Last Update：2022-01-01 11:31:58
(+)-3-(3-tert-Butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate - Reference Information
| structure and physical and chemical properties | timolol maleate is a white crystalline powder, odorless and bitter. The melting point is 199-203 ℃, and it decomposes when melting. It is dissolved in water or methanol, slightly soluble in ethanol, slightly soluble in chloroform, and almost insoluble in ether. |
| indications | timolol maleate is mainly used for primary open-angle glaucoma, aphakic glaucoma, some secondary glaucoma and ocular hypertension; it is also suitable for some glaucoma that is not effective for drug or surgical treatment. |
| pharmacological effects and mechanism of action | timolol maleate is a β-adrenergic receptor blocker and is used for glaucoma eyes. the intensity of action is 8 times that of przailol, which can reduce the generation of aqueous humor in the eye and has a significant effect on reducing intraocular pressure. There was no significant endogenous sympathomimetic activity and no local anesthetic effect. Do not shrink the pupil, do not affect the visual acuity, do not cause ciliary muscle spasm, do not appear obvious blurred vision or night blindness. 20 minutes after the eye drop, the intraocular pressure began to drop, 2 hours after the maximum decline, and can continue to act for 24 hours. Timolol maleate has a good effect on glaucoma, especially primary and open-angle glaucoma, which is superior to traditional intraocular pressure lowering drugs. It is characterized by fast onset, small side effects and good tolerance. It has no effect on pupil size, light response and vision. For some patients, timolol maleate has an additive effect with some anti-glaucoma drugs. In addition, it also has certain curative effects on aphakic glaucoma, some secondary glaucoma, ocular hypertension and other glaucoma that are ineffective for drugs and surgery. |
| adverse reactions | when timolol maleate is used to treat glaucoma, the common dosage form is timolol maleate eye drops, which is easily accepted by the majority of patients because of its convenient use and good compliance. however, it has the disadvantages of low bioavailability of drugs and repeated administration, and may cause some adverse reactions due to the absorption of nasolacrimal duct. Timolol maleate was approved to enter the market by the United States in September 1978 to January, due to systemic adverse reactions caused by the use of timolol maleate eye drops. A total of 3000 adverse reactions were reported, including 450 severe adverse reactions of respiratory system and cardiovascular system and 32 deaths. |
Last Update：2024-04-10 22:29:15
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Product Name: Timolol Impurity 1 (Timolol EP Impurity A Maleate Salt) Visit Supplier Webpage Request for quotationCAS: 26839-77-0
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Timolol Impurity 1 (Timolol EP Impurity A Maleate Salt) Visit Supplier Webpage Request for quotationCAS: 26839-77-0
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
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