• YAKHAK HOEJI
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• v.33 no.4
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• pp.237-240
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• 1989

A new synthetic method for tiaprofenic acid, which is a potent anti-inflammatory agent, was described. Friedel-Crafts reaction of thiophene with ethyl ${\alpha}-chloro-{\alpha}-(methylthio)$ acetate (1) gave ethyl ${\alpha}-methylthio-2-thiopheneacetate$ (3). Ethyl ${\alpha}-methyl-2-thiopheneacetate$ (5) was prepared by treatment of (3) with NaH and MeI, followed by desulfurization with zinc dust-acetic acid of the resultant ethyl ${\alpha}-methyl-{\alpha}-methylthio-2-thiopheneacetate$ (4). Tiaprofenic acid (7) could be easily synthesized by benzoylation of (5) and hydrolysis of the resultant ethyl $5-benzoyl-{\alpha}-methyl-2-thiopheneacetate$ (6).

• Journal of Pharmaceutical Investigation
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• v.16 no.2
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• pp.55-67
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• 1986

Inclusion complexation of tiaprofenic acid (TPA) with cyclodextrins $({\alpha}-,\;{\beta}-,\;{\gamma}-CyDs)$ in aqueous solution and in solid phase was investigated by solubility method, measurement of partition coefficient, ultra-violet, circular dichroism, infrared spectroscopies, powder X-ray diffractometry and differential scanning calorimetry. Investigations were made to prepare inclusion complexes of TPA with ${\beta}-CyD$ in solid powdered form by coprecipitation, freeze-drying, spray-drying and co-pulverization methods. The coprecipitation, freeze-drying and spray-drying methods were successful in obtaining inclusion complexes. The results showed that the latter two methods might be originally superior to the former in obtaining powdered inclusion completes. Especially, it was shown by powder X-ray diffractometry that spray-dried ${\beta}-CyD$ alone, TPA-spray-dried ${\beta}-CyD$ physical mixture, and spray-dried $TPA-{\beta}-CyD$ complex were amorphous. The dissolution behaviours of $TPA-{\beta}-CyD$ systems prepared by above four methods were compared with those of TPA alone and $TPA-{\beta}-CyD$ physical mixture, and the rates of dissolution of TPA in pH 1.2 buffer were greatly enhanced by inclusion complexation and copulverization.

• Journal of Pharmaceutical Investigation
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• v.29 no.2
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• pp.117-126
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• 1999

Differential scanning calorimetry(DSC) was used as a screening technique for assessing the compatibility of some drugs with excipients. On the basis of DSC results, interaction of ibuprofen with PVP K40 was found and eutectic formations with PEG 6000 or magnesium stearate were demonstrated. Fenoprofen Ca was found to interact with PEG 6000. Naproxen showed interactions with PEG 6000, PVP K40, PVPP and Mg stearate. Interactions of tiaprofenic acid with PVP K40 or PVPP were found and eutectic formations with PEG 6000 or Mg stearate were observed. Bisoprolol hemifumarate, metoprolol tartrate and penbutolol sulfate were found to interact with lactose.

• Korean Journal of Bronchoesophagology
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• v.4 no.2
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• pp.171-176
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• 1998

Postoperative pain following tonsillectomy remains a significant obstacle to speedy recovery and smooth convalescence. Inadequate analgesia causes poor oral intake and influences the length of hospital stay and ability to return to normal activity. Patient Controlled Analgesia (PCA) is a method of analgesia adminstration that consists of a computer driven pump with a button that the patient may press to adminster a small dose of analgesic drug. The aim of this study was to examine whether Intravenous Patient Controlled Analgesia (IV-PCA) can reduce postoperative pain after tonsillectomy. The 100 patients undergoing tonsillectomy with general anesthesia were divided into two groups. The PCA group patients (n=80) received a mixture of nalbuphine and ketorolac by Walkmed PCA infusor during first 48 postoperative hours. In control group (n=20), the patients received oral acetoaminophen (Tyrenol) regularly and tiaprofenic acid (Surgam) intramuscularly on a p.r.n basis. Analgesic efficacy was evaluated with visual linear analogue scale (VAS) and the adverse effects were evaluated with 4 point scale. The patients of PCA group had less pain than those of control group. The adverse effects in the PCA group were nausea and vomiting. This study suggests that IV-PCA may be safe and effective method of pain control after adult tonsillectomy and is better accepted than oral or intramuscular pain medications.