摘要:
Bioerodible poly(ortho esters) useful as orthopedic implants or vehicles for the sustained delivery of pharmaceutical, cosmetic and agricultural agents from dioxane-based di(ketene acetals). Block copolymers contain these bioerodible poly(ortho esters). These block copolymers have both hydrophilic and hydrophobic blocks. They form micelles in aqueous solution, making them suitable for encapsulation or solubilization of hydrophobic or water-insoluble materials; and they also form bioerodible matrices for the sustained release of active agents.
摘要:
A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.
摘要:
A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.
摘要:
Amphiphilic copolymer, containing at least a hydrophilic chain segment (A) and a hydrophobic chain segment (B), wherein the hydrophilic chain segment (A) contains peptides and wherein the hydrophobic chain segment (B) contains acetal groups or orthoester groups. The hydrophilic chain segment (A) preferably contains glutamine/glutamic acid units or asparagines/aspartic acid units, making a biodegradable copolymer which can form a thermogel.
摘要:
A pharmaceutical composition for the sustained release of an effective amount of a selective 5-hydroxytryptamine 3 (5-HT3) receptor antagonist for the prevention, reduction or alleviation of acute and delayed chemotherapy-induced nausea and vomiting (CINV) following a course of emetogenic chemotherapy, wherein the composition is administered by subcutaneous injection, the composition comprising a 5-HT3 receptor antagonist, a semi-solid delivery vehicle and a pharmaceutically acceptable liquid excipient; wherein the composition, when administered in a single dosage, provides a controlled release of the 5-HT3 receptor antagonist and prolonging the release of the 5-HT3 receptor antagonist that tracks the profile of the incidence of vomiting.
摘要:
The present invention provides graft copolymer delivery vehicle which comprises a polyethyleneglycol (PEG)-polyacetal (PA) copolymer or a polyethyleneglycol (PEG)-polyacetal (PA)-polyorthoester (POE) copolymer. The polyethyleneglycol-polyacetal graft copolymers or the polyethyleneglycol-polyacetal-polyorthoester graft copolymers, in particular, the PA-g-PEG or the PA-POE-g-PEG suitable for the invention are represented by Formulae I and V:
摘要:
Bioerodible polyorthoesters useful as orthopedic implants or vehicles for the sustained delivery of pharmaceutical, cosmetic and agricultural agents contain hydrogen bonding groups and &agr;-hydroxy acid-containing groups.
摘要:
A composition for the transdermal delivery of a biologically active peptide having a molecular weight of about 5,000 or less comprising at lest one biologically active peptide, at least one higher alcohol, ester and/or higher amide in combination with at least one pyrrolidone compound of the formula: ##STR1## where R.sub.5 is hydrogen or a lower alkyl group having 1 to 4 carbon atoms, R.sub.6 is hydrogen or a lower alkyl group having 1 to 3 carbon atoms and n is 3, 4 or 5. A method for percutaneously administering such a composition is also disclosed.
摘要:
Transdermal drug delivery systems comprise a backing or enclosure having a matrix layer which incorporates a drug and a percutaneous enhancer for the drug. The percutaneous enhancer and/or drug will be contained within polymeric particles dispersed through the matrix layer, where the polymeric particles define pore networks which are sized to release the enhancer and/or drug into the matrix layer at rate(s) selected to provide for a desired rate of drug penetration. By isolating the enhancer within the polymeric particles, adverse interactions between the enhancer and the matrix layer and/or the drug can be minimized. Moreover, the release rate of the enhancer into the matrix layer can be carefully controlled, which in turn controls the penetration rate of the drug into the treated host.
摘要:
Water-soluble polyacetal or polyketal having the formula ##STR1## wherein R.sub.1, and R.sub.2 are aliphatic, cycloaliphatic or aromatic groups, for ketals; R.sub.1 is hydrogen and R.sub.2 is aliphatic, cycloaliphatic, or aromatic groups for acetals; R.sub.3 and R.sub.4 are also aliphatic, alkoxy, cycloaliphatic or aromatic groups X represents groups as (CH.sub.2).sub.n, O(CH.sub.2).sub.N O or ##STR2## that connect the pendant unsaturation to the aliphatic, cycloaliphatic or aromatic R.sup.4 groups, the ratio of a to b is 0.5 to 10, and n is 10-100.
摘要翻译:具有式“IMAGE”的水溶性聚缩醛或聚缩酮,其中R1和R2是脂肪族,脂环族或芳族基团,用于缩酮; R1是氢,R2是用于缩醛的脂族,脂环族或芳族基团; R 3和R 4也是脂族,烷氧基,脂环族或芳族基团X表示将侧基不饱和键连接到脂肪族,脂环族或芳族R 4基团上的(CH 2)n,O(CH 2)NO或 b为0.5〜10,n为10〜100。