Octadecanoic acid, 12-hydroxy-, polymer with .alpha.-hydro-.omega.-hydroxypoly(oxy-1,2-ethanediyl)
Octadecanoic acid, 12-hydroxy-, polymer with .alpha.-hydro-.omega.-hydroxypoly(oxy-1,2-ethanediyl)
CAS: 70142-34-6
Molecular Formula: (C18H36O3.(C2H4O)nH2O)x
Octadecanoic acid, 12-hydroxy-, polymer with .alpha.-hydro-.omega.-hydroxypoly(oxy-1,2-ethanediyl) - Names and Identifiers
Octadecanoic acid, 12-hydroxy-, polymer with .alpha.-hydro-.omega.-hydroxypoly(oxy-1,2-ethanediyl) - Physico-chemical Properties
| Molecular Formula | (C18H36O3.(C2H4O)nH2O)x |
| Flash Point | 272℃ |
| Storage Condition | Room Temprature |
Octadecanoic acid, 12-hydroxy-, polymer with .alpha.-hydro-.omega.-hydroxypoly(oxy-1,2-ethanediyl) - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 43 - May cause sensitization by skin contact |
| Safety Description | S24 - Avoid contact with skin. S37 - Wear suitable gloves. |
Octadecanoic acid, 12-hydroxy-, polymer with .alpha.-hydro-.omega.-hydroxypoly(oxy-1,2-ethanediyl) - Xuesaitong injection preparation containing polyethylene glycol dodecylhydroxystearate and preparation method thereof
from Baidu Library
patent type:
invention patent
Application (patent) number:
CN201310635290.2
application date:
20131203
Public/Announcement Number:
CN104666379A
Public/announcement date:
20150603
applicant (patent):
Chengdu list Pharmaceutical Co., Ltd.
inventor:
Zhang Hao , Gold (red) Liang Huirong
National and provincial code:
CN510104
Abstract:
The invention provides Xuesaitong injection preparation containing polyethylene glycol dodecydroxystearate and a preparation method thereof. The Xuesaitong injection preparation is mainly prepared by co-dissolving Panax notoginseng saponins, disodium ethylenediamine tetraacetate and polyethylene glycol dodecydroxystearate as a solubilizer in water for injection, the amount of polyethylene glycol dodecylhydroxystearate used was 0.01g. The invention adopts polyethylene glycol dodecydroxystearate with higher safety as a solubilizer to prepare Xuesaitong injection preparation, thereby solving the problems of certain potential safety hazard and product quality in the current commercially available Xuesaitong injection, the adverse drug reactions caused by polysorbate 80 are effectively avoided, and the safety of Xuesaitong injection in clinical medication is greatly improved.
Last Update：2024-01-02 23:10:35
Octadecanoic acid, 12-hydroxy-, polymer with .alpha.-hydro-.omega.-hydroxypoly(oxy-1,2-ethanediyl) - Effect of polyethylene glycol -12-hydroxystearate on the in vitro dissolution and oral absorption of nimodipine
from hownet
Author:
Abstract:
nimodipine is a drug for the treatment of hypertension and cerebrovascular diseases. The existing dosage forms include tablets and solution injections. Since nimodipine is almost insoluble in water, the bioavailability of its oral preparation is only 10% ~ 30%. Therefore, it is necessary to improve its water solubility through preparation solubilization technology. In this paper, a new surfactant polyethylene glycol -12-hydroxy stearate (Solutol HS-15) is used as the carrier material by dispersion technology, the effects of carrier materials on the solubility and in vitro dissolution of nimodipine were investigated by solvent dispersion method. The results showed that the higher the proportion of Solutol HS-15 in the complex of Solutol HS-15 and Nimodipine, the higher the solubility of nimodipine in water. Nimodipine is a drug for the treatment of hypertension and cerebrovascular diseases. The existing dosage forms include tablets and solution injections. Since nimodipine is almost insoluble in water, the bioavailability of its oral preparation is only 10% ~ 30%. Therefore, it is necessary to improve its water solubility through preparation solubilization technology. In this paper, a new surfactant polyethylene glycol -12-hydroxy stearate (Solutol HS-15) is used as the carrier material by dispersion technology, the effects of carrier materials on the solubility and in vitro dissolution of nimodipine were investigated by solvent dispersion method. The results showed that the higher the proportion of Solutol HS-15 in the complex of Solutol HS-15 and Nimodipine, the higher the solubility of nimodipine in water. Tablets were prepared from drug carrier material complexes. Solutol HS-15 was superior to conventional solid dispersions prepared with polyethylene glycol 4000 in the ratio of Solutol HS-15 to nimodipine of 1:1, the solubility of the drug in water at 37 C was increased by 7.4 times, and the solubilization effect of Solutol HS-15 was better than that of polyethylene glycol 4000 at the same dosage. The in vitro dissolution of the tablets prepared by the compound of Solutol HS-15 and nimodipine was investigated, the dissolution of nimodipine in artificial gastric juice and artificial intestinal juice was significantly improved compared with the dissolution of the tablets without Solutol HS-15, the in vitro dissolution rate of the drug is also higher than that of the currently marketed domestic tablets. The oral absorption and pharmacokinetic tests in rabbits showed that: the in vitro dissolution of the tablets with Solutol HS-15 was 4.8 times higher than that of the powder capsules without Solutol HS-15, and the bioavailability was 25% higher than that of the commercially available tablets. As a new non-toxic and non-irritating surfactant, Solutol HS-15 can be used in injection to increase the solubility of drugs, it can also be used in oral solid formulations for improving in vitro dissolution and absorption and bioavailability of drugs after oral administration. The research methods and results of this subject have certain reference significance for the development of nimodipine oral solid preparations and the improvement of bioavailability of other poorly water soluble oral solid preparations. Close up
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Key words:
nimodipine; Solutol HS-15; Solubilization; Polyethylene glycol; solid Dispersion
degree level:
MSc
DOI:
CNKI:CDMD:2.1016.186942
Last Update：2023-08-16 22:09:50
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