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Gelling agent for controlling and releasing 5-HT3 acceptor antagon and method of preparing the same
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A receptor antagonist and release gel technology, applied in the field of 5-HT3 receptor antagonist controlled release gel and its preparation, can solve the problems of inconvenient use, poor compliance, short half-life, etc., and achieve convenient medication , delayed release, and reduced toxic and side effects
Inactive Publication Date: 2009-12-09
SHANDONG UNIV
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Problems solved by technology
Due to the first-pass effect, oral administration is mainly metabolized by the liver, and the bioavailability is only about 60%; moreover, the patient itself has symptoms of nausea and vomiting, and the compliance of oral administration is poor; if the injection is administered, due to the short half-life (about 3h ), to maintain effective treatment, multiple injections are required, which is inconvenient to use and poor in compliance
At present, there is no long-acting preparation for gel controlled release mucosal administration (nasal mucosa, oral mucosa, vaginal mucosa and rectal mucosa) available
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Embodiment 1
[0024] Example 1: 5-HT 3 Receptor antagonist controlled release gel, the components are as follows:
[0025] Ondansetron Hydrochloride 4.0g
[0026] Hydroxypropyl-β-cyclodextrin 15.3g
[0027] Poloxamer 160.0g
[0028] Add water to 1000ml
[0029] Preparation method, the steps are as follows:
[0030] Weigh 160.0g of poloxamer, add it to 900ml of water, stir for 50min and place it at 4°C to make it fully swell and disperse evenly to obtain a clear solution of the gel matrix, then weigh 4.0g of ondansetron hydrochloride Put 15.3g of hydroxypropyl-β-cyclodextrin in the above-mentioned clear solution of the gel matrix, ultrasonically dissolve, add water to 1000ml, stir for 50min, and store in the refrigerator.
[0031] Determination of gelation temperature:
[0032] Take the above-mentioned ondansetron hydrochloride controlled-release gel, and insert a thermometer into the gel. Place the vial in a water bath and raise the temperature slowly at a rate of about 0.5-1°C / min. ...
Embodiment 2
[0035] Example 2: 5-HT 3 The preparation method of receptor antagonist controlled release gel is as described in Example 1, the difference is that the components are as follows:
[0036] Ondansetron Hydrochloride 40.0g
[0037] Hydroxypropyl-β-cyclodextrin 115g
[0038] Poloxamer 220.0g
[0039] Water was added to 1000ml.
[0040] Tests show that the controlled release time of the best release medium is more than 12 hours in 0.9% NaCl solution with a pH of 5.5-6.5.
Embodiment 3
[0041] Example 3: 5-HT 3The preparation method of receptor antagonist controlled release gel is as described in Example 1, the difference is that the components are as follows:
[0042] Ondansetron Hydrochloride 80.0g
[0043] Hydroxypropyl-β-cyclodextrin 306g
[0044] Poloxamer 300.0g
[0045] Water was added to 1000ml.
[0046] Tests show that the controlled release time of the best release medium is more than 12 hours in 0.9% NaCl solution with a pH of 5.5-6.5.
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Abstract
The invention relates to a 5-HT3 receptor antagonist controlled-release gel and a preparation method thereof. The components of the controlled-release gel include a 5-HT3 receptor antagonist, cyclodextrin or derivatives thereof, a gel matrix and water. The controlled release gel of the present invention has unique temperature control performance, its preparation method is simple, the product quality is easy to control, the stability is good, the sustained release is long-acting, the medicine is convenient, and it is suitable for clinical wide application, especially suitable for treating tumor chemotherapy and radiotherapy nausea and vomiting afterwards.
Description
technical field [0001] The present invention relates to a non-oral administration, mucosal absorption (nasal mucosa, oral mucosa, vaginal mucosa and rectal mucosa) gel controlled release preparation, to be precise, it is a kind of preparation that can be expected to be applied to the prevention and treatment of tumor chemotherapy / radiotherapy and surgery highly selective 5-HT for nausea and vomiting after 3 Receptor antagonist controlled release gel and preparation method thereof. Background technique [0002] Setron 5-HT 3 Receptor (5-hydroxytryptamine 3 receptor) antagonists are mainly used to treat nausea and vomiting caused by tumor chemotherapy and radiotherapy, and can also be used to prevent and treat nausea and vomiting caused by surgery. As disclosed on March 14, 2007, the Chinese patent with publication number CN1927398 (application number 200610096452.X) discloses a 5-hydroxytryptamine 3 receptor antagonist and H 2 The pharmaceutical composition in which the re...
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